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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
