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Assay Detail

CHEMBL4842495

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

Binding
Displacement of [3H]-CP55940 from human recombinant CB2 receptor expressed in CHO-K1 cell membrane measured after 3 hrs by scintillation spectrometry
ChEMBL ↗
67
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and SAR evaluation of coumarin derivatives as potent cannabinoid receptor agonists.
Mohr F, Hurrle T, Burggraaff L, Langer L, Bemelmans MP, Knab M, Nieger M, van Westen GJP, Heitman LH, Bräse S.
Eur J Med Chem (2021) 220 : 113354 -113354
PubMed 33915369 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 67 7.07 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4847976 — — 2 8.19
CHEMBL4863350 — — 2 7.90
CHEMBL4846991 — — 2 7.86
CHEMBL4854325 — — 2 7.73
CHEMBL4857976 — — 2 7.41
CHEMBL4877653 — — 2 7.25
CHEMBL4850004 — — 2 7.22
CHEMBL4852456 — — 2 7.14
CHEMBL4862930 — — 2 7.08
CHEMBL4849400 — — 2 6.98
CHEMBL2181540 — — 1 6.68
CHEMBL4852077 — — 2 6.65
CHEMBL4852553 — — 2 6.64
CHEMBL4865342 — — 2 6.51
CHEMBL2177264 — — 1 6.33
CHEMBL4852184 — — 1 6.00
CHEMBL2181539 — — 1 5.52
CHEMBL2177263 — — 1 5.38
CHEMBL4864753 — — 1 -
CHEMBL4847366 — — 1 -
CHEMBL4856291 — — 1 -
CHEMBL4847428 — — 1 -
CHEMBL4848227 — — 1 -
CHEMBL4846226 — — 1 -
CHEMBL4867914 — — 1 -
CHEMBL4852990 — — 1 -
CHEMBL4848593 — — 1 -
CHEMBL4875313 — — 1 -
CHEMBL4850028 — — 1 -
CHEMBL4852503 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4847976 — Ki = 6.457 nM 8.19
CHEMBL4847976 — Ki = 6.5 nM 8.19
CHEMBL4863350 — Ki = 12.59 nM 7.90
CHEMBL4863350 — Ki = 12.5 nM 7.90
CHEMBL4846991 — Ki = 13.7 nM 7.86
CHEMBL4846991 — Ki = 13.8 nM 7.86
CHEMBL4854325 — Ki = 18.6 nM 7.73
CHEMBL4854325 — Ki = 18.62 nM 7.73
CHEMBL4857976 — Ki = 39.1 nM 7.41
CHEMBL4857976 — Ki = 38.9 nM 7.41
CHEMBL4877653 — Ki = 56.5 nM 7.25
CHEMBL4877653 — Ki = 56.23 nM 7.25
CHEMBL4850004 — Ki = 60.26 nM 7.22
CHEMBL4850004 — Ki = 60.6 nM 7.22
CHEMBL4852456 — Ki = 72.44 nM 7.14
CHEMBL4852456 — Ki = 71.9 nM 7.14
CHEMBL4862930 — Ki = 83.18 nM 7.08
CHEMBL4862930 — Ki = 82.4 nM 7.08
CHEMBL4849400 — Ki = 104.71 nM 6.98
CHEMBL4849400 — Ki = 106.0 nM 6.97
CHEMBL2181540 — Ki = 210.0 nM 6.68
CHEMBL4852077 — Ki = 223.87 nM 6.65
CHEMBL4852077 — Ki = 222.0 nM 6.65
CHEMBL4852553 — Ki = 229.09 nM 6.64
CHEMBL4852553 — Ki = 231.0 nM 6.64
CHEMBL4865342 — Ki = 309.03 nM 6.51
CHEMBL4865342 — Ki = 310.0 nM 6.51
CHEMBL2177264 — Ki = 465.0 nM 6.33
CHEMBL4852184 — Ki = 1000.0 nM 6.00
CHEMBL2181539 — Ki = 3010.0 nM 5.52
CHEMBL2177263 — Ki = 4120.0 nM 5.38
CHEMBL4871926 — Ki > 1000.0 nM -
CHEMBL4878295 — Ki > 1000.0 nM -
CHEMBL4855966 — Ki > 1000.0 nM -
CHEMBL4856291 — Ki > 1000.0 nM -
CHEMBL4862523 — Ki > 1000.0 nM -
CHEMBL4860325 — Ki > 1000.0 nM -
CHEMBL4850969 — Ki > 1000.0 nM -
CHEMBL4850045 — Ki > 1000.0 nM -
CHEMBL4853820 — Ki > 1000.0 nM -
CHEMBL4858513 — Ki > 1000.0 nM -
CHEMBL4872254 — Ki > 1000.0 nM -
CHEMBL4855282 — Ki > 1000.0 nM -
CHEMBL4849409 — Ki > 1000.0 nM -
CHEMBL4852503 — Ki > 1000.0 nM -
CHEMBL4850028 — Ki > 1000.0 nM -
CHEMBL4875313 — Ki > 1000.0 nM -
CHEMBL4848593 — Ki > 1000.0 nM -
CHEMBL4867914 — Ki > 1000.0 nM -
CHEMBL4848227 — Ki > 1000.0 nM -