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Assay Detail

CHEMBL3227900

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

Binding
Inhibition of human FAAH expressed in HEK293-TRex cells using arachadonyl 7-amino 4-methyl coumarin amide as substrate by fluorescence assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293-TRex
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of potent, non-carbonyl inhibitors of fatty acid amide hydrolase (FAAH)
Gowlugari S, DeFalco J, Nguyen MT, Kaub C, Chi C, Duncton MAJ, Emerling DE, Kelly MG, Kincaid J, Vincent F
Medchemcomm (2012) 3 : 1258 -1263
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.32 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3220531 1 8.59
CHEMBL184238 URB-597 1.0 1 8.52
CHEMBL3220532 1 7.89
CHEMBL3220529 1 7.68
CHEMBL3220530 1 7.55
CHEMBL3220527 1 7.35
CHEMBL3220528 1 7.35
CHEMBL3220519 1 7.12
CHEMBL3220526 1 7.03
CHEMBL3220525 1 6.72
CHEMBL3220520 1 6.32
CHEMBL3220522 1 5.67
CHEMBL3220521 1 -
CHEMBL3220523 1 -
CHEMBL3220524 1 -
CHEMBL3220533 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3220531 IC50 = 2.6 nM 8.59
CHEMBL184238 URB-597 IC50 = 3.0 nM 8.52
CHEMBL3220532 IC50 = 13.0 nM 7.89
CHEMBL3220529 IC50 = 21.0 nM 7.68
CHEMBL3220530 IC50 = 28.0 nM 7.55
CHEMBL3220527 IC50 = 45.0 nM 7.35
CHEMBL3220528 IC50 = 45.0 nM 7.35
CHEMBL3220519 IC50 = 76.0 nM 7.12
CHEMBL3220526 IC50 = 93.0 nM 7.03
CHEMBL3220525 IC50 = 190.0 nM 6.72
CHEMBL3220520 IC50 = 479.0 nM 6.32
CHEMBL3220522 IC50 = 2124.0 nM 5.67
CHEMBL3220521 IC50 > 10000.0 nM -
CHEMBL3220523 IC50 > 10000.0 nM -
CHEMBL3220524 IC50 > 10000.0 nM -
CHEMBL3220533 IC50 > 10000.0 nM -