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Assay Detail

CHEMBL4409077

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

Binding
Inhibition of FAAH in mouse brain membranes using [14C]-AEA as substrate incubated for 15 mins by scintillation counting method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Brain
Subcellular Membranes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fatty-acid amide hydrolase 1 (CHEMBL3455)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Development of novel multipotent compounds modulating endocannabinoid and dopaminergic systems.
Grillo A, Chemi G, Brogi S, Brindisi M, Relitti N, Fezza F, Fazio D, Castelletti L, Perdona E, Wong A, Lamponi S, Pecorelli A, Benedusi M, Fantacci M, Valoti M, Valacchi G, Micheli F, Novellino E, Campiani G, Butini S, Maccarrone M, Gemma S.
Eur J Med Chem (2019) 183 : 111674 -111674
PubMed 31518969 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.96 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4471658 1 9.05
CHEMBL4565200 1 7.58
CHEMBL4473519 1 7.24
CHEMBL4540218 1 7.21
CHEMBL4554053 1 7.03
CHEMBL184238 URB-597 1.0 1 6.96
CHEMBL4520982 1 6.76
CHEMBL4449756 1 6.71
CHEMBL4520184 1 6.12
CHEMBL4517296 1 6.10
CHEMBL4446507 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4471658 IC50 = 0.89 nM 9.05
CHEMBL4565200 IC50 = 26.0 nM 7.58
CHEMBL4473519 IC50 = 58.0 nM 7.24
CHEMBL4540218 IC50 = 62.0 nM 7.21
CHEMBL4554053 IC50 = 94.0 nM 7.03
CHEMBL184238 URB-597 IC50 = 110.0 nM 6.96
CHEMBL4520982 IC50 = 175.0 nM 6.76
CHEMBL4449756 IC50 = 195.0 nM 6.71
CHEMBL4520184 IC50 = 757.0 nM 6.12
CHEMBL4517296 IC50 = 791.0 nM 6.10
CHEMBL4446507 IC50 = 1600.0 nM 5.80