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Assay Detail

CHEMBL970758

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

Binding
Inhibition of human recombinant FAAH expressed in african green monkey COS7 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase.
Garfunkle J, Ezzili C, Rayl TJ, Hochstatter DG, Hwang I, Boger DL.
J Med Chem (2008) 51 : 4392 -4403
PubMed 18630870 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.06 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL469198 1 9.04
CHEMBL178398 1 8.92
CHEMBL477372 1 8.52
CHEMBL467368 1 8.26
CHEMBL177577 1 8.05
CHEMBL469051 1 7.80
CHEMBL219942 1 7.58
CHEMBL461163 1 7.43
CHEMBL468220 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL469198 Ki = 0.92 nM 9.04
CHEMBL178398 Ki = 1.2 nM 8.92
CHEMBL477372 Ki = 3.0 nM 8.52
CHEMBL467368 Ki = 5.5 nM 8.26
CHEMBL177577 Ki = 9.0 nM 8.05
CHEMBL469051 Ki = 16.0 nM 7.80
CHEMBL219942 Ki = 26.0 nM 7.58
CHEMBL461163 Ki = 37.0 nM 7.43
CHEMBL468220 Ki = 110.0 nM 6.96