PF750 [Ligand Id: 5244] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL560590 (PF-750)
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Human [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
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  • epoxide hydrolase 2 in Human [GtoPdb: 2970] [UniProtKB: P34913]
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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 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 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]