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Assay Detail

CHEMBL887466

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

Binding
Displacement of [3H]U-69593 from rat cloned KOR
5
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Kappa-type opioid receptor (CHEMBL3614)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B.
Bikbulatov RV, Yan F, Roth BL, Zjawiony JK.
Bioorg Med Chem Lett (2007) 17 : 2229 -2232
PubMed 17303418 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.44 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445332 SALVINORIN A 1.0 2 9.12
CHEMBL231536 2-THIOSALVINORIN B 1 7.26
CHEMBL231537 2-EPI-2-THIOSALVINORIN A 1 6.82
CHEMBL231638 2-EPI-2-THIOSALVINORIN B 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445332 SALVINORIN A Ki = 0.75 nM 9.12
CHEMBL445332 SALVINORIN A Ki = 18.4 nM 7.74
CHEMBL231536 2-THIOSALVINORIN B Ki = 54.5 nM 7.26
CHEMBL231537 2-EPI-2-THIOSALVINORIN A Ki = 151.0 nM 6.82
CHEMBL231638 2-EPI-2-THIOSALVINORIN B Ki = 546.0 nM 6.26