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Assay Detail

CHEMBL911052

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

Binding
Displacement of [3H]CP-55940 from CD1 mouse brain CB1 receptor
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cannabinoid receptor 1 (CHEMBL3037)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2',4'-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide.
Murineddu G, Lazzari P, Ruiu S, Sanna A, Loriga G, Manca I, Falzoi M, Dessì C, Curzu MM, Chelucci G, Pani L, Pinna GA.
J Med Chem (2006) 49 : 7502 -7512
PubMed 17149879 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.20 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559612 CP-55940 1 8.82
CHEMBL381689 SR-144528 1 7.16
CHEMBL216276 1 6.44
CHEMBL386014 1 6.08
CHEMBL216735 1 6.05
CHEMBL386644 1 6.04
CHEMBL216595 1 5.92
CHEMBL218957 1 5.69
CHEMBL374889 1 5.64
CHEMBL385268 1 5.62
CHEMBL386858 1 5.58
CHEMBL216335 1 5.35
CHEMBL385151 1 -
CHEMBL218432 1 -
CHEMBL219578 1 -
CHEMBL216333 1 -
CHEMBL219037 1 -
CHEMBL414366 1 -
CHEMBL216659 1 -
CHEMBL218571 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559612 CP-55940 Ki = 1.5 nM 8.82
CHEMBL381689 SR-144528 Ki = 70.0 nM 7.16
CHEMBL216276 Ki = 363.0 nM 6.44
CHEMBL386014 Ki = 833.0 nM 6.08
CHEMBL216735 Ki = 900.0 nM 6.05
CHEMBL386644 Ki = 916.0 nM 6.04
CHEMBL216595 Ki = 1200.0 nM 5.92
CHEMBL218957 Ki = 2050.0 nM 5.69
CHEMBL374889 Ki = 2275.0 nM 5.64
CHEMBL385268 Ki = 2409.0 nM 5.62
CHEMBL386858 Ki = 2625.0 nM 5.58
CHEMBL216335 Ki = 4500.0 nM 5.35
CHEMBL385151 Ki > 10000.0 nM -
CHEMBL218432 Ki > 5000.0 nM -
CHEMBL219578 Ki > 10000.0 nM -
CHEMBL216333 Ki > 10000.0 nM -
CHEMBL219037 Ki > 10000.0 nM -
CHEMBL414366 Ki > 5000.0 nM -
CHEMBL216659 Ki > 5000.0 nM -
CHEMBL218571 Ki > 10000.0 nM -