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Assay Detail

CHEMBL930039

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Binding
Inhibition of human recombinant FAAH after 15 mins
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fatty-acid amide hydrolase 1 (CHEMBL2243)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Influence of sulfur oxidation state and steric bulk upon trifluoromethyl ketone (TFK) binding kinetics to carboxylesterases and fatty acid amide hydrolase (FAAH).
Wheelock CE, Nishi K, Ying A, Jones PD, Colvin ME, Olmstead MM, Hammock BD.
Bioorg Med Chem (2008) 16 : 2114 -2130
PubMed 18023188 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.94 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL270375 1 7.05
CHEMBL270374 1 6.77
CHEMBL257071 1 6.55
CHEMBL89506 1 6.52
CHEMBL273138 1 6.22
CHEMBL269931 1 5.87
CHEMBL86668 1 5.75
CHEMBL440542 1 5.60
CHEMBL272075 1 5.52
CHEMBL270373 1 4.86
CHEMBL273139 1 4.65
CHEMBL402615 1 -
CHEMBL155621 1 -
CHEMBL155396 1 -
CHEMBL403288 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL270375 IC50 = 89.0 nM 7.05
CHEMBL270374 IC50 = 170.0 nM 6.77
CHEMBL257071 IC50 = 280.0 nM 6.55
CHEMBL89506 IC50 = 300.0 nM 6.52
CHEMBL273138 IC50 = 600.0 nM 6.22
CHEMBL269931 IC50 = 1350.0 nM 5.87
CHEMBL86668 IC50 = 1800.0 nM 5.75
CHEMBL440542 IC50 = 2500.0 nM 5.60
CHEMBL272075 IC50 = 3000.0 nM 5.52
CHEMBL270373 IC50 = 13900.0 nM 4.86
CHEMBL273139 IC50 = 22500.0 nM 4.65
CHEMBL402615 IC50 > 40000.0 nM -
CHEMBL155621 IC50 > 40000.0 nM -
CHEMBL155396 IC50 > 40000.0 nM -
CHEMBL403288 IC50 > 40000.0 nM -