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Assay Detail

CHEMBL838864

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Binding
Inhibition of [3H]U-69593 binding to rat opioid receptor kappa 1 expressed in HEK 293 cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Studies toward the pharmacophore of salvinorin A, a potent kappa opioid receptor agonist.
Munro TA, Rizzacasa MA, Roth BL, Toth BA, Yan F.
J Med Chem (2005) 48 : 345 -348
PubMed 15658846 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.23 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445332 SALVINORIN A 1.0 1 8.40
CHEMBL370678 1 8.22
CHEMBL194545 1 8.22
CHEMBL370680 1 7.75
CHEMBL365533 1 7.75
CHEMBL195344 1 7.23
CHEMBL364058 1 6.81
CHEMBL435108 SALVINORIN A (ESTER) 1 6.79
CHEMBL425016 1 6.46
CHEMBL365547 1 5.99
CHEMBL237054 1-ALPHA-HYDROXYSALVINORIN A 1 5.95
CHEMBL191597 1 -
CHEMBL363482 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445332 SALVINORIN A Ki = 4.0 nM 8.40
CHEMBL370678 Ki = 6.0 nM 8.22
CHEMBL194545 Ki = 6.0 nM 8.22
CHEMBL370680 Ki = 18.0 nM 7.75
CHEMBL365533 Ki = 18.0 nM 7.75
CHEMBL195344 Ki = 59.0 nM 7.23
CHEMBL364058 Ki = 156.0 nM 6.81
CHEMBL435108 SALVINORIN A (ESTER) Ki = 163.0 nM 6.79
CHEMBL425016 Ki = 347.0 nM 6.46
CHEMBL365547 Ki = 1022.0 nM 5.99
CHEMBL237054 1-ALPHA-HYDROXYSALVINORIN A Ki = 1125.0 nM 5.95
CHEMBL191597 Ki > 10000.0 nM -
CHEMBL363482 Ki > 10000.0 nM -