oxaprozin [Ligand Id: 7252] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL1071 (Daypro, NSC-310839, Oxaprozin, WY-21,743, WY-21743) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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] |
| 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 Gal4-fused Nurr1 (unknown origin) | B | 4.4 | pIC50 | 40000 | nM | IC50 | J Med Chem (2022) 65: 9548-9563 [PMID:35797147] |
| 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 (2016) |
ChEMBL data shown on this page come from version 34:
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]
