rofecoxib [Ligand Id: 2893] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL122 (M01AH02, MK0966, Rofecoxib, Vioxx, MK-0966, MK-966)
  • 5-LOX/Arachidonate 5-lipoxygenase in Human [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
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  • Cytochrome c oxidase subunit 2 in Human [ChEMBL: CHEMBL6174] [UniProtKB: P00403]
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  • epoxide hydrolase 2/Epoxide hydratase in Human [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
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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 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 B 6.12 pIC50 760 nM IC50 J. Nat. Prod. (2005) 68: 985-991 [PMID:16038536]
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 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 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 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 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 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 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 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 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. U.S.A. (1999) 96: 7563-8 [PMID:10377455]
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 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 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 cyclooxygenase-2 expressed in COS cells B 7.49 pIC50 32 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 7.49 pIC50 32 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 4504-4508 [PMID:19520573]
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 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 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 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 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 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 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