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Assay Detail

CHEMBL871152

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

Binding
Displacement of [3H]SR141716A from CB1 receptor in rat cerebellum
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebellum
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cannabinoid receptor 1 (CHEMBL3571)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and activity of 1,3,5-triphenylimidazolidine-2,4-diones and 1,3,5-triphenyl-2-thioxoimidazolidin-4-ones: characterization of new CB1 cannabinoid receptor inverse agonists/antagonists.
Muccioli GG, Wouters J, Charlier C, Scriba GK, Pizza T, Di Pace P, De Martino P, Poppitz W, Poupaert JH, Lambert DM.
J Med Chem (2006) 49 : 872 -882
PubMed 16451053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.99 8.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL558598 RIMONABANT HYDROCHLORIDE 1 8.91
CHEMBL307696 1 8.56
CHEMBL380415 1 6.61
CHEMBL383287 1 6.51
CHEMBL201383 1 5.76
CHEMBL381560 1 5.58
CHEMBL383228 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL558598 RIMONABANT HYDROCHLORIDE Ki = 1.23 nM 8.91
CHEMBL307696 Ki = 2.75 nM 8.56
CHEMBL380415 Ki = 247.0 nM 6.61
CHEMBL383287 Ki = 311.0 nM 6.51
CHEMBL201383 Ki = 1744.0 nM 5.76
CHEMBL381560 Ki = 2618.0 nM 5.58
CHEMBL383228 Ki - -