rofecoxib [Ligand Id: 2893] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL122 (M01AH02, MK-0966, MK0966, MK-966, NSC-720256, NSC-758705, Rofecoxib, TRM-201, TRM201, Vioxx) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-LOX/Arachidonate 5-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917] | ||||||||
| ChEMBL | The compound was evaluated for its inhibitory activity against 5-lipoxygenase using granulocytes-type cells | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 779-782 [PMID:11859001] |
| COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219] | ||||||||
| ChEMBL | Inhibition of human cyclooxygenase-1 expressed in COS cells | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5445-5448 [PMID:15454242] |
| 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 | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573] |
| 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 COX1 in human whole blood assessed as TxB2 production after 1 hr | B | 4.19 | pIC50 | 64000 | nM | IC50 | J Med Chem (2007) 50: 1449-1457 [PMID:17335184] |
| ChEMBL | In vitro inhibitory concentration against Prostaglandin G/H synthase 1 (COX-1) in human whole blood | B | 4.21 | pIC50 | 62000 | nM | IC50 | J Med Chem (2005) 48: 3930-3934 [PMID:15916445] |
| ChEMBL | In vitro inhibition of Prostaglandin G/H synthase 1 in human whole blood | B | 4.4 | pIC50 | 40000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6049-6052 [PMID:15546727] |
| ChEMBL | Compound was evaluated for inhibition concentration of prostaglandin G/H synthase 1 in human blood | B | 4.4 | pIC50 | 40000 | nM | IC50 | J Med Chem (2004) 47: 2180-2193 [PMID:15084117] |
| ChEMBL | Compound was tested for the inhibition of human Prostaglandin G/H synthase 1 (COX-1) in human whole blood | B | 4.4 | pIC50 | 40000 | nM | IC50 | J Med Chem (2003) 46: 5484-5504 [PMID:14640557] |
| ChEMBL | Inhibition of COX1 | B | 4.4 | pIC50 | 40000 | nM | IC50 | Eur J Med Chem (2008) 43: 2792-2799 [PMID:18262309] |
| ChEMBL | DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) | B | 4.5 | pIC50 | 31868 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Inhibitory effect on Prostaglandin G/H synthase 1 activity was evaluated in human whole blood as TXB2 production | F | 4.54 | pIC50 | 28700 | nM | IC50 | J Med Chem (2002) 45: 1402-1411 [PMID:11906281] |
| ChEMBL | Inhibitory concentration against Prostaglandin G/H synthase 1 | B | 4.59 | pIC50 | 26000 | nM | IC50 | J Med Chem (2001) 44: 3039-3042 [PMID:11520213] |
| ChEMBL | Inhibition of COX1 | B | 4.59 | pIC50 | 26000 | nM | IC50 | J Med Chem (2012) 55: 2287-2300 [PMID:22263894] |
| ChEMBL | Inhibition of human Prostaglandin G/H synthase 1 | B | 4.59 | pIC50 | 26000 | nM | IC50 | J Med Chem (2002) 45: 1511-1517 [PMID:11906292] |
| ChEMBL | In vitro inhibitory potency against human COX-1 (HWB COX-2) by whole blood assay | B | 4.72 | pIC50 | 19000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3181-3186 [PMID:10576684] |
| ChEMBL | Inhibitory concentration was measured against Prostaglandin G/H synthase 1 in human whole blood | B | 4.72 | pIC50 | 19000 | 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 | 4.72 | pIC50 | 19000 | 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 | 4.72 | pIC50 | 19000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2207-2212 [PMID:10465547] |
| ChEMBL | In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 1 | B | 4.72 | pIC50 | 19000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1773-1778 [PMID:10406640] |
| ChEMBL | The compound was evaluated for its inhibitory activity against COX- 1. | B | 4.73 | pIC50 | 18800 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2683-2686 [PMID:11128651] |
| ChEMBL | Inhibitory potency against Prostaglandin G/H synthase 1 in human whole blood assay | B | 4.73 | pIC50 | 18800 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1201-1203 [PMID:14980665] |
| ChEMBL | Tested in vitro for inhibition of cyclooxygenase-1 in human blood assay | F | 4.74 | pIC50 | 18300 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 533-537 [PMID:11844666] |
| ChEMBL | Inhibition of COX1 in human whole blood assessed as inhibition of lipopolysaccharide-induced TxB2 production after 30 min by enzyme immunoassay | B | 4.81 | pIC50 | 15500 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573] |
| ChEMBL | In vitro inhibitory activity against human whole cells Prostaglandin G/H synthase 1 | B | 4.82 | pIC50 | >15000 | 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 assay as TXB2 generation | B | 4.94 | pIC50 | 11400 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 657-660 [PMID:12639552] |
| ChEMBL | Inhibition concentration against cyclooxygenase-1 (COX-1) in human whole blood | B | 4.94 | pIC50 | 11400 | nM | IC50 | J Med Chem (2004) 47: 3874-3886 [PMID:15239665] |
| ChEMBL | In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2003) 46: 3463-3475 [PMID:12877584] |
| ChEMBL | Inhibition of arachidonic acid induced TXB2 generation in isolated human platelets (Prostaglandin G/H synthase 1 cell assay) | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2002) 45: 1402-1411 [PMID:11906281] |
| ChEMBL | The compound was evaluated for its inhibitory activity against Prostaglandin G/H synthase 1 using monocytes-like cells | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 779-782 [PMID:11859001] |
| ChEMBL | Inhibition of COX-1 in U-937 (human lymphoma) cell microsomes. | B | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3187-3192 [PMID:10576685] |
| ChEMBL | In vitro inhibitory potency against U-937 microsomal COX-1 | B | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3181-3186 [PMID:10576684] |
| ChEMBL | In vitro potency against human Prostaglandin G/H synthase 1 (hCOX-1) in the human whole blood assay. | B | 5.72 | pIC50 | 1900 | nM | IC50 | J Med Chem (1999) 42: 1274-1281 [PMID:10197970] |
| ChEMBL | In vitro potency against human Prostaglandin G/H synthase 1 in U937 microsomes. | B | 5.77 | pIC50 | 1700 | 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 | 5.77 | pIC50 | 1700 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1195-1198 [PMID:12643942] |
| Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979] | ||||||||
| ChEMBL | Inhibition of ovine COX1 assessed as reduction in PGF2alpha production by ELISA | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2017) 139: 936-946 [PMID:28881288] |
| ChEMBL | In vitro inhibitory concentration against ovine Cyclooxygenase-1 | B | 4 | pIC50 | >100000 | 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 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4911-4914 [PMID:15341950] |
| ChEMBL | Inhibition of ovine Prostaglandin G/H synthase 1 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2004) 47: 3972-3990 [PMID:15267236] |
| ChEMBL | In vitro inhibition of ovine prostaglandin G/H synthase 1 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2004) 47: 6108-6111 [PMID:15537365] |
| ChEMBL | In vitro inhibitory activity against ovine cyclooxygenase 1 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4842-4845 [PMID:16143531] |
| ChEMBL | Inhibitory activity against ovine COX1 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2006) 49: 1668-1683 [PMID:16509583] |
| ChEMBL | Inhibition of ovine COX1 by enzyme immunoassay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2007) 15: 1056-1061 [PMID:17067801] |
| ChEMBL | Inhibition of ovine COX1 by enzyme immuno assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2007) 15: 6796-6801 [PMID:17764958] |
| ChEMBL | Inhibition of ovine COX1 by enzyme immuno assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3951-3956 [PMID:21641217] |
| ChEMBL | Inhibition of ovine COX1 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 163-168 [PMID:23200247] |
| ChEMBL | In vitro inhibitory concentration against ovine Cyclooxygenase-1 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 439-442 [PMID:15603969] |
| ChEMBL | Inhibition of ovine COX1 by enzyme immuno assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2008) 16: 1948-1956 [PMID:18023187] |
| ChEMBL | Inhibition of ovine COX1 by enzyme immunoassay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2008) 16: 3302-3308 [PMID:18096394] |
| ChEMBL | Inhibition of ovine COX1 by enzyme immunoassay | B | 4 | pIC50 | >=100000 | nM | IC50 | Eur J Med Chem (2009) 44: 1830-1837 [PMID:19084295] |
| ChEMBL | Inhibition of ovine COX1 assessed as inhibition of PGF2a formation after 20 mins by Ellman's method | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2010) 53: 3707-3717 [PMID:20387815] |
| ChEMBL | Inhibition of sheep COX1 by enzyme immunoassay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2010) 18: 6367-6376 [PMID:20692174] |
| ChEMBL | Inhibition of ovine COX1 | B | 4.4 | pIC50 | 40000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 85-89 [PMID:18061444] |
| ChEMBL | Inhibition of ovine COX-1 assessed as inhibition of [14C]arachidonic acid to radiolabeled prostaglandins preincubated for 15 mins by TLC-based assay | B | 4.6 | pIC50 | >25000 | nM | IC50 | ACS Med Chem Lett (2014) 5: 1254-1258 [PMID:25408841] |
| ChEMBL | Inhibition of sheep COX1 by spectrophotometry | B | 4.63 | pIC50 | 23500 | nM | IC50 | J Med Chem (2010) 53: 6560-6571 [PMID:20804197] |
| COX-1 /Cyclooxygenase-1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2649] [GtoPdb: 1375] [UniProtKB: P22437] | ||||||||
| ChEMBL | In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2005) 48: 3428-3432 [PMID:15857149] |
| COX-1 /Cyclooxygenase-1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4042] [GtoPdb: 1375] [UniProtKB: Q63921] | ||||||||
| ChEMBL | In vitro inhibitory concentration against rat prostaglandin G/H synthase 1 | B | 4.94 | pIC50 | 11400 | 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 COX2 expressed in human osteosarcoma cells assessed as reduction in PGE2 release | B | 4.59 | pIC50 | 26000 | nM | IC50 | Eur J Med Chem (2019) 171: 66-92 [PMID:30909021] |
| ChEMBL | Inhibition of human COX2 expressed in CHO cells cells assessed as reduction in PGE2 release | B | 4.74 | pIC50 | 18000 | nM | IC50 | Eur J Med Chem (2019) 171: 66-92 [PMID:30909021] |
| ChEMBL | Inhibitory effect on Prostaglandin G/H synthase 2 activity was evaluated in human whole blood as LPS-induced PGE-2 generation | F | 5.47 | pIC50 | 3400 | nM | IC50 | J Med Chem (2002) 45: 1402-1411 [PMID:11906281] |
| ChEMBL | Inhibition of human recombinant COX-2 after 2 mins by fluorescence assay | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2011) 54: 3037-3050 [PMID:21434686] |
| ChEMBL | Activity of COX2 in human heparinized blood assessed as inhibition of LPS-induced PGE2 production after 24 hrs | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2007) 50: 1449-1457 [PMID:17335184] |
| ChEMBL | Compound was tested for the inhibition of recombinant human Prostaglandin G/H synthase 2 (COX-2) | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2003) 46: 5484-5504 [PMID:14640557] |
| ChEMBL | Tested in vitro for inhibition of cyclooxygenase-2 in human blood assay | F | 6.08 | pIC50 | 830 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 533-537 [PMID:11844666] |
| ChEMBL | Inhibition of COX2 in human whole blood | B | 6.12 | pIC50 | 760 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3209-3212 [PMID:16616494] |
| ChEMBL | Inhibition concentration against cyclooxygenase-2 (COX-2) in human whole blood | B | 6.12 | pIC50 | 760 | nM | IC50 | J Med Chem (2004) 47: 3874-3886 [PMID:15239665] |
| ChEMBL | Inhibition of COX2 | B | 6.12 | pIC50 | 760 | nM | IC50 | J Nat Prod (2005) 68: 985-991 [PMID:16038536] |
| ChEMBL | Inhibition of COX2 by scintillation proximity assay | B | 6.12 | pIC50 | 760 | nM | IC50 | J Nat Prod (2002) 65: 1517-1521 [PMID:12444669] |
| ChEMBL | Inhibition of COX2 in human whole blood | B | 6.12 | pIC50 | 760 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3605-3608 [PMID:16647258] |
| ChEMBL | DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) | B | 6.17 | pIC50 | 679 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Inhibitory potency against cyclooxygenase-2 in human whole blood assay | B | 6.28 | pIC50 | 530 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1201-1203 [PMID:14980665] |
| ChEMBL | The compound was evaluated for its inhibitory activity against COX- 2. | B | 6.28 | pIC50 | 530 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2683-2686 [PMID:11128651] |
| ChEMBL | Inhibitory concentration was measured against Prostaglandin G/H synthase 2 in human whole blood | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1195-1198 [PMID:12643942] |
| ChEMBL | Inhibitory potency against PGE-2 production in the human whole blood (HWB COX-2) assay | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3187-3192 [PMID:10576685] |
| ChEMBL | In vitro potency against human Prostaglandin G/H synthase 2 in the human whole blood assay. | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (1999) 42: 1274-1281 [PMID:10197970] |
| ChEMBL | In vitro inhibitory potency against human COX-2 (HWB COX-2) by whole blood assay | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3181-3186 [PMID:10576684] |
| ChEMBL | In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 2 | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1773-1778 [PMID:10406640] |
| ChEMBL | Inhibition of Prostaglandin G/H synthase 2 in human whole blood | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2207-2212 [PMID:10465547] |
| ChEMBL | In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 2 | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1773-1778 [PMID:10406640] |
| ChEMBL | In vitro inhibitory concentration against Prostaglandin G/H synthase 2 (COX-2) in human whole blood | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2005) 48: 3930-3934 [PMID:15916445] |
| ChEMBL | Inhibition of human recombinant COX2 by enzyme immuno assay | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3951-3956 [PMID:21641217] |
| ChEMBL | Inhibition of COX-2 in human whole blood | B | 6.3 | pIC50 | 500 | nM | IC50 | Eur J Med Chem (2019) 162: 1-17 [PMID:30396033] |
| ChEMBL | Inhibition of human recombinant COX2 | B | 6.32 | pIC50 | 480 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 163-168 [PMID:23200247] |
| ChEMBL | In vitro inhibitory concentration of compound required to inhibit Prostaglandin G/H synthase 2 enzyme was determined | B | 6.37 | pIC50 | 427.9 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 2753-2756 [PMID:12217369] |
| ChEMBL | Inhibition of human recombinant COX-2 by enzyme immunoassay | B | 6.44 | pIC50 | 360 | nM | IC50 | Bioorg Med Chem (2014) 22: 2529-2534 [PMID:24650702] |
| ChEMBL | Inhibition of COX2 | B | 6.47 | pIC50 | 340 | nM | IC50 | J Med Chem (2012) 55: 2287-2300 [PMID:22263894] |
| ChEMBL | Inhibitory concentration against Prostaglandin G/H synthase 2 | B | 6.47 | pIC50 | 340 | nM | IC50 | J Med Chem (2001) 44: 3039-3042 [PMID:11520213] |
| ChEMBL | Inhibition of human Prostaglandin G/H synthase 2 | B | 6.47 | pIC50 | 340 | nM | IC50 | J Med Chem (2002) 45: 1511-1517 [PMID:11906292] |
| ChEMBL | In vitro inhibitory activity against recombinant human Prostaglandin G/H synthase 2 | B | 6.48 | pIC50 | 329 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1639-1643 [PMID:12729631] |
| GtoPdb | - | - | 6.5 | pIC50 | - | - | - | Proc Natl Acad Sci USA (1999) 96: 7563-8 [PMID:10377455] |
| ChEMBL | Compound was tested for the inhibition of human Prostaglandin G/H synthase 2 (COX-2) in human whole blood | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2003) 46: 5484-5504 [PMID:14640557] |
| ChEMBL | In vitro inhibition of Prostaglandin G/H synthase 2 in human whole blood | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6049-6052 [PMID:15546727] |
| ChEMBL | Inhibition of COX2 | B | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2008) 43: 2792-2799 [PMID:18262309] |
| ChEMBL | Compound was evaluated for inhibition concentration of prostaglandin G/H synthase 2 in human blood | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2004) 47: 2180-2193 [PMID:15084117] |
| ChEMBL | Inhibition of human COX2 | B | 6.53 | pIC50 | 292 | nM | IC50 | Bioorg Med Chem (2008) 16: 2183-2199 [PMID:18158247] |
| ChEMBL | In vitro percent inhibition of Prostaglandin G/H synthase 2 (COX-2) in human whole blood was determined | B | 6.55 | pIC50 | 280 | nM | IC50 | J Med Chem (2003) 46: 3463-3475 [PMID:12877584] |
| ChEMBL | In vitro inhibition of PGE-2 generation by LPS-stimulated monocytes isolated from human blood. | F | 6.55 | pIC50 | 280 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 533-537 [PMID:11844666] |
| ChEMBL | Inhibition of COX2 in human whole blood assessed as inhibition of lipopolysaccharide-stimulated PGE2 production after 24 hrs by enzyme immunoassay | B | 6.59 | pIC50 | 260 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573] |
| ChEMBL | Inhibition of human COX2 in human whole blood | B | 6.68 | pIC50 | 211 | nM | IC50 | Bioorg Med Chem (2008) 16: 2183-2199 [PMID:18158247] |
| ChEMBL | Inhibition of PGE-2 generation in LPS-stimulated human monocytes (Prostaglandin G/H synthase 2 cell assay) | F | 6.68 | pIC50 | 210 | nM | IC50 | J Med Chem (2002) 45: 1402-1411 [PMID:11906281] |
| ChEMBL | Inhibitory concentration against Prostaglandin G/H synthase 2 | B | 6.71 | pIC50 | 196 | nM | IC50 | J Med Chem (2001) 44: 3039-3042 [PMID:11520213] |
| ChEMBL | Inhibition of human recombinant COX2 expressed in Sf21 cells assessed as conversion of arachidonic acid to PGE2 preincubated for 15 mins measured after 5 mins by enzyme immunoassay | B | 6.77 | pIC50 | 170 | nM | IC50 | Bioorg Med Chem (2011) 19: 6316-6328 [PMID:21958737] |
| ChEMBL | Inhibition of human recombinant COX2 expressed in Sf21 cells using arachidonic acid as substrate preincubated for 15 mins before arachidonic acid addition measured after 5 mins | B | 6.77 | pIC50 | 170 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4307-4309 [PMID:22652053] |
| ChEMBL | Inhibition of human recombinant COX2 expressed in Sf21 cells assessed as PGE2 production using arachidonic acid as substrate preincubated for 15 mins measured after 5 mins by EIA | B | 6.81 | pIC50 | 156 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4888-4890 [PMID:21752640] |
| ChEMBL | Inhibition of human recombinant COX2 expressed in insect Sf21 cells by EIA assay | B | 6.92 | pIC50 | 120 | nM | IC50 | J Nat Prod (2007) 70: 859-862 [PMID:17378609] |
| 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 | 6.97 | pIC50 | 107 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573] |
| ChEMBL | Inhibition of human recombinant COX2 expressed in Sf21 cells assessed as effect on prostaglandin E2 production by ELISA | B | 7.13 | pIC50 | 74.5 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 459-461 [PMID:19056264] |
| ChEMBL | Inhibitory activity against Prostaglandin G/H synthase 2 in human whole blood assay as LPS induced PGE-2 generation. | B | 7.24 | pIC50 | 57 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 657-660 [PMID:12639552] |
| 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 | 7.49 | pIC50 | 32 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573] |
| ChEMBL | Inhibition of human cyclooxygenase-2 expressed in COS cells | B | 7.49 | pIC50 | 32 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5445-5448 [PMID:15454242] |
| ChEMBL | Inhibitory concentration against COX-2; (valus obtained by Kato et al.) | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2005) 48: 6997-7004 [PMID:16250658] |
| ChEMBL | In vitro inhibitory activity against human whole cells (CHO) Prostaglandin G/H synthase 2 | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1773-1778 [PMID:10406640] |
| ChEMBL | Inhibition of PGE-2 production in CHO cells expressing human COX-2. | B | 7.7 | pIC50 | 20 | 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 | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (1999) 42: 1274-1281 [PMID:10197970] |
| ChEMBL | In vitro inhibitory potency against human COX-2 in stably transfected chinese hamster ovary (CHO) cells | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3181-3186 [PMID:10576684] |
| ChEMBL | Inhibitory of human Prostaglandin G/H synthase 2 expressed in CHO cells. | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1195-1198 [PMID:12643942] |
| ChEMBL | Inhibitory concentration against COX-2 upon incubation for 15 minutes at 37 degree C | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2005) 48: 6997-7004 [PMID:16250658] |
| ChEMBL | In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (COX-2) in 143982 cells | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2003) 46: 3463-3475 [PMID:12877584] |
| ChEMBL | The compound was evaluated for prostaglandin E2 inhibition using recombinant Prostaglandin G/H synthase 2 | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 779-782 [PMID:11859001] |
| Cyclooxygenase-2 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3331] [UniProtKB: O62698] | ||||||||
| ChEMBL | In vitro inhibitory activity against prostaglandin G/H synthase 2 (COX-2) | B | 6.37 | pIC50 | 430 | nM | IC50 | J Med Chem (2003) 46: 4872-4882 [PMID:14584938] |
| Cyclooxygenase-2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4102] [UniProtKB: P79208] | ||||||||
| ChEMBL | Inhibition of sheep COX2 by spectrophotometry | B | 6.11 | pIC50 | 780 | nM | IC50 | J Med Chem (2010) 53: 6560-6571 [PMID:20804197] |
| ChEMBL | Inhibition of ovine COX-2 assessed as using arachidonic acid as substrate preincubated for 5 mins prior to substrate addition measured after 2 hrs by enzyme immunoassay | B | 6.3 | pIC50 | 500 | nM | IC50 | Eur J Med Chem (2013) 65: 323-336 [PMID:23735281] |
| ChEMBL | Inhibitory activity against ovine COX2 | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2006) 49: 1668-1683 [PMID:16509583] |
| ChEMBL | Inhibition of ovine COX2 by enzyme immunoassay | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem (2007) 15: 1056-1061 [PMID:17067801] |
| ChEMBL | Inhibition of ovine COX2 by enzyme immuno assay | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem (2007) 15: 6796-6801 [PMID:17764958] |
| ChEMBL | Inhibition of ovine COX2 by enzyme immuno assay | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem (2008) 16: 1948-1956 [PMID:18023187] |
| ChEMBL | Inhibition of ovine COX2 by enzyme immunoassay | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem (2008) 16: 3302-3308 [PMID:18096394] |
| ChEMBL | Inhibition of ovine COX2 assessed as inhibition of PGF2a formation after 20 mins by Ellman's method | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2010) 53: 3707-3717 [PMID:20387815] |
| ChEMBL | In vitro inhibitory concentration against ovine Cyclooxygenase-2 | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 439-442 [PMID:15603969] |
| ChEMBL | In vitro inhibitory concentration against ovine Cyclooxygenase-2 | B | 6.3 | pIC50 | 500 | 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 | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4911-4914 [PMID:15341950] |
| ChEMBL | Inhibition of ovine Prostaglandin G/H synthase 2 | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2004) 47: 3972-3990 [PMID:15267236] |
| ChEMBL | In vitro inhibition of ovine prostaglandin G/H synthase 2 | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2004) 47: 6108-6111 [PMID:15537365] |
| ChEMBL | In vitro inhibitory activity against ovine cyclooxygenase 2 | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4842-4845 [PMID:16143531] |
| ChEMBL | In vitro inhibitory activity against prostaglandin G/H synthase 2 from ovine | B | 6.37 | pIC50 | 430 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1953-1956 [PMID:15050635] |
| ChEMBL | In vitro inhibitory activity against prostaglandin G/H synthase 2 from ovine | B | 6.37 | pIC50 | >430 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1957-1960 [PMID:15050636] |
| ChEMBL | In vitro inhibition against ovine Prostaglandin G/H synthase 2 | B | 6.37 | pIC50 | 427.9 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2205-2209 [PMID:12798335] |
| ChEMBL | Inhibition of sheep COX2 by enzyme immunoassay | B | 6.4 | pIC50 | 398 | nM | IC50 | Bioorg Med Chem (2010) 18: 6367-6376 [PMID:20692174] |
| ChEMBL | Inhibition of ovine COX2 by enzyme immunoassay | B | 6.4 | pIC50 | 398 | nM | IC50 | Eur J Med Chem (2009) 44: 1830-1837 [PMID:19084295] |
| ChEMBL | Inhibition of ovine COX2 | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 85-89 [PMID:18061444] |
| COX-2 /Cyclooxygenase-2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4321] [GtoPdb: 1376] [UniProtKB: Q05769] | ||||||||
| ChEMBL | Inhibition of mouse COX-2 assessed as inhibition of [14C]arachidonic acid to radiolabeled prostaglandins preincubated for 15 mins by TLC-based assay | B | 7.22 | pIC50 | 60 | nM | IC50 | ACS Med Chem Lett (2014) 5: 1254-1258 [PMID:25408841] |
| ChEMBL | In vitro inhibitory activity against Prostaglandin G/H synthase 2 in murine J774 cells | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2005) 48: 3428-3432 [PMID:15857149] |
| 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 | 6.12 | pIC50 | 760 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2687-2690 [PMID:11591502] |
| Cytochrome c oxidase subunit 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6173] [UniProtKB: P00395] | ||||||||
| ChEMBL | Inhibition of COX1 (unknown origin) | B | 4.82 | pIC50 | >15000 | nM | IC50 | Eur J Med Chem (2019) 182: 111601-111601 [PMID:31445233] |
| 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 | 5.52 | pIC50 | 3000 | nM | IC50 | Eur J Med Chem (2017) 139: 936-946 [PMID:28881288] |
| ChEMBL | Inhibition of COX2 (unknown origin) | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2019) 182: 111601-111601 [PMID:31445233] |
| 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] |
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]
