Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1069389

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

Functional
Antagonist activity at human CB2 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in presence of JWH133
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies.
Lange JH, van der Neut MA, Wals HC, Kuil GD, Borst AJ, Mulder A, den Hartog AP, Zilaout H, Goutier W, van Stuivenberg HH, van Vliet BJ.
Bioorg Med Chem Lett (2010) 20 : 1084 -1089
PubMed 20031412 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 8.31 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL382728 1 9.00
CHEMBL600683 1 9.00
CHEMBL599071 1 8.80
CHEMBL599882 1 8.30
CHEMBL381689 SR-144528 1 8.20
CHEMBL597083 1 8.10
CHEMBL178372 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL382728 Kd = 1.0 nM 9.00
CHEMBL600683 Kd = 1.0 nM 9.00
CHEMBL599071 Kd = 1.585 nM 8.80
CHEMBL599882 Kd = 5.012 nM 8.30
CHEMBL381689 SR-144528 Kd = 6.31 nM 8.20
CHEMBL597083 Kd = 7.943 nM 8.10
CHEMBL178372 Kd = 158.49 nM 6.80