carprofen [Ligand Id: 7141] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1316 (Carprofen, Carprofen for veterinary use, NSC-297935, Rimadyl, Ro-205720000, RO 20-5720/000) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612] | ||||||||
| ChEMBL | Inhibition of FAAH in rat brain homogenates pre-incubated for 10 mins before addition of [3H]anandamide and [3H]AEA substrates for 30 mins by liquid scintillation counting | B | 4.1 | pIC50 | 78600 | nM | IC50 | J Med Chem (2012) 55: 8807-8826 [PMID:23043222] |
| ChEMBL | Inhibition of rat brain FAAH using [3H]AEA as substrate | B | 4.49 | pIC50 | 32000 | nM | IC50 | Eur J Med Chem (2017) 136: 523-542 [PMID:28535469] |
| 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 | 6.24 | pKd | 580 | 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] | ||||||||
| ChEMBL | Inhibition of COX1 in human whole blood | B | 4.23 | pIC50 | 59000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4655-4657 [PMID:18667313] |
| ChEMBL | Inhibitory activity against cell-free canine COX-1 | B | 4.88 | pIC50 | 13200 | nM | IC50 | J Med Chem (2001) 44: 641-659 [PMID:11262075] |
| Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979] | ||||||||
| ChEMBL | Inhibition of ovine COX1 pre-incubated for 10 mins before arachidonic acid substrate addition by enzyme immunoassay | B | 4.65 | pIC50 | 22300 | nM | IC50 | J Med Chem (2012) 55: 8807-8826 [PMID:23043222] |
| ChEMBL | Inhibition of ovine COX-1 assessed as residual activity by measuring formation of 12-HHT from arachidonic acid by HPLC analysis | B | 4.88 | pIC50 | 13200 | nM | IC50 | Bioorg Med Chem (2011) 19: 5372-5382 [PMID:21873070] |
| ChEMBL | Inhibition of ovine COX1 after 5 mins | B | 4.89 | pIC50 | 13000 | nM | IC50 | J Med Chem (2010) 53: 4691-4700 [PMID:20503989] |
| COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] | ||||||||
| ChEMBL | Inhibition of COX2 in human whole blood | B | 4.42 | pIC50 | 38000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4655-4657 [PMID:18667313] |
| ChEMBL | Inhibition of human COX2 pre-incubated for 10 mins before substrate addition by enzyme immunoassay | B | 5.41 | pIC50 | 3900 | nM | IC50 | J Med Chem (2012) 55: 8807-8826 [PMID:23043222] |
| GtoPdb | Inhibition of COX-2-induced conversion of arachadonic acid to 12-HHT. | - | 6.99 | pIC50 | 102 | nM | IC50 | Bioorg Med Chem (2011) 19: 5372-82 [PMID:21873070] |
| ChEMBL | Inhibitory activity against cell-free canine COX-2 | B | 6.99 | pIC50 | 102 | nM | IC50 | J Med Chem (2001) 44: 641-659 [PMID:11262075] |
| ChEMBL | Inhibition of human recombinant COX-2 assessed as residual activity by measuring formation of 12-HHT from arachidonic acid by HPLC analysis | B | 6.99 | pIC50 | 102 | nM | IC50 | Bioorg Med Chem (2011) 19: 5372-5382 [PMID:21873070] |
| ChEMBL | Inhibition of human recombinant COX2 after 5 mins | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2010) 53: 4691-4700 [PMID:20503989] |
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]
