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Assay Detail

CHEMBL959188

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

Binding
Displacement of [3H]CP-55940 from human recombinant cannabinoid CB2 receptor expressed in HEK293 cells
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and pharmacological evaluation of coumarin derivatives as cannabinoid receptor antagonists and inverse agonists.
Behrenswerth A, Volz N, Toräng J, Hinz S, Bräse S, Müller CE.
Bioorg Med Chem (2009) 17 : 2842 -2851
PubMed 19278853 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 39 5.90 9.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559612 CP-55940 1 9.36
CHEMBL188 WIN-552122 1 8.92
CHEMBL471248 1 5.99
CHEMBL470602 1 5.81
CHEMBL469340 1 5.69
CHEMBL470618 1 5.67
CHEMBL470016 1 5.56
CHEMBL511304 1 5.47
CHEMBL505327 1 5.46
CHEMBL470017 1 5.44
CHEMBL476833 1 5.38
CHEMBL470224 1 5.37
CHEMBL470619 1 5.32
CHEMBL470212 1 5.28
CHEMBL470018 1 5.25
CHEMBL471249 1 5.24
CHEMBL513034 1 5.03
CHEMBL508042 1 -
CHEMBL447225 1 -
CHEMBL471247 1 -
CHEMBL511303 1 -
CHEMBL443168 1 -
CHEMBL469519 1 -
CHEMBL472068 1 -
CHEMBL513763 1 -
CHEMBL472493 1 -
CHEMBL453459 1 -
CHEMBL470820 1 -
CHEMBL455557 1 -
CHEMBL472634 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559612 CP-55940 Ki = 0.439 nM 9.36
CHEMBL188 WIN-552122 Ki = 1.2 nM 8.92
CHEMBL471248 Ki = 1030.0 nM 5.99
CHEMBL470602 Ki = 1540.0 nM 5.81
CHEMBL469340 Ki = 2060.0 nM 5.69
CHEMBL470618 Ki = 2160.0 nM 5.67
CHEMBL470016 Ki = 2780.0 nM 5.56
CHEMBL511304 Ki = 3370.0 nM 5.47
CHEMBL505327 Ki = 3490.0 nM 5.46
CHEMBL470017 Ki = 3650.0 nM 5.44
CHEMBL476833 Ki = 4200.0 nM 5.38
CHEMBL470224 Ki = 4270.0 nM 5.37
CHEMBL470619 Ki = 4760.0 nM 5.32
CHEMBL470212 Ki = 5240.0 nM 5.28
CHEMBL470018 Ki = 5670.0 nM 5.25
CHEMBL471249 Ki = 5810.0 nM 5.24
CHEMBL513034 Ki = 9390.0 nM 5.03
CHEMBL470019 Ki > 10000.0 nM -
CHEMBL506746 Ki > 10000.0 nM -
CHEMBL472067 Ki > 10000.0 nM -
CHEMBL512509 Ki > 10000.0 nM -
CHEMBL470199 Ki >= 10000.0 nM -
CHEMBL470198 Ki > 10000.0 nM -
CHEMBL470197 Ki >= 10000.0 nM -
CHEMBL516339 Ki > 10000.0 nM -
CHEMBL472635 Ki > 10000.0 nM -
CHEMBL472634 Ki >= 10000.0 nM -
CHEMBL455557 Ki > 10000.0 nM -
CHEMBL470820 Ki > 10000.0 nM -
CHEMBL453459 Ki > 10000.0 nM -
CHEMBL472493 Ki > 10000.0 nM -
CHEMBL513763 Ki >= 10000.0 nM -
CHEMBL472068 Ki > 10000.0 nM -
CHEMBL469519 Ki >= 10000.0 nM -
CHEMBL443168 Ki >= 10000.0 nM -
CHEMBL511303 Ki > 10000.0 nM -
CHEMBL471247 Ki > 10000.0 nM -
CHEMBL447225 Ki >= 10000.0 nM -
CHEMBL508042 Ki >= 10000.0 nM -