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Assay Detail

CHEMBL1022320

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

Binding
Displacement of [3H]CP-55940 from human recombinant CB2 receptor
23
Total Activities
23
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of novel CB2 receptor ligands by a pharmacophore-based virtual screening workflow.
Markt P, Feldmann C, Rollinger JM, Raduner S, Schuster D, Kirchmair J, Distinto S, Spitzer GM, Wolber G, Laggner C, Altmann KH, Langer T, Gertsch J.
J Med Chem (2009) 52 : 369 -378
PubMed 19143566 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 8.07 10.64
IC50 1 9.11 9.11
EC50 1 7.30 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL371214 1 10.64
CHEMBL262865 1 9.11
CHEMBL429797 1 9.09
CHEMBL522719 1 8.87
CHEMBL525381 1 8.75
CHEMBL496781 1 8.68
CHEMBL497811 1 8.21
CHEMBL249024 1 8.10
CHEMBL400399 1 7.96
CHEMBL72374 1 7.85
CHEMBL498346 1 7.75
CHEMBL308777 1 7.66
CHEMBL524058 1 7.64
CHEMBL399948 1 7.56
CHEMBL522550 1 7.52
CHEMBL524822 1 7.40
CHEMBL225411 GW842166X 2.0 1 7.30
CHEMBL400051 1 7.05
CHEMBL495546 1 6.47
CHEMBL496578 1 -
CHEMBL523749 1 -
CHEMBL495756 1 -
CHEMBL495755 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL371214 Ki = 0.023 nM 10.64
CHEMBL262865 IC50 = 0.77 nM 9.11
CHEMBL429797 Ki = 0.82 nM 9.09
CHEMBL522719 Ki = 1.35 nM 8.87
CHEMBL525381 Ki = 1.78 nM 8.75
CHEMBL496781 Ki = 2.1 nM 8.68
CHEMBL497811 Ki = 6.1 nM 8.21
CHEMBL249024 Ki = 7.9 nM 8.10
CHEMBL400399 Ki = 11.1 nM 7.96
CHEMBL72374 Ki = 14.0 nM 7.85
CHEMBL498346 Ki = 18.0 nM 7.75
CHEMBL308777 Ki = 22.0 nM 7.66
CHEMBL524058 Ki = 23.0 nM 7.64
CHEMBL399948 Ki = 27.6 nM 7.56
CHEMBL522550 Ki = 30.0 nM 7.52
CHEMBL524822 Ki = 40.0 nM 7.40
CHEMBL225411 GW842166X EC50 = 50.0 nM 7.30
CHEMBL400051 Ki = 88.1 nM 7.05
CHEMBL495546 Ki = 342.0 nM 6.47
CHEMBL496578 Ki < 25.0 nM -
CHEMBL523749 Ki < 25.0 nM -
CHEMBL495756 Ki < 25.0 nM -
CHEMBL495755 Ki < 25.0 nM -