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Assay Detail

CHEMBL832509

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

Functional
Effective concentration for activation of human Opioid receptor kappa 1 expressed in chinese hamster ovary cells to enhance [35S]GTP-gamma-S, binding
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type ovary
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
EC50 16 7.28 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445332 SALVINORIN A 1.0 1 8.35
CHEMBL290543 1 8.35
CHEMBL3349979 1 8.21
CHEMBL379138 1 8.00
CHEMBL378635 DEOXY SALVINORIN A 1 7.73
CHEMBL370272 1 7.69
CHEMBL255969 SALVINORIN A PROPYL ETHER 1 7.17
CHEMBL384411 1 7.16
CHEMBL3349980 1 6.98
CHEMBL3349984 1 6.84
CHEMBL3349987 1 6.79
CHEMBL3349983 1 6.70
CHEMBL213567 1 6.46
CHEMBL424698 SALVINORIN B 1 6.43
CHEMBL413774 1 6.41
CHEMBL3219942 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445332 SALVINORIN A EC50 = 4.5 nM 8.35
CHEMBL290543 EC50 = 4.5 nM 8.35
CHEMBL3349979 EC50 = 6.2 nM 8.21
CHEMBL379138 EC50 = 9.9 nM 8.00
CHEMBL378635 DEOXY SALVINORIN A EC50 = 18.6 nM 7.73
CHEMBL370272 EC50 = 20.4 nM 7.69
CHEMBL255969 SALVINORIN A PROPYL ETHER EC50 = 67.4 nM 7.17
CHEMBL384411 EC50 = 68.9 nM 7.16
CHEMBL3349980 EC50 = 104.0 nM 6.98
CHEMBL3349984 EC50 = 145.0 nM 6.84
CHEMBL3349987 EC50 = 161.0 nM 6.79
CHEMBL3349983 EC50 = 201.0 nM 6.70
CHEMBL213567 EC50 = 343.0 nM 6.46
CHEMBL424698 SALVINORIN B EC50 = 371.0 nM 6.43
CHEMBL413774 EC50 = 389.0 nM 6.41
CHEMBL3219942 EC50 > 1000.0 nM -