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Assay Detail

CHEMBL1832979

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

Binding
Displacement of [3H]-CP55940 from human CB1 receptor expressed in CHO cells by liquid scintillation counting
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity.
Blaazer AR, Lange JH, van der Neut MA, Mulder A, den Boon FS, Werkman TR, Kruse CG, Wadman WJ.
Eur J Med Chem (2011) 46 : 5086 -5098
PubMed 21885167 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.58 8.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559612 CP-55940 1 8.90
CHEMBL1828805 1 8.90
CHEMBL561013 1 8.70
CHEMBL2218896 NABILONE 4.0 1 8.40
CHEMBL1828801 1 8.20
CHEMBL1828800 1 8.10
CHEMBL1828809 1 7.90
CHEMBL1828799 1 7.50
CHEMBL1828806 1 7.20
CHEMBL188 WIN-552122 1 7.10
CHEMBL1828632 1 6.80
CHEMBL1828804 1 6.60
CHEMBL1828803 1 6.60
CHEMBL1828812 1 6.50
CHEMBL1828810 1 6.30
CHEMBL1828807 1 -
CHEMBL1828808 1 -
CHEMBL1828802 1 -
CHEMBL1828811 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559612 CP-55940 Ki = 1.259 nM 8.90
CHEMBL1828805 Ki = 1.259 nM 8.90
CHEMBL561013 Ki = 1.995 nM 8.70
CHEMBL2218896 NABILONE Ki = 3.981 nM 8.40
CHEMBL1828801 Ki = 6.31 nM 8.20
CHEMBL1828800 Ki = 7.943 nM 8.10
CHEMBL1828809 Ki = 12.59 nM 7.90
CHEMBL1828799 Ki = 31.62 nM 7.50
CHEMBL1828806 Ki = 63.1 nM 7.20
CHEMBL188 WIN-552122 Ki = 79.43 nM 7.10
CHEMBL1828632 Ki = 158.49 nM 6.80
CHEMBL1828804 Ki = 251.19 nM 6.60
CHEMBL1828803 Ki = 251.19 nM 6.60
CHEMBL1828812 Ki = 316.23 nM 6.50
CHEMBL1828810 Ki = 501.19 nM 6.30
CHEMBL1828807 Ki > 1000.0 nM -
CHEMBL1828808 Ki > 1000.0 nM -
CHEMBL1828802 Ki > 1000.0 nM -
CHEMBL1828811 Ki > 1000.0 nM -