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Assay Detail

CHEMBL2176391

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

Binding
Inhibition of rat histidine tagged FAAH expressed in Escherichia coli by coumarin ester substrate fluorescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fatty-acid amide hydrolase 1 (CHEMBL3229)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Assay and inhibition of diacylglycerol lipase activity.
Johnston M, Bhatt SR, Sikka S, Mercier RW, West JM, Makriyannis A, Gatley SJ, Duclos RI.
Bioorg Med Chem Lett (2012) 22 : 4585 -4592
PubMed 22738638 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.04 8.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL184238 URB-597 1.0 1 8.31
CHEMBL94809 HEXADECANESULFONYL FLUORIDE 1 8.20
CHEMBL175247 ORLISTAT 4.0 1 8.00
CHEMBL190503 PHENYLMETHYLSULFONYLFLUORIDE 1 6.08
CHEMBL576786 1 6.01
CHEMBL158897 1 5.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL184238 URB-597 IC50 = 4.9 nM 8.31
CHEMBL94809 HEXADECANESULFONYL FLUORIDE IC50 = 6.3 nM 8.20
CHEMBL175247 ORLISTAT IC50 = 10.0 nM 8.00
CHEMBL190503 PHENYLMETHYLSULFONYLFLUORIDE IC50 = 833.0 nM 6.08
CHEMBL576786 IC50 = 974.0 nM 6.01
CHEMBL158897 IC50 = 2240.0 nM 5.65