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Assay Detail

CHEMBL4138798

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

Binding
Inhibition of FAAH in rat brain microsomes assessed as reduction in enzyme-mediated 4-pyren-1-ylbutanoic acid release using N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide as substrate incubated fro 60 mins by reversed phase HPLC method
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

(Indolylalkyl)piperidine carbamates as inhibitors of fatty acid amide hydrolase (FAAH).
Dahlhaus H, Hanekamp W, Lehr M.
Medchemcomm (2017) 8 : 616 -620
PubMed 30108777 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.52 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4176744 1 7.34
CHEMBL4162665 1 7.28
CHEMBL184238 URB-597 1.0 1 7.22
CHEMBL3585525 1 7.05
CHEMBL3585524 1 7.03
CHEMBL4163613 1 6.96
CHEMBL4166118 1 6.96
CHEMBL4170471 1 6.89
CHEMBL4167061 1 6.75
CHEMBL4159300 1 6.75
CHEMBL4167359 1 6.70
CHEMBL3585526 1 6.62
CHEMBL3585519 1 6.60
CHEMBL4166514 1 6.51
CHEMBL4169537 1 6.44
CHEMBL4165979 1 6.39
CHEMBL4173379 1 6.39
CHEMBL4159152 1 6.24
CHEMBL4173907 1 6.16
CHEMBL4174430 1 6.10
CHEMBL3585523 1 6.02
CHEMBL4161620 1 6.01
CHEMBL4175232 1 5.80
CHEMBL4169941 1 5.77
CHEMBL4174293 1 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4176744 IC50 = 46.0 nM 7.34
CHEMBL4162665 IC50 = 52.0 nM 7.28
CHEMBL184238 URB-597 IC50 = 60.0 nM 7.22
CHEMBL3585525 IC50 = 90.0 nM 7.05
CHEMBL3585524 IC50 = 94.0 nM 7.03
CHEMBL4163613 IC50 = 110.0 nM 6.96
CHEMBL4166118 IC50 = 110.0 nM 6.96
CHEMBL4170471 IC50 = 130.0 nM 6.89
CHEMBL4167061 IC50 = 180.0 nM 6.75
CHEMBL4159300 IC50 = 180.0 nM 6.75
CHEMBL4167359 IC50 = 200.0 nM 6.70
CHEMBL3585526 IC50 = 240.0 nM 6.62
CHEMBL3585519 IC50 = 250.0 nM 6.60
CHEMBL4166514 IC50 = 310.0 nM 6.51
CHEMBL4169537 IC50 = 360.0 nM 6.44
CHEMBL4165979 IC50 = 410.0 nM 6.39
CHEMBL4173379 IC50 = 410.0 nM 6.39
CHEMBL4159152 IC50 = 570.0 nM 6.24
CHEMBL4173907 IC50 = 700.0 nM 6.16
CHEMBL4174430 IC50 = 790.0 nM 6.10
CHEMBL3585523 IC50 = 960.0 nM 6.02
CHEMBL4161620 IC50 = 970.0 nM 6.01
CHEMBL4175232 IC50 = 1600.0 nM 5.80
CHEMBL4169941 IC50 = 1700.0 nM 5.77
CHEMBL4174293 IC50 = 9800.0 nM 5.01