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Assay Detail

CHEMBL758257

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

Binding
Binding affinity using guinea pig brain membrane preparations, towards Opioid receptor kappa 1 using [3H]- U-69,593 as radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands.
Takayama H, Ishikawa H, Kurihara M, Kitajima M, Aimi N, Ponglux D, Koyama F, Matsumoto K, Moriyama T, Yamamoto LT, Watanabe K, Murayama T, Horie S.
J Med Chem (2002) 45 : 1949 -1956
PubMed 11960505 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.24 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL58362 1 7.10
CHEMBL61630 1 6.91
CHEMBL70 MORPHINE 4.0 1 6.33
CHEMBL299031 1 5.96
CHEMBL60533 CORYNANRHEIDINE 1 5.59
CHEMBL292521 1 5.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL58362 Ki = 79.43 nM 7.10
CHEMBL61630 Ki = 123.03 nM 6.91
CHEMBL70 MORPHINE Ki = 467.74 nM 6.33
CHEMBL299031 Ki = 1096.48 nM 5.96
CHEMBL60533 CORYNANRHEIDINE Ki = 2570.4 nM 5.59
CHEMBL292521 Ki = 2951.21 nM 5.53