oxaprozin [Ligand Id: 7252] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1071 (Daypro, NSC-310839, Oxaprozin, WY-21743, WY-21,743)
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  • epoxide hydrolase 2/Epoxide hydratase in Human [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
  • epoxide hydrolase 2/Epoxide hydratase in Mouse [ChEMBL: CHEMBL4140] [GtoPdb: 2970] [UniProtKB: P34914]
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  • epoxide hydrolase 2 in Human [GtoPdb: 2970] [UniProtKB: P34913]
  • epoxide hydrolase 2/Epoxide hydrolase 2 in Rat [ChEMBL: CHEMBL5669] [GtoPdb: 2970] [UniProtKB: P80299]
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  • Retinoid X receptor-α/Retinoid X receptor alpha in Human [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
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  • Retinoid X receptor-β/Retinoid X receptor beta in Human [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702]
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  • Retinoid X receptor-γ/Retinoid X receptor gamma in Human [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443]
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  • Serine hydroxymethyltransferase, mitochondrial in Human [ChEMBL: CHEMBL4295747] [UniProtKB: P34897]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Complement C5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2364163] [UniProtKB: P01031]
ChEMBL Binding affinity to human C5a assessed as dissociation constant after 1 hr by circular dichroism analysis B 6.19 pKd 640 nM Kd Bioorg Med Chem (2019) 27: 115052-115052 [PMID:31447248]
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
GtoPdb - - 5.66 pIC50 2200 nM IC50 Eur J Pharmacol (1998) 347: 87-94 [PMID:9650852]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) B 6.07 pIC50 856 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of COX1 in A23187-stimulated human platelets assessed as reduction in TXA2 production B 6.13 pIC50 740 nM IC50 J Med Chem (2019) 62: 8443-8460 [PMID:31436984]
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
GtoPdb - - 4.44 pIC50 36000 nM IC50 Eur J Pharmacol (1998) 347: 87-94 [PMID:9650852]
ChEMBL Inhibition of COX2 in LPS-stimulated human monocytes assessed as reduction in PGE2 production by LC-tandem MIS analysis B 6.96 pIC50 110 nM IC50 J Med Chem (2019) 62: 8443-8460 [PMID:31436984]
epoxide hydrolase 2/Epoxide hydratase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
ChEMBL Inhibition of phosphatase activity of full length human soluble epoxide hydrolase pre-incubated for 30 mins before FDP substrate addition by fluorescence based assay B 4.15 pIC50 70000 nM IC50 J Med Chem (2019) 62: 8443-8460 [PMID:31436984]
GtoPdb Inhibition of sEH's phosphatase activity in vitro using bacterially-expressed recombinant N-terminal domain of sEH. - 5.3 pIC50 5000 nM IC50 J Biomol Screen (2016) 21: 689-94 [PMID:27009944]
epoxide hydrolase 2/Epoxide hydratase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4140] [GtoPdb: 2970] [UniProtKB: P34914]
ChEMBL Inhibition of phosphatase activity of full length mouse soluble epoxide hydrolase pre-incubated for 30 mins before FDP substrate addition by fluorescence based assay B 4.45 pIC50 35500 nM IC50 J Med Chem (2019) 62: 8443-8460 [PMID:31436984]
epoxide hydrolase 2 in Human [GtoPdb: 2970] [UniProtKB: P34913]
GtoPdb Inhibition of sEH's phosphatase activity in vitro using bacterially-expressed recombinant N-terminal domain of sEH. - 5.3 pIC50 5000 nM IC50 J Biomol Screen (2016) 21: 689-94 [PMID:27009944]
epoxide hydrolase 2/Epoxide hydrolase 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5669] [GtoPdb: 2970] [UniProtKB: P80299]
ChEMBL Inhibition of phosphatase activity of full length rat soluble epoxide hydrolase pre-incubated for 30 mins before FDP substrate addition by fluorescence based assay B 4.2 pIC50 62500 nM IC50 J Med Chem (2019) 62: 8443-8460 [PMID:31436984]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 4.8 pIC50 15848.93 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 4.8 pIC50 15848.93 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 4.9 pIC50 12589.25 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 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
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 3D7 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
ChEMBL Agonist activity at human RXRalpha transfected in human HEK293T cells co-expressing pFR/pRL-Luc incubated for 14 to 16 hrs by hybrid reporter gene assay B 4.79 pEC50 16100 nM EC50 J Med Chem (2021) 64: 5123-5136 [PMID:33793232]
Retinoid X receptor-β/Retinoid X receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702]
ChEMBL Agonist activity at human RXRbeta transfected in human HEK293T cells co-expressing pFR/pRL-Luc incubated for 14 to 16 hrs by hybrid reporter gene assay B 4.6 pEC50 25000 nM EC50 J Med Chem (2021) 64: 5123-5136 [PMID:33793232]
Retinoid X receptor-γ/Retinoid X receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443]
ChEMBL Agonist activity at human RXRgamma transfected in human HEK293T cells co-expressing pFR/pRL-Luc incubated for 14 to 16 hrs by hybrid reporter gene assay B 4.4 pEC50 40100 nM EC50 J Med Chem (2021) 64: 5123-5136 [PMID:33793232]
Serine hydroxymethyltransferase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295747] [UniProtKB: P34897]
ChEMBL Inhibition of His-tagged human recombinant SHMT2 expressed in Escherichia coli BLR(DE3) assessed as reduction in NADPH level using L-serine, THF and NADP+ incubated for 5 mins by SHMT2-MTHFD coupled reaction based fluorescence assay B 5.71 pIC50 1949.84 nM IC50 WO-2016085990-A1. Compositions and methods relating to inhibiting serine hyrdoxymethyltransferase 2 activity (null)

ChEMBL data shown on this page come from version 32:

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]