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Assay Detail

CHEMBL884380

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

Functional
Concentration required to enhance [35S]GTP-gamma-S, binding to human Opioid receptor kappa expressed in CHO cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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 C(4) modified salvinorin A analogues.
Lee DY, He M, Kondaveti L, Liu-Chen LY, Ma Z, Wang Y, Chen Y, Li JG, Beguin C, Carlezon WA, Cohen B.
Bioorg Med Chem Lett (2005) 15 : 4169 -4173
PubMed 16051487 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 6.98 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290543 1 8.47
CHEMBL196419 1 7.33
CHEMBL196734 1 7.24
CHEMBL197037 1 7.13
CHEMBL362953 1 7.03
CHEMBL383785 1 6.72
CHEMBL415460 1 6.65
CHEMBL263576 1 6.64
CHEMBL196096 1 6.46
CHEMBL194896 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290543 EC50 = 3.4 nM 8.47
CHEMBL196419 EC50 = 46.7 nM 7.33
CHEMBL196734 EC50 = 58.2 nM 7.24
CHEMBL197037 EC50 = 74.1 nM 7.13
CHEMBL362953 EC50 = 94.4 nM 7.03
CHEMBL383785 EC50 = 191.0 nM 6.72
CHEMBL415460 EC50 = 223.5 nM 6.65
CHEMBL263576 EC50 = 227.0 nM 6.64
CHEMBL196096 EC50 = 348.0 nM 6.46
CHEMBL194896 EC50 = 840.0 nM 6.08