SC-58125 [Ligand Id: 11391] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL274990 (SC-58125)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL Inhibition of human Prostaglandin G/H synthase 1 at 10 ug/mL expressed as the mean percent inhibition of control PGE-2 production B 4 pIC50 >100000 nM IC50 J Med Chem (1997) 40: 980-989 [PMID:9083488]
ChEMBL In vitro inhibition of prostaglandin G/H synthase 1. B 4 pIC50 >100000 nM IC50 J Med Chem (1995) 38: 4570-4578 [PMID:7473585]
ChEMBL Tested for inhibition against Prostaglandin G/H synthase 1 B 4 pIC50 >100000 nM IC50 J Med Chem (1994) 37: 3878-3881 [PMID:7966148]
ChEMBL In vitro inhibitory concentration against recombinant human COX-1 (Cyclooxygenase-1) B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (1997) 7: 2121-2124
ChEMBL Inhibitory activity against human recombinant Prostaglandin G/H synthase 1 expressed in microsomes taken from baculovirus infected Sf9 cells B 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem Lett (1996) 6: 87-92
ChEMBL Inhibition of human COX1 expressed in african green monkey COS cells assessed as inhibition of arachidonic acid-stimulated PGE2 production by enzyme immunoassay B 4.49 pIC50 32000 nM IC50 Bioorg Med Chem Lett (2009) 19: 4509-4514 [PMID:19523822]
ChEMBL IC50 value against Prostaglandin G/H synthase 1 of human platelet rich plasma B 4.7 pIC50 >20000 nM IC50 J Med Chem (1999) 42: 1161-1169 [PMID:10197960]
ChEMBL IC50 against Prostaglandin G/H synthase 1 from human platelet rich plasma B 4.7 pIC50 >20000 nM IC50 J Med Chem (1999) 42: 1151-1160 [PMID:10197959]
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979]
ChEMBL IC50 value against ovine Prostaglandin G/H synthase 1 B 4.7 pIC50 >20000 nM IC50 J Med Chem (1999) 42: 1161-1169 [PMID:10197960]
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
ChEMBL Inhibition of COX-2 (unknown origin) B 5.96 pIC50 1100 nM IC50 Bioorg Med Chem Lett (2016) 26: 1516-1520 [PMID:26898334]
ChEMBL IC50 against recombinant human Prostaglandin G/H synthase 2 B 6.51 pIC50 310 nM IC50 J Med Chem (1999) 42: 1151-1160 [PMID:10197959]
ChEMBL Inhibition of recombinant human prostaglandin G/H synthase 2 (COX-2) B 6.51 pIC50 310 nM IC50 J Med Chem (1999) 42: 1161-1169 [PMID:10197960]
ChEMBL Inhibitory activity against human recombinant Prostaglandin G/H synthase 2 expressed in microsomes taken from baculovirus infected Sf9 cells B 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (1996) 6: 87-92
ChEMBL Inhibition of human cyclooxygenase-2 (hCOX-2) enzyme. B 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (1999) 9: 1167-1170 [PMID:10328306]
ChEMBL Inhibition of human Prostaglandin G/H synthase 2 B 7 pIC50 100 nM IC50 J Med Chem (2001) 44: 3223-3230 [PMID:11563921]
ChEMBL In vitro inhibitory concentration against human Prostaglandin G/H synthase 2 B 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (1997) 7: 2121-2124
ChEMBL In vitro inhibitory concentration required to block human recombinant prostaglandin G/H synthase 2 (COX-2) B 7 pIC50 100 nM IC50 J Med Chem (1997) 40: 1347-1365 [PMID:9135032]
ChEMBL Tested for inhibition against Prostaglandin G/H synthase 2 B 7.05 pIC50 90 nM IC50 J Med Chem (1994) 37: 3878-3881 [PMID:7966148]
ChEMBL Inhibition of human Prostaglandin G/H synthase 2 at 10 ug/mL expressed as the mean percent inhibition of control PGE-2 production B 7.05 pIC50 90 nM IC50 J Med Chem (1997) 40: 980-989 [PMID:9083488]
ChEMBL Inhibition of human COX2 expressed in african green monkey COS cells assessed as inhibition of arachidonic acid-stimulated PGE2 production by enzyme immunoassay B 7.18 pIC50 66 nM IC50 Bioorg Med Chem Lett (2009) 19: 4509-4514 [PMID:19523822]
ChEMBL In vitro inhibition of prostaglandin G/H synthase 2 (COX-2). B 7.3 pIC50 50 nM IC50 J Med Chem (1995) 38: 4570-4578 [PMID:7473585]
GtoPdb - - 7.39 pIC50 - - - J Biol Chem (1996) 271: 15810-4 [PMID:8663121]
COX-2 /Cyclooxygenase-2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4321] [GtoPdb: 1376] [UniProtKB: Q05769]
ChEMBL IC50 value was determined against Prostaglandin G/H synthase 2 of J7744A.1 cell lines. B 7.15 pIC50 70 nM IC50 J Med Chem (1999) 42: 1151-1160 [PMID:10197959]
ChEMBL IC50 value against Prostaglandin G/H synthase 2 of murine J774A.1 cell line B 7.15 pIC50 70 nM IC50 J Med Chem (1999) 42: 1161-1169 [PMID:10197960]

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]