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Assay Detail

CHEMBL4380083

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

Binding
Displacement of [3H]U69,593 from human recombinant kappa opioid receptor expressed in rat RBL cell membranes incubated for 60 mins
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL237)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
Obeng S, Kamble SH, Reeves ME, Restrepo LF, Patel A, Behnke M, Chear NJ, Ramanathan S, Sharma A, León F, Hiranita T, Avery BA, McMahon LR, McCurdy CR.
J Med Chem (2020) 63 : 433 -439
PubMed 31834797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.20 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290543 1 9.52
CHEMBL61630 1 7.13
CHEMBL4546925 1 6.94
CHEMBL299031 1 6.70
CHEMBL60533 CORYNANRHEIDINE 1 5.72
CHEMBL292521 1 -
CHEMBL38874 DAMGO 1 -
CHEMBL31421 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290543 Ki = 0.3 nM 9.52
CHEMBL61630 Ki = 74.1 nM 7.13
CHEMBL4546925 Ki = 116.0 nM 6.94
CHEMBL299031 Ki = 198.0 nM 6.70
CHEMBL60533 CORYNANRHEIDINE Ki = 1910.0 nM 5.72
CHEMBL292521 Ki - -
CHEMBL38874 DAMGO Ki - -
CHEMBL31421 Ki - -