SC-560 [Ligand Id: 10240] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL26915 (SC-560)
  • 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 9/Carbonic anhydrase IX in Human [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
ChEMBL Inhibitory activity against human carbonic anhydrase I was determined B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2004) 47: 550-557 [PMID:14736236]
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 was determined B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2004) 47: 550-557 [PMID:14736236]
Carbonic anhydrase IV in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL281] [UniProtKB: Q95323]
ChEMBL Inhibitory activity against bovine carbonic anhydrase IV was determined B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2004) 47: 550-557 [PMID:14736236]
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 was determined B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2004) 47: 550-557 [PMID:14736236]
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL Inhibition of COX-1 in human OVCAR3 cells using [14C] arachidonic acid as substrate preincubated for 30 mins before substrate addition measured after 30 mins B 6.8 pIC50 160 nM IC50 J. Med. Chem. (2012) 55: 2287-2300 [PMID:22263894]
ChEMBL Inhibition of COX1 by microplate reader B 8 pIC50 10 nM IC50 J. Nat. Prod. (2010) 73: 1234-1239 [PMID:20540535]
ChEMBL Inhibition of COX1 B 8.05 pIC50 9 nM IC50 J. Med. Chem. (2012) 55: 2287-2300 [PMID:22263894]
GtoPdb - - 8.05 pIC50 9 nM IC50 Proc Natl Acad Sci USA (1998) 95: 13313-8 [PMID:9789085]
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 8.05 pIC50 8.9 nM IC50 Bioorg. Med. Chem. (2013) 21: 2355-2362 [PMID:23473947]
ChEMBL Inhibition of COX1 B 8.11 pIC50 7.8 nM IC50 Eur. J. Med. Chem. (2011) 46: 191-200 [PMID:21106277]
ChEMBL In vitro inhibitory concentration required to block recombinant human prostaglandin G/H synthase 1 (COX-1) B 8.15 pIC50 7 nM IC50 J. Med. Chem. (1997) 40: 1347-1365 [PMID:9135032]
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979]
ChEMBL Inhibition of ovine COX1 by peroxidase activity-based colorimetric assay B 7.11 pIC50 77 nM IC50 Eur. J. Med. Chem. (2014) 74: 606-618 [PMID:24531199]
ChEMBL Inhibition of ovine recombinant COX1 assessed as decrease in formation of PGE2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 45 mins by LC-MS analysis B 7.41 pIC50 39 nM IC50 J Nat Prod (2019) 82: 3311-3320 [PMID:31774676]
ChEMBL Inhibition of ovine recombinant COX1 assessed as decrease in formation of PGE2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 45 mins by LC-MS analysis B 7.41 pIC50 39 nM IC50 J Nat Prod (2019) 82: 3311-3320 [PMID:31774676]
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 8 pIC50 10 nM IC50 Eur J Med Chem (2019) 180: 86-98 [PMID:31301566]
ChEMBL Inhibition of ovine COX1 by fluorescence assay B 8.07 pIC50 8.5 nM IC50 Bioorg. Med. Chem. (2012) 20: 2912-2922 [PMID:22475926]
ChEMBL Inhibition of ovine COX-1 assessed as inhibition of PGH2 production using arachidonic acid as substrate by TMPD oxidation based colorimetric assay B 8.15 pIC50 7 nM IC50 Eur. J. Med. Chem. (2015) 94: 252-264 [PMID:25768707]
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
ChEMBL In vitro inhibitory concentration required to block human recombinant prostaglandin G/H synthase 2 (COX-2) B 4.13 pIC50 74900 nM IC50 J. Med. Chem. (1997) 40: 1347-1365 [PMID:9135032]
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 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 4135-4146 [PMID:28475316]
GtoPdb - - 5.2 pIC50 6300 nM IC50 Proc Natl Acad Sci USA (1998) 95: 13313-8 [PMID:9789085]
ChEMBL Inhibition of COX2 B 5.2 pIC50 6300 nM IC50 J. Med. Chem. (2012) 55: 2287-2300 [PMID:22263894]
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 5.48 pIC50 >3300 nM IC50 Eur J Med Chem (2019) 180: 86-98 [PMID:31301566]
Cyclooxygenase-2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4102] [UniProtKB: P79208]
ChEMBL Inhibition of ovine COX-2 assessed as inhibition of PGH2 production using arachidonic acid as substrate by TMPD oxidation based colorimetric assay B 4.13 pIC50 74900 nM IC50 Eur. J. Med. Chem. (2015) 94: 252-264 [PMID:25768707]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]