celecoxib [Ligand Id: 2892] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL118 (Celebra, Celebrex, Celecoxib, DFN-15, DFN15, Elyxyb, NSC-719627, NSC-758624, Onsenal, SC-58635)
  • 3-phosphoinositide dependent protein kinase 1/3-phosphoinositide dependent protein kinase-1 in Human [ChEMBL: CHEMBL2534] [GtoPdb: 1519] [UniProtKB: O15530]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • Alpha carbonic anhydrase in Stylophora pistillata [ChEMBL: CHEMBL1075028] [UniProtKB: B5SU02]
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  • 5-LOX/Arachidonate 5-lipoxygenase in Human [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
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  • Carbonate dehydratase in Sulfurihydrogenibium sp. (strain YO3AOP1) [ChEMBL: CHEMBL3745586] [UniProtKB: B2V8E3]
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  • Carbonic anhydrase in Mycobacterium tuberculosis [ChEMBL: CHEMBL6068] [UniProtKB: P9WPJ9]
  • Carbonic anhydrase in Methanosarcina thermophila [ChEMBL: CHEMBL3932] [UniProtKB: P40881]
  • Carbonic anhydrase in Stylophora pistillata [ChEMBL: CHEMBL1649055] [UniProtKB: C0IX24]
  • Carbonic anhydrase in Methanobacterium thermoautotrophicum [ChEMBL: CHEMBL3926] [UniProtKB: Q50565]
  • Carbonic anhydrase in Candida albicans (strain SC5314 / ATCC MYA-2876) (Yeast) [ChEMBL: CHEMBL5337] [UniProtKB: Q5AJ71]
  • Carbonic anhydrase in Candida glabrata CBS 138 [ChEMBL: CHEMBL6185] [UniProtKB: Q6FTL6]
  • Carbonic anhydrase in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL5931] [UniProtKB: P53615]
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  • Carbonic anhydrase 2 in Cryptococcus neoformans var. grubii [ChEMBL: CHEMBL1697676] [UniProtKB: Q3I4V7]
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  • Carbonic anhydrase, alpha family in Thiomicrospira crunogena (strain XCL-2) [ChEMBL: CHEMBL3621035] [UniProtKB: Q31FD6]
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  • carbonic anhydrase 1/Carbonic anhydrase I in Human [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
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  • carbonic anhydrase 2/Carbonic anhydrase II in Human [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
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  • carbonic anhydrase 4/Carbonic anhydrase IV in Human [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748]
  • Carbonic anhydrase IV in Bovine [ChEMBL: CHEMBL281] [UniProtKB: Q95323]
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  • carbonic anhydrase 9/Carbonic anhydrase IX in Human [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
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  • carbonic anhydrase 5A/Carbonic anhydrase VA in Human [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218]
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  • carbonic anhydrase 7/Carbonic anhydrase VII in Human [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166]
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  • carbonic anhydrase 12/Carbonic anhydrase XII in Human [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
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  • carbonic anhydrase 13/Carbonic anhydrase XIII in Human [ChEMBL: CHEMBL3912] [GtoPdb: 2748] [UniProtKB: Q8N1Q1]
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  • carbonic anhydrase 14/Carbonic anhydrase XIV in Human [ChEMBL: CHEMBL3510] [GtoPdb: 2598] [UniProtKB: Q9ULX7]
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  • Cytochrome c oxidase subunit 1 in Sheep [ChEMBL: CHEMBL6011] [UniProtKB: O78749]
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  • Delta carbonic anhydrase in Thalassiosira weissflogii [ChEMBL: CHEMBL3097982] [UniProtKB: Q5U9J1]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • epoxide hydrolase 2/Epoxide hydratase in Human [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
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  • histone deacetylase 1/Histone deacetylase 1 in Human [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
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  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • phosphodiesterase 5A/Phosphodiesterase 5A in Human [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
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  • PROBABLE TRANSMEMBRANE CARBONIC ANHYDRASE (CARBONATE DEHYDRATASE) (CARBONIC DEHYDRATASE) in Mycobacterium tuberculosis [ChEMBL: CHEMBL5767] [UniProtKB: P96878]
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  • Quinolone resistance protein norA in S.aureus [ChEMBL: CHEMBL5114] [UniProtKB: P0A0J7]
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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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  • Uncharacterized protein Rv1284/MT1322 in Mycobacterium tuberculosis [ChEMBL: CHEMBL5631] [UniProtKB: P9WPJ7]
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  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
3-phosphoinositide dependent protein kinase 1/3-phosphoinositide dependent protein kinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2534] [GtoPdb: 1519] [UniProtKB: O15530]
ChEMBL Inhibition of recombinant PDK1 using RPRAATF as substrate by scintillation counting B 4.32 pIC50 48000 nM IC50 Bioorg Med Chem Lett (2012) 22: 1629-1632 [PMID:22266037]
ChEMBL Inhibition of PDK1-mediated Akt activation in human PC3 cells after 2 hrs by Western blotting analysis B 4.32 pIC50 48000 nM IC50 Eur J Med Chem (2013) 65: 323-336 [PMID:23735281]
ChEMBL In Vitro Kinase Assay: PDK-1 kinase activity This in vitro assay was performed using a PDK-1 kinase assay kit (Upstate, Lake Placid, N.Y.) according to the vendor's instructions. This cell-free assay is based on the ability of recombinant PDK-1, in the presence of DMSO vehicle or the test agent, to activate its downstream kinase serum- and glucocorticoid-regulated kinase (SGK.) which, in turn, phosphorylates the Akt/SGK-specific peptide substrate RPRAATF with [γ-32]-ATP. The [32P]-phosphorylated peptide substrate was then separated from the residual [γ-32P]-ATP using PS1 phosphocellulose paper and quantitated by a scintillation counter after three washes with 0.75% phosphoric acid. B 4.32 pIC50 48000 nM IC50 US-8741944-B2. Anti-infective agents against intracellular pathogens (2014)
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 4.86 pKi 13917 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 4.61 pIC50 24622 nM IC50 DrugMatrix in vitro pharmacology data
AGAP002992-PA in Anopheles gambiae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3399914] [UniProtKB: Q5TU56]
ChEMBL Inhibition of Anopheles gambiae carbonic anhydrase pre-incubated for 15 mins by stopped-flow CO2 hydration assay B 6.76 pKi 173 nM Ki Bioorg Med Chem (2015) 23: 2303-2309 [PMID:25882523]
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 6.16 pKi 692 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 5.82 pIC50 1516 nM IC50 DrugMatrix in vitro pharmacology data
Alpha carbonic anhydrase in Stylophora pistillata (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075028] [UniProtKB: B5SU02]
ChEMBL Inhibition of cloned Stylophora pistillata alpha-CA expressed in human HEK293 cells by stopped-flow CO2 assay B 7.47 pKi 34.2 nM Ki Bioorg Med Chem (2009) 17: 5054-5058 [PMID:19520577]
ChEMBL Inhibition of Stylophora pistillata carbonic anhydrase by stopped-flow CO2 hydration assay B 7.47 pKi 34.2 nM Ki Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801]
5-LOX/Arachidonate 5-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
ChEMBL Inhibition of 5LOX in human whole blood assessed as inhibition of calcium ionophore A 23187-stimulated 5HETE production by HPLC analysis F 5 pIC50 >10000 nM IC50 J Med Chem (2004) 47: 6195-6206 [PMID:15566290]
ChEMBL Inhibition of 5-LOX (unknown origin) using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 10 mins B 5.76 pIC50 1720 nM IC50 Eur J Med Chem (2020) 189: 112066-112066 [PMID:31982653]
Astrosclerin-3 in Astrosclera willeyana (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944499] [UniProtKB: A6YCJ1]
ChEMBL Inhibition of GST-tagged astrosclera willeyana Astrosclerin-3 expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay B 6.14 pKi 732 nM Ki Bioorg Med Chem (2012) 20: 1403-1410 [PMID:22285172]
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 4.92 pKi 12093 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 4.79 pIC50 16124 nM IC50 DrugMatrix in vitro pharmacology data
Carbonate dehydratase in Sulfurihydrogenibium sp. (strain YO3AOP1) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3745586] [UniProtKB: B2V8E3]
ChEMBL Inhibition of recombinant Sulfurihydrogenibium yellowstonense YO3AOP1 carbonic anhydrase by stopped flow CO2 hydrase assay B 8.16 pKi 6.9 nM Ki Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758]
Carbonic anhydrase in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6068] [UniProtKB: P9WPJ9]
ChEMBL Inhibition of full length Mycobacterium tuberculosis H37Rv recombinant carbonic anhydrase 2 encoded by RV3588c by stopped flow CO2 hydration assay B 6.15 pKi 713 nM Ki Bioorg Med Chem Lett (2009) 19: 6649-6654 [PMID:19846301]
ChEMBL Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv3588c pre-incubated for 15 mins by stopped-flow CO2 hydration method B 6.15 pKi 713 nM Ki J Med Chem (2012) 55: 9619-9629 [PMID:23067387]
Carbonic anhydrase in Methanosarcina thermophila (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3932] [UniProtKB: P40881]
ChEMBL Inhibitory activity against alpha carbonic anhydrase (Co-Cam) from Methanosarcina thermophila B 6 pKi 1010 nM Ki Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717]
ChEMBL Inhibitory activity against alpha carbonic anhydrase (Zn-Cam) from Methanosarcina thermophila B 6.85 pKi 140 nM Ki Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717]
Carbonic anhydrase in Stylophora pistillata (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1649055] [UniProtKB: C0IX24]
ChEMBL Inhibition of Stylophora pistillata carbonic anhydrase 2 by stopped-flow CO2 hydration assay B 6.16 pKi 690 nM Ki Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801]
Carbonic anhydrase in Methanobacterium thermoautotrophicum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3926] [UniProtKB: Q50565]
ChEMBL Inhibitory activity against beta carbonic anhydrase (Cab) from Methanobacterium thermoautotrophicum B 4.41 pKi 38500 nM Ki Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717]
Carbonic anhydrase in Candida albicans (strain SC5314 / ATCC MYA-2876) (Yeast) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5337] [UniProtKB: Q5AJ71]
ChEMBL Inhibition of Candida albicans recombinant Nce103 by stopped-flow CO2 hydration assay B 5.99 pKi 1017 nM Ki Bioorg Med Chem (2009) 17: 4503-4509 [PMID:19450983]
ChEMBL Inhibition of Candida albicans CaNce103 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method B 5.99 pKi 1017 nM Ki J Med Chem (2012) 55: 3513-3520 [PMID:22424239]
Carbonic anhydrase in Candida glabrata CBS 138 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6185] [UniProtKB: Q6FTL6]
ChEMBL Inhibition of recombinant full length Candida glabrata NCE103 expressed in Escherichia coli BL21 preincubated for 15 mins by stopped-flow CO2 hydrase assay B 6.94 pKi 116 nM Ki Bioorg Med Chem Lett (2013) 23: 2647-2652 [PMID:23511020]
Carbonic anhydrase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5931] [UniProtKB: P53615]
ChEMBL Inhibition of Saccharomyces cerevisiae recombinant CA expressed in Escherichia coli by stopped-flow CO2 hydrase assay B 6.97 pKi 108 nM Ki Bioorg Med Chem (2009) 17: 1158-1163 [PMID:19124253]
Carbonic anhydrase 15 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5973] [UniProtKB: Q99N23]
ChEMBL Inhibition of mouse recombinant carbonic anhydrase 15 by stopped flow CO2 hydrase assay B 7.35 pKi 45 nM Ki J Med Chem (2009) 52: 646-654 [PMID:19193158]
ChEMBL Inhibition of mouse recombinant carbonic anhydrase 15 after 15 mins by stopped-flow CO2 hydration assay B 7.35 pKi 45 nM Ki Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094]
Carbonic anhydrase 2 in Cryptococcus neoformans var. grubii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697676] [UniProtKB: Q3I4V7]
ChEMBL Inhibition of Cryptococcus neoformans Can2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method B 5.51 pKi 3056 nM Ki J Med Chem (2012) 55: 3513-3520 [PMID:22424239]
Carbonic anhydrase, alpha family in Thiomicrospira crunogena (strain XCL-2) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3621035] [UniProtKB: Q31FD6]
ChEMBL Inhibition of recombinant Thiomicrospira crunogena XCL-2 carbonic anhydrase by stopped flow CO2 hydrase assay B 6.01 pKi 981 nM Ki Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758]
carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
ChEMBL Inhibition of full length human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stop flow CO2 hydrase assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem Lett (2016) 26: 4184-4190 [PMID:27485387]
ChEMBL Inhibitory activity against human carbonic anhydrase I at 0.09 uM B 4.3 pKi 50000 nM Ki Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717]
ChEMBL Inhibitory activity against cloned human CA1 B 4.3 pKi 50000 nM Ki Bioorg Med Chem Lett (2006) 16: 437-442 [PMID:16290146]
ChEMBL Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration method B 4.3 pKi 50000 nM Ki J Med Chem (2009) 52: 2226-2232 [PMID:19317447]
ChEMBL Inhibition of human recombinant CA1 by stopped-flow CO2 hydrase assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2009) 17: 1158-1163 [PMID:19124253]
ChEMBL Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydrase assay B 4.3 pKi 50000 nM Ki J Med Chem (2009) 52: 646-654 [PMID:19193158]
ChEMBL Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay B 4.3 pKi 50000 nM Ki J Med Chem (2009) 52: 3116-3120 [PMID:19338333]
ChEMBL Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase method B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2009) 17: 4503-4509 [PMID:19450983]
ChEMBL Inhibition of human recombinant CA1 by stopped-flow CO2 assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2009) 17: 5054-5058 [PMID:19520577]
ChEMBL Inhibition of human recombinant carbonic anhydrase 1 after 15 mins by stopped-flow CO2 hydration assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094]
ChEMBL Inhibition of wild type human recombinant carbonic anhydrase 1 expressed in Escherichia coli BL21 (DE3) after 15 mins by CO2 hydration method B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2010) 18: 5498-5503 [PMID:20624682]
ChEMBL Inhibition of human recombinant CA1 by stopped-flow CO2 hydration assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801]
ChEMBL Inhibition of human carbonic anhydrase I by spectrophotometry at pH 7.5 B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2011) 19: 1172-1178 [PMID:21251841]
ChEMBL Inhibition of human recombinant carbonic anhydrase 1 at pH 7.5 by stopped flow CO2 hydration assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2011) 19: 5023-5030 [PMID:21757360]
ChEMBL Inhibition of human carbonic anhydrase 1-catalyzed CO2 hydration activity by stopped flow assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem Lett (2011) 21: 5892-5896 [PMID:21852133]
ChEMBL Inhibition of human recombinant carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2012) 20: 1403-1410 [PMID:22285172]
ChEMBL Inhibition of human recombinant full length CA1 pre-incubated for 15 mins by stopped-flow CO2 hydration method B 4.3 pKi 50000 nM Ki J Med Chem (2012) 55: 9619-9629 [PMID:23067387]
ChEMBL Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydrase assay B 4.3 pKi 50000 nM Ki J Med Chem (2012) 55: 10742-10748 [PMID:23181552]
ChEMBL Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay B 4.3 pKi 50000 nM Ki J Med Chem (2013) 56: 1761-1771 [PMID:23391336]
ChEMBL Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration stopped-flow assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2013) 21: 1534-1538 [PMID:22883029]
ChEMBL Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2013) 21: 5168-5174 [PMID:23867389]
ChEMBL Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2013) 21: 5973-5982 [PMID:23965175]
ChEMBL Inhibition of human cytosolic carbonic anhydrase 1 by stopped-flow CO2 hydration assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2014) 22: 1586-1595 [PMID:24513184]
ChEMBL Inhibition of human carbonic anhydrase-1 by stopped-flow CO2 hydration assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2014) 22: 2939-2946 [PMID:24792813]
ChEMBL Inhibition of human recombinant Carbonic anhydrase 1 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2014) 22: 4537-4543 [PMID:25129169]
ChEMBL Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydration assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2015) 23: 526-531 [PMID:25533402]
ChEMBL Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydrase assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2015) 23: 1728-1734 [PMID:25773015]
ChEMBL Inhibition of human carbonic anhydrase 1 pre-incubated for 15 mins by stopped-flow CO2 hydration assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2015) 23: 2303-2309 [PMID:25882523]
ChEMBL Inhibition of human recombinant CA-1 after 15 mins by stopped-flow CO2 hydrase assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2015) 23: 1828-1840 [PMID:25766630]
ChEMBL Inhibition of human CA1 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem Lett (2015) 25: 5485-5489 [PMID:26525863]
ChEMBL Inhibition of recombinant human carbonic anhydrase-1 by stopped flow CO2 hydrase assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758]
ChEMBL Inhibition of human Carbonic anhydrase1 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2016) 24: 1115-1120 [PMID:26850377]
ChEMBL Inhibition of human carbonic anhydrase 1 incubated for 15 mins by stopped-flow CO2 hydration assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem Lett (2016) 26: 1821-1826 [PMID:26920803]
ChEMBL Inhibition of recombinant human carbonic anhydrase 1 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis B 4.3 pKi 50000 nM Ki Bioorg Med Chem Lett (2017) 27: 490-495 [PMID:28025002]
ChEMBL Inhibitory activity against human carbonic anhydrase I (hCAI) B 4.3 pKi 50000 nM Ki Bioorg Med Chem Lett (2005) 15: 1149-1154 [PMID:15686931]
ChEMBL Inhibition of human carbonic anhydrase-1 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay B 4.3 pKi 50000 nM Ki Bioorg Med Chem (2017) 25: 3555-3561 [PMID:28511911]
ChEMBL Inhibition of recombinant human cytosolic carbonic anhydrase 1 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay B 5 pKi >10000 nM Ki Bioorg Med Chem (2017) 25: 2210-2217 [PMID:28256371]
ChEMBL Inhibitory activity against human carbonic anhydrase I was determined B 4.3 pIC50 50000 nM IC50 J Med Chem (2004) 47: 550-557 [PMID:14736236]
ChEMBL Inhibitory activity of compound against human carbonic anhydrase I F 4.3 pIC50 50000 nM IC50 Bioorg Med Chem Lett (2004) 14: 337-341 [PMID:14698154]
ChEMBL Inhibitory concentration against carbonic anhydrase I B 5 pIC50 >10000 nM IC50 J Med Chem (2005) 48: 6523-6543 [PMID:16220969]
carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
ChEMBL Inhibitory activity against human carbonic anhydrase II at 0.01 uM B 4.68 pKi 21000 nM Ki Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717]
ChEMBL Inhibition of human wild type carbonic anhydrase 2 Asn67Ile mutant expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay B 6.38 pKi 421 nM Ki Bioorg Med Chem (2012) 20: 2208-2213 [PMID:22386980]
ChEMBL Inhibition of human wild type carbonic anhydrase 2 Gln92Val mutant expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay B 7.11 pKi 76.8 nM Ki Bioorg Med Chem (2012) 20: 2208-2213 [PMID:22386980]
ChEMBL Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration method B 7.68 pKi 21 nM Ki J Med Chem (2009) 52: 2226-2232 [PMID:19317447]
ChEMBL Inhibition of human recombinant CA2 by stopped-flow CO2 hydrase assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2009) 17: 1158-1163 [PMID:19124253]
ChEMBL Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay B 7.68 pKi 21 nM Ki J Med Chem (2009) 52: 646-654 [PMID:19193158]
ChEMBL Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay B 7.68 pKi 21 nM Ki J Med Chem (2009) 52: 3116-3120 [PMID:19338333]
ChEMBL Inhibition of Helicobacter pylori beta-carbonic anhydrase by stopped-flow CO2 hydration assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2009) 17: 4503-4509 [PMID:19450983]
ChEMBL Inhibition of human recombinant CA2 by stopped-flow CO2 assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2009) 17: 5054-5058 [PMID:19520577]
ChEMBL Inhibition of human recombinant CA2 by stopped-flow hydration assay B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2009) 19: 6649-6654 [PMID:19846301]
ChEMBL Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by stopped-flow CO2 hydration assay B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094]
ChEMBL Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by CO2 hydration method B 7.68 pKi 21 nM Ki Bioorg Med Chem (2010) 18: 5498-5503 [PMID:20624682]
ChEMBL Inhibition of human recombinant CA2 by stopped-flow CO2 hydration assay B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801]
ChEMBL Inhibition of human carbonic anhydrase II by spectrophotometry at pH 7.5 B 7.68 pKi 21 nM Ki Bioorg Med Chem (2011) 19: 1172-1178 [PMID:21251841]
ChEMBL Inhibition of human recombinant carbonic anhydrase 2 at pH 7.5 by stopped flow CO2 hydration assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2011) 19: 5023-5030 [PMID:21757360]
ChEMBL Inhibition of human carbonic anhydrase 2-catalyzed CO2 hydration activity by stopped flow assay B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2011) 21: 5892-5896 [PMID:21852133]
ChEMBL Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2012) 20: 1403-1410 [PMID:22285172]
ChEMBL Inhibition of human carbonic anhydrase 2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method B 7.68 pKi 21 nM Ki J Med Chem (2012) 55: 3513-3520 [PMID:22424239]
ChEMBL Inhibition of human recombinant full length CA2 pre-incubated for 15 mins by stopped-flow CO2 hydration method B 7.68 pKi 21 nM Ki J Med Chem (2012) 55: 9619-9629 [PMID:23067387]
ChEMBL Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydrase assay B 7.68 pKi 21 nM Ki J Med Chem (2012) 55: 10742-10748 [PMID:23181552]
ChEMBL Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay B 7.68 pKi 21 nM Ki J Med Chem (2013) 56: 1761-1771 [PMID:23391336]
ChEMBL Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2013) 21: 1534-1538 [PMID:22883029]
ChEMBL Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2013) 21: 5168-5174 [PMID:23867389]
ChEMBL Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2013) 21: 5973-5982 [PMID:23965175]
ChEMBL Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2014) 24: 275-279 [PMID:24314394]
ChEMBL Inhibition of human cytosolic carbonic anhydrase 2 by stopped-flow CO2 hydration assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2014) 22: 1586-1595 [PMID:24513184]
ChEMBL Inhibition of human carbonic anhydrase-2 by stopped-flow CO2 hydration assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2014) 22: 2939-2946 [PMID:24792813]
ChEMBL Inhibition of human recombinant Carbonic anhydrase 2 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method B 7.68 pKi 21 nM Ki Bioorg Med Chem (2014) 22: 4537-4543 [PMID:25129169]
ChEMBL Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydration assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2015) 23: 526-531 [PMID:25533402]
ChEMBL Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2015) 23: 1728-1734 [PMID:25773015]
ChEMBL Inhibition of human carbonic anhydrase 2 pre-incubated for 15 mins by stopped-flow CO2 hydration assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2015) 23: 2303-2309 [PMID:25882523]
ChEMBL Inhibition of human recombinant CA-2 after 15 mins by stopped-flow CO2 hydrase assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2015) 23: 1828-1840 [PMID:25766630]
ChEMBL Inhibition of human recombinant carbonic anhydrase-2 by stopped flow CO2 hydrase assay method B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2015) 25: 3550-3555 [PMID:26174556]
ChEMBL Inhibition of human CA2 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2015) 25: 5485-5489 [PMID:26525863]
ChEMBL Inhibition of recombinant human carbonic anhydrase-2 by stopped flow CO2 hydrase assay B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758]
ChEMBL Inhibition of human Carbonic anhydrase2 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2016) 24: 1115-1120 [PMID:26850377]
ChEMBL Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydrase stopped flow assay B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2016) 26: 1253-1259 [PMID:26832216]
ChEMBL Inhibition of human carbonic anhydrase 2 incubated for 15 mins by stopped-flow CO2 hydration assay B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2016) 26: 1821-1826 [PMID:26920803]
ChEMBL Inhibition of human carbonic anhydrase 2 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2017) 27: 490-495 [PMID:28025002]
ChEMBL Inhibition of recombinant human carbonic anhydrase 2 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2017) 25: 2210-2217 [PMID:28256371]
ChEMBL Inhibition of human carbonic anhydrase-2 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay B 7.68 pKi 21 nM Ki Bioorg Med Chem (2017) 25: 3555-3561 [PMID:28511911]
ChEMBL Inhibitory activity against human carbonic anhydrase II (hCAII) B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2005) 15: 1149-1154 [PMID:15686931]
ChEMBL Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stop flow CO2 hydrase assay B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2016) 26: 4184-4190 [PMID:27485387]
ChEMBL Inhibition of cloned human carbonic anhydrase II B 7.68 pKi 21 nM Ki J Med Chem (2005) 48: 5721-5727 [PMID:16134940]
ChEMBL Inhibitory activity against cloned human CA2 B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2006) 16: 437-442 [PMID:16290146]
ChEMBL DRUGMATRIX: Carbonic Anhydrase II enzyme inhibition (substrate: 4-Nitrophenyl acetate (4-NPA)) B 6.74 pIC50 181 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibitory activity against human carbonic anhydrase II was determined B 7.68 pIC50 21 nM IC50 J Med Chem (2004) 47: 550-557 [PMID:14736236]
ChEMBL Inhibitory activity of compound against human carbonic anhydrase II F 7.68 pIC50 21 nM IC50 Bioorg Med Chem Lett (2004) 14: 337-341 [PMID:14698154]
ChEMBL Inhibitory concentration against carbonic anhydrase II B 7.68 pIC50 21 nM IC50 J Med Chem (2005) 48: 6523-6543 [PMID:16220969]
Carbonic anhydrase III in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2885] [UniProtKB: P07451]
ChEMBL Inhibition of human recombinant carbonic anhydrase 3 after 15 mins by stopped-flow CO2 hydration assay B 4.15 pKi 70000 nM Ki Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094]
ChEMBL Inhibition of human recombinant full length CA3 pre-incubated for 15 mins by stopped-flow CO2 hydration method B 5.13 pKi 7400 nM Ki J Med Chem (2012) 55: 9619-9629 [PMID:23067387]
carbonic anhydrase 4/Carbonic anhydrase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748]
ChEMBL Inhibitory activity against human carbonic anhydrase IV (hCAIV) B 6.06 pKi 880 nM Ki Bioorg Med Chem Lett (2005) 15: 1149-1154 [PMID:15686931]
ChEMBL Inhibition of human recombinant carbonic anhydrase 4 after 15 mins by stopped-flow CO2 hydration assay B 6.06 pKi 880 nM Ki Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094]
ChEMBL Inhibition of human recombinant full length CA4 pre-incubated for 15 mins by stopped-flow CO2 hydration method B 6.06 pKi 880 nM Ki J Med Chem (2012) 55: 9619-9629 [PMID:23067387]
ChEMBL Inhibition of recombinant human membrane-associated carbonic anhydrase 4 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay B 6.54 pKi 290 nM Ki Bioorg Med Chem (2017) 25: 2210-2217 [PMID:28256371]
Carbonic anhydrase IV in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL281] [UniProtKB: Q95323]
ChEMBL Inhibitory activity against bovine carbonic anhydrase IV (bCAIV) B 6.54 pKi 290 nM Ki Bioorg Med Chem Lett (2005) 15: 1149-1154 [PMID:15686931]
ChEMBL Inhibitory activity against CA4 isolated from bovine lung microsomes B 6.54 pKi 290 nM Ki Bioorg Med Chem Lett (2006) 16: 437-442 [PMID:16290146]
ChEMBL Inhibitory activity against bovine carbonic anhydrase IV was determined B 6.54 pIC50 290 nM IC50 J Med Chem (2004) 47: 550-557 [PMID:14736236]
ChEMBL Inhibitory activity of compound against bovine carbonic anhydrase IV F 6.54 pIC50 290 nM IC50 Bioorg Med Chem Lett (2004) 14: 337-341 [PMID:14698154]
carbonic anhydrase 9/Carbonic anhydrase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
ChEMBL Inhibitory activity against human carbonic anhydrase IX at 0.09 uM B 4.8 pKi 16000 nM Ki Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717]
ChEMBL Inhibition of recombinant human tumor-associated carbonic anhydrase 9 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay B 7.7 pKi 20 nM Ki Bioorg Med Chem (2017) 25: 2210-2217 [PMID:28256371]
ChEMBL Inhibitory activity against cloned human CA9 B 7.8 pKi 16 nM Ki Bioorg Med Chem Lett (2006) 16: 437-442 [PMID:16290146]
ChEMBL Inhibition of human recombinant carbonic anhydrase 9 catalytic domain by stopped flow CO2 hydrase assay B 7.8 pKi 16 nM Ki J Med Chem (2009) 52: 646-654 [PMID:19193158]
ChEMBL Inhibition of human recombinant carbonic anhydrase 9 after 15 mins by stopped-flow CO2 hydration assay B 7.8 pKi 16 nM Ki Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094]
ChEMBL Inhibition of human carbonic anhydrase 9-catalyzed CO2 hydration activity by stopped flow assay B 7.8 pKi 16 nM Ki Bioorg Med Chem Lett (2011) 21: 5892-5896 [PMID:21852133]
ChEMBL Inhibition of human recombinant CA9 catalytic domain pre-incubated for 15 mins by stopped-flow CO2 hydration method B 7.8 pKi 16 nM Ki J Med Chem (2012) 55: 9619-9629 [PMID:23067387]
ChEMBL Inhibition of human membrane bound carbonic anhydrase 9 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay B 7.8 pKi 16 nM Ki Bioorg Med Chem (2013) 21: 5973-5982 [PMID:23965175]
ChEMBL Inhibition of human transmembrane carbonic anhydrase 9 by stopped-flow CO2 hydration assay B 7.8 pKi 16 nM Ki Bioorg Med Chem (2014) 22: 1586-1595 [PMID:24513184]
ChEMBL Inhibition of human recombinant CA-9 after 15 mins by stopped-flow CO2 hydrase assay B 7.8 pKi 16 nM Ki Bioorg Med Chem (2015) 23: 1828-1840 [PMID:25766630]
ChEMBL Inhibition of catalytic domain of human recombinant carbonic anhydrase IX B 7.8 pKi 16 nM Ki J Med Chem (2005) 48: 5721-5727 [PMID:16134940]
ChEMBL Inhibitory activity against human carbonic anhydrase IX was determined B 7.8 pIC50 16 nM IC50 J Med Chem (2004) 47: 550-557 [PMID:14736236]
ChEMBL Inhibitory concentration against carbonic anhydrase IX B 7.8 pIC50 16 nM IC50 J Med Chem (2005) 48: 6523-6543 [PMID:16220969]
carbonic anhydrase 5A/Carbonic anhydrase VA in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218]
ChEMBL Inhibition of human recombinant carbonic anhydrase 5a after 15 mins by stopped-flow CO2 hydration assay B 6.1 pKi 794 nM Ki Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094]
ChEMBL Inhibition of human recombinant full length CA5A pre-incubated for 15 mins by stopped-flow CO2 hydration method B 6.1 pKi 794 nM Ki J Med Chem (2012) 55: 9619-9629 [PMID:23067387]
Carbonic anhydrase VB in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3969] [UniProtKB: Q9Y2D0]
ChEMBL Inhibition of human recombinant carbonic anhydrase 5b after 15 mins by stopped-flow CO2 hydration assay B 7.03 pKi 93 nM Ki Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094]
ChEMBL Inhibition of human recombinant full length CA5B pre-incubated for 15 mins by stopped-flow CO2 hydration method B 7.03 pKi 93 nM Ki J Med Chem (2012) 55: 9619-9629 [PMID:23067387]
Carbonic anhydrase VI in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3025] [UniProtKB: P23280]
ChEMBL Inhibition of human full length recombinant carbonic anhydrase 6 by stopped flow CO2 hydrase assay B 7.03 pKi 94 nM Ki J Med Chem (2009) 52: 646-654 [PMID:19193158]
ChEMBL Inhibition of human recombinant carbonic anhydrase 6 after 15 mins by stopped-flow CO2 hydration assay B 7.03 pKi 94 nM Ki Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094]
ChEMBL Inhibition of human recombinant full length CA6 pre-incubated for 15 mins by stopped-flow CO2 hydration method B 7.03 pKi 94 nM Ki J Med Chem (2012) 55: 9619-9629 [PMID:23067387]
carbonic anhydrase 7/Carbonic anhydrase VII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166]
ChEMBL Inhibition of human recombinant carbonic anhydrase 7 after 15 mins by stopped-flow CO2 hydration assay B 5.66 pKi 2170 nM Ki Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094]
ChEMBL Inhibition of human recombinant full length CA7 pre-incubated for 15 mins by stopped-flow CO2 hydration method B 5.66 pKi 2170 nM Ki J Med Chem (2012) 55: 9619-9629 [PMID:23067387]
ChEMBL Inhibition of human cytosolic carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay B 5.66 pKi 2170 nM Ki Bioorg Med Chem (2013) 21: 5168-5174 [PMID:23867389]
ChEMBL Inhibition of human cytosolic carbonic anhydrase 7 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay B 5.66 pKi 2170 nM Ki Bioorg Med Chem (2013) 21: 5973-5982 [PMID:23965175]
ChEMBL Inhibition of human recombinant carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay B 5.66 pKi 2170 nM Ki Eur J Med Chem (2014) 71: 105-111 [PMID:24287559]
ChEMBL Inhibition of human recombinant CA-7 after 15 mins by stopped-flow CO2 hydrase assay B 5.66 pKi 2170 nM Ki Bioorg Med Chem (2015) 23: 1828-1840 [PMID:25766630]
carbonic anhydrase 12/Carbonic anhydrase XII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
GtoPdb - - 7.74 pKi 18 nM Ki Bioorg Med Chem (2013) 21: 5973-82 [PMID:23965175]
ChEMBL Inhibitory activity against cloned human CA12 B 7.74 pKi 18 nM Ki Bioorg Med Chem Lett (2006) 16: 437-442 [PMID:16290146]
ChEMBL Inhibition of human recombinant carbonic anhydrase 12 after 15 mins by stopped-flow CO2 hydration assay B 7.74 pKi 18 nM Ki Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094]
ChEMBL Inhibition of human carbonic anhydrase 12-catalyzed CO2 hydration activity by stopped flow assay B 7.74 pKi 18 nM Ki Bioorg Med Chem Lett (2011) 21: 5892-5896 [PMID:21852133]
ChEMBL Inhibition of human recombinant CA12 catalytic domain pre-incubated for 15 mins by stopped-flow CO2 hydration method B 7.74 pKi 18 nM Ki J Med Chem (2012) 55: 9619-9629 [PMID:23067387]
ChEMBL Inhibition of human membrane bound carbonic anhydrase 12 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay B 7.74 pKi 18 nM Ki Bioorg Med Chem (2013) 21: 5973-5982 [PMID:23965175]
ChEMBL Inhibition of human transmembrane carbonic anhydrase 12 by stopped-flow CO2 hydration assay B 7.74 pKi 18 nM Ki Bioorg Med Chem (2014) 22: 1586-1595 [PMID:24513184]
ChEMBL Inhibition of human recombinant CA-12 after 15 mins by stopped-flow CO2 hydrase assay B 7.74 pKi 18 nM Ki Bioorg Med Chem (2015) 23: 1828-1840 [PMID:25766630]
carbonic anhydrase 13/Carbonic anhydrase XIII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3912] [GtoPdb: 2748] [UniProtKB: Q8N1Q1]
ChEMBL Inhibition of human recombinant carbonic anhydrase 13 after 15 mins by stopped-flow CO2 hydration assay B 7.01 pKi 98 nM Ki Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094]
ChEMBL Inhibition of human recombinant CA13 catalytic domain pre-incubated for 15 mins by stopped-flow CO2 hydration method B 7.01 pKi 98 nM Ki J Med Chem (2012) 55: 9619-9629 [PMID:23067387]
carbonic anhydrase 14/Carbonic anhydrase XIV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3510] [GtoPdb: 2598] [UniProtKB: Q9ULX7]
ChEMBL Inhibition of human recombinant carbonic anhydrase 14 after 15 mins by stopped-flow CO2 hydration assay B 6.16 pKi 689 nM Ki Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094]
ChEMBL Inhibition of human recombinant CA14 catalytic domain pre-incubated for 15 mins by stopped-flow CO2 hydration method B 6.16 pKi 689 nM Ki J Med Chem (2012) 55: 9619-9629 [PMID:23067387]
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL Inhibition of human platelets COX1 after 2 mins B 4 pIC50 >100000 nM IC50 Eur J Med Chem (2010) 45: 6027-6038 [PMID:20970223]
ChEMBL Compound was tested for the inhibition of recombinant human Prostaglandin G/H synthase 1 (COX-1) B 4 pIC50 <100000 nM IC50 J Med Chem (2003) 46: 5484-5504 [PMID:14640557]
ChEMBL Inhibition of human COX1 expressed in sf9 cells B 4 pIC50 >100000 nM IC50 J Nat Prod (2005) 68: 1514-1518 [PMID:16252917]
ChEMBL Inhibition of human platelet COX1 B 4 pIC50 >100000 nM IC50 Eur J Med Chem (2008) 43: 456-463 [PMID:17532544]
ChEMBL Inhibition of COX1 in human OVCAR-3 cells assessed as reduction in PGE2 level incubated for 30 mins by ELISA B 4.09 pIC50 80900 nM IC50 ACS Med Chem Lett (2021) 12: 798-804 [PMID:34055228]
ChEMBL Inhibition of human COX1 using arachidonic acid assessed as production of PGF2alpha after 5 mins by ELISA B 4.36 pIC50 43370 nM IC50 Bioorg Med Chem Lett (2016) 26: 3491-3498 [PMID:27349331]
ChEMBL Inhibition of COX1 (unknown origin) assessed as reduction in PGE2 level using arachidonic acid as substrate after 5 mins in presence of heme by ELISA B 4.44 pIC50 36440 nM IC50 Bioorg Med Chem Lett (2017) 27: 3653-3660 [PMID:28720504]
ChEMBL Inhibition of human recombinant COX1 by ELISA B 4.49 pIC50 32600 nM IC50 Bioorg Med Chem Lett (2015) 25: 1947-1951 [PMID:25866240]
ChEMBL Inhibition of human COX1 using arachidonic acid as substrate incubated for 2 mins by ELISA method B 4.56 pIC50 27830 nM IC50 Eur J Med Chem (2020) 185: 111780-111780 [PMID:31655429]
ChEMBL Inhibition of COX1 by chemiluminescent enzyme assay B 4.56 pIC50 27500 nM IC50 Bioorg Med Chem (2011) 19: 6827-6832 [PMID:22000948]
ChEMBL Inhibition of COX-1 (unknown origin) by chemiluminescence assay B 4.56 pIC50 27500 nM IC50 Eur J Med Chem (2013) 62: 222-231 [PMID:23353741]
ChEMBL Inhibition of human Prostaglandin G/H synthase 1 B 4.57 pIC50 27000 nM IC50 J Med Chem (2002) 45: 1511-1517 [PMID:11906292]
ChEMBL Inhibitory effect on Prostaglandin G/H synthase 1 activity was evaluated in human whole blood as TXB2 production F 4.58 pIC50 26400 nM IC50 J Med Chem (2002) 45: 1402-1411 [PMID:11906281]
ChEMBL Inhibition of COX1 (unknown origin) B 4.59 pIC50 25740 nM IC50 Eur J Med Chem (2013) 70: 579-588 [PMID:24211633]
ChEMBL Inhibition of COX1 (unknown origin) B 4.6 pIC50 25390 nM IC50 Bioorg Med Chem Lett (2017) 27: 1017-1025 [PMID:28089698]
ChEMBL Inhibition of COX1 (unknown origin) using arachidonic acid as substrate incubated for 10 mins by Ellman's reagent based COX-1/COX-2 ELISA assay B 4.61 pIC50 24470 nM IC50 Eur J Med Chem (2019) 169: 168-184 [PMID:30877972]
ChEMBL Inhibition of COX1 B 4.61 pIC50 24300 nM IC50 Bioorg Med Chem Lett (2007) 17: 5634-5637 [PMID:17822894]
ChEMBL Inhibition of COX1 in human whole blood assessed as effect on A-23187-stimulated TxB2 production B 4.63 pIC50 23470 nM IC50 Bioorg Med Chem (2008) 16: 2697-2706 [PMID:18063374]
ChEMBL Colorimetric Assay: The activities of COX-1 and COX-2 were measured after the addition of arachidonic acid and incubation at 25° C. for 5 min by absorbance at 590 nm as specified by the manufacturer. B 4.64 pIC50 23000 nM IC50 US-9388139-B2. Derivatives of celeboxib, use thereof and preparation thereof (2016)
ChEMBL Inhibitory concentration against Prostaglandin G/H synthase 1 B 4.64 pIC50 22900 nM IC50 J Med Chem (2001) 44: 3039-3042 [PMID:11520213]
ChEMBL Inhibition of human Prostaglandin G/H synthase 1 B 4.64 pIC50 22900 nM IC50 J Med Chem (2001) 44: 2921-2927 [PMID:11520200]
ChEMBL In vitro inhibitory concentration of compound required to inhibit Prostaglandin G/H synthase 1 enzyme was determined B 4.64 pIC50 22900 nM IC50 Bioorg Med Chem Lett (2002) 12: 2753-2756 [PMID:12217369]
ChEMBL Inhibition of COX-1 (unknown origin) B 4.69 pIC50 20400 nM IC50 Eur J Med Chem (2014) 81: 204-217 [PMID:24836072]
ChEMBL Inhibition of COX1 assessed as TBX2 production in human whole blood F 4.7 pIC50 20030 nM IC50 Bioorg Med Chem Lett (2006) 16: 4440-4443 [PMID:16814546]
ChEMBL Inhibition of COX-1 (unknown origin) assessed as reduction in PGH2 formation using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by enzyme immunoassay B 4.7 pIC50 19880 nM IC50 Bioorg Med Chem Lett (2021) 33: 127743-127743 [PMID:33316405]
ChEMBL Inhibition of COX1 in human whole blood assessed as inhibition of LPS-stimulated PGE2 production by radioimmunoassay B 4.8 pIC50 16000 nM IC50 Bioorg Med Chem (2008) 16: 8072-8081 [PMID:18752957]
GtoPdb - - 4.82 pIC50 15000 nM IC50 Eur J Med Chem (2017) 141: 306-321 [PMID:29031075];
J Med Chem (1997) 40: 1347-65 [PMID:9135032]
ChEMBL Inhibition of COX1 (unknown origin) by solid phase ELISA method B 4.82 pIC50 15030 nM IC50 Bioorg Med Chem (2014) 22: 4109-4118 [PMID:24934992]
ChEMBL In Vitro activity of compound against human recombinant Prostaglandin G/H synthase 1 B 4.82 pIC50 15000 nM IC50 J Med Chem (2000) 43: 775-777 [PMID:10715145]
ChEMBL In Vitro activity of compound against human recombinant Prostaglandin G/H synthase 1 B 4.82 pIC50 15000 nM IC50 J Med Chem (2000) 43: 775-777 [PMID:10715145]
ChEMBL Inhibition of human COX1 using arachidonic acid as substrate assessed as PGE2 formation incubated for 10 mins prior to substrate addition measured after 10 mins by ELISA B 4.82 pIC50 15000 nM IC50 Eur J Med Chem (2014) 76: 494-505 [PMID:24602792]
ChEMBL Inhibition of human Prostaglandin G/H synthase 1 B 4.82 pIC50 15000 nM IC50 Bioorg Med Chem Lett (1999) 9: 1171-1174 [PMID:10328307]
ChEMBL In vitro inhibitory concentration required to block recombinant human prostaglandin G/H synthase 1 (COX-1) B 4.82 pIC50 15000 nM IC50 J Med Chem (1997) 40: 1347-1365 [PMID:9135032]
ChEMBL Inhibition of COX1 B 4.82 pIC50 15000 nM IC50 J Med Chem (2012) 55: 2287-2300 [PMID:22263894]
ChEMBL Inhibition of human COX1 B 4.82 pIC50 15000 nM IC50 Bioorg Med Chem Lett (2011) 21: 993-996 [PMID:21215625]
ChEMBL Inhibition of COX1 in human whole blood assessed as reduction in calcium ionophore-stimulated TXB2 production incubated for 1 hr by ELISA B 4.83 pIC50 14800 nM IC50 J Med Chem (2021) 64: 11570-11596 [PMID:34279934]
ChEMBL Inhibitory activity against prostaglandin G/H synthase 1 B 4.85 pIC50 14200 nM IC50 J Med Chem (2000) 43: 214-223 [PMID:10649977]
ChEMBL In vitro inhibitory concentration against Prostaglandin G/H synthase 1 (COX-1) in human whole blood B 4.85 pIC50 14000 nM IC50 J Med Chem (2005) 48: 3930-3934 [PMID:15916445]
ChEMBL Compound was tested for the inhibition of human Prostaglandin G/H synthase 1 (COX-1) in human whole blood B 4.85 pIC50 14000 nM IC50 J Med Chem (2003) 46: 5484-5504 [PMID:14640557]
ChEMBL Compound was evaluated for inhibition concentration of prostaglandin G/H synthase 1 in human blood B 4.85 pIC50 14000 nM IC50 J Med Chem (2004) 47: 2180-2193 [PMID:15084117]
ChEMBL In vitro inhibition of Prostaglandin G/H synthase 1 in human whole blood B 4.85 pIC50 14000 nM IC50 Bioorg Med Chem Lett (2004) 14: 6049-6052 [PMID:15546727]
ChEMBL Inhibition of COX1 in human whole blood assessed as TxB2 production after 1 hr B 4.85 pIC50 14000 nM IC50 J Med Chem (2007) 50: 1449-1457 [PMID:17335184]
ChEMBL Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production B 4.85 pIC50 14000 nM IC50 J Med Chem (2007) 50: 6367-6382 [PMID:17994684]
ChEMBL Inhibition of COX1 B 4.85 pIC50 14000 nM IC50 Eur J Med Chem (2008) 43: 2792-2799 [PMID:18262309]
ChEMBL Inhibition of COX1 expressed in CHO cells assessed as inhibition of arachidonic acid-stimulated PGE2 production by enzyme immunoassay F 4.87 pIC50 13500 nM IC50 J Med Chem (2004) 47: 6195-6206 [PMID:15566290]
ChEMBL Inhibition of COX1 in human whole blood assessed as inhibition of 12-hydroxyheptadecatrienoic acid production by HPLC method B 4.88 pIC50 13100 nM IC50 Bioorg Med Chem (2010) 18: 3910-3924 [PMID:20451397]
ChEMBL Inhibition of COX1 in human whole blood assessed as thromboxane B2 production by RIA B 4.9 pIC50 12500 nM IC50 J Med Chem (2010) 53: 723-733 [PMID:19957931]
ChEMBL Inhibition of COX1 in human whole blood assessed as TXB2 production B 4.9 pIC50 12500 nM IC50 J Med Chem (2007) 50: 5403-5411 [PMID:17915854]
ChEMBL Inhibition of platelet COX1-mediated TXB2 production in LPS-induced human whole blood after 60 mins by radioimmunoassay B 4.9 pIC50 12470 nM IC50 J Med Chem (2011) 54: 7759-7771 [PMID:21992176]
ChEMBL Inhibition of COX-1 in human whole blood assessed as thromboxane B2 production by RIA B 4.9 pIC50 12470 nM IC50 Bioorg Med Chem (2014) 22: 772-786 [PMID:24373735]
ChEMBL In vitro inhibitory activity against recombinant human Prostaglandin G/H synthase 1 B 4.97 pIC50 10700 nM IC50 Bioorg Med Chem Lett (2003) 13: 1639-1643 [PMID:12729631]
ChEMBL Inhibition of COX1 in human whole blood assessed as inhibition of lipopolysaccharide-induced TxB2 production after 30 min by enzyme immunoassay B 4.99 pIC50 10194 nM IC50 Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573]
ChEMBL Inhibition of COX-1 by chemiluminescent assay B 5 pIC50 10000 nM IC50 Bioorg Med Chem (2012) 20: 6648-6654 [PMID:23062711]
ChEMBL Biochemical index for Prostaglandin G/H synthase 1 measured as, thromboxane 2 (TXB2) levels following blood coagulation B 5.01 pIC50 9730 nM IC50 Bioorg Med Chem Lett (2000) 10: 1745-1748 [PMID:10937738]
ChEMBL Inhibition of COX1 by enzyme immunoassay B 5.11 pIC50 7700 nM IC50 Bioorg Med Chem (2009) 17: 1146-1151 [PMID:19157881]
ChEMBL Inhibition of human whole blood COX-1 assessed as production of TXB2 after 24 hrs by EIA B 5.15 pIC50 7000 nM IC50 Bioorg Med Chem (2011) 19: 3299-3311 [PMID:21570308]
ChEMBL Inhibition of COX1 in human blood assessed as PGE2 level incubated for 15 mins prior to LPS-challenge measured after 24 hrs by enzyme immunoassay B 5.18 pIC50 6650 nM IC50 Bioorg Med Chem (2013) 21: 2355-2362 [PMID:23473947]
ChEMBL Inhibitory concentration was measured against Prostaglandin G/H synthase 1 in human whole blood B 5.2 pIC50 6300 nM IC50 Bioorg Med Chem Lett (2003) 13: 1195-1198 [PMID:12643942]
ChEMBL In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 1 B 5.2 pIC50 6300 nM IC50 Bioorg Med Chem Lett (1999) 9: 1773-1778 [PMID:10406640]
ChEMBL Inhibitory activity against Prostaglandin G/H synthase 1 in human whole blood B 5.2 pIC50 6300 nM IC50 Bioorg Med Chem Lett (1999) 9: 2207-2212 [PMID:10465547]
ChEMBL In vitro potency against human Prostaglandin G/H synthase 1 (hCOX-1) in the human whole blood assay. B 5.2 pIC50 6300 nM IC50 J Med Chem (1999) 42: 1274-1281 [PMID:10197970]
ChEMBL In vitro inhibitory potency against human COX-1 (HWB COX-2) by whole blood assay B 5.2 pIC50 6300 nM IC50 Bioorg Med Chem Lett (1999) 9: 3181-3186 [PMID:10576684]
ChEMBL Inhibition of Prostaglandin G/H synthase 1 in U-937 cells from human histiocytic lymphoma B 5.29 pIC50 5100 nM IC50 J Med Chem (2001) 44: 350-361 [PMID:11462976]
ChEMBL In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells B 5.29 pIC50 5100 nM IC50 J Med Chem (2003) 46: 3463-3475 [PMID:12877584]
ChEMBL Inhibition of COX-1 in human whole blood assessed as thromboxane B2 level in serum after 5 mins by enzyme immunoassay B 5.59 pIC50 2600 nM IC50 Eur J Med Chem (2014) 74: 12-22 [PMID:24440378]
ChEMBL Inhibition of COX1 in human whole blood assessed as inhibition of calcium ionophore A-23187-stimulated platelet aggregation by measuring TXB2 production B 5.59 pIC50 2600 nM IC50 J Med Chem (2004) 47: 6749-6759 [PMID:15615524]
ChEMBL Inhibition of COX1 in human whole blood assessed as TXB2 production by enzyme immunoassay B 5.59 pIC50 2600 nM IC50 J Med Chem (2009) 52: 5864-5871 [PMID:19791801]
ChEMBL Inhibition of arachidonic acid induced TXB2 generation in isolated human platelets (Prostaglandin G/H synthase 1 cell assay) F 5.7 pIC50 2000 nM IC50 J Med Chem (2002) 45: 1402-1411 [PMID:11906281]
ChEMBL In vitro inhibition of cyclooxygenase-1 by inhibition of TXB2 generation with 1 uM arachidonic acid in human platelets F 5.73 pIC50 1880 nM IC50 Bioorg Med Chem Lett (2002) 12: 533-537 [PMID:11844666]
ChEMBL Inhibition of human COX1 expressed in african green monkey COS cells assessed as inhibition of arachidonic acid-stimulated PGE2 treated 1 hr before arachidonic acid challenge by enzyme immunoassay B 5.77 pIC50 1689 nM IC50 Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573]
ChEMBL Inhibition of human cyclooxygenase-1 expressed in COS cells B 5.77 pIC50 1689 nM IC50 Bioorg Med Chem Lett (2004) 14: 5445-5448 [PMID:15454242]
ChEMBL Inhibition of human COX1 expressed in baculovirus-infected SF9 cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay B 6 pIC50 >1000 nM IC50 Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) B 6.14 pIC50 723 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of human recombinant COX1 assessed as reduction in PGF2alpha formation using arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition for 30 secs and measured after 1 hr by microplate reader based enzyme immunoassay B 6.88 pIC50 131.97 nM IC50 Eur J Med Chem (2019) 171: 332-342 [PMID:30928706]
ChEMBL Inhibition of COX1 (unknown origin) using arachidonic acid as substrate pretreated for 10 mins followed by substrate addition measured after 2 mins by enzyme-immunoassay B 6.9 pIC50 125 nM IC50 Bioorg Med Chem Lett (2017) 27: 2377-2383 [PMID:28427813]
ChEMBL In vitro inhibitory potency against U-937 microsomal COX-1 B 7.3 pIC50 50 nM IC50 Bioorg Med Chem Lett (1999) 9: 3181-3186 [PMID:10576684]
ChEMBL Inhibition of COX-1 in U-937 (human lymphoma) cell microsomes. B 7.3 pIC50 50 nM IC50 Bioorg Med Chem Lett (1999) 9: 3187-3192 [PMID:10576685]
ChEMBL In vitro potency against human Prostaglandin G/H synthase 1 in U937 microsomes. B 7.3 pIC50 50 nM IC50 J Med Chem (1999) 42: 1274-1281 [PMID:10197970]
ChEMBL Inhibitory concentration was measured against Prostaglandin G/H synthase 1 in the sensitive U937 microsome assay B 7.3 pIC50 50 nM IC50 Bioorg Med Chem Lett (2003) 13: 1195-1198 [PMID:12643942]
Cyclooxygenase-1 in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4133] [UniProtKB: Q8HZR1]
ChEMBL In vitro inhibitory activity against canine prostaglandin G/H synthase 1. B 5.25 pIC50 5570 nM IC50 Bioorg Med Chem Lett (2004) 14: 95-98 [PMID:14684306]
Cyclooxygenase-1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2860] [UniProtKB: O62664]
ChEMBL Inhibition of Bos taurus (bovine) COX-1 by Chemoiluminescence assay B 4.61 pIC50 24300 nM IC50 Med Chem Res (2010) 19: 782-793
ChEMBL Inhibition of bovine COX1 assessed as PGE2 formation preincubated for 10 mins by ELISA B 4.67 pIC50 21610 nM IC50 Eur J Med Chem (2011) 46: 5763-5768 [PMID:22019186]
ChEMBL Inhibition of COX1 in calf endotheliocyte assessed as 6keto-PGF1alpha production pretreated for 20 mins followed by addition of 10 uM arachidonic acid as substrate for 20 mins by radioimmuno assay B 5.09 pIC50 8200 nM IC50 Eur J Med Chem (2016) 108: 89-103 [PMID:26638042]
ChEMBL Inhibition of COX1 in bovine platelets assessed as formation of 12-hydroxyheptadecatrienoic acid by HPLC B 5.1 pIC50 8000 nM IC50 Bioorg Med Chem (2009) 17: 558-568 [PMID:19097798]
ChEMBL Inhibition of bovine COX1 by enzyme immunoassay B 5.11 pIC50 7700 nM IC50 J Med Chem (2009) 52: 1525-1529 [PMID:19296694]
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979]
ChEMBL Inhibition of ovine COX-1 assessed as reduction of prostaglandin-G2 to prostaglandin-H2 and oxidation of 10-acetyl-3,7-dihydroxyphenoxazine to resorufin after 5 mins by fluorescence based assay B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2015) 25: 3295-3300 [PMID:26081289]
ChEMBL Inhibition of ovine COX1 by enzyme immuno assay B 4 pIC50 >100000 nM IC50 Bioorg Med Chem (2008) 16: 3907-3916 [PMID:18272371]
ChEMBL Inhibition of recombinant ovine COX1 B 4 pIC50 >100000 nM IC50 ACS Med Chem Lett (2021) 12: 798-804 [PMID:34055228]
ChEMBL Inhibition of ovine COX1-mediated prostaglandin alpha production by enzyme immuno assay B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2013) 23: 2601-2605 [PMID:23528298]
ChEMBL Inhibition of ovine COX-1 using arachidonic acid as substrate assessed as production of PGH2-alpha preincubated for 5 mins followed by addition of substrate measured after 2 mins by EIA B 4 pIC50 >100000 nM IC50 Bioorg Med Chem (2016) 24: 2032-2042 [PMID:27025563]
ChEMBL Inhibition of ovine COX1 preincubated for 5 mins followed by addition of arachidonic acid as substrate measured after 2 mins by enzyme immunoassay B 4 pIC50 >100000 nM IC50 Eur J Med Chem (2016) 115: 121-131 [PMID:26999325]
ChEMBL Inhibition of ovine COX1 after 2 mins by EIA B 4 pIC50 >100000 nM IC50 Eur J Med Chem (2014) 80: 167-174 [PMID:24780593]
ChEMBL Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition by ELISA B 4 pIC50 >100000 nM IC50 Bioorg Med Chem (2016) 24: 3818-3828 [PMID:27344214]
ChEMBL Inhibition of ovine COX1 after 5 mins by enzyme immunoassay B 4 pIC50 >100000 nM IC50 Eur J Med Chem (2011) 46: 1648-1655 [PMID:21388719]
ChEMBL Inhibition of ovine COX1 using arachidonic acid as substrate pretreated for 5 mins followed by substrate addition and measured after 2 mins by fluorescence based enzyme immunoassay B 4 pIC50 >100000 nM IC50 Eur J Med Chem (2019) 180: 86-98 [PMID:31301566]
ChEMBL Inhibition of ovine COX-1 using arachidonic acid after 5 mins by colorimetric method B 4 pIC50 >100000 nM IC50 Bioorg Med Chem (2015) 23: 6807-6814 [PMID:26455657]
ChEMBL Inhibition of ovine COX1 assessed as inhibition of PGF2alpha production from PGH2 preincubated for 5 mins before arachidonic acid addition measured after 2 mins by enzyme immunoassay B 4 pIC50 >100000 nM IC50 Eur J Med Chem (2015) 92: 115-123 [PMID:25549551]
ChEMBL Inhibition of ovine COX1 pre-incubated for 15 mins followed by addition of heme and fluorometric substrate and further incubated for 15 mins in presence of arachidonic acid by fluorescence based assay B 4.09 pIC50 81700 nM IC50 Bioorg Med Chem Lett (2015) 25: 2469-2472 [PMID:25980909]
ChEMBL Inhibition of ovine COX-1 using arachidonic acid after 15 mins by fluorescence based assay B 4.11 pIC50 78400 nM IC50 Bioorg Med Chem Lett (2015) 25: 4082-4084 [PMID:26316467]
ChEMBL Inhibition of ovine COX1 using fluorometric substrate after 15 mins B 4.11 pIC50 78400 nM IC50 Bioorg Med Chem Lett (2015) 25: 1986-1989 [PMID:25819096]
ChEMBL Inhibition of sheep COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by UV-visible spectrophotometric method B 4.14 pIC50 72520 nM IC50 Eur J Med Chem (2020) 186: 111863-111863 [PMID:31740050]
ChEMBL Inhibition of ovine COX1 assessed as reduction in PGH2 production using arachidonic acid substrate by enzyme immunoassay B 4.3 pIC50 >50000 nM IC50 Eur J Med Chem (2014) 86: 122-132 [PMID:25147154]
ChEMBL Inhibition of ovine COX1 assessed as PGF2alpha production from PGH2 after 5 mins by enzyme immunoassay B 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem (2011) 19: 3416-3424 [PMID:21570309]
ChEMBL Inhibition of ovine COX1 assessed as reduction in PGH2-dervied PGF2alpha production using arachidonic acid substrate by enzyme immunoassay B 4.3 pIC50 >50000 nM IC50 Eur J Med Chem (2014) 87: 868-880 [PMID:24576797]
ChEMBL Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by enzyme immunoassay B 4.3 pIC50 >50000 nM IC50 Eur J Med Chem (2014) 76: 482-493 [PMID:24607877]
ChEMBL Inhibition of ovine COX1 by enzyme immuno assay B 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem (2012) 20: 3306-3316 [PMID:22516672]
ChEMBL Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay B 4.3 pIC50 >50000 nM IC50 Medchemcomm (2016) 7: 2309-2327
ChEMBL Inhibition of ovine COX1 assessed as PGF2alpha production by enzyme immunoassay B 4.46 pIC50 34500 nM IC50 Eur J Med Chem (2012) 47: 111-124 [PMID:22119153]
ChEMBL Inhibition of ovine COX1 by enzyme immuno assay B 4.48 pIC50 33100 nM IC50 Bioorg Med Chem (2008) 16: 1948-1956 [PMID:18023187]
ChEMBL In vitro inhibitory concentration against ovine Cyclooxygenase-1 B 4.48 pIC50 33100 nM IC50 Bioorg Med Chem Lett (2005) 15: 439-442 [PMID:15603969]
ChEMBL In vitro inhibitory concentration against ovine Cyclooxygenase-1 B 4.48 pIC50 33100 nM IC50 Bioorg Med Chem Lett (2005) 15: 439-442 [PMID:15603969]
ChEMBL In vitro inhibitory concentration against ovine Prostaglandin G/H synthase 1 B 4.48 pIC50 33100 nM IC50 Bioorg Med Chem Lett (2004) 14: 4911-4914 [PMID:15341950]
ChEMBL Inhibition of ovine Prostaglandin G/H synthase 1 B 4.48 pIC50 33100 nM IC50 J Med Chem (2004) 47: 3972-3990 [PMID:15267236]
ChEMBL In vitro inhibition of ovine prostaglandin G/H synthase 1 B 4.48 pIC50 33100 nM IC50 J Med Chem (2004) 47: 6108-6111 [PMID:15537365]
ChEMBL Inhibitory activity against ovine COX1 B 4.48 pIC50 33100 nM IC50 J Med Chem (2006) 49: 1668-1683 [PMID:16509583]
ChEMBL Inhibition of ovine COX1 by enzyme immuno assay B 4.48 pIC50 33100 nM IC50 Bioorg Med Chem (2007) 15: 6796-6801 [PMID:17764958]
ChEMBL Inhibition of ovine COX1 by enzyme immunoassay B 4.48 pIC50 33100 nM IC50 Bioorg Med Chem (2008) 16: 3302-3308 [PMID:18096394]
ChEMBL Inhibition of ovine COX1 by enzyme-immuno assay B 4.48 pIC50 33100 nM IC50 Eur J Med Chem (2009) 44: 3798-3804 [PMID:19457595]
ChEMBL Inhibition of ovine COX1 assessed as inhibition of PGF2a formation after 20 mins by Ellman's method B 4.48 pIC50 33100 nM IC50 J Med Chem (2010) 53: 3707-3717 [PMID:20387815]
ChEMBL Inhibition of ovine COX1 B 4.49 pIC50 32000 nM IC50 Bioorg Med Chem Lett (2014) 24: 5324-5329 [PMID:25444084]
ChEMBL Inhibition of ovine COX1 using arachidonic acid as substrate assessed as conversion of PGH2 to PGF2alpha after 10 mins by EIA B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem (2014) 22: 2080-2089 [PMID:24631365]
ChEMBL Inhibition of ovine COX1 using arachidonic acid as substrate assessed as production of PGF2alpha preincubated for 10 mins followed by substrate addition measured after 2 mins by EIA in presence of stannous chloride B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem (2013) 21: 4581-4590 [PMID:23769654]
ChEMBL Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 10 mins before substrate addition measured after 5 mins by EIA B 4.52 pIC50 >30000 nM IC50 Eur J Med Chem (2014) 80: 47-56 [PMID:24763362]
ChEMBL Inhibition of purified ovine COX1 pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay B 4.52 pIC50 30000 nM IC50 ACS Med Chem Lett (2014) 5: 983-988 [PMID:25221653]
ChEMBL Inhibition of ovine COX1 using arachidonic acid as substrate B 4.56 pIC50 27250 nM IC50 ACS Med Chem Lett (2014) 5: 512-516 [PMID:24900871]
ChEMBL Inhibition of ovine COX1 B 4.57 pIC50 26610 nM IC50 Bioorg Med Chem Lett (2006) 16: 4440-4443 [PMID:16814546]
ChEMBL Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 5 mins followed by substrate addition measured after 2 mins by colorimetric based ELISA B 4.6 pIC50 >25000 nM IC50 Eur J Med Chem (2018) 158: 134-143 [PMID:30216848]
ChEMBL Inhibition of ovine COX1 by chemiluminescent enzyme assay B 4.61 pIC50 24300 nM IC50 Bioorg Med Chem (2009) 17: 5312-5317 [PMID:19560931]
ChEMBL Inhibition of ovine COX1 by enzyme chemiluminescent enzyme assay B 4.61 pIC50 24300 nM IC50 Bioorg Med Chem (2010) 18: 1029-1033 [PMID:20061161]
ChEMBL Inhibition of ovine COX1 by chemiluminescence assay B 4.61 pIC50 24300 nM IC50 Eur J Med Chem (2010) 45: 4013-4017 [PMID:20691338]
ChEMBL Inhibition of ovine COX1 by chemiluminescent assay B 4.61 pIC50 24300 nM IC50 Bioorg Med Chem Lett (2009) 19: 3162-3165 [PMID:19447036]
ChEMBL Inhibition of Ovine COX-1 by chemiluminescent enzyme method B 4.61 pIC50 24300 nM IC50 Bioorg Med Chem (2021) 32: 115960-115960 [PMID:33477020]
ChEMBL Inhibition of Ovis aries (sheep) COX1 using arachidonic acid as substrate using cyclic naphthalene hydrazide by chemiluminescence assay B 4.61 pIC50 24300 nM IC50 Med Chem Res (2012) 21: 1869-1875
ChEMBL Inhibition of Ovis aries (sheep) COX1 using arachidonic acid as substrate using cyclic naphthalene hydrazide by chemiluminescence assay B 4.61 pIC50 24300 nM IC50 Med Chem Res (2012) 21: 1803-1810
ChEMBL Inhibition of Ovis aries (sheep) cyclooxygenase-1 using arachidonic acid as substrate by chemiluminescent assay B 4.61 pIC50 24300 nM IC50 Med Chem Res (2013) 22: 3881-3887
ChEMBL Inhibition of ovine COX1 by chemiluminescence assay B 4.61 pIC50 24300 nM IC50 Bioorg Med Chem (2009) 17: 5369-5373 [PMID:19596198]
ChEMBL Inhibition of ovine COX1 using arachidonic acid as substrate by chemiluminescence assay B 4.61 pIC50 24300 nM IC50 Bioorg Med Chem (2014) 22: 865-873 [PMID:24361187]
ChEMBL Inhibition of ovine COX1 by chemiluminescent assay B 4.61 pIC50 24300 nM IC50 Bioorg Med Chem Lett (2008) 18: 1336-1339 [PMID:18226898]
ChEMBL Inhibition of Ovis aries (sheep) COX-1 assessed as decrease in PGF2a production from PGH2 upon reduction with stannous chloride using arachidonic acid as substrate pre-incubated with enzyme for 5 min prior to substrate addition by enzyme immunoassay B 4.64 pIC50 23000 nM IC50 Med Chem Res (2013) 22: 2493-2504
ChEMBL In vitro inhibitory activity against prostaglandin G/H synthase 1 from ovine B 4.64 pIC50 23000 nM IC50 Bioorg Med Chem Lett (2004) 14: 1953-1956 [PMID:15050635]
ChEMBL Inhibition of ram seminal vesicle COX-1 assessed as conversion of arachidonic acid to PGH2 B 4.64 pIC50 22900 nM IC50 Bioorg Med Chem Lett (2014) 24: 317-324 [PMID:24295787]
ChEMBL In vitro inhibitory activity against Prostaglandin G/H synthase 1 (COX-1) B 4.64 pIC50 22900 nM IC50 J Med Chem (2003) 46: 4872-4882 [PMID:14584938]
ChEMBL In vitro inhibition against ovine Prostaglandin G/H synthase 1 B 4.64 pIC50 22900 nM IC50 Bioorg Med Chem Lett (2003) 13: 2205-2209 [PMID:12798335]
ChEMBL Inhibition of ovine COX1 by measuring PGE2 B 4.72 pIC50 19030 nM IC50 Bioorg Med Chem (2007) 15: 6109-6118 [PMID:17604631]
ChEMBL Inhibition of ovine COX-1 assessed as production of PGE2 using arachidonic acid as a substrate preincubated for 60 mins followed by substrate addition and measured after 2 mins by ELISA analysis B 4.78 pIC50 16520 nM IC50 Bioorg Med Chem (2021) 46: 116344-116344 [PMID:34438337]
ChEMBL Inhibition of ovine COX-1 assessed as reduction in oxidation of TMPD using arachidonic acid as substrate preincubated for 5 mins followed by substrate and TMPD addition measured after 5 mins by colorimetric assay B 4.79 pIC50 16200 nM IC50 Bioorg Med Chem (2017) 25: 665-676 [PMID:27916468]
ChEMBL In vitro inhibition against Prostaglandin G/H synthase 1 from ram seminal vesicles B 4.81 pIC50 15330 nM IC50 J Med Chem (2003) 46: 3975-3984 [PMID:12954051]
ChEMBL Inhibitory activity against prostaglandin G/H synthase 1 (COX-1) B 4.82 pIC50 15135.61 nM IC50 J Med Chem (2002) 45: 4816-4827 [PMID:12383007]
ChEMBL Inhibition of ovine COX1 by enzyme immunoassay B 4.82 pIC50 15130 nM IC50 Bioorg Med Chem (2016) 24: 5626-5632 [PMID:27658794]
ChEMBL Inhibition of ovine COX-1 by EIA method B 4.82 pIC50 15100 nM IC50 Eur J Med Chem (2019) 183: 111693-111693 [PMID:31539778]
ChEMBL Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 5 mins by ELISA B 4.82 pIC50 15000 nM IC50 Bioorg Med Chem Lett (2018) 28: 952-957 [PMID:29426771]
ChEMBL Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins followed by substrate addition and measured after 2 mins by EIA assay B 4.82 pIC50 15000 nM IC50 Bioorg Med Chem (2020) 28: 115246-115246 [PMID:31843462]
ChEMBL Inhibition of ovine COX-1 assessed as decrease in prostaglandin production using arachidonic acid as substrate incubated with enzyme for 10 mins prior to substrate challenge by enzyme immunoassay B 4.82 pIC50 15000 nM IC50 Eur J Med Chem (2014) 77: 185-192 [PMID:24631898]
ChEMBL Inhibition of ovine COX1 assessed as reduction in PGH2-derived PGF2alpha using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 2 mins by enzyme immunoassay B 4.82 pIC50 15000 nM IC50 J Med Chem (2016) 59: 3920-3934 [PMID:27019010]
ChEMBL Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by spectrophotometry B 4.82 pIC50 15000 nM IC50 Bioorg Med Chem Lett (2014) 24: 77-82 [PMID:24332492]
ChEMBL Inhibition of ovine COX-1 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA B 4.82 pIC50 15000 nM IC50 J Med Chem (2021) 64: 9550-9566 [PMID:34137625]
ChEMBL Inhibition of ovine COX-1 assessed as PGF2alpha formation using arachidonic acid as substrate pretreated with compound for 20 mins prior to substrate addition by spectrophotometric analysis B 4.82 pIC50 15000 nM IC50 Eur J Med Chem (2015) 97: 104-123 [PMID:25956953]
ChEMBL Inhibition of ovine COX1 by fluorescence assay B 4.82 pIC50 15000 nM IC50 Bioorg Med Chem (2012) 20: 2221-2226 [PMID:22386983]
ChEMBL Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 1 min prior to substrate addition measured for 25 secs by TMPD-based chromogenic assay B 4.82 pIC50 15000 nM IC50 Bioorg Med Chem Lett (2012) 22: 6745-6749 [PMID:23010270]
ChEMBL Inhibition of ovine COX-1 preincubated for 5 mins followed by addition of arachidonic acid as substrate measured after 2 mins by fluorescence analysis B 4.82 pIC50 15000 nM IC50 Bioorg Med Chem Lett (2016) 26: 1516-1520 [PMID:26898334]
ChEMBL Inhibition of ovine COX1 assessed as reduction in PGH2 formation by measuring PGF2alpha by colorimetric assay B 4.83 pIC50 14800 nM IC50 Bioorg Med Chem (2017) 25: 5637-5651 [PMID:28916158]
ChEMBL Inhibition of ovine COX1 assessed as reduction in PGF2alpha production using arachidonic acid as substrate by colorimetric method B 4.83 pIC50 14800 nM IC50 Eur J Med Chem (2018) 144: 635-650 [PMID:29289887]
ChEMBL Inhibition of ovine COX -1 by colorimetric inhibitor screening assay kit method B 4.83 pIC50 14800 nM IC50 Eur J Med Chem (2019) 167: 161-186 [PMID:30771604]
ChEMBL Inhibition of ovine COX1 catalytic activity using arachidonic acid as substrate pre-incubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA method B 4.83 pIC50 14800 nM IC50 Eur J Med Chem (2019) 167: 562-582 [PMID:30818268]
ChEMBL Inhibition of ovine COX1 by colorimetric analysis B 4.83 pIC50 14700 nM IC50 Eur J Med Chem (2020) 200: 112439-112439 [PMID:32485532]
ChEMBL Inhibition of ovine COX1 assessed as reduction in PGF2alpha production by ELISA B 4.85 pIC50 14000 nM IC50 Eur J Med Chem (2017) 139: 936-946 [PMID:28881288]
ChEMBL Inhibition of ovine COX1 peroxidase activity assessed as reduction of PGG2 to PGH2 by measuring oxidized TMPD level by colorimetric assay B 4.85 pIC50 14000 nM IC50 Bioorg Med Chem (2014) 22: 2855-2866 [PMID:24751552]
ChEMBL Inhibition of ovine COX1 B 4.89 pIC50 13000 nM IC50 Bioorg Med Chem (2008) 16: 276-283 [PMID:17937989]
ChEMBL Inhibitory activity against prostaglandin G/H synthase 1 from ram seminal vesicles B 4.97 pIC50 10700 nM IC50 Bioorg Med Chem Lett (2004) 14: 499-504 [PMID:14698190]
ChEMBL In vitro inhibitory activity against prostaglandin G/H synthase 1 from the microsomal fraction of ram seminal vesicles B 4.97 pIC50 10700 nM IC50 Bioorg Med Chem Lett (2004) 14: 1683-1688 [PMID:15026050]
ChEMBL Competitive inhibition of ovine COX1 by enzyme immunoassay B 5 pIC50 10000 nM IC50 Bioorg Med Chem Lett (2012) 22: 2235-2238 [PMID:22341941]
ChEMBL Inhibition of ovine COX-1 by fluorescence assay B 5.03 pIC50 9400 nM IC50 Bioorg Med Chem Lett (2011) 21: 1823-1826 [PMID:21316237]
ChEMBL Inhibition of ovine COX-1 assessed as inhibition of transformation of AA to PGH2 by EIA B 5.08 pIC50 8320 nM IC50 Bioorg Med Chem Lett (2009) 19: 6922-6925 [PMID:19880317]
ChEMBL Inhibition of ovine COX1 assessed as PGF2alpha level by EIA B 5.09 pIC50 8100 nM IC50 Bioorg Med Chem (2011) 19: 2074-2083 [PMID:21349729]
ChEMBL Inhibition of ovine COX1 by enzyme immuno assay B 5.11 pIC50 7700 nM IC50 Bioorg Med Chem (2008) 16: 9694-9698 [PMID:18930406]
ChEMBL Inhibition of ovine COX1 by enzyme immuno assay B 5.11 pIC50 7700 nM IC50 Bioorg Med Chem Lett (2009) 19: 584-588 [PMID:19136259]
ChEMBL Inhibition of ovine COX1 using arachidonic acid as substrate by colorimetric enzyme immune assay B 5.11 pIC50 7700 nM IC50 Bioorg Med Chem Lett (2017) 27: 4358-4369 [PMID:28844389]
ChEMBL Inhibition of ovine COX1 by enzyme immuno assay B 5.11 pIC50 7700 nM IC50 Bioorg Med Chem Lett (2008) 18: 6138-6141 [PMID:18945614]
ChEMBL Inhibition of ovine COX1 by enzyme immunoassay B 5.11 pIC50 7700 nM IC50 Bioorg Med Chem (2009) 17: 5182-5188 [PMID:19500994]
ChEMBL Inhibition of ovine COX1 by enzyme immunoassay B 5.11 pIC50 7700 nM IC50 Bioorg Med Chem Lett (2010) 20: 1324-1329 [PMID:20097072]
ChEMBL Inhibition of ovine COX1 by enzyme immuno assay B 5.11 pIC50 7700 nM IC50 Bioorg Med Chem Lett (2011) 21: 3951-3956 [PMID:21641217]
ChEMBL Inhibition of ovine COX1 B 5.11 pIC50 7700 nM IC50 Bioorg Med Chem Lett (2013) 23: 163-168 [PMID:23200247]
ChEMBL Inhibition of ovine COX1 by enzyme immuno assay B 5.11 pIC50 7700 nM IC50 Bioorg Med Chem Lett (2011) 21: 6074-6080 [PMID:21890358]
ChEMBL Inhibition of ovine COX-1 by enzyme immuno assay B 5.11 pIC50 7700 nM IC50 Bioorg Med Chem Lett (2012) 22: 2154-2159 [PMID:22361134]
ChEMBL Inhibition of ovine COX-1 assessed as reduction in PGF2-alpha formation using arachidonic acid as substrate by enzyme immunoassay B 5.12 pIC50 7600 nM IC50 Eur J Med Chem (2016) 118: 250-258 [PMID:27131067]
ChEMBL Inhibition of ovine COX1 assessed as PGH2 formation preincubated for 10 mins followed by addition of arachidonic acid as substrate measured after 2 mins by ELISA B 5.15 pIC50 7000 nM IC50 Bioorg Med Chem Lett (2016) 26: 4757-4762 [PMID:27567369]
ChEMBL Inhibition of ovine COX-1 preincubated for 2 mins prior to arachidonic acid addition by enzyme immuno assay B 5.16 pIC50 6900 nM IC50 Bioorg Med Chem Lett (2015) 25: 5787-5791 [PMID:26546221]
ChEMBL Inhibition of sheep COX1 by spectrophotometry B 5.16 pIC50 6860 nM IC50 J Med Chem (2010) 53: 6560-6571 [PMID:20804197]
ChEMBL Inhibition of ovine COX1 by enzyme immuno assay B 5.17 pIC50 6700 nM IC50 Bioorg Med Chem Lett (2016) 26: 406-412 [PMID:26691756]
ChEMBL Inhibition of ovine COX-1 preincubated for 5 mins followed by arachidonic acid substrate addition by colorimetric enzyme immunoassay B 5.17 pIC50 6700 nM IC50 Bioorg Med Chem (2017) 25: 4424-4432 [PMID:28669741]
ChEMBL Inhibition of ovine COX1 assessed as reduction in Prostaglandin production by enzyme immunoassay B 5.21 pIC50 6200 nM IC50 Bioorg Med Chem (2018) 26: 891-902 [PMID:29373271]
ChEMBL Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay B 5.25 pIC50 5640 nM IC50 Eur J Med Chem (2017) 127: 10-21 [PMID:28038322]
ChEMBL Inhibition of ovine purified COX1 after 20 mins B 5.4 pIC50 >4000 nM IC50 ACS Med Chem Lett (2011) 2: 160-164 [PMID:21318094]
ChEMBL Inhibition of ovine COX1 by fluorescence assay B 6 pIC50 >1000 nM IC50 Bioorg Med Chem (2013) 21: 4288-4295 [PMID:23706267]
ChEMBL Inhibition of ovine COX-1 assessed as decrease in PGH2 production using arachidonic acid as substrate treated with enzyme for 10 mins prior to substrate challenge for 2 mins by enzyme immunoassay B 6 pIC50 >1000 nM IC50 Bioorg Med Chem Lett (2014) 24: 1958-1962 [PMID:24656662]
ChEMBL Inhibition of ovine COX1 B 6.68 pIC50 210 nM IC50 Bioorg Med Chem (2007) 15: 1976-1982 [PMID:17258905]
ChEMBL Inhibition of ovine COX-1 using arachidonic acid as substrate by fluorescence assay B 7.04 pIC50 91 nM IC50 Eur J Med Chem (2021) 224: 113682-113682 [PMID:34245948]
ChEMBL Inhibition of COX1 B 8.43 pIC50 3.7 nM IC50 Bioorg Med Chem Lett (2006) 16: 4483-4487 [PMID:16806914]
COX-1 /Cyclooxygenase-1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2649] [GtoPdb: 1375] [UniProtKB: P22437]
ChEMBL Inhibition of COX1-dependent PGE2 production in LPS-stimulated mouse J774 cells by RIA B 5.29 pIC50 5100 nM IC50 J Med Chem (2010) 53: 723-733 [PMID:19957931]
ChEMBL In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells B 5.29 pIC50 5100 nM IC50 J Med Chem (2005) 48: 3428-3432 [PMID:15857149]
ChEMBL Inhibition of COX-1-mediated PGE2 production in arachidonic acid-stimulated mouse J774 cells incubated for 15 mins prior to arachidonic acid-challenge by radioimmunoassay B 5.42 pIC50 3840 nM IC50 J Med Chem (2011) 54: 7759-7771 [PMID:21992176]
ChEMBL Inhibition of COX1 in mouse J774 cells using arachidonic acid as substrate assessed as inhibition of PGE2 production incubated for 15 mins prior to substrate addition measured after 30 mins by radioimmunoassay B 5.42 pIC50 3840 nM IC50 Bioorg Med Chem (2013) 21: 3695-3701 [PMID:23680444]
ChEMBL Inhibition of COX1 in arachidonic acid-stimulated mouse J774 cells assessed as inhibition of PGE2 production after 15 mins by radioimmunoassay B 5.43 pIC50 3700 nM IC50 Bioorg Med Chem (2008) 16: 8072-8081 [PMID:18752957]
ChEMBL Inhibition of COX1 in mouse J774 cells assessed as arachidonic acid-induced PGE2 levels by radio immunoassay B 5.43 pIC50 3700 nM IC50 J Med Chem (2007) 50: 5403-5411 [PMID:17915854]
ChEMBL Tested for inhibition against Prostaglandin G/H synthase 2 from mouse resident macrophages B 9.15 pIC50 0.7 nM IC50 J Med Chem (2000) 43: 4582-4593 [PMID:11101350]
COX-1 /Cyclooxygenase-1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4042] [GtoPdb: 1375] [UniProtKB: Q63921]
ChEMBL Inhibition of rat seminal vesicle COX-1 using arachidonic acid as substrate assessed as reduction of PGG2 to PGH2 incubated for 1 min prior to substrate addition measured after 25 secs by chromogenic assay B 4.82 pIC50 15000 nM IC50 Bioorg Med Chem Lett (2014) 24: 2251-2255 [PMID:24745964]
ChEMBL In vitro inhibitory concentration against rat prostaglandin G/H synthase 1 B 4.85 pIC50 14200 nM IC50 Bioorg Med Chem Lett (2001) 11: 2687-2690 [PMID:11591502]
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
ChEMBL Inhibition of human recombinant COX-2 using arachidonic acid as substrate preincubated for 60 mins followed by substrate addition for 2 secs by ADPH based fluorometric analysis B 9.33 pKi 0.47 nM Ki J Med Chem (2021) 64: 11570-11596 [PMID:34279934]
ChEMBL Inhibitory effect on Prostaglandin G/H synthase 2 activity was evaluated in human whole blood as LPS-induced PGE-2 generation F 5.44 pIC50 3600 nM IC50 J Med Chem (2002) 45: 1402-1411 [PMID:11906281]
ChEMBL Inhibition of PGHS2 in human whole blood assessed as inhibition of TXB2 production by radioimmunoassay B 5.54 pIC50 2900 nM IC50 Bioorg Med Chem (2009) 17: 74-84 [PMID:19059783]
ChEMBL Inhibition of COX2 (unknown origin) by colorimetric method B 5.58 pIC50 2660 nM IC50 Bioorg Med Chem Lett (2014) 24: 1952-1957 [PMID:24661847]
ChEMBL Inhibition of human COX2 expressed in insect cells using arachidonic acid as substrate pretreated for 3 mins followed by substrate addition measured immediately B 5.88 pIC50 1310 nM IC50 J Nat Prod (2017) 80: 2472-2477 [PMID:28885836]
ChEMBL Inhibition of recombinant human COX2 using arachidonic acid as substrate pretreated for 5 mins followed by substrate addition and measured after 2 mins by fluorescence based enzyme immunoassay B 5.88 pIC50 1310 nM IC50 Eur J Med Chem (2019) 180: 86-98 [PMID:31301566]
ChEMBL Activity of COX2 in human heparinized blood assessed as inhibition of LPS-induced PGE2 production after 24 hrs B 5.89 pIC50 1300 nM IC50 J Med Chem (2007) 50: 1449-1457 [PMID:17335184]
ChEMBL Compound was evaluated for inhibition concentration of prostaglandin G/H synthase 2 in human blood B 5.92 pIC50 1200 nM IC50 J Med Chem (2004) 47: 2180-2193 [PMID:15084117]
ChEMBL Inhibition of COX2 B 5.92 pIC50 1200 nM IC50 Eur J Med Chem (2008) 43: 2792-2799 [PMID:18262309]
ChEMBL Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production B 5.92 pIC50 1200 nM IC50 J Med Chem (2007) 50: 6367-6382 [PMID:17994684]
ChEMBL Compound was tested for the inhibition of human Prostaglandin G/H synthase 2 (COX-2) in human whole blood B 5.92 pIC50 1200 nM IC50 J Med Chem (2003) 46: 5484-5504 [PMID:14640557]
ChEMBL In vitro inhibitory concentration against Prostaglandin G/H synthase 2 (COX-2) in human whole blood B 5.92 pIC50 1200 nM IC50 J Med Chem (2005) 48: 3930-3934 [PMID:15916445]
ChEMBL In vitro inhibition of Prostaglandin G/H synthase 2 in human whole blood B 5.92 pIC50 1200 nM IC50 Bioorg Med Chem Lett (2004) 14: 6049-6052 [PMID:15546727]
ChEMBL Inhibition of recombinant human COX2 using arachidonic acid as substrate by colorimetric enzyme immune assay B 5.94 pIC50 1140 nM IC50 Bioorg Med Chem Lett (2017) 27: 4358-4369 [PMID:28844389]
ChEMBL Inhibitory activity against prostaglandin G/H synthase 2 B 5.96 pIC50 1100 nM IC50 J Med Chem (2000) 43: 214-223 [PMID:10649977]
ChEMBL Inhibition of human recombinant COX2 assessed as decrease in prostaglandin production using arachidonic acid as substrate pretreated for 15 mins followed by substrate addition and measured after 2 mins by enzyme immunoassay B 5.97 pIC50 1070 nM IC50 Medchemcomm (2019) 10: 1775-1788 [PMID:31803395]
ChEMBL Inhibition of Prostaglandin G/H synthase 2 in human whole blood B 6 pIC50 1000 nM IC50 Bioorg Med Chem Lett (1999) 9: 2207-2212 [PMID:10465547]
ChEMBL Inhibitory potency against PGE-2 production in the human whole blood (HWB COX-2) assay B 6 pIC50 1000 nM IC50 Bioorg Med Chem Lett (1999) 9: 3187-3192 [PMID:10576685]
ChEMBL Inhibition of human COX2 B 6 pIC50 1000 nM IC50 Eur J Med Chem (2008) 43: 1152-1159 [PMID:17976864]
ChEMBL In vitro inhibitory potency against human COX-2 (HWB COX-2) by whole blood assay B 6 pIC50 1000 nM IC50 Bioorg Med Chem Lett (1999) 9: 3181-3186 [PMID:10576684]
ChEMBL In vitro potency against human Prostaglandin G/H synthase 2 in the human whole blood assay. B 6 pIC50 1000 nM IC50 J Med Chem (1999) 42: 1274-1281 [PMID:10197970]
ChEMBL Inhibitory concentration was measured against Cyclooxygenase-2 in human whole blood B 6 pIC50 1000 nM IC50 Bioorg Med Chem Lett (2003) 13: 1195-1198 [PMID:12643942]
ChEMBL In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 2 B 6 pIC50 1000 nM IC50 Bioorg Med Chem Lett (1999) 9: 1773-1778 [PMID:10406640]
ChEMBL Inhibition of human recombinant COX-2 preincubated for 2 mins prior to arachidonic acid addition by enzyme immuno assay B 6.05 pIC50 900 nM IC50 Bioorg Med Chem Lett (2015) 25: 5787-5791 [PMID:26546221]
ChEMBL Inhibition of recombinant human COX2 using arachidonic acid as substrate assessed as decrease in PGF2 production preincubated for 15 mins followed by substrate addition measured after 2 mins by enzyme immunoassay B 6.06 pIC50 880 nM IC50 Eur J Med Chem (2017) 127: 972-985 [PMID:27837994]
ChEMBL Inhibition of COX2 in human blood assessed as TxB2 level after 1 hr by enzyme immunoassay B 6.06 pIC50 870 nM IC50 Bioorg Med Chem (2013) 21: 2355-2362 [PMID:23473947]
ChEMBL Inhibition of human COX-2 preincubated for 5 mins followed by arachidonic acid substrate addition by colorimetric enzyme immunoassay B 6.06 pIC50 870 nM IC50 Bioorg Med Chem (2017) 25: 4424-4432 [PMID:28669741]
ChEMBL Inhibition of human recombinant COX2 by enzyme immuno assay B 6.06 pIC50 870 nM IC50 Bioorg Med Chem Lett (2016) 26: 406-412 [PMID:26691756]
ChEMBL Inhibition of human recombinant COX2 by enzyme immuno assay B 6.06 pIC50 870 nM IC50 Medchemcomm (2017) 8: 492-500 [PMID:30108767]
ChEMBL Inhibition of COX2 (unknown origin) by EIA B 6.08 pIC50 840 nM IC50 Eur J Med Chem (2019) 180: 486-508 [PMID:31330449]
ChEMBL Inhibition of COX2 in human whole blood assessed as inhibition of 12-hydroxyheptadecatrienoic acid production by HPLC method B 6.1 pIC50 800 nM IC50 Bioorg Med Chem (2010) 18: 3910-3924 [PMID:20451397]
ChEMBL Inhibition of COX2 in LPS-stimulated human blood B 6.1 pIC50 800 nM IC50 Bioorg Med Chem (2009) 17: 558-568 [PMID:19097798]
ChEMBL Inhibition of human COX2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay B 6.11 pIC50 780 nM IC50 Eur J Med Chem (2017) 127: 10-21 [PMID:28038322]
ChEMBL Inhibition of human COX2 assessed as reduction in PGF2alpha formation using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA B 6.15 pIC50 700 nM IC50 Eur J Med Chem (2020) 189: 112066-112066 [PMID:31982653]
ChEMBL Inhibition of COX2 (unknown origin) B 6.19 pIC50 640 nM IC50 Bioorg Med Chem Lett (2017) 27: 1017-1025 [PMID:28089698]
ChEMBL In vitro percent inhibition of Prostaglandin G/H synthase 2 (COX-2) in human whole blood was determined B 6.22 pIC50 600 nM IC50 J Med Chem (2003) 46: 3463-3475 [PMID:12877584]
ChEMBL Inhibition of COX2 in LPS-induced monocyte assessed as PGE2 production in human whole blood B 6.27 pIC50 540 nM IC50 J Med Chem (2007) 50: 5403-5411 [PMID:17915854]
ChEMBL Inhibition of COX2 in human whole blood assessed as inhibition of LPS-induced PGE2 production by RIA B 6.27 pIC50 540 nM IC50 J Med Chem (2010) 53: 723-733 [PMID:19957931]
ChEMBL Inhibition of COX-2 in human whole blood assessed as prostaglandin E2 production by RIA B 6.27 pIC50 540 nM IC50 Bioorg Med Chem (2014) 22: 772-786 [PMID:24373735]
ChEMBL Inhibition of COX2-mediated PGE2 production in LPS-induced human whole blood after 60 mins by radioimmunoassay B 6.27 pIC50 540 nM IC50 J Med Chem (2011) 54: 7759-7771 [PMID:21992176]
ChEMBL Inhibition of COX2 in human whole blood assessed as inhibition of TXB2 production by radioimmunoassay B 6.27 pIC50 540 nM IC50 Bioorg Med Chem (2008) 16: 8072-8081 [PMID:18752957]
ChEMBL Biochemical index for Prostaglandin G/H synthase 2 measured as, PGE-2 levels in lipopolysaccharide (LPS)-challenged human whole blood B 6.28 pIC50 530 nM IC50 Bioorg Med Chem Lett (2000) 10: 1745-1748 [PMID:10937738]
ChEMBL Colorimetric Assay: The activities of COX-1 and COX-2 were measured after the addition of arachidonic acid and incubation at 25° C. for 5 min by absorbance at 590 nm as specified by the manufacturer. B 6.3 pIC50 500 nM IC50 US-9388139-B2. Derivatives of celeboxib, use thereof and preparation thereof (2016)
ChEMBL DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) B 6.32 pIC50 484 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of COX2 in human whole blood assessed as reduction in LPS stimulated PGE2 production incubated for 1 hr by ELISA B 6.36 pIC50 440 nM IC50 J Med Chem (2021) 64: 11570-11596 [PMID:34279934]
ChEMBL Inhibition of COX2 (unknown origin) assessed as reduction in PGE2 level using arachidonic acid as substrate after 5 mins in presence of heme by ELISA B 6.39 pIC50 410 nM IC50 Bioorg Med Chem Lett (2017) 27: 3653-3660 [PMID:28720504]
ChEMBL Inhibition of human COX2 using [14C]arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 45 mins by TLC B 6.44 pIC50 360 nM IC50 Bioorg Med Chem (2018) 26: 3731-3762 [PMID:30017112]
ChEMBL Inhibition of COX2 (unknown origin) using arachidonic acid as substrate pretreated for 10 mins followed by substrate addition and measured after 2 mins by ELISA B 6.44 pIC50 360 nM IC50 Bioorg Med Chem (2018) 26: 4264-4275 [PMID:30031652]
ChEMBL Inhibition of COX-2 in human whole blood assessed as PGE2 level in plasma after 5 mins by enzyme immunoassay B 6.46 pIC50 350 nM IC50 Eur J Med Chem (2014) 74: 12-22 [PMID:24440378]
ChEMBL Inhibition of COX2 in human whole blood assessed as inhibition of LPS-stimulated PGE2 production B 6.46 pIC50 350 nM IC50 J Med Chem (2004) 47: 6749-6759 [PMID:15615524]
ChEMBL Inhibition of COX2 in LPS-stimulated human whole blood assessed as PGE2 production by enzyme immunoassay B 6.46 pIC50 350 nM IC50 J Med Chem (2009) 52: 5864-5871 [PMID:19791801]
ChEMBL Inhibition of human recombinant COX-2 assessed as reduction in oxidation of TMPD using arachidonic acid as substrate preincubated for 5 mins followed by substrate and TMPD addition measured after 5 mins by colorimetric assay B 6.47 pIC50 340 nM IC50 Bioorg Med Chem (2017) 25: 665-676 [PMID:27916468]
ChEMBL Inhibition of COX2 in human whole blood assessed as inhibition of lipopolysaccharide-stimulated PGE2 production after 24 hrs by enzyme immunoassay B 6.47 pIC50 336 nM IC50 Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573]
ChEMBL Inhibition of COX2 assessed as LPS-stimulated PGE2 production in human whole blood leukocyte F 6.48 pIC50 330 nM IC50 Bioorg Med Chem Lett (2006) 16: 4440-4443 [PMID:16814546]
ChEMBL Inhibition of human recombinant COX2 expressed in insect cell expression system using TMPD and arachidonic acid as substrate incubated for 1 min prior to substrate addition by spectrophotometry B 6.49 pIC50 320 nM IC50 Eur J Med Chem (2013) 70: 579-588 [PMID:24211633]
ChEMBL Inhibition of human COX2 using arachidonic acid assessed as production of PGF2alpha after 5 mins by ELISA B 6.51 pIC50 310 nM IC50 Bioorg Med Chem Lett (2016) 26: 3491-3498 [PMID:27349331]
GtoPdb - - 6.52 pIC50 300 nM IC50 Eur J Med Chem (2017) 141: 306-321 [PMID:29031075]
ChEMBL Inhibition of human recombinant COX2 B 6.52 pIC50 <300 nM IC50 Eur J Med Chem (2008) 43: 456-463 [PMID:17532544]
ChEMBL Inhibition of human COX-2 using [14C]-arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 45 mins by thin layer chromatographic method B 6.52 pIC50 300 nM IC50 Eur J Med Chem (2017) 141: 306-321 [PMID:29031075]
ChEMBL Inhibition of human recombinant COX2 after 45 mins B 6.52 pIC50 <300 nM IC50 Eur J Med Chem (2010) 45: 6027-6038 [PMID:20970223]
ChEMBL Inhibition of COX2 in human whole blood assessed as effect on LPS-stimulated PGE2 production B 6.52 pIC50 300 nM IC50 Bioorg Med Chem (2008) 16: 2697-2706 [PMID:18063374]
ChEMBL Inhibition of human recombinant COX2 using arachidonic acid as substrate B 6.54 pIC50 290 nM IC50 ACS Med Chem Lett (2014) 5: 512-516 [PMID:24900871]
ChEMBL Inhibition of human recombinant COX2 after 2 mins by EIA B 6.55 pIC50 280 nM IC50 Eur J Med Chem (2014) 80: 167-174 [PMID:24780593]
ChEMBL Inhibition of human recombinant COX2 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by enzyme immunoassay B 6.55 pIC50 280 nM IC50 Eur J Med Chem (2014) 76: 482-493 [PMID:24607877]
ChEMBL Inhibition of COX-2 (unknown origin) B 6.57 pIC50 270 nM IC50 Eur J Med Chem (2014) 81: 204-217 [PMID:24836072]
ChEMBL Inhibition of COX2 (unknown origin) B 6.57 pIC50 270 nM IC50 Bioorg Med Chem Lett (2020) 30: 127376-127376 [PMID:32738961]
ChEMBL Inhibition of COX-2 (unknown origin) B 6.59 pIC50 260 nM IC50 Eur J Med Chem (2016) 108: 89-103 [PMID:26638042]
ChEMBL Inhibition of recombinant N-terminal His6-tagged human COX-2 expressed in Baculovirus infected Sf21 cells using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 1 hr B 6.59 pIC50 260 nM IC50 Bioorg Med Chem (2018) 26: 5388-5396 [PMID:30293795]
ChEMBL Inhibition of COX2 (unknown origin) using arachidonic acid as substrate incubated for 10 mins by Ellman's reagent based COX-1/COX-2 ELISA assay B 6.6 pIC50 250 nM IC50 Eur J Med Chem (2019) 169: 168-184 [PMID:30877972]
ChEMBL Inhibition of human COX2 using arachidonic acid as substrate incubated for 2 mins by ELISA method B 6.6 pIC50 250 nM IC50 Eur J Med Chem (2020) 185: 111780-111780 [PMID:31655429]
ChEMBL Inhibition of COX-2 (unknown origin) assessed as reduction in PGH2 formation using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by enzyme immunoassay B 6.62 pIC50 240 nM IC50 Bioorg Med Chem Lett (2021) 33: 127743-127743 [PMID:33316405]
ChEMBL Inhibition of human Prostaglandin G/H synthase 2 B 6.64 pIC50 230 nM IC50 J Med Chem (2002) 45: 1511-1517 [PMID:11906292]
ChEMBL Inhibition of COX2 (unknown origin) B 6.66 pIC50 220 nM IC50 Bioorg Med Chem Lett (2019) 29: 1909-1912 [PMID:31160177]
ChEMBL Inhibition of COX2 assessed as inhibition of PGE2 production using arachidonic acid as substrate after 10 mins by ELISA B 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (2012) 22: 793-796 [PMID:22217871]
ChEMBL Inhibition of human whole blood COX-2 assessed as production of PGE2 after 24 hrs by EIA B 6.72 pIC50 190 nM IC50 Bioorg Med Chem (2011) 19: 3299-3311 [PMID:21570308]
ChEMBL Inhibition of human COX2 assessed as fluorescence by microplate reader B 6.8 pIC50 160 nM IC50 Eur J Med Chem (2021) 222: 113564-113564 [PMID:34091208]
ChEMBL Inhibition of COX2 B 6.82 pIC50 150 nM IC50 Bioorg Med Chem Lett (2011) 21: 1612-1616 [PMID:21345672]
ChEMBL Inhibition of recombinant human N-terminal His-tagged COX2 expressed in baculovirus infected Sf21 cells assessed as reduction in prostaglandin production by enzyme immunoassay B 6.82 pIC50 150 nM IC50 Bioorg Med Chem (2018) 26: 891-902 [PMID:29373271]
ChEMBL Inhibition of COX2 in human whole blood assessed as inhibition of LPS-induced PGE2 synthesis up to 24 hrs by radioimmunoassay B 6.85 pIC50 140 nM IC50 Bioorg Med Chem Lett (2012) 22: 5031-5034 [PMID:22749420]
ChEMBL Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate measured after 10 mins by fluorometric based multimode microplate reader B 6.88 pIC50 132 nM IC50 Eur J Med Chem (2021) 209: 112918-112918 [PMID:33071054]
ChEMBL Inhibition of recombinant human COX-2 assessed as reduction of prostaglandin-G2 to prostaglandin-H2 and oxidation of 10-acetyl-3,7-dihydroxyphenoxazine to resorufin after 5 mins by fluorescence based assay B 6.89 pIC50 130 nM IC50 Bioorg Med Chem Lett (2015) 25: 3295-3300 [PMID:26081289]
ChEMBL Inhibition of PGE-2 generation in LPS-stimulated human monocytes (Prostaglandin G/H synthase 2 cell assay) F 6.92 pIC50 120 nM IC50 J Med Chem (2002) 45: 1402-1411 [PMID:11906281]
ChEMBL Inhibition of human recombinant COX2 by enzyme immunoassay B 6.92 pIC50 120 nM IC50 Bioorg Med Chem Lett (2010) 20: 1324-1329 [PMID:20097072]
ChEMBL Inhibition of human recombinant COX2 by enzyme immunoassay B 6.92 pIC50 120 nM IC50 Bioorg Med Chem (2009) 17: 5182-5188 [PMID:19500994]
ChEMBL Inhibition of human recombinant COX2 by enzyme immunoassay B 6.92 pIC50 120 nM IC50 J Med Chem (2009) 52: 1525-1529 [PMID:19296694]
ChEMBL Inhibition of COX2 by chemiluminescent enzyme assay B 6.92 pIC50 120 nM IC50 Bioorg Med Chem (2011) 19: 6827-6832 [PMID:22000948]
ChEMBL Inhibition of human recombinant COX2 by enzyme immuno assay B 6.92 pIC50 120 nM IC50 Bioorg Med Chem Lett (2009) 19: 584-588 [PMID:19136259]
ChEMBL In vitro inhibition of PGE-2 generation by LPS-stimulated monocytes isolated from human blood. F 6.96 pIC50 110 nM IC50 Bioorg Med Chem Lett (2002) 12: 533-537 [PMID:11844666]
ChEMBL Inhibition of COX-2 (unknown origin) by chemiluminescence assay B 7 pIC50 100 nM IC50 Eur J Med Chem (2013) 62: 222-231 [PMID:23353741]
ChEMBL Inhibition of COX-2 by chemiluminescent assay B 7 pIC50 100 nM IC50 Bioorg Med Chem (2012) 20: 6648-6654 [PMID:23062711]
ChEMBL Inhibition of human recombinant COX-2 assessed as PGF2alpha production by enzyme immunoassay B 7 pIC50 100 nM IC50 Eur J Med Chem (2012) 47: 111-124 [PMID:22119153]
ChEMBL Inhibition of recombinant human COX2 B 7.05 pIC50 90 nM IC50 ACS Med Chem Lett (2021) 12: 798-804 [PMID:34055228]
ChEMBL Inhibition of COX2 human HCA7 cells B 7.05 pIC50 90 nM IC50 J Med Chem (2020) 63: 3817-3833 [PMID:31820982]
ChEMBL Inhibition of human COX2 expressed in sf9 cells B 7.1 pIC50 80 nM IC50 J Nat Prod (2005) 68: 1514-1518 [PMID:16252917]
ChEMBL Inhibition of Prostaglandin G/H synthase 2 in 143.98.2 from human osteosarcoma cells B 7.1 pIC50 80 nM IC50 J Med Chem (2001) 44: 350-361 [PMID:11462976]
ChEMBL In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (COX-2) in 143982 cells B 7.1 pIC50 79 nM IC50 J Med Chem (2003) 46: 3463-3475 [PMID:12877584]
ChEMBL Inhibition of human recombinant COX-2 assessed as decrease in PGH2 production using arachidonic acid as substrate treated with enzyme for 10 mins prior to substrate challenge for 2 mins by enzyme immunoassay B 7.14 pIC50 72 nM IC50 Bioorg Med Chem Lett (2014) 24: 1958-1962 [PMID:24656662]
ChEMBL Inhibition of human recombinant COX-2 by enzyme immunoassay B 7.15 pIC50 70 nM IC50 Bioorg Med Chem (2014) 22: 2529-2534 [PMID:24650702]
ChEMBL Inhibition of human COX2 assessed as reduction in PGE2 production incubated for 2 mins using arachidonic acid substrate by enzyme immuno assay B 7.15 pIC50 70 nM IC50 Medchemcomm (2017) 8: 492-500 [PMID:30108767]
ChEMBL Inhibition of COX2 by enzyme immunoassay B 7.15 pIC50 70 nM IC50 Bioorg Med Chem (2009) 17: 1146-1151 [PMID:19157881]
ChEMBL Inhibition of human COX2 B 7.15 pIC50 70 nM IC50 J Med Chem (2020) 63: 3817-3833 [PMID:31820982]
ChEMBL In vitro inhibition against human Prostaglandin G/H synthase 2 B 7.15 pIC50 70 nM IC50 J Med Chem (2003) 46: 3975-3984 [PMID:12954051]
ChEMBL Inhibition of human recombinant COX2 B 7.15 pIC50 70 nM IC50 Bioorg Med Chem Lett (2013) 23: 163-168 [PMID:23200247]
ChEMBL Inhibition of human recombinant COX2 by enzyme immuno assay B 7.15 pIC50 70 nM IC50 Bioorg Med Chem Lett (2011) 21: 3951-3956 [PMID:21641217]
ChEMBL Inhibition of human recombinant COX-2 by enzyme immuno assay B 7.15 pIC50 70 nM IC50 Bioorg Med Chem Lett (2012) 22: 2154-2159 [PMID:22361134]
ChEMBL Inhibition of human cyclooxygenase-2 expressed in COS cells B 7.17 pIC50 68 nM IC50 Bioorg Med Chem Lett (2004) 14: 5445-5448 [PMID:15454242]
ChEMBL Inhibition of human COX2 expressed in african green monkey COS cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay B 7.17 pIC50 68 nM IC50 Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573]
ChEMBL Inhibition of human COX2 by enzyme immunoassay B 7.19 pIC50 65 nM IC50 Bioorg Med Chem Lett (2010) 20: 4544-4549 [PMID:20576432]
ChEMBL Inhibition of human recombinant COX2 by EIA B 7.19 pIC50 65 nM IC50 Bioorg Med Chem Lett (2010) 20: 5245-5250 [PMID:20655211]
ChEMBL Inhibition of human COX2 expressed in baculovirus-infected SF9 cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay B 7.2 pIC50 63 nM IC50 Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573]
ChEMBL Competitive inhibition of human recombinant COX2 by enzyme immunoassay B 7.22 pIC50 60 nM IC50 Bioorg Med Chem Lett (2012) 22: 2235-2238 [PMID:22341941]
ChEMBL Inhibition of COX2 B 7.22 pIC50 60 nM IC50 Bioorg Med Chem Lett (2007) 17: 5634-5637 [PMID:17822894]
ChEMBL Inhibition of human COX2 by fluorescence based assay B 7.22 pIC50 60 nM IC50 Medchemcomm (2017) 8: 492-500 [PMID:30108767]
ChEMBL Inhibition of human recombinant COX2 by enzymatic fluorescence assay B 7.22 pIC50 60 nM IC50 Bioorg Med Chem (2012) 20: 3410-3421 [PMID:22560838]
ChEMBL Inhibition of COX-2 (unknown origin) by ELISA B 7.24 pIC50 57 nM IC50 Bioorg Med Chem Lett (2014) 24: 317-324 [PMID:24295787]
ChEMBL Inhibition of COX2 (unknown origin) expressed in HEK293 TRex cells assessed as reduction in PGE2 production using arachidonic acid as substrate preincubated for 60 mins followed by substrate addition for 1 hr in presence of 10% FBS by RapidFire High-Throughput Mass Spectrometry B 7.24 pIC50 57 nM IC50 J Med Chem (2021) 64: 11570-11596 [PMID:34279934]
ChEMBL Inhibition of COX2 (unknown origin) B 7.24 pIC50 57 nM IC50 Med Chem Res (2013) 22: 1529-1537
ChEMBL In vitro inhibitory concentration of compound required to inhibit Prostaglandin G/H synthase 2 enzyme was determined B 7.25 pIC50 56.7 nM IC50 Bioorg Med Chem Lett (2002) 12: 2753-2756 [PMID:12217369]
ChEMBL Inhibitory concentration against Prostaglandin G/H synthase 2 B 7.25 pIC50 56.7 nM IC50 J Med Chem (2001) 44: 2921-2927 [PMID:11520200]
ChEMBL Inhibition of human recombinant COX-2 assessed as production of PGE2 using arachidonic acid as a substrate preincubated for 60 mins followed by substrate addition and measured after 2 mins by ELISA analysis B 7.25 pIC50 56 nM IC50 Bioorg Med Chem (2021) 46: 116344-116344 [PMID:34438337]
ChEMBL Inhibition of COX-2 in human HNSCC 1483 cells using [14C] arachidonic acid as substrate preincubated for 30 mins before substrate addition measured after 30 mins B 7.27 pIC50 54 nM IC50 J Med Chem (2012) 55: 2287-2300 [PMID:22263894]
ChEMBL Compound was tested for the inhibition of recombinant human Prostaglandin G/H synthase 2 (COX-2) B 7.27 pIC50 54 nM IC50 J Med Chem (2003) 46: 5484-5504 [PMID:14640557]
ChEMBL Inhibition of human recombinant COX2 by ELISA B 7.28 pIC50 52 nM IC50 Bioorg Med Chem Lett (2015) 25: 1947-1951 [PMID:25866240]
ChEMBL Inhibitory concentration against Prostaglandin G/H synthase 2 B 7.29 pIC50 50.7 nM IC50 J Med Chem (2001) 44: 3039-3042 [PMID:11520213]
ChEMBL Inhibition of human recombinant COX2 catalytic activity using arachidonic acid as substrate pre-incubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA method B 7.3 pIC50 50 nM IC50 Eur J Med Chem (2019) 167: 562-582 [PMID:30818268]
ChEMBL Inhibition of human recombinant COX2 by colorimetric analysis B 7.3 pIC50 50 nM IC50 Eur J Med Chem (2020) 200: 112439-112439 [PMID:32485532]
ChEMBL Inhibition of human recombinant COX2 assessed as reduction in PGH2 formation by measuring PGF2alpha by colorimetric assay B 7.3 pIC50 50 nM IC50 Bioorg Med Chem (2017) 25: 5637-5651 [PMID:28916158]
ChEMBL Inhibition of human recombinant COX2 pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay B 7.3 pIC50 50 nM IC50 ACS Med Chem Lett (2014) 5: 983-988 [PMID:25221653]
ChEMBL Inhibition of recombinant human COX2 assessed as reduction in PGF2alpha production using arachidonic acid as substrate by colorimetric method B 7.3 pIC50 50 nM IC50 Eur J Med Chem (2018) 144: 635-650 [PMID:29289887]
ChEMBL Inhibition of human recombinant COX-2 by EIA method B 7.31 pIC50 49 nM IC50 Eur J Med Chem (2019) 183: 111693-111693 [PMID:31539778]
ChEMBL Inhibition of human recombinant COX2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA B 7.35 pIC50 45 nM IC50 Bioorg Med Chem (2020) 28: 115403-115403 [PMID:32127262]
ChEMBL Inhibition of human recombinant COX-2 using arachidonic acid as substrate preincubated with enzyme for 5 mins followed by substrate addition by colorimetric analysis B 7.35 pIC50 45 nM IC50 Eur J Med Chem (2021) 219: 113457-113457 [PMID:33892270]
ChEMBL Inhibition of human recombinant COX2 expressed in insect cells using arachidonic acid as substrate incubated for 1 min prior to substrate addition measured for 25 secs by TMPD-based chromogenic assay B 7.38 pIC50 42 nM IC50 Bioorg Med Chem Lett (2012) 22: 6745-6749 [PMID:23010270]
ChEMBL Inhibition of human COX2 using arachidonic acid as substrate assessed as PGE2 formation incubated for 10 mins prior to substrate addition measured after 10 mins by ELISA B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2014) 76: 494-505 [PMID:24602792]
ChEMBL Inhibition of human recombinant COX-2 expressed in insect cell system using arachidonic acid as substrate assessed as reduction of PGG2 to PGH2 incubated for 1 min prior to substrate addition measured after 25 secs by chromogenic assay B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2014) 24: 2251-2255 [PMID:24745964]
ChEMBL Inhibition of human recombinant COX2 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by spectrophotometry B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2014) 24: 77-82 [PMID:24332492]
ChEMBL Inhibition of human recombinant COX-2 assessed as decrease in prostaglandin production using arachidonic acid as substrate incubated with enzyme for 10 mins prior to substrate challenge by enzyme immunoassay B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2014) 77: 185-192 [PMID:24631898]
ChEMBL Inhibition of COX2 (unknown origin) by solid phase ELISA method B 7.4 pIC50 40 nM IC50 Bioorg Med Chem (2014) 22: 4109-4118 [PMID:24934992]
ChEMBL Inhibition of human recombinant COX-2 assessed as PGF2 alpha formation using arachidonic acid as substrate pretreated with compound for 20 mins prior to substrate addition by spectrophotometric analysis B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2015) 97: 104-123 [PMID:25956953]
ChEMBL Inhibition of COX2 B 7.4 pIC50 40 nM IC50 J Med Chem (2012) 55: 2287-2300 [PMID:22263894]
ChEMBL Inhibition of COX2 (unknown origin) B 7.4 pIC50 40 nM IC50 Medchemcomm (2015) 6: 2081-2123
ChEMBL Inhibition of COX-2 (unknown origin) B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2016) 26: 1516-1520 [PMID:26898334]
ChEMBL Inhibition of recombinant human COX-2 preincubated for 5 mins followed by addition of arachidonic acid as substrate measured after 2 mins by fluorescence analysis B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2016) 26: 1516-1520 [PMID:26898334]
ChEMBL Inhibition of human recombinant COX2 assessed as reduction in PGH2-derived PGF2alpha using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 2 mins by enzyme immunoassay B 7.4 pIC50 40 nM IC50 J Med Chem (2016) 59: 3920-3934 [PMID:27019010]
ChEMBL Inhibition of human recombinant COX2 by fluorescence assay B 7.4 pIC50 40 nM IC50 Bioorg Med Chem (2012) 20: 2221-2226 [PMID:22386983]
ChEMBL Inhibition of human COX2 B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2011) 21: 993-996 [PMID:21215625]
ChEMBL Inhibition of human COX2 pre-incubated for 10 mins before arachidonic acid addition and measured after 2 mins by EIA method B 7.4 pIC50 40 nM IC50 J Med Chem (2018) 61: 7929-7941 [PMID:30095904]
ChEMBL In vitro inhibitory concentration required to block human recombinant prostaglandin G/H synthase 2 (COX-2) B 7.4 pIC50 40 nM IC50 J Med Chem (1997) 40: 1347-1365 [PMID:9135032]
ChEMBL Inhibition of recombinant human COX-2 expressed in Baculovirus infected sf9 cells using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by ELISA B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2019) 162: 1-17 [PMID:30396033]
ChEMBL In vitro inhibitory activity against human Prostaglandin G/H synthase 2 B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (1999) 9: 1171-1174 [PMID:10328307]
ChEMBL Inhibition of recombinant human COX-2 assessed as reduction in prostaglandin production preincubated for 10 mins followed by arachidonic acid addition and measured after 2 mins by EIA method B 7.4 pIC50 40 nM IC50 J Med Chem (2019) 62: 6363-6376 [PMID:31244108]
ChEMBL Inhibition of human COX2 using arachidonic acid as substrate incubated for 10 mins followed by substrate addition and measured after 2 mins by EIA assay B 7.4 pIC50 40 nM IC50 Bioorg Med Chem (2020) 28: 115246-115246 [PMID:31843462]
ChEMBL Inhibitory concentration against human prostaglandin G/H synthase 2 at 25 degrees. B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2002) 12: 267-270 [PMID:11814774]
ChEMBL In Vitro activity of compound against human recombinant Prostaglandin G/H synthase 2 B 7.4 pIC50 40 nM IC50 J Med Chem (2000) 43: 775-777 [PMID:10715145]
ChEMBL In Vitro activity of compound against human recombinant Prostaglandin G/H synthase 2 B 7.4 pIC50 40 nM IC50 J Med Chem (2000) 43: 775-777 [PMID:10715145]
ChEMBL Inhibition of human COX-2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA B 7.4 pIC50 40 nM IC50 J Med Chem (2021) 64: 9550-9566 [PMID:34137625]
ChEMBL Inhibition of human Prostaglandin G/H synthase 2 B 7.4 pIC50 39.81 nM IC50 J Med Chem (2001) 44: 3223-3230 [PMID:11563921]
ChEMBL Inhibitory activity against human Prostaglandin G/H synthase 2 expressed in sf-9 cells infected with baculovirus B 7.44 pIC50 36 nM IC50 Bioorg Med Chem Lett (2004) 14: 499-504 [PMID:14698190]
ChEMBL In vitro inhibitory activity against recombinant human Prostaglandin G/H synthase 2 B 7.44 pIC50 36 nM IC50 Bioorg Med Chem Lett (2003) 13: 1639-1643 [PMID:12729631]
ChEMBL In vitro inhibitory activity against human recombinant prostaglandin G/H synthase 2 expressed in sf-9 cells infected with baculovirus B 7.44 pIC50 36 nM IC50 Bioorg Med Chem Lett (2004) 14: 1683-1688 [PMID:15026050]
ChEMBL Inhibition of COX2 expressed in CHO cells assessed as inhibition of arachidonic acid-stimulated PGE2 production by enzyme immunoassay F 7.44 pIC50 36 nM IC50 J Med Chem (2004) 47: 6195-6206 [PMID:15566290]
ChEMBL Inhibition of human recombinant COX-2 assessed as reduction in PGF2alpha formation using arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition for 30 secs and measured after 1 hr by microplate reader based enzyme immunoassay B 7.45 pIC50 35.56 nM IC50 Eur J Med Chem (2019) 171: 332-342 [PMID:30928706]
ChEMBL Inhibition of human recombinant COX2 by measuring PGE2 B 7.46 pIC50 35 nM IC50 Bioorg Med Chem (2007) 15: 6109-6118 [PMID:17604631]
ChEMBL Inhibition of COX2 by fluorescence assay B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (2012) 22: 3567-3570 [PMID:22516282]
ChEMBL Inhibition of human recombinant COX-2 by fluorescence assay B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (2011) 21: 1823-1826 [PMID:21316237]
ChEMBL Inhibition of human recombinant COX2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by ADHP probe-based fluorescence assay B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (2017) 27: 1721-1726 [PMID:28284805]
ChEMBL Inhibition of human recombinant COX-2 assessed as reduction in peroxidase activity using arachidonic acid as substrate preincubated for 60 mins followed by substrate addition for 2 secs by ADPH based fluorometric analysis B 7.55 pIC50 28 nM IC50 J Med Chem (2021) 64: 11570-11596 [PMID:34279934]
ChEMBL Inhibition of recombinant human COX2 assessed as PGH2 formation preincubated for 10 mins followed by addition of arachidonic acid as substrate measured after 2 mins by ELISA B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2016) 26: 4757-4762 [PMID:27567369]
ChEMBL Inhibition of human recombinant COX2 by fluorescence assay B 7.7 pIC50 20 nM IC50 Bioorg Med Chem (2013) 21: 4288-4295 [PMID:23706267]
ChEMBL Inhibition of human recombinant COX-2 using arachidonic acid after 15 mins by fluorescence based assay B 7.72 pIC50 19 nM IC50 Bioorg Med Chem Lett (2015) 25: 4082-4084 [PMID:26316467]
ChEMBL Inhibition of human recombinant COX2 using fluorometric substrate after 15 mins B 7.72 pIC50 19 nM IC50 Bioorg Med Chem Lett (2015) 25: 1986-1989 [PMID:25819096]
ChEMBL Inhibition of human COX2 assessed as reduction in PGF2alpha production using arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition by ELISA B 7.75 pIC50 17.79 nM IC50 Eur J Med Chem (2019) 171: 25-37 [PMID:30904755]
ChEMBL Inhibition of human recombinant COX2 pre-incubated for 15 mins followed by addition of heme and fluorometric substrate and further incubated for 15 mins in presence of arachidonic acid by fluorescence based assay B 7.8 pIC50 16 nM IC50 Bioorg Med Chem Lett (2015) 25: 2469-2472 [PMID:25980909]
ChEMBL Inhibition of human COX2 assessed as reduction in PGF2alpha level using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition by ELISA B 7.92 pIC50 12 nM IC50 Bioorg Med Chem (2018) 26: 141-151 [PMID:29191502]
ChEMBL Inhibition of human COX-2 using arachidonic acid as substrate incubated for 5 mins by fluorescence-based assay B 7.95 pIC50 11.2 nM IC50 Eur J Med Chem (2019) 180: 41-50 [PMID:31299586]
ChEMBL Inhibition of human recombinant COX-2 after 2 mins by fluorescence assay B 8 pIC50 10 nM IC50 J Med Chem (2011) 54: 3037-3050 [PMID:21434686]
ChEMBL Inhibition of recombinant human COX-2 preincubated for 15 mins followed by fluorometric substrate/heme addition for 15 mins subsequently incubated with arachidonic acid for 2 mins by fluorescence analysis B 8.15 pIC50 7 nM IC50 J Med Chem (2017) 60: 4135-4146 [PMID:28475316]
ChEMBL Inhibitory concentration against COX-2; (valus obtained by Kato et al.) B 8.17 pIC50 6.8 nM IC50 J Med Chem (2005) 48: 6997-7004 [PMID:16250658]
ChEMBL Inhibition of human recombinant COX-2 using arachidonic acid as substrate by fluorescence assay B 8.22 pIC50 6 nM IC50 Eur J Med Chem (2021) 224: 113682-113682 [PMID:34245948]
ChEMBL Inhibitory concentration against COX-2 upon incubation for 15 minutes at 37 degree C B 8.22 pIC50 6 nM IC50 J Med Chem (2005) 48: 6997-7004 [PMID:16250658]
ChEMBL Inhibition of COX2 (unknown origin) using arachidonic acid as substrate pretreated for 10 mins followed by substrate addition measured after 2 mins by enzyme-immunoassay B 8.32 pIC50 4.8 nM IC50 Bioorg Med Chem Lett (2017) 27: 2377-2383 [PMID:28427813]
ChEMBL Inhibition of COX2 B 8.66 pIC50 2.2 nM IC50 Bioorg Med Chem Lett (2006) 16: 4483-4487 [PMID:16806914]
ChEMBL In vitro inhibitory potency against human COX-2 in stably transfected chinese hamster ovary (CHO) cells B 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (1999) 9: 3181-3186 [PMID:10576684]
ChEMBL Inhibition of PGE-2 production in CHO cells expressing human COX-2. B 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (1999) 9: 3187-3192 [PMID:10576685]
ChEMBL In vitro potency against human Prostaglandin G/H synthase 2 in transfected CHO cells. B 8.7 pIC50 2 nM IC50 J Med Chem (1999) 42: 1274-1281 [PMID:10197970]
ChEMBL Inhibitory of human Prostaglandin G/H synthase 2 expressed in CHO cells. B 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2003) 13: 1195-1198 [PMID:12643942]
GtoPdb - - 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2003) 13: 1195-8 [PMID:12643942]
ChEMBL Inhibition of COX2 B 9.28 pIC50 0.52 nM IC50 Eur J Med Chem (2008) 43: 1297-1303 [PMID:17714833]
ChEMBL Inhibition of COX2 B 9.28 pIC50 0.52 nM IC50 Eur J Med Chem (2008) 43: 1297-1303 [PMID:17714833]
Cyclooxygenase-2 in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4033] [UniProtKB: Q8SPQ9]
ChEMBL In vitro inhibitory activity against canine prostaglandin G/H synthase 2. B 6.05 pIC50 900 nM IC50 Bioorg Med Chem Lett (2004) 14: 95-98 [PMID:14684306]
Cyclooxygenase-2 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3331] [UniProtKB: O62698]
ChEMBL Inhibition of Bos taurus (bovine) COX-2 by Chemoiluminescence assay B 7.22 pIC50 60 nM IC50 Med Chem Res (2010) 19: 782-793
ChEMBL In vitro inhibitory activity against prostaglandin G/H synthase 2 (COX-2) B 7.24 pIC50 57 nM IC50 J Med Chem (2003) 46: 4872-4882 [PMID:14584938]
Cyclooxygenase-2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4102] [UniProtKB: P79208]
ChEMBL Inhibitory concentration against Prostaglandin G/H synthase 2 from sheep placenta at 100 uM B 5.69 pIC50 2050 nM IC50 Bioorg Med Chem Lett (2005) 15: 1793-1797 [PMID:15780608]
ChEMBL Inhibition of ovine COX2 by enzyme immuno assay B 5.77 pIC50 1710 nM IC50 Bioorg Med Chem (2008) 16: 3907-3916 [PMID:18272371]
ChEMBL Inhibition of ovine COX-2 assessed as reduction in PGF2-alpha formation using arachidonic acid as substrate by enzyme immunoassay B 5.81 pIC50 1540 nM IC50 Eur J Med Chem (2016) 118: 250-258 [PMID:27131067]
ChEMBL Inhibition of Ovine COX-2 assessed as decrease in prostaglandin production using arachidonic acid as substrate pretreated for 15 mins followed by substrate addition and measured after 2 mins by enzyme immunoassay B 5.81 pIC50 1540 nM IC50 Bioorg Med Chem Lett (2016) 26: 2893-2899 [PMID:27158139]
ChEMBL Inhibition of ovine COX-2 assessed as appearance of oxidized TMPD level by EIA method B 5.81 pIC50 1540 nM IC50 Eur J Med Chem (2016) 123: 803-813 [PMID:27541263]
ChEMBL Inhibition of ovine COX2 B 6.18 pIC50 660 nM IC50 Bioorg Med Chem Lett (2017) 27: 3378-3381 [PMID:28610982]
ChEMBL Inhibition of ovine COX-2 using arachidonic acid after 5 mins by colorimetric method B 6.25 pIC50 560 nM IC50 Bioorg Med Chem (2015) 23: 6807-6814 [PMID:26455657]
ChEMBL Inhibition of ovine COX2 by colorimetric assay B 6.27 pIC50 540 nM IC50 Eur J Med Chem (2019) 162: 435-447 [PMID:30469039]
ChEMBL Inhibition of ovine COX2 B 6.36 pIC50 440 nM IC50 Bioorg Med Chem Lett (2006) 16: 4440-4443 [PMID:16814546]
ChEMBL Inhibition of ovine COX2 assessed as PGE2 formation preincubated for 10 mins by ELISA B 6.44 pIC50 360 nM IC50 Eur J Med Chem (2011) 46: 5763-5768 [PMID:22019186]
ChEMBL Inhibition of ovine COX2 assessed as reduction in PGF2alpha production using arachidonic acid as substrate preincubated with enzyme for 5 mins followed by substrate addition and measured after 2 mins by colorimetric analysis B 6.48 pIC50 330 nM IC50 Eur J Med Chem (2016) 121: 410-421 [PMID:27318118]
ChEMBL Inhibition of ovine COX2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition by ELISA B 6.52 pIC50 300 nM IC50 Bioorg Med Chem (2016) 24: 3818-3828 [PMID:27344214]
ChEMBL Inhibition of ovine COX2 assessed as reduction in PGH2-dervied PGF2alpha production preincubated for 5 mins followed by addition of arachidonic acid as substrate measured after 2 mins by enzyme immunoassay B 6.52 pIC50 300 nM IC50 Eur J Med Chem (2016) 115: 121-131 [PMID:26999325]
ChEMBL Inhibition of ovine COX-2 using arachidonic acid as substrate assessed as production of PGH2-alpha preincubated for 5 mins followed by addition of substrate measured after 2 mins by EIA B 6.52 pIC50 300 nM IC50 Bioorg Med Chem (2016) 24: 2032-2042 [PMID:27025563]
ChEMBL Inhibition of ovine COX2 assessed as PGF2alpha production from PGH2 after 5 mins by enzyme immunoassay B 6.52 pIC50 300 nM IC50 Bioorg Med Chem (2011) 19: 3416-3424 [PMID:21570309]
ChEMBL Inhibition of ovine COX2 B 6.52 pIC50 300 nM IC50 Bioorg Med Chem Lett (2014) 24: 5324-5329 [PMID:25444084]
ChEMBL Inhibition of ovine COX2 after 5 mins by enzyme immunoassay B 6.52 pIC50 300 nM IC50 Eur J Med Chem (2011) 46: 1648-1655 [PMID:21388719]
ChEMBL Inhibition of ovine COX2 by enzyme immuno assay B 6.55 pIC50 280 nM IC50 Bioorg Med Chem (2012) 20: 3306-3316 [PMID:22516672]
ChEMBL Inhibition of ovine COX2 by peroxidase activity-based colorimetric assay B 6.55 pIC50 280 nM IC50 Eur J Med Chem (2014) 74: 606-618 [PMID:24531199]
ChEMBL Inhibition of ovine COX2 assessed as reduction in PGH2 production using arachidonic acid substrate by enzyme immunoassay B 6.55 pIC50 280 nM IC50 Eur J Med Chem (2014) 86: 122-132 [PMID:25147154]
ChEMBL Inhibition of ovine COX2 assessed as reduction in PGH2-dervied PGF2alpha production using arachidonic acid substrate by enzyme immunoassay B 6.55 pIC50 280 nM IC50 Eur J Med Chem (2014) 87: 868-880 [PMID:24576797]
ChEMBL Inhibition of ovine COX2-mediated prostaglandin alpha production by enzyme immuno assay B 6.59 pIC50 260 nM IC50 Bioorg Med Chem Lett (2013) 23: 2601-2605 [PMID:23528298]
ChEMBL Inhibition of ovine COX2 assessed as inhibition of PGF2alpha production from PGH2 preincubated for 5 mins before arachidonic acid addition measured after 2 mins by enzyme immunoassay B 6.59 pIC50 260 nM IC50 Eur J Med Chem (2015) 92: 115-123 [PMID:25549551]
ChEMBL Inhibition of ovine COX2 using arachidonic acid as substrate assessed as conversion of PGH2 to PGF2alpha after 10 mins by EIA B 6.66 pIC50 220 nM IC50 Bioorg Med Chem (2014) 22: 2080-2089 [PMID:24631365]
ChEMBL Inhibition of ovine COX2 using arachidonic acid as substrate incubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay B 6.74 pIC50 180 nM IC50 Medchemcomm (2016) 7: 2309-2327
ChEMBL Inhibition of ovine COX2 assessed as reduction in PGF2alpha formation incubated for 18 hrs by enzyme immunoassay B 6.82 pIC50 150 nM IC50 Bioorg Med Chem Lett (2014) 24: 4638-4642 [PMID:25219899]
ChEMBL Inhibition of ovine COX2 using arachidonic acid as substrate preincubated for 10 mins before substrate addition measured after 5 mins by EIA B 6.82 pIC50 150 nM IC50 Eur J Med Chem (2014) 80: 47-56 [PMID:24763362]
ChEMBL Inhibition of ovine COX2 using arachidonic acid as substrate assessed as production of PGF2alpha preincubated for 10 mins followed by substrate addition measured after 2 mins by EIA in presence of stannous chloride B 6.82 pIC50 150 nM IC50 Bioorg Med Chem (2013) 21: 4581-4590 [PMID:23769654]
ChEMBL Inhibition of ovine COX-2 assessed as inhibition of transformation of AA to PGH2 by EIA B 6.95 pIC50 113 nM IC50 Bioorg Med Chem Lett (2009) 19: 6922-6925 [PMID:19880317]
ChEMBL Inhibition of ovine COX2 using arachidonic acid as substrate incubated for 5 mins followed by substrate addition measured after 2 mins by colorimetric based ELISA B 6.96 pIC50 110 nM IC50 Eur J Med Chem (2018) 158: 134-143 [PMID:30216848]
ChEMBL Inhibition of sheep COX2 by spectrophotometry B 7 pIC50 100 nM IC50 J Med Chem (2010) 53: 6560-6571 [PMID:20804197]
ChEMBL Inhibition of ovine COX2 using arachidonic acid substrate by TMPD dye based colorimetry B 7 pIC50 100 nM IC50 Medchemcomm (2017) 8: 492-500 [PMID:30108767]
ChEMBL Inhibition of ovine COX2 by ELISA B 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (2020) 30: 127173-127173 [PMID:32278513]
ChEMBL Inhibition of ovine COX2 by enzyme immuno assay B 7.15 pIC50 70 nM IC50 Bioorg Med Chem (2008) 16: 9694-9698 [PMID:18930406]
ChEMBL In vitro inhibitory concentration against ovine Cyclooxygenase-2 B 7.15 pIC50 70 nM IC50 Bioorg Med Chem Lett (2005) 15: 439-442 [PMID:15603969]
ChEMBL In vitro inhibitory concentration against ovine Cyclooxygenase-2 B 7.15 pIC50 70 nM IC50 Bioorg Med Chem Lett (2005) 15: 439-442 [PMID:15603969]
ChEMBL In vitro inhibitory concentration against ovine Prostaglandin G/H synthase 2 B 7.15 pIC50 70 nM IC50 Bioorg Med Chem Lett (2004) 14: 4911-4914 [PMID:15341950]
ChEMBL Inhibition of ovine Prostaglandin G/H synthase 2 B 7.15 pIC50 70 nM IC50 J Med Chem (2004) 47: 3972-3990 [PMID:15267236]
ChEMBL In vitro inhibition of ovine prostaglandin G/H synthase 2 B 7.15 pIC50 70 nM IC50 J Med Chem (2004) 47: 6108-6111 [PMID:15537365]
ChEMBL Inhibitory activity against ovine COX2 B 7.15 pIC50 70 nM IC50 J Med Chem (2006) 49: 1668-1683 [PMID:16509583]
ChEMBL Inhibition of ovine COX2 by enzyme immuno assay B 7.15 pIC50 70 nM IC50 Bioorg Med Chem (2007) 15: 6796-6801 [PMID:17764958]
ChEMBL Inhibition of ovine COX2 by enzyme immuno assay B 7.15 pIC50 70 nM IC50 Bioorg Med Chem (2008) 16: 1948-1956 [PMID:18023187]
ChEMBL Inhibition of ovine COX2 by enzyme immunoassay B 7.15 pIC50 70 nM IC50 Bioorg Med Chem (2008) 16: 3302-3308 [PMID:18096394]
ChEMBL Inhibition of ovine COX2 by enzyme immuno assay B 7.15 pIC50 70 nM IC50 Bioorg Med Chem Lett (2008) 18: 6138-6141 [PMID:18945614]
ChEMBL Inhibition of ovine COX2 by enzyme-immuno assay B 7.15 pIC50 70 nM IC50 Eur J Med Chem (2009) 44: 3798-3804 [PMID:19457595]
ChEMBL Inhibition of ovine COX2 assessed as inhibition of PGF2a formation after 20 mins by Ellman's method B 7.15 pIC50 70 nM IC50 J Med Chem (2010) 53: 3707-3717 [PMID:20387815]
ChEMBL Inhibition of ovine COX2 by enzyme immuno assay B 7.15 pIC50 70 nM IC50 Bioorg Med Chem Lett (2011) 21: 6074-6080 [PMID:21890358]
ChEMBL Inhibition of ovine COX2 by chemiluminescent enzyme assay B 7.22 pIC50 60 nM IC50 Bioorg Med Chem (2009) 17: 5312-5317 [PMID:19560931]
ChEMBL Inhibition of ovine COX2 by chemiluminescence assay B 7.22 pIC50 60 nM IC50 Bioorg Med Chem (2009) 17: 5369-5373 [PMID:19596198]
ChEMBL Inhibition of Ovis aries (sheep) cyclooxygenase-2 using arachidonic acid as substrate by chemiluminescent assay B 7.22 pIC50 60 nM IC50 Med Chem Res (2013) 22: 3881-3887
ChEMBL Inhibition of ovine COX2 using arachidonic acid as substrate by chemiluminescence assay B 7.22 pIC50 60 nM IC50 Bioorg Med Chem (2014) 22: 865-873 [PMID:24361187]
ChEMBL Inhibition of Ovis aries (sheep) COX2 using arachidonic acid as substrate using cyclic naphthalene hydrazide by chemiluminescence assay B 7.22 pIC50 60 nM IC50 Med Chem Res (2012) 21: 1803-1810
ChEMBL Inhibition of Ovis aries (sheep) COX2 using arachidonic acid as substrate using cyclic naphthalene hydrazide by chemiluminescence assay B 7.22 pIC50 60 nM IC50 Med Chem Res (2012) 21: 1869-1875
ChEMBL Inhibition of ovine COX2 by chemiluminescent assay B 7.22 pIC50 60 nM IC50 Bioorg Med Chem Lett (2009) 19: 3162-3165 [PMID:19447036]
ChEMBL Inhibition of Ovine COX-2 by chemiluminescent enzyme method B 7.22 pIC50 60 nM IC50 Bioorg Med Chem (2021) 32: 115960-115960 [PMID:33477020]
ChEMBL Inhibition of ovine COX2 by chemiluminescence assay B 7.22 pIC50 60 nM IC50 Eur J Med Chem (2010) 45: 4013-4017 [PMID:20691338]
ChEMBL Inhibition of ovine COX2 by enzyme chemiluminescent enzyme assay B 7.22 pIC50 60 nM IC50 Bioorg Med Chem (2010) 18: 1029-1033 [PMID:20061161]
ChEMBL Inhibition of ovine COX2 by chemiluminescent assay B 7.22 pIC50 60 nM IC50 Bioorg Med Chem Lett (2008) 18: 1336-1339 [PMID:18226898]
ChEMBL In vitro inhibitory activity against prostaglandin G/H synthase 2 from ovine B 7.24 pIC50 57 nM IC50 Bioorg Med Chem Lett (2004) 14: 1953-1956 [PMID:15050635]
ChEMBL Inhibition of Ovis aries (sheep) COX-2 assessed as decrease in PGF2a production from PGH2 upon reduction with stannous chloride using arachidonic acid as substrate pre-incubated with enzyme for 5 min prior to substrate addition by enzyme immunoassay B 7.24 pIC50 57 nM IC50 Med Chem Res (2013) 22: 2493-2504
ChEMBL In vitro inhibition against ovine Prostaglandin G/H synthase 2 B 7.25 pIC50 56.7 nM IC50 Bioorg Med Chem Lett (2003) 13: 2205-2209 [PMID:12798335]
ChEMBL Inhibition of ovine COX2 assessed as reduction in PGH2 production by enzyme immunoassay B 7.29 pIC50 50.7 nM IC50 Bioorg Med Chem (2018) 26: 4113-4126 [PMID:29980364]
ChEMBL Inhibition of ovine COX2 assessed as reduction in oxidized TMPD using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetric assay B 7.3 pIC50 50 nM IC50 Eur J Med Chem (2019) 171: 372-382 [PMID:30928709]
ChEMBL Inhibition of ovine COX -2 by colorimetric inhibitor screening assay kit method B 7.3 pIC50 50 nM IC50 Eur J Med Chem (2019) 167: 161-186 [PMID:30771604]
ChEMBL Inhibition of ovine COX2 assessed as PGF2alpha level by EIA B 7.3 pIC50 50 nM IC50 Bioorg Med Chem (2011) 19: 2074-2083 [PMID:21349729]
ChEMBL Inhibition of ovine COX2 by enzyme immunoassay B 7.4 pIC50 40 nM IC50 Bioorg Med Chem (2016) 24: 5626-5632 [PMID:27658794]
ChEMBL Inhibition of ovine COX2 peroxidase activity assessed as reduction of PGG2 to PGH2 by measuring oxidized TMPD level by colorimetric assay B 7.4 pIC50 40 nM IC50 Bioorg Med Chem (2014) 22: 2855-2866 [PMID:24751552]
ChEMBL Inhibition of ovine COX2 B 7.4 pIC50 40 nM IC50 Bioorg Med Chem (2008) 16: 276-283 [PMID:17937989]
COX-2 /Cyclooxygenase-2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4321] [GtoPdb: 1376] [UniProtKB: Q05769]
ChEMBL Inhibition of COX2-dependent PGE2 production in LPS-stimulated mouse J774 cells at 10 uM by RIA B 4.02 pIC50 95000 nM IC50 J Med Chem (2010) 53: 723-733 [PMID:19957931]
ChEMBL Inhibition of COX2-dependent PGE2 production in LPS-stimulated mouse J774 cells at 1 uM by RIA B 4.1 pIC50 80000 nM IC50 J Med Chem (2010) 53: 723-733 [PMID:19957931]
ChEMBL Inhibition of mouse COX2 B 4.6 pIC50 >25000 nM IC50 Bioorg Med Chem (2007) 15: 1976-1982 [PMID:17258905]
ChEMBL Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production B 6.92 pIC50 120 nM IC50 Eur J Med Chem (2013) 62: 222-231 [PMID:23353741]
ChEMBL Inhibition of COX2-dependent PGE2 production in LPS-stimulated mouse J774 cells by RIA B 7.1 pIC50 79 nM IC50 J Med Chem (2010) 53: 723-733 [PMID:19957931]
ChEMBL In vitro inhibitory activity against Prostaglandin G/H synthase 2 in murine J774 cells B 7.1 pIC50 79 nM IC50 J Med Chem (2005) 48: 3428-3432 [PMID:15857149]
ChEMBL Inhibition of COX-2-mediated PGE2 production in LPS-stimulated mouse J774 cells after 24 hrs by radioimmunoassay B 7.21 pIC50 61 nM IC50 J Med Chem (2011) 54: 7759-7771 [PMID:21992176]
ChEMBL Inhibition of COX2 in mouse J774 cells assessed as inhibition of LPS-induced PGE2 production by radioimmunoassay B 7.21 pIC50 61 nM IC50 Bioorg Med Chem (2013) 21: 3695-3701 [PMID:23680444]
ChEMBL Inhibition of COX2 in LPS-stimulated mouse J774 cells assessed as inhibition of PGE2 production after 15 mins by radioimmunoassay B 7.22 pIC50 60 nM IC50 Bioorg Med Chem (2008) 16: 8072-8081 [PMID:18752957]
ChEMBL Inhibition of COX2 in LPS-stimulated J774 cells assessed as inhibition of PGE2 levels by radioimmunoassay B 7.22 pIC50 60 nM IC50 J Med Chem (2007) 50: 5403-5411 [PMID:17915854]
ChEMBL Inhibitory activity against prostaglandin G/H synthase 2 (COX-2) B 7.4 pIC50 39.81 nM IC50 J Med Chem (2002) 45: 4816-4827 [PMID:12383007]
ChEMBL Inhibition of mouse purified COX2 after 20 mins B 7.52 pIC50 30 nM IC50 ACS Med Chem Lett (2011) 2: 160-164 [PMID:21318094]
ChEMBL Tested for inhibition against Prostaglandin G/H synthase 1 from mouse resident macrophages B 8.03 pIC50 9.3 nM IC50 J Med Chem (2000) 43: 4582-4593 [PMID:11101350]
ChEMBL Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production treated prior to LPS challenge by enzyme immunoassay B 8.06 pIC50 8.7 nM IC50 Bioorg Med Chem Lett (2014) 24: 1958-1962 [PMID:24656662]
ChEMBL In vivo inhibition of COX2 in po dosed C57BL/6J mouse model of spontaneous GI-tract tumor Apc-min assessed as chemopreventive effect by measuring reduction in polyp area and relevant plasma exposures F 8.49 pIC50 3.2 nM IC50 J Med Chem (2021) 64: 11570-11596 [PMID:34279934]
ChEMBL In vivo inhibition of COX2 in po dosed C57BL/6J mouse model of spontaneous GI-tract tumor Apc-min assessed as chemopreventive effect by measuring reduction in polyp area and relevant ileum exposures F 8.49 pIC50 3.2 nM IC50 J Med Chem (2021) 64: 11570-11596 [PMID:34279934]
ChEMBL Inhibition of LPS-induced COX2 activity in C57BL/6J mouse peritoneal macrophages by RIA B 9.29 pIC50 0.51 nM IC50 J Nat Prod (2006) 69: 1591-1595 [PMID:17125227]
COX-2 /Cyclooxygenase-2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2977] [GtoPdb: 1376] [UniProtKB: P35355]
ChEMBL In vitro inhibitory concentration against rat Prostaglandin G/H synthase 2 B 5.96 pIC50 1100 nM IC50 Bioorg Med Chem Lett (2001) 11: 2687-2690 [PMID:11591502]
ChEMBL Inhibition of COX2 in rat abdominal macrophages assessed as PGE2 production pretreated for 30 mins followed by addition of 10 uM arachidonic acid as substrate for 20 mins by EIA B 6.85 pIC50 140 nM IC50 Eur J Med Chem (2016) 108: 89-103 [PMID:26638042]
ChEMBL Inhibition of COX-2 in rat peritoneal macrophages assessed as reduction in PGE2 production using radiolabelled-arachidonic acid as substrate pretreated for 30 mins followed by substrate addition measured after 30 mins B 7.15 pIC50 71 nM IC50 Bioorg Med Chem (2017) 25: 4887-4893 [PMID:28757100]
Cytochrome c oxidase subunit 1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6011] [UniProtKB: O78749]
ChEMBL Inhibition of ovine COX1 assessed as reduction in PGF2alpha incubated for 2 mins using arachidonic acid as substrate by ELISA B 4.56 pIC50 27250 nM IC50 Eur J Med Chem (2019) 182: 111601-111601 [PMID:31445233]
ChEMBL Inhibition of sheep COX1 B 4.61 pIC50 24300 nM IC50 Bioorg Med Chem (2010) 18: 5855-5860 [PMID:20650641]
ChEMBL Inhibition of ovine COX1 preincubated for 5 mins followed by arachidonic acid addition and measured after 2 mins by colorimetric method B 5.19 pIC50 6500 nM IC50 Bioorg Med Chem (2019) 27: 3979-3997 [PMID:31401008]
Cytochrome c oxidase subunit 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6174] [UniProtKB: P00403]
ChEMBL Inhibition of human COX2 assessed as reduction in PGF2alpha production by ELISA B 6.27 pIC50 540 nM IC50 Eur J Med Chem (2017) 139: 936-946 [PMID:28881288]
ChEMBL Inhibition of recombinant human COX2 assessed as reduction in PGF2alpha incubated for 2 mins using arachidonic acid as substrate by ELISA B 6.53 pIC50 293 nM IC50 Eur J Med Chem (2019) 182: 111601-111601 [PMID:31445233]
ChEMBL Inhibition of recombinant human COX2 expressed in baculovirus infected Sf21 cells using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by UV-visible spectrophotometric method B 6.55 pIC50 280 nM IC50 Eur J Med Chem (2020) 186: 111863-111863 [PMID:31740050]
Cytochrome c oxidase subunit 2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1250404] [UniProtKB: O78750]
ChEMBL Inhibition of sheep COX2 B 7.22 pIC50 60 nM IC50 Bioorg Med Chem (2010) 18: 5855-5860 [PMID:20650641]
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
ChEMBL DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 6 pIC50 1000 nM IC50 DrugMatrix in vitro pharmacology data
Delta carbonic anhydrase in Thalassiosira weissflogii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3097982] [UniProtKB: Q5U9J1]
ChEMBL Inhibition of Thalassiosira weissflogii delta carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay B 6.58 pKi 265 nM Ki Bioorg Med Chem Lett (2014) 24: 275-279 [PMID:24314394]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 4.85 pKi 13997 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 4.55 pIC50 27994 nM IC50 DrugMatrix in vitro pharmacology data
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.71 pKi 1931 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.61 pIC50 2431 nM IC50 DrugMatrix in vitro pharmacology data
epoxide hydrolase 2/Epoxide hydratase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
ChEMBL Inhibition of human recombinant soluble epoxide hydrolase after 10 mins by fluorescent-based assay B 6 pIC50 >1000 nM IC50 J Med Chem (2011) 54: 3037-3050 [PMID:21434686]
histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
ChEMBL Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay B 5.93 pIC50 1185 nM IC50 Bioorg Med Chem (2018) 26: 1418-1425 [PMID:29500130]
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay B 6.19 pIC50 643 nM IC50 Bioorg Med Chem (2018) 26: 1418-1425 [PMID:29500130]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Inhibitory concentration against p38 alpha MAP kinase calculated by CoMFA model; FlexX score=-12.4 kcal/mol B 6.09 pIC50 810 nM IC50 Bioorg Med Chem Lett (2005) 15: 3506-3509 [PMID:15990304]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.14 pKi 7247 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.14 pIC50 7308 nM IC50 DrugMatrix in vitro pharmacology data
phosphodiesterase 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
ChEMBL Inhibition of recombinant 6His-tagged PDE5A1 catalytic domain (unknown origin) expressed in Escherichia coli using TAMRA-cGMP or FAM-cAMP as substrate incubated for 1.5 hrs by IMAP-FP assay B 4 pIC50 >100000 nM IC50 J Med Chem (2021) 64: 4462-4477 [PMID:33793216]
ChEMBL Inhibition of recombinant full length GST-tagged PDE5A1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using TAMRA-cGMP as substrate incubated for 1.5 hrs by IMAP-FP assay B 4.43 pIC50 37000 nM IC50 J Med Chem (2021) 64: 4462-4477 [PMID:33793216]
ChEMBL Fluorescence Polarization Assay: PDE activity was measured using the IMAP fluorescence polarization assay (Molecular Devices) in which binding of hydrolyzed cyclic nucleotide substrate to immobilized metal coordination complexes increases fluorescence polarization (FP). Tetramethylrhodamine (TAMRA)-cGMP and fluorescein-cAMP were used as substrates, each at final concentration of 50 nmol/L. The PDE assay was done according to the manufacturer's specifications using either whole cell lysates or recombinant enzymes. FP was measured at excitation, emission wavelengths of either 530,590 nm for TAMRA-cGMP or 485,530 nm for fluorescein-cAMP using a Synergy4 (Biotek) microplate reader. B 4.44 pIC50 36000 nM IC50 US-9388139-B2. Derivatives of celeboxib, use thereof and preparation thereof (2016)
PROBABLE TRANSMEMBRANE CARBONIC ANHYDRASE (CARBONATE DEHYDRATASE) (CARBONIC DEHYDRATASE) in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5767] [UniProtKB: P96878]
ChEMBL Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv3273 pre-incubated for 15 mins by stopped-flow CO2 hydration method B 5.11 pKi 7760 nM Ki J Med Chem (2012) 55: 9619-9629 [PMID:23067387]
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0]
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 5.63 pKi 2362 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 4.74 pIC50 18109 nM IC50 DrugMatrix in vitro pharmacology data
mPGES1/Prostaglandin E synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684]
ChEMBL Inhibition of mPGES1 (unknown origin) by enzymatic assay B 6.27 pIC50 540 nM IC50 J Med Chem (2016) 59: 194-205 [PMID:26653180]
ChEMBL Inhibition of mPGES-1 in human whole blood assessed as reduction in LPS-induced PGE2 production preincubated for 30 mins followed by LPS stimulation for 20 to 24 hrs by LC/MS/MS analysis B 6.27 pIC50 540 nM IC50 Bioorg Med Chem Lett (2016) 26: 4824-4828 [PMID:27554445]
ChEMBL Inhibition of human microsomal PGES1 expressed in 293E cells by LC/MS/MS analysis B 6.37 pIC50 425 nM IC50 J Med Chem (2016) 59: 194-205 [PMID:26653180]
Quinolone resistance protein norA in S.aureus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5114] [UniProtKB: P0A0J7]
ChEMBL Inhibition of norA-mediated EtBr efflux in Staphylococcus aureus SA1199B overexpressing norA and expressing A116E GrlA mutation by fluorometry B 4.4 pIC50 >40000 nM IC50 J Med Chem (2012) 55: 3568-3572 [PMID:22432682]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.48 pKi 3334 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.2 pIC50 6276 nM IC50 DrugMatrix in vitro pharmacology data
Uncharacterized protein Rv1284/MT1322 in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5631] [UniProtKB: P9WPJ7]
ChEMBL Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase 1 encoded by Rv1284 by stopped flow CO2 hydration assay B 4.99 pKi 10350 nM Ki J Med Chem (2009) 52: 3116-3120 [PMID:19338333]
ChEMBL Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv1284 pre-incubated for 15 mins by stopped-flow CO2 hydration method B 4.99 pKi 10350 nM Ki J Med Chem (2012) 55: 9619-9629 [PMID:23067387]
Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
ChEMBL Inhibition of Cav1.2 calcium current measured using whole Cell patch clamp in guinea pig ventricular myocytes F 4.97 pIC50 10600 nM IC50 IC50 data for the L-type calcium channel extracted from a set of literature articles

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]