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Assay Detail

CHEMBL854384

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

Binding
Displacement of [3H]CP-55940 from human CB2 receptor
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 28 7.02 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307696 1 8.14
CHEMBL188 WIN-552122 1 8.04
CHEMBL264521 1 7.87
CHEMBL559612 CP-55940 1 7.81
CHEMBL372544 1 7.80
CHEMBL201571 1 7.79
CHEMBL371214 1 7.69
CHEMBL200143 1 7.43
CHEMBL381689 SR-144528 1 7.29
CHEMBL380610 1 7.22
CHEMBL426107 1 7.15
CHEMBL370770 1 6.90
CHEMBL197598 1 6.76
CHEMBL201175 1 6.70
CHEMBL199907 1 6.43
CHEMBL201056 1 6.37
CHEMBL200179 1 6.34
CHEMBL371735 1 6.23
CHEMBL381431 1 6.18
CHEMBL200646 1 6.11
CHEMBL373169 1 6.11
CHEMBL200100 1 6.07
CHEMBL200364 1 -
CHEMBL199779 1 -
CHEMBL383363 1 -
CHEMBL199721 1 -
CHEMBL372119 1 -
CHEMBL199783 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307696 Ki = 7.3 nM 8.14
CHEMBL188 WIN-552122 Ki = 9.1 nM 8.04
CHEMBL264521 Ki = 13.4 nM 7.87
CHEMBL559612 CP-55940 Ki = 15.4 nM 7.81
CHEMBL372544 Ki = 15.8 nM 7.80
CHEMBL201571 Ki = 16.4 nM 7.79
CHEMBL371214 Ki = 20.3 nM 7.69
CHEMBL200143 Ki = 37.1 nM 7.43
CHEMBL381689 SR-144528 Ki = 51.7 nM 7.29
CHEMBL380610 Ki = 60.2 nM 7.22
CHEMBL426107 Ki = 70.8 nM 7.15
CHEMBL370770 Ki = 125.0 nM 6.90
CHEMBL197598 Ki = 174.0 nM 6.76
CHEMBL201175 Ki = 201.0 nM 6.70
CHEMBL199907 Ki = 371.0 nM 6.43
CHEMBL201056 Ki = 426.0 nM 6.37
CHEMBL200179 Ki = 455.0 nM 6.34
CHEMBL371735 Ki = 584.0 nM 6.23
CHEMBL381431 Ki = 664.0 nM 6.18
CHEMBL200646 Ki = 784.0 nM 6.11
CHEMBL373169 Ki = 772.0 nM 6.11
CHEMBL200100 Ki = 844.0 nM 6.07
CHEMBL200364 Ki > 1000.0 nM -
CHEMBL199779 Ki > 1000.0 nM -
CHEMBL383363 Ki > 5000.0 nM -
CHEMBL199721 Ki > 1000.0 nM -
CHEMBL372119 Ki > 1000.0 nM -
CHEMBL199783 Ki > 1000.0 nM -