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Assay Detail

CHEMBL1287585

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

Binding
Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells after 1 hr by liquid scintillation spectrophotometry
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

1-Bromo-3-(1',1'-dimethylalkyl)-1-deoxy-Δ(8)-tetrahydrocannabinols: New selective ligands for the cannabinoid CB(2) receptor.
Huffman JW, Hepburn SA, Lyutenko N, Thompson AL, Wiley JL, Selley DE, Martin BR.
Bioorg Med Chem (2010) 18 : 7809 -7815
PubMed 20943404 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.33 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL371214 1 8.47
CHEMBL498346 1 7.75
CHEMBL1277592 1 7.55
CHEMBL1277593 1 7.47
CHEMBL465 DRONABINOL 4.0 1 7.44
CHEMBL1277499 1 7.15
CHEMBL1277498 1 6.58
CHEMBL1277409 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL371214 Ki = 3.4 nM 8.47
CHEMBL498346 Ki = 18.0 nM 7.75
CHEMBL1277592 Ki = 28.0 nM 7.55
CHEMBL1277593 Ki = 34.0 nM 7.47
CHEMBL465 DRONABINOL Ki = 36.0 nM 7.44
CHEMBL1277499 Ki = 71.0 nM 7.15
CHEMBL1277498 Ki = 265.0 nM 6.58
CHEMBL1277409 Ki = 555.0 nM 6.26