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Assay Detail

CHEMBL4157966

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

Binding
Displacement of [3H]CP55940 from membrane bound human CB2 receptor after 1 hr by beta scintillation counting method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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 of oxidative metabolites of CRA13 and their analogs: Identification of CRA13 active metabolites and analogs thereof with selective CB2R affinity.
Hassan AHE, Cho MC, Kim HI, Yang JS, Park KT, Hwang JY, Jang CG, Park KD, Lee YS.
Bioorg Med Chem (2018) 26 : 5069 -5078
PubMed 30217464 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.20 5.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4166345 1 5.97
CHEMBL4169849 1 5.77
CHEMBL4161845 1 5.30
CHEMBL244403 1 5.28
CHEMBL4161451 1 4.90
CHEMBL4167940 1 4.83
CHEMBL4159535 1 4.32
CHEMBL4176969 1 -
CHEMBL4176556 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4166345 IC50 = 1080.0 nM 5.97
CHEMBL4169849 IC50 = 1690.0 nM 5.77
CHEMBL4161845 IC50 = 5050.0 nM 5.30
CHEMBL244403 IC50 = 5300.0 nM 5.28
CHEMBL4161451 IC50 = 12620.0 nM 4.90
CHEMBL4167940 IC50 = 14670.0 nM 4.83
CHEMBL4159535 IC50 = 47710.0 nM 4.32
CHEMBL4176969 IC50 > 10000.0 nM -
CHEMBL4176556 IC50 > 100000.0 nM -