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

CHEMBL3383063

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

Functional
Agonist activity at human recombinant CB2R expressed in WIN-55212-stimulated U2OS cells assessed as reduction in forskolin-mediated cAMP level after 30 mins by time-resolved fluorescence assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

CB2-selective cannabinoid receptor ligands: synthesis, pharmacological evaluation, and molecular modeling investigation of 1,8-Naphthyridin-2(1H)-one-3-carboxamides.
Lucchesi V, Hurst DP, Shore DM, Bertini S, Ehrmann BM, Allarà M, Lawrence L, Ligresti A, Minutolo F, Saccomanni G, Sharir H, Macchia M, Di Marzo V, Abood ME, Reggio PH, Manera C.
J Med Chem (2014) 57 : 8777 -8791
PubMed 25272206 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.59 7.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3353436 1 7.69
CHEMBL466223 1 7.55
CHEMBL466651 1 7.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3353436 EC50 = 20.6 nM 7.69
CHEMBL466223 EC50 = 28.0 nM 7.55
CHEMBL466651 EC50 = 29.6 nM 7.53