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Assay Detail

CHEMBL1767553

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

Binding
Displacement of [3H]CP55940 from CB1 receptor
21
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL218)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-(4-cyanotetrahydro-2H-pyran-4-yl) and N-(1-cyanocyclohexyl) derivatives of 1,5-diarylpyrazole-3-carboxamides showing high affinity for 18 kDa translocator protein and/or cannabinoid receptors.
Donohue SR, Dannals RF, Halldin C, Pike VW.
J Med Chem (2011) 54 : 2961 -2970
PubMed 21428406 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.95 8.85
IC50 1 9.15 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL226591 1 9.15
CHEMBL111 RIMONABANT 4.0 1 8.85
CHEMBL1765684 1 7.80
CHEMBL1765820 1 7.26
CHEMBL1765683 1 7.21
CHEMBL1765682 1 6.94
CHEMBL1765679 1 6.59
CHEMBL1765672 1 6.53
CHEMBL1765819 1 6.45
CHEMBL1765677 1 6.36
CHEMBL1765681 1 6.30
CHEMBL1765685 1 6.17
CHEMBL1765673 1 -
CHEMBL1765674 1 -
CHEMBL1765096 1 -
CHEMBL1765675 1 -
CHEMBL1765676 1 -
CHEMBL1765678 1 -
CHEMBL1765680 1 -
CHEMBL1765818 1 -
CHEMBL1765821 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL226591 IC50 = 0.7 nM 9.15
CHEMBL111 RIMONABANT Ki = 1.4 nM 8.85
CHEMBL1765684 Ki = 15.7 nM 7.80
CHEMBL1765820 Ki = 55.0 nM 7.26
CHEMBL1765683 Ki = 62.2 nM 7.21
CHEMBL1765682 Ki = 115.0 nM 6.94
CHEMBL1765679 Ki = 259.0 nM 6.59
CHEMBL1765672 Ki = 297.0 nM 6.53
CHEMBL1765819 Ki = 356.0 nM 6.45
CHEMBL1765677 Ki = 437.0 nM 6.36
CHEMBL1765681 Ki = 500.0 nM 6.30
CHEMBL1765685 Ki = 680.0 nM 6.17
CHEMBL1765673 Ki > 10000.0 nM -
CHEMBL1765674 Ki > 10000.0 nM -
CHEMBL1765096 Ki > 10000.0 nM -
CHEMBL1765675 Ki > 10000.0 nM -
CHEMBL1765676 Ki > 10000.0 nM -
CHEMBL1765678 Ki > 10000.0 nM -
CHEMBL1765680 Ki > 10000.0 nM -
CHEMBL1765818 Ki > 10000.0 nM -
CHEMBL1765821 Ki > 10000.0 nM -