oxaprozin [Ligand Id: 7252] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1071 (Coxanto, Daypro, NSC-310839, Oxaprozin, Oxaprozina, Oxaprozine, 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 |
|---|---|---|---|---|---|---|---|---|
| epoxide hydrolase 2/Bifunctional epoxide hydrolase 2 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/Bifunctional epoxide hydrolase 2 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/Bifunctional 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] |
| 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] |
| Nuclear receptor related 1/Nuclear receptor subfamily 4 group A member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5002] [GtoPdb: 630] [UniProtKB: P43354] | ||||||||
| ChEMBL | Inverse agonist activity at human Nurr1 LBD transiently transfected in HEK293T cells incubated for 16 hrs by Gal4-hybrid reporter gene based Dual-glo luciferase assay | B | 4.4 | pIC50 | 40000 | nM | IC50 | J Med Chem (2023) 66: 15362-15369 [PMID:37918435] |
| ChEMBL | Inverse agonist activity at Gal4-fused human full length Nurr1 LBD transfected in HEK293T cells assessed as suppression of Nurr1 activation incubated for 12 to 14 hrs by firefly/renilla based Dual-Glo luciferase assay | B | 4.4 | pIC50 | 40000 | nM | IC50 | J Med Chem (2024) 67: 13324-13348 [PMID:39081058] |
| ChEMBL | Inverse agonist activity at Gal4-fused Nurr1 (unknown origin) | B | 4.4 | pIC50 | 40000 | nM | IC50 | J Med Chem (2022) 65: 9548-9563 [PMID:35797147] |
| ChEMBL | Inverse agonist activity at Gal4-fused wild type human Nurr1 transfected in HEK293T cells incubated for 16 hrs by firefly/renilla based Dual-Glo luciferase assay | B | 4.48 | pIC50 | 33000 | nM | IC50 | J Med Chem (2024) 67: 13324-13348 [PMID:39081058] |
| ChEMBL | Inverse agonist activity at Gal4-fused human full length Nurr1 homodimer transfected in HEK293T cells cotransfected with pFR-Luc-NurRE/pRL-SV40 (NurRE) incubated for 12 to 14 hrs by firefly/renilla based Dual-Glo luciferase assay | B | 4.77 | pIC50 | 17000 | nM | IC50 | J Med Chem (2024) 67: 13324-13348 [PMID:39081058] |
| ChEMBL | Inverse agonist activity at Gal4-fused human full length Nurr1 monomer transfected in HEK293T cells cotransfected with pFR-Luc-NBRE/pRL-SV40 (NBRE) incubated for 12 to 14 hrs by firefly/renilla based Dual-Glo luciferase assay | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2024) 67: 13324-13348 [PMID:39081058] |
| ChEMBL | Inverse agonist activity at Gal4-fused human full length Nurr1 heterodimer transfected in HEK293T cells cotransfected with pSG5-RXR/pFR-Luc-DR5/pRL-SV40 (DR5) incubated for 12 to 14 hrs by firefly/renilla based Dual-Glo luciferase assay | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2024) 67: 13324-13348 [PMID:39081058] |
| Neuron-derived orphan receptor 1/Nuclear receptor subfamily 4 group A member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1961792] [GtoPdb: 631] [UniProtKB: Q92570] | ||||||||
| ChEMBL | Inverse agonist activity at human NOR-1 LBD transiently transfected in HEK293T cells incubated for 16 hrs by Gal4-hybrid reporter gene based Dual-glo luciferase assay | B | 4.66 | pIC50 | 22000 | nM | IC50 | J Med Chem (2023) 66: 15362-15369 [PMID:37918435] |
| Nerve Growth factor IB/Nuclear receptor subfamily 4immunitygroup A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293229] [GtoPdb: 629] [UniProtKB: P22736] | ||||||||
| ChEMBL | Inverse agonist activity at human Nur77 (358 to 598 residues) transfected in HEK293T cells assessed as fold remaining activity incubated for 12 to 14 hrs by firefly/renilla based Dual-Glo luciferase assay relative to control | B | 4.66 | pIC50 | 22000 | nM | IC50 | J Med Chem (2024) 67: 13324-13348 [PMID:39081058] |
| ChEMBL | Inverse agonist activity at human Nur77 LBD transiently transfected in HEK293T cells incubated for 16 hrs by Gal4-hybrid reporter gene based Dual-glo luciferase assay | B | 4.8 | pIC50 | 16000 | nM | IC50 | J Med Chem (2023) 66: 15362-15369 [PMID:37918435] |
| ChEMBL | Inverse agonist activity at human Nur77 (358 to 598 residues) transfected in HEK293T cells incubated for 12 to 14 hrs by firefly/renilla based Dual-Glo luciferase assay | B | 4.8 | pIC50 | 16000 | nM | IC50 | J Med Chem (2024) 67: 13324-13348 [PMID:39081058] |
| 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] |
| COX-1 /Prostaglandin G/H synthase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219] | ||||||||
| ChEMBL | Inhibition of COX-1 in human platelet | B | 5.66 | pIC50 | 2200 | nM | IC50 | Eur J Med Chem (2023) 256: 115434-115434 [PMID:37148849] |
| 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 /Prostaglandin G/H synthase 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 COX-2 in IL-1-stimulated human synovial cell | B | 4.44 | pIC50 | 36000 | nM | IC50 | Eur J Med Chem (2023) 256: 115434-115434 [PMID:37148849] |
| 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] |
| Retinoid X receptor-α/Retinoic acid receptor RXR-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/Retinoic acid receptor RXR-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/Retinoic acid receptor RXR-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 (2016) |
ChEMBL data shown on this page come from version 36:
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]
