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Assay Detail

CHEMBL911053

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

Binding
Displacement of [3H]CP-55940 from CD1 mouse spleen CB2 receptor
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cannabinoid receptor 2 (CHEMBL5373)
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 7.61 10.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL216276 1 10.43
CHEMBL381689 SR-144528 1 9.55
CHEMBL218957 1 9.47
CHEMBL559612 CP-55940 1 8.96
CHEMBL216735 1 8.12
CHEMBL386014 1 7.60
CHEMBL385268 1 7.48
CHEMBL216659 1 7.21
CHEMBL374889 1 7.20
CHEMBL414366 1 7.13
CHEMBL216595 1 7.07
CHEMBL216333 1 6.94
CHEMBL218571 1 6.75
CHEMBL386644 1 6.70
CHEMBL216335 1 5.67
CHEMBL218432 1 5.52
CHEMBL219578 1 -
CHEMBL386858 1 -
CHEMBL385151 1 -
CHEMBL219037 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL216276 Ki = 0.037 nM 10.43
CHEMBL381689 SR-144528 Ki = 0.28 nM 9.55
CHEMBL218957 Ki = 0.34 nM 9.47
CHEMBL559612 CP-55940 Ki = 1.11 nM 8.96
CHEMBL216735 Ki = 7.6 nM 8.12
CHEMBL386014 Ki = 25.0 nM 7.60
CHEMBL385268 Ki = 32.8 nM 7.48
CHEMBL216659 Ki = 61.0 nM 7.21
CHEMBL374889 Ki = 63.0 nM 7.20
CHEMBL414366 Ki = 74.0 nM 7.13
CHEMBL216595 Ki = 85.0 nM 7.07
CHEMBL216333 Ki = 114.0 nM 6.94
CHEMBL218571 Ki = 177.0 nM 6.75
CHEMBL386644 Ki = 200.0 nM 6.70
CHEMBL216335 Ki = 2116.0 nM 5.67
CHEMBL218432 Ki = 3000.0 nM 5.52
CHEMBL219578 Ki > 10000.0 nM -
CHEMBL386858 Ki > 5000.0 nM -
CHEMBL385151 Ki > 5000.0 nM -
CHEMBL219037 Ki > 5000.0 nM -