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Assay Detail

CHEMBL839963

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

Binding
Inhibition of [3H]diprenorphine binding to human Opioid receptor kappa 1 expressed in chinese hamster ovary cells
21
Total Activities
21
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 evaluation of salvinorin A analogues modified at C(2).
Béguin C, Richards MR, Wang Y, Chen Y, Liu-Chen LY, Ma Z, Lee DY, Carlezon WA, Cohen BM.
Bioorg Med Chem Lett (2005) 15 : 2761 -2765
PubMed 15869877 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.60 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445332 SALVINORIN A 1.0 1 8.89
CHEMBL290543 1 8.85
CHEMBL3349979 1 8.49
CHEMBL379138 1 8.31
CHEMBL370272 1 8.14
CHEMBL378635 DEOXY SALVINORIN A 1 8.10
CHEMBL255969 SALVINORIN A PROPYL ETHER 1 7.54
CHEMBL384411 1 7.54
CHEMBL3349980 1 7.45
CHEMBL3349984 1 7.22
CHEMBL3349987 1 7.12
CHEMBL3349983 1 7.08
CHEMBL213567 1 7.04
CHEMBL424698 SALVINORIN B 1 6.81
CHEMBL413774 1 6.66
CHEMBL3219942 1 6.33
CHEMBL215076 1 -
CHEMBL1644773 1 -
CHEMBL3350046 1 -
CHEMBL3349985 1 -
CHEMBL3349986 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
CHEMBL3349979 Ki = 3.2 nM 8.49
CHEMBL379138 Ki = 4.9 nM 8.31
CHEMBL370272 Ki = 7.2 nM 8.14
CHEMBL378635 DEOXY SALVINORIN A Ki = 7.9 nM 8.10
CHEMBL255969 SALVINORIN A PROPYL ETHER Ki = 28.7 nM 7.54
CHEMBL384411 Ki = 28.9 nM 7.54
CHEMBL3349980 Ki = 35.8 nM 7.45
CHEMBL3349984 Ki = 60.1 nM 7.22
CHEMBL3349987 Ki = 75.7 nM 7.12
CHEMBL3349983 Ki = 83.0 nM 7.08
CHEMBL213567 Ki = 90.9 nM 7.04
CHEMBL424698 SALVINORIN B Ki = 155.0 nM 6.81
CHEMBL413774 Ki = 220.0 nM 6.66
CHEMBL3219942 Ki = 462.0 nM 6.33
CHEMBL215076 Ki > 10000.0 nM -
CHEMBL1644773 Ki > 10000.0 nM -
CHEMBL3350046 Ki > 10000.0 nM -
CHEMBL3349985 Ki > 10000.0 nM -
CHEMBL3349986 Ki > 10000.0 nM -