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Assay Detail

CHEMBL3411784

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

Functional
Antagonist activity at CB2 receptor (unknown origin) expressed in CHO cells up to 10 uM incubated for 10 mins prior to CP55940 addition by calcium mobilization assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, syntheses, structure-activity relationships and docking studies of coumarin derivatives as novel selective ligands for the CB2 receptor.
Han S, Zhang FF, Qian HY, Chen LL, Pu JB, Xie X, Chen JZ.
Eur J Med Chem (2015) 93 : 16 -32
PubMed 25644673 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.67 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3410728 1 7.72
CHEMBL3410727 1 7.70
CHEMBL3410722 1 7.66
CHEMBL3410726 1 7.55
CHEMBL3410723 1 7.21
CHEMBL3410715 1 7.05
CHEMBL3410725 1 6.79
CHEMBL3410729 1 6.19
CHEMBL3410718 1 6.13
CHEMBL3410721 1 6.09
CHEMBL3410724 1 5.93
CHEMBL3410716 1 5.66
CHEMBL558598 RIMONABANT HYDROCHLORIDE 1 5.01
CHEMBL3407533 1 -
CHEMBL3410720 1 -
CHEMBL3410719 1 -
CHEMBL3410717 1 -
CHEMBL3410714 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3410728 IC50 = 19.0 nM 7.72
CHEMBL3410727 IC50 = 20.0 nM 7.70
CHEMBL3410722 IC50 = 22.0 nM 7.66
CHEMBL3410726 IC50 = 28.0 nM 7.55
CHEMBL3410723 IC50 = 61.0 nM 7.21
CHEMBL3410715 IC50 = 90.0 nM 7.05
CHEMBL3410725 IC50 = 162.0 nM 6.79
CHEMBL3410729 IC50 = 644.0 nM 6.19
CHEMBL3410718 IC50 = 746.0 nM 6.13
CHEMBL3410721 IC50 = 807.0 nM 6.09
CHEMBL3410724 IC50 = 1177.0 nM 5.93
CHEMBL3410716 IC50 = 2190.0 nM 5.66
CHEMBL558598 RIMONABANT HYDROCHLORIDE IC50 = 9800.0 nM 5.01
CHEMBL3407533 IC50 > 10000.0 nM -
CHEMBL3410720 IC50 > 10000.0 nM -
CHEMBL3410719 IC50 > 10000.0 nM -
CHEMBL3410717 IC50 > 10000.0 nM -
CHEMBL3410714 IC50 > 10000.0 nM -