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Assay Detail

CHEMBL3399659

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

Binding
Displacement of [3H]CP55,940 from human recombinant CB2 receptor expressed in HEK293 cell membranes after 90 mins
14
Total Activities
14
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

Synthesis, biological activity and molecular modeling of new biphenylic carboxamides as potent and selective CB2 receptor ligands.
Bertini S, Parkkari T, Savinainen JR, Arena C, Saccomanni G, Saguto S, Ligresti A, Allarà M, Bruno A, Marinelli L, Di Marzo V, Novellino E, Manera C, Macchia M.
Eur J Med Chem (2015) 90 : 526 -536
PubMed 25486424 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.50 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL381689 SR-144528 1 9.22
CHEMBL371214 1 8.52
CHEMBL3397520 1 7.94
CHEMBL3397522 1 7.66
CHEMBL3397517 1 7.22
CHEMBL3397519 1 7.22
CHEMBL3397449 1 7.05
CHEMBL3397518 1 7.05
CHEMBL3397448 1 7.00
CHEMBL3397521 1 6.84
CHEMBL3397450 1 6.82
CHEMBL3397445 1 -
CHEMBL3397446 1 -
CHEMBL3397447 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL381689 SR-144528 Ki = 0.6 nM 9.22
CHEMBL371214 Ki = 3.0 nM 8.52
CHEMBL3397520 Ki = 11.48 nM 7.94
CHEMBL3397522 Ki = 22.0 nM 7.66
CHEMBL3397517 Ki = 60.0 nM 7.22
CHEMBL3397519 Ki = 60.0 nM 7.22
CHEMBL3397449 Ki = 90.0 nM 7.05
CHEMBL3397518 Ki = 90.0 nM 7.05
CHEMBL3397448 Ki = 100.0 nM 7.00
CHEMBL3397521 Ki = 143.0 nM 6.84
CHEMBL3397450 Ki = 150.0 nM 6.82
CHEMBL3397445 Ki > 10000.0 nM -
CHEMBL3397446 Ki > 10000.0 nM -
CHEMBL3397447 Ki > 10000.0 nM -