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Assay Detail

CHEMBL895094

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

Binding
Displacement of [3H]CP-55940 human CB2 receptor expressed in CHOK1 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration.
Dziadulewicz EK, Bevan SJ, Brain CT, Coote PR, Culshaw AJ, Davis AJ, Edwards LJ, Fisher AJ, Fox AJ, Gentry C, Groarke A, Hart TW, Huber W, James IF, Kesingland A, La Vecchia L, Loong Y, Lyothier I, McNair K, O'Farrell C, Peacock M, Portmann R, Schopfer U, Yaqoob M, Zadrobilek J.
J Med Chem (2007) 50 : 3851 -3856
PubMed 17630726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.87 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559612 CP-55940 1 8.89
CHEMBL188 WIN-552122 1 8.05
CHEMBL244402 1 7.07
CHEMBL243334 1 7.05
CHEMBL244403 1 7.01
CHEMBL390675 1 6.92
CHEMBL244606 1 6.18
CHEMBL244607 1 5.70
CHEMBL244189 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559612 CP-55940 IC50 = 1.3 nM 8.89
CHEMBL188 WIN-552122 IC50 = 8.9 nM 8.05
CHEMBL244402 IC50 = 85.0 nM 7.07
CHEMBL243334 IC50 = 90.0 nM 7.05
CHEMBL244403 IC50 = 98.0 nM 7.01
CHEMBL390675 IC50 = 120.0 nM 6.92
CHEMBL244606 IC50 = 660.0 nM 6.18
CHEMBL244607 IC50 = 2000.0 nM 5.70
CHEMBL244189 IC50 = 11000.0 nM 4.96