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Assay Detail

CHEMBL4480765

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 cell membranes after 1 hr by beta-counting analysis
24
Total Activities
24
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

Benzo[d]thiazol-2(3H)-ones as new potent selective CB<sub>2</sub> agonists with anti-inflammatory properties.
Leleu-Chavain N, Baudelet D, Heloire VM, Rocha DE, Renault N, Barczyk A, Djouina M, Body-Malapel M, Carato P, Millet R.
Eur J Med Chem (2019) 165 : 347 -362
PubMed 30583970 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 7.05 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188 WIN-552122 1 8.80
CHEMBL371214 1 8.10
CHEMBL4517991 1 7.87
CHEMBL4519981 1 7.58
CHEMBL4550003 1 7.41
CHEMBL4581598 1 7.30
CHEMBL4574224 1 6.84
CHEMBL4538593 1 6.68
CHEMBL4539849 1 6.60
CHEMBL4533329 1 6.57
CHEMBL4518631 1 6.55
CHEMBL4571345 1 6.46
CHEMBL4516391 1 6.36
CHEMBL4542489 1 6.30
CHEMBL4548364 1 6.28
CHEMBL4578601 1 -
CHEMBL4536203 1 -
CHEMBL4565332 1 -
CHEMBL4575258 1 -
CHEMBL4562588 1 -
CHEMBL4513395 1 -
CHEMBL4586935 1 -
CHEMBL4585561 1 -
CHEMBL4514301 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188 WIN-552122 Ki = 1.57 nM 8.80
CHEMBL371214 Ki = 8.0 nM 8.10
CHEMBL4517991 Ki = 13.5 nM 7.87
CHEMBL4519981 Ki = 26.0 nM 7.58
CHEMBL4550003 Ki = 39.0 nM 7.41
CHEMBL4581598 Ki = 49.5 nM 7.30
CHEMBL4574224 Ki = 144.0 nM 6.84
CHEMBL4538593 Ki = 210.0 nM 6.68
CHEMBL4539849 Ki = 251.0 nM 6.60
CHEMBL4533329 Ki = 272.0 nM 6.57
CHEMBL4518631 Ki = 280.5 nM 6.55
CHEMBL4571345 Ki = 344.0 nM 6.46
CHEMBL4516391 Ki = 438.0 nM 6.36
CHEMBL4542489 Ki = 506.0 nM 6.30
CHEMBL4548364 Ki = 525.8 nM 6.28
CHEMBL4578601 Ki > 1000.0 nM -
CHEMBL4536203 Ki > 1000.0 nM -
CHEMBL4565332 Ki > 1000.0 nM -
CHEMBL4575258 Ki > 1000.0 nM -
CHEMBL4562588 Ki > 1000.0 nM -
CHEMBL4513395 Ki > 1000.0 nM -
CHEMBL4586935 Ki > 1000.0 nM -
CHEMBL4585561 Ki > 1000.0 nM -
CHEMBL4514301 Ki > 1000.0 nM -