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Assay Detail

CHEMBL4367879

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

Binding
Displacement of [3H]CP55940 from recombinant human CB2R expressed in HEK293 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structure-activity relationships of thiazole and benzothiazole derivatives as selective cannabinoid CB2 agonists with in vivo anti-inflammatory properties.
Ghonim AE, Ligresti A, Rabbito A, Mahmoud AM, Di Marzo V, Osman NA, Abadi AH.
Eur J Med Chem (2019) 180 : 154 -170
PubMed 31302448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 7.17 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4559193 1 8.70
CHEMBL4437741 1 7.92
CHEMBL381791 1 6.93
CHEMBL4592199 1 6.34
CHEMBL4450995 1 5.97
CHEMBL4451793 1 -
CHEMBL4450238 1 -
CHEMBL4456654 1 -
CHEMBL4461356 1 -
CHEMBL4459664 1 -
CHEMBL4587737 1 -
CHEMBL4443713 1 -
CHEMBL4450401 1 -
CHEMBL4446746 1 -
CHEMBL4445661 1 -
CHEMBL4451217 1 -
CHEMBL4533663 1 -
CHEMBL4579868 1 -
CHEMBL4576974 1 -
CHEMBL4544293 1 -
CHEMBL4519212 1 -
CHEMBL4462864 1 -
CHEMBL4483617 1 -
CHEMBL4556046 1 -
CHEMBL4550200 1 -
CHEMBL4556423 1 -
CHEMBL3596703 1 -
CHEMBL1385951 1 -
CHEMBL4470152 1 -
CHEMBL4441442 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4559193 Ki = 2.0 nM 8.70
CHEMBL4437741 Ki = 12.0 nM 7.92
CHEMBL381791 Ki = 117.0 nM 6.93
CHEMBL4592199 Ki = 460.0 nM 6.34
CHEMBL4450995 Ki = 1060.0 nM 5.97
CHEMBL4456654 Ki > 10000.0 nM -
CHEMBL4473769 Ki > 10000.0 nM -
CHEMBL4461356 Ki > 10000.0 nM -
CHEMBL4459664 Ki > 10000.0 nM -
CHEMBL4587737 Ki > 10000.0 nM -
CHEMBL4443713 Ki > 10000.0 nM -
CHEMBL4450401 Ki > 10000.0 nM -
CHEMBL4446746 Ki > 10000.0 nM -
CHEMBL4445661 Ki > 10000.0 nM -
CHEMBL4451217 Ki > 10000.0 nM -
CHEMBL4533663 Ki > 10000.0 nM -
CHEMBL4450238 Ki > 10000.0 nM -
CHEMBL4515942 Ki > 10000.0 nM -
CHEMBL4468254 Ki > 10000.0 nM -
CHEMBL4451793 Ki - -
CHEMBL4579868 Ki > 10000.0 nM -
CHEMBL4576974 Ki > 10000.0 nM -
CHEMBL4544293 Ki > 10000.0 nM -
CHEMBL4519212 Ki > 10000.0 nM -
CHEMBL4462864 Ki > 10000.0 nM -
CHEMBL4483617 Ki > 10000.0 nM -
CHEMBL4556046 Ki > 10000.0 nM -
CHEMBL4550200 Ki > 10000.0 nM -
CHEMBL4556423 Ki > 10000.0 nM -
CHEMBL3596703 Ki > 10000.0 nM -
CHEMBL1385951 Ki > 10000.0 nM -
CHEMBL4470152 Ki > 10000.0 nM -
CHEMBL4441442 Ki > 10000.0 nM -