oxaprozin [Ligand Id: 7252] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1071 (Daypro, NSC-310839, Oxaprozin, WY-21,743, WY-21743) |
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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 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]
