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)
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
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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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]