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Assay Detail

CHEMBL855031

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

Binding
Displacement of [3H]CP-55940 from CB2 receptor in DBA/J2 mouse spleen
27
Total Activities
27
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

Design, synthesis, and biological evaluation of new 1,8-naphthyridin-4(1H)-on-3-carboxamide and quinolin-4(1H)-on-3-carboxamide derivatives as CB2 selective agonists.
Manera C, Benetti V, Castelli MP, Cavallini T, Lazzarotti S, Pibiri F, Saccomanni G, Tuccinardi T, Vannacci A, Martinelli A, Ferrarini PL.
J Med Chem (2006) 49 : 5947 -5957
PubMed 17004710 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.82 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL387001 1 9.00
CHEMBL216382 1 8.85
CHEMBL217094 1 8.48
CHEMBL385808 1 8.32
CHEMBL217266 1 8.29
CHEMBL217549 1 8.08
CHEMBL384595 1 8.00
CHEMBL386489 1 7.89
CHEMBL216057 1 7.87
CHEMBL218295 1 7.79
CHEMBL216888 1 7.74
CHEMBL217583 1 7.67
CHEMBL386725 1 7.61
CHEMBL216067 1 7.45
CHEMBL216438 1 7.39
CHEMBL214511 1 7.31
CHEMBL385508 1 7.30
CHEMBL371214 1 7.19
CHEMBL214229 1 7.17
CHEMBL151167 1 6.92
CHEMBL385057 1 -
CHEMBL217247 1 -
CHEMBL216690 1 -
CHEMBL216555 1 -
CHEMBL446364 1 -
CHEMBL386966 1 -
CHEMBL216196 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL387001 Ki = 1.0 nM 9.00
CHEMBL216382 Ki = 1.4 nM 8.85
CHEMBL217094 Ki = 3.3 nM 8.48
CHEMBL385808 Ki = 4.8 nM 8.32
CHEMBL217266 Ki = 5.1 nM 8.29
CHEMBL217549 Ki = 8.4 nM 8.08
CHEMBL384595 Ki = 10.0 nM 8.00
CHEMBL386489 Ki = 13.0 nM 7.89
CHEMBL216057 Ki = 13.4 nM 7.87
CHEMBL218295 Ki = 16.3 nM 7.79
CHEMBL216888 Ki = 18.1 nM 7.74
CHEMBL217583 Ki = 21.4 nM 7.67
CHEMBL386725 Ki = 24.6 nM 7.61
CHEMBL216067 Ki = 35.8 nM 7.45
CHEMBL216438 Ki = 40.5 nM 7.39
CHEMBL214511 Ki = 48.6 nM 7.31
CHEMBL385508 Ki = 50.0 nM 7.30
CHEMBL371214 Ki = 65.0 nM 7.19
CHEMBL214229 Ki = 67.2 nM 7.17
CHEMBL151167 Ki = 120.8 nM 6.92
CHEMBL385057 Ki > 1000.0 nM -
CHEMBL217247 Ki > 1000.0 nM -
CHEMBL216690 Ki > 1000.0 nM -
CHEMBL216555 Ki > 1000.0 nM -
CHEMBL446364 Ki - -
CHEMBL386966 Ki - -
CHEMBL216196 Ki - -