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ChEMBL ligand: CHEMBL560590 (PF-750) |
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519] | ||||||||
ChEMBL | Irreversible inhibition of human recombinant FAAH using N-arachidonyl-7-amino-4-methylcoumarin as substrate preincubated for 20 mins before substrate addition by fluorescence assay | B | 5.96 | pIC50 | 1090 | nM | IC50 | Bioorg Med Chem (2013) 21: 5188-5197 [PMID:23891163] |
ChEMBL | Inhibition of recombinant human N-terminal -His6 tagged FAAH (32 to 579 residues) expressed in Escherichia coli BL21-AI preincubated for 5 mins followed by olamide substrate addition measured every 10 sec intervals for 30 mins by spectrophotometry | B | 6.23 | pIC50 | 595 | nM | IC50 | J Med Chem (2017) 60: 4-46 [PMID:27766867] |
ChEMBL | Reversible inhibition of human recombinant FAAH assessed as hydrolysis of [3H]-AEA after 10 mins by liquid scintillation counting | B | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (2011) 54: 6812-6823 [PMID:21899370] |
ChEMBL | Inhibition of FAAH | B | 7.79 | pIC50 | 16.2 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4241-4244 [PMID:19515560] |
ChEMBL | Inhibition of recombinant human N-terminal -His6 tagged FAAH (32 to 579 residues) expressed in Escherichia coli BL21 preincubated for 60 mins followed by olamide substrate addition measured every 10 sec intervals for 30 mins by spectrophotometry | B | 7.79 | pIC50 | 16.2 | nM | IC50 | J Med Chem (2017) 60: 4-46 [PMID:27766867] |
ChEMBL | Inhibition of FAAH (unknown origin) | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem (2013) 21: 28-41 [PMID:23218778] |
GtoPdb | - | - | 7.8 | pIC50 | 15.8 | nM | IC50 | Biochemistry (2007) 46: 13019-30 [PMID:17949010] |
GtoPdb | Following a 5 min preincubation with inhibitor. | - | 8.19 | pIC50 | 6.4 | nM | IC50 | ACS Omega (2018) 3: 14076-14086 [PMID:30411058] |
ChEMBL | Inhibition of human FAAH expressed in HEK293 cells using arachadonyl 7-amino 4-methyl coumarin amide as substrate by fluorimetric assay | B | 8.34 | pIC50 | 4.6 | nM | IC50 | Medchemcomm (2012) 3: 611-619 |
Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612] | ||||||||
ChEMBL | Inhibition of rat FAAH expressed in HEK293 cells using arachadonyl 7-amino 4-methyl coumarin amide as substrate by fluorimetric assay | B | 7.77 | pIC50 | 17 | nM | IC50 | Medchemcomm (2012) 3: 611-619 |
epoxide hydrolase 2 in Human [GtoPdb: 2970] [UniProtKB: P34913] | ||||||||
GtoPdb | - | - | 6.19 | pIC50 | 640 | nM | IC50 | ACS Omega (2018) 3: 14076-14086 [PMID:30411058] |
GtoPdb | Following a 5 min preincubation with inhibitor. | - | 6.44 | pIC50 | 360 | nM | IC50 | ACS Omega (2018) 3: 14076-14086 [PMID:30411058] |
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]