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Assay Detail

CHEMBL752210

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

Binding
Binding affinity for kappa opioid receptor
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Kappa-type opioid receptor (CHEMBL237)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New scaffolds in the development of mu opioid-receptor ligands.
Pagé D, Nguyen N, Bernard S, Coupal M, Gosselin M, Lepage J, Adam L, Brown W.
Bioorg Med Chem Lett (2003) 13 : 1585 -1589
PubMed 12699761 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.57 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288468 1 7.40
CHEMBL40993 1 6.96
CHEMBL39272 1 6.89
CHEMBL41736 1 6.71
CHEMBL288205 1 6.52
CHEMBL39968 1 6.51
CHEMBL40859 1 6.39
CHEMBL40825 1 6.32
CHEMBL289137 1 6.32
CHEMBL41883 1 6.29
CHEMBL40548 1 6.28
CHEMBL41946 1 6.26
CHEMBL441427 1 -
CHEMBL287981 1 -
CHEMBL418616 1 -
CHEMBL416788 1 -
CHEMBL289494 1 -
CHEMBL38874 DAMGO 1 -
CHEMBL41550 1 -
CHEMBL38511 1 -
CHEMBL289320 1 -
CHEMBL41245 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288468 Ki = 39.5 nM 7.40
CHEMBL40993 Ki = 109.0 nM 6.96
CHEMBL39272 Ki = 130.0 nM 6.89
CHEMBL41736 Ki = 194.0 nM 6.71
CHEMBL288205 Ki = 303.0 nM 6.52
CHEMBL39968 Ki = 310.0 nM 6.51
CHEMBL40859 Ki = 405.0 nM 6.39
CHEMBL40825 Ki = 480.0 nM 6.32
CHEMBL289137 Ki = 481.0 nM 6.32
CHEMBL41883 Ki = 511.0 nM 6.29
CHEMBL40548 Ki = 530.0 nM 6.28
CHEMBL41946 Ki = 543.0 nM 6.26
CHEMBL441427 Ki > 1000.0 nM -
CHEMBL287981 Ki > 1000.0 nM -
CHEMBL418616 Ki > 1000.0 nM -
CHEMBL416788 Ki > 1000.0 nM -
CHEMBL289494 Ki > 1000.0 nM -
CHEMBL38874 DAMGO Ki > 1000.0 nM -
CHEMBL41245 Ki > 1000.0 nM -
CHEMBL41550 Ki > 1000.0 nM -
CHEMBL38511 Ki > 1000.0 nM -
CHEMBL289320 Ki > 1000.0 nM -
CHEMBL41245 Ki > 1000.0 nM -