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Assay Detail

CHEMBL3117477

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Apparent inhibition of human FAAH expressed in CHOK1 cells using AMCAA as substrate after 30 mins by fluorescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase inhibitors.
Kono M, Matsumoto T, Imaeda T, Kawamura T, Fujimoto S, Kosugi Y, Odani T, Shimizu Y, Matsui H, Shimojo M, Kori M.
Bioorg Med Chem (2014) 22 : 1468 -1478
PubMed 24440478 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.72 10.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3113272 1 10.60
CHEMBL3113271 1 10.14
CHEMBL3113274 1 10.10
CHEMBL3113273 1 9.14
CHEMBL3113270 1 8.96
CHEMBL3113269 1 8.82
CHEMBL3113268 1 8.66
CHEMBL3113264 1 7.64
CHEMBL3113266 1 7.55
CHEMBL3113265 1 7.44
CHEMBL3113267 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3113272 IC50 = 0.025 nM 10.60
CHEMBL3113271 IC50 = 0.072 nM 10.14
CHEMBL3113274 IC50 = 0.08 nM 10.10
CHEMBL3113273 IC50 = 0.72 nM 9.14
CHEMBL3113270 IC50 = 1.1 nM 8.96
CHEMBL3113269 IC50 = 1.5 nM 8.82
CHEMBL3113268 IC50 = 2.2 nM 8.66
CHEMBL3113264 IC50 = 23.0 nM 7.64
CHEMBL3113266 IC50 = 28.0 nM 7.55
CHEMBL3113265 IC50 = 36.0 nM 7.44
CHEMBL3113267 IC50 = 140.0 nM 6.85