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Assay Detail

CHEMBL841778

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

Binding
Inhibition of [3H]SR-141,716A binding to human CB1 receptor expressed in CHO cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cannabinoid receptor 1 (CHEMBL218)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted 5,5'-diphenyl-2-thioxoimidazolidin-4-one as CB1 cannabinoid receptor ligands: synthesis and pharmacological evaluation.
Muccioli GG, Martin D, Scriba GK, Poppitz W, Poupaert JH, Wouters J, Lambert DM.
J Med Chem (2005) 48 : 2509 -2517
PubMed 15801840 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 5.97 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL111 RIMONABANT 4.0 1 8.27
CHEMBL334533 DEXANABINOL 3.0 1 7.73
CHEMBL190316 1 6.23
CHEMBL195445 1 6.14
CHEMBL192991 1 6.06
CHEMBL192436 1 6.00
CHEMBL364312 1 5.85
CHEMBL365241 1 5.76
CHEMBL192958 1 5.75
CHEMBL426455 1 5.74
CHEMBL195396 1 5.68
CHEMBL189056 1 5.66
CHEMBL190043 1 5.66
CHEMBL189160 1 5.46
CHEMBL371614 1 5.44
CHEMBL434941 1 5.42
CHEMBL188 WIN-552122 1 5.42
CHEMBL190411 1 5.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL111 RIMONABANT Ki = 5.4 nM 8.27
CHEMBL334533 DEXANABINOL Ki = 18.6 nM 7.73
CHEMBL190316 Ki = 589.0 nM 6.23
CHEMBL195445 Ki = 724.0 nM 6.14
CHEMBL192991 Ki = 871.0 nM 6.06
CHEMBL192436 Ki = 993.0 nM 6.00
CHEMBL364312 Ki = 1412.0 nM 5.85
CHEMBL365241 Ki = 1738.0 nM 5.76
CHEMBL192958 Ki = 1778.0 nM 5.75
CHEMBL426455 Ki = 1820.0 nM 5.74
CHEMBL195396 Ki = 2089.0 nM 5.68
CHEMBL189056 Ki = 2193.0 nM 5.66
CHEMBL190043 Ki = 2188.0 nM 5.66
CHEMBL189160 Ki = 3467.0 nM 5.46
CHEMBL371614 Ki = 3630.0 nM 5.44
CHEMBL434941 Ki = 3801.0 nM 5.42
CHEMBL188 WIN-552122 Ki = 3802.0 nM 5.42
CHEMBL190411 Ki = 5495.0 nM 5.26