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Assay Detail

CHEMBL657908

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

Binding
Binding affinity against human cannabinoid receptor by using radioligand ([3H]CP-55940) assay.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure activity relationships of tetrahydrocannabinol analogues on human cannabinoid receptors
Gareau Y, Dufresne C, Gallant M, Rochette C, Sawyer N, Slipetz DM, Tremblay N, Weech PK, Metters KM, Labelle M
Bioorg Med Chem Lett (1996) 6 : 189 -194
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.39 9.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL411626 1 9.08
CHEMBL57802 1 8.74
CHEMBL2218896 NABILONE 4.0 1 8.66
CHEMBL59540 1 8.65
CHEMBL56799 1 7.90
CHEMBL58501 1 7.41
CHEMBL56288 1 7.10
CHEMBL294472 1 7.01
CHEMBL57723 1 6.60
CHEMBL57840 1 6.46
CHEMBL56747 1 6.21
CHEMBL57367 1 4.80
CHEMBL61038 1 -
CHEMBL61037 1 -
CHEMBL294013 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL411626 Ki = 0.83 nM 9.08
CHEMBL57802 Ki = 1.82 nM 8.74
CHEMBL2218896 NABILONE Ki = 2.19 nM 8.66
CHEMBL59540 Ki = 2.24 nM 8.65
CHEMBL56799 Ki = 12.5 nM 7.90
CHEMBL58501 Ki = 38.8 nM 7.41
CHEMBL56288 Ki = 79.1 nM 7.10
CHEMBL294472 Ki = 97.0 nM 7.01
CHEMBL57723 Ki = 249.7 nM 6.60
CHEMBL57840 Ki = 350.3 nM 6.46
CHEMBL56747 Ki = 621.0 nM 6.21
CHEMBL57367 Ki = 15850.0 nM 4.80
CHEMBL61038 Ki > 30000.0 nM -
CHEMBL61037 Ki > 20000.0 nM -
CHEMBL294013 Ki > 20000.0 nM -