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Assay Detail

CHEMBL862781

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

Functional
Effect on [35S]GTP-gamma-S binding to human CB2 receptor
18
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cannabinoid receptor 2 (CHEMBL253)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling.
Stern E, Muccioli GG, Millet R, Goossens JF, Farce A, Chavatte P, Poupaert JH, Lambert DM, Depreux P, Hénichart JP.
J Med Chem (2006) 49 : 70 -79
PubMed 16392793 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.75 8.68
Emax 9 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL381689 SR-144528 2 8.68
CHEMBL307696 2 8.39
CHEMBL559612 CP-55940 2 8.21
CHEMBL372544 2 7.85
CHEMBL200143 2 7.78
CHEMBL264521 2 7.61
CHEMBL188 WIN-552122 2 7.61
CHEMBL371214 2 6.84
CHEMBL380610 2 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL381689 SR-144528 EC50 = 2.1 nM 8.68
CHEMBL307696 EC50 = 4.1 nM 8.39
CHEMBL559612 CP-55940 EC50 = 6.1 nM 8.21
CHEMBL372544 EC50 = 14.1 nM 7.85
CHEMBL200143 EC50 = 16.8 nM 7.78
CHEMBL188 WIN-552122 EC50 = 24.6 nM 7.61
CHEMBL264521 EC50 = 24.8 nM 7.61
CHEMBL371214 EC50 = 145.6 nM 6.84
CHEMBL380610 EC50 = 157.4 nM 6.80
CHEMBL264521 Emax = 126.0 % -
CHEMBL307696 Emax = 135.1 % -
CHEMBL371214 Emax = 149.0 % -
CHEMBL559612 CP-55940 Emax = 145.6 % -
CHEMBL381689 SR-144528 Emax = 21.6 % -
CHEMBL380610 Emax = 123.5 % -
CHEMBL200143 Emax = 128.7 % -
CHEMBL372544 Emax = 124.1 % -
CHEMBL188 WIN-552122 Emax = 126.2 % -