carprofen [Ligand Id: 7141] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1316 (Carprofen, Carprofene, Carprofen for veterinary use, Carprofeno, 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 |
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| 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] |
| ChEMBL | Inhibition of human COX1 | B | 8.28 | pIC50 | 5.3 | nM | IC50 | RSC Med Chem (2024) 15: 788-808 [PMID:38516587] |
| 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 | Inhibition of COX2 (unknown origin) fluorescence based analysis | B | 8.28 | pIC50 | 5.3 | nM | IC50 | RSC Med Chem (2024) 15: 788-808 [PMID:38516587] |
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]
