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Assay Detail

CHEMBL2383352

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

Functional
Agonist activity at CB1 receptor in mouse Neuro2a cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 15 mins by liquid scintillation spectrophotometry
8
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type Neuro2a
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL3037)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design, synthesis, and biological evaluation of aminoalkylindole derivatives as cannabinoid receptor ligands with potential for treatment of alcohol abuse.
Vasiljevik T, Franks LN, Ford BM, Douglas JT, Prather PL, Fantegrossi WE, Prisinzano TE.
J Med Chem (2013) 56 : 4537 -4550
PubMed 23631463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.66 8.77
IC50 2 7.00 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2380420 2 8.77
CHEMBL2380416 1 7.89
CHEMBL2380428 1 7.81
CHEMBL2380417 2 7.62
CHEMBL2380408 1 7.43
CHEMBL2380418 1 6.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2380420 Ki = 1.7 nM 8.77
CHEMBL2380416 Ki = 12.9 nM 7.89
CHEMBL2380428 Ki = 15.4 nM 7.81
CHEMBL2380417 Ki = 24.2 nM 7.62
CHEMBL2380408 Ki = 37.3 nM 7.43
CHEMBL2380420 IC50 = 45.0 nM 7.35
CHEMBL2380417 IC50 = 225.0 nM 6.65
CHEMBL2380418 Ki = 387.0 nM 6.41