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Assay Detail

CHEMBL1686909

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

Binding
Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in insect Sf9 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 2 (CHEMBL253)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists.
Kiyoi T, Adam JM, Clark JK, Davies K, Easson AM, Edwards D, Feilden H, Fields R, Francis S, Jeremiah F, McArthur D, Morrison AJ, Prosser A, Ratcliffe PD, Schulz J, Wishart G, Baker J, Campbell R, Cottney JE, Deehan M, Epemolu O, Evans L.
Bioorg Med Chem Lett (2011) 21 : 1748 -1753
PubMed 21316962 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.85 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559612 CP-55940 1 9.50
CHEMBL1209708 1 9.10
CHEMBL188 WIN-552122 1 8.60
CHEMBL1682272 1 8.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559612 CP-55940 Ki = 0.3162 nM 9.50
CHEMBL1209708 Ki = 0.7943 nM 9.10
CHEMBL188 WIN-552122 Ki = 2.512 nM 8.60
CHEMBL1682272 Ki = 6.31 nM 8.20