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Assay Detail

CHEMBL909560

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

Binding
Displacement of [3H]diprenorphine binding from human kappa opioid receptor expressed in CHO cells
26
Total Activities
26
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 Expert

Target

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

Publication

Synthesis and in vitro pharmacological studies of new C(4)-modified salvinorin A analogues.
Lee DY, He M, Liu-Chen LY, Wang Y, Li JG, Xu W, Ma Z, Carlezon WA, Cohen B.
Bioorg Med Chem Lett (2006) 16 : 5498 -5502
PubMed 16945525 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 7.55 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445332 SALVINORIN A 1.0 1 8.89
CHEMBL290543 1 8.85
CHEMBL425016 1 7.36
CHEMBL197037 1 7.31
CHEMBL386185 1 6.66
CHEMBL217971 1 6.21
CHEMBL193690 1 -
CHEMBL218259 1 -
CHEMBL385422 1 -
CHEMBL415642 1 -
CHEMBL384366 1 -
CHEMBL218477 1 -
CHEMBL218235 1 -
CHEMBL385525 1 -
CHEMBL374704 1 -
CHEMBL218158 1 -
CHEMBL220712 1 -
CHEMBL218069 1 -
CHEMBL218942 1 -
CHEMBL218418 1 -
CHEMBL219166 1 -
CHEMBL376212 1 -
CHEMBL222063 1 -
CHEMBL218140 1 -
CHEMBL376868 1 -
CHEMBL374194 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445332 SALVINORIN A Ki = 1.3 nM 8.89
CHEMBL290543 Ki = 1.4 nM 8.85
CHEMBL425016 Ki = 43.4 nM 7.36
CHEMBL197037 Ki = 48.6 nM 7.31
CHEMBL386185 Ki = 221.0 nM 6.66
CHEMBL217971 Ki = 613.0 nM 6.21
CHEMBL193690 Ki > 1000.0 nM -
CHEMBL218259 Ki > 1000.0 nM -
CHEMBL385422 Ki > 1000.0 nM -
CHEMBL415642 Ki > 1000.0 nM -
CHEMBL384366 Ki > 1000.0 nM -
CHEMBL218477 Ki > 1000.0 nM -
CHEMBL218235 Ki > 1000.0 nM -
CHEMBL385525 Ki > 1000.0 nM -
CHEMBL374704 Ki > 1000.0 nM -
CHEMBL218158 Ki > 1000.0 nM -
CHEMBL220712 Ki > 1000.0 nM -
CHEMBL218069 Ki > 1000.0 nM -
CHEMBL218942 Ki > 1000.0 nM -
CHEMBL218418 Ki > 1000.0 nM -
CHEMBL219166 Ki > 1000.0 nM -
CHEMBL376212 Ki > 1000.0 nM -
CHEMBL222063 Ki > 1000.0 nM -
CHEMBL218140 Ki > 1000.0 nM -
CHEMBL376868 Ki > 1000.0 nM -
CHEMBL374194 Ki > 1000.0 nM -