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Assay Detail

CHEMBL3391582

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 Sf9 insect cells after 70 mins by scintillation counting
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

Design, synthesis, and structureactivity relationships of indole-3-carboxamides as novel water soluble cannabinoid CB1 receptor agonists
Adam JM, Cairns J, Caulfield W, Cowley P, Cumming I, Easson M, Edwards D, Ferguson M, Goodwin R, Jeremiah F, Kiyoi T, Mistry A, Moir E, Morphy R, Tierney J, York M, Baker J, Cottney JE, Houghton AK, Westwood PJ, Walker G
Medchemcomm (2010) 1 : 54 -60
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 9.00 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559612 CP-55940 1 9.50
CHEMBL3347370 1 9.10
CHEMBL3347369 1 8.80
CHEMBL188 WIN-552122 1 8.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559612 CP-55940 Ki = 0.3162 nM 9.50
CHEMBL3347370 Ki = 0.7943 nM 9.10
CHEMBL3347369 Ki = 1.585 nM 8.80
CHEMBL188 WIN-552122 Ki = 2.512 nM 8.60