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Assay Detail

CHEMBL4372810

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Binding
Agonist activity at Tango-KOR (unknown origin) expressed in HTLA cells harboring TEV-fused-beta-arrestin 2 assessed as increase in beta arrestin 2 recruitment after overnight incubation by BrightGlo reagent based assay
10
Total Activities
10
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

Development of Novel Quinoxaline-Based κ-Opioid Receptor Agonists for the Treatment of Neuroinflammation.
Tangherlini G, Kalinin DV, Schepmann D, Che T, Mykicki N, Ständer S, Loser K, Wünsch B.
J Med Chem (2019) 62 : 893 -907
PubMed 30543421 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 7.60 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4069231 1 8.42
CHEMBL445332 SALVINORIN A 1.0 1 8.29
CHEMBL4582146 1 8.10
CHEMBL4467644 1 7.92
CHEMBL4462000 1 7.77
CHEMBL4561040 1 7.48
CHEMBL4483681 1 7.38
CHEMBL4463652 1 7.37
CHEMBL4555496 1 6.64
CHEMBL4438714 1 6.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4069231 EC50 = 3.8 nM 8.42
CHEMBL445332 SALVINORIN A EC50 = 5.1 nM 8.29
CHEMBL4582146 EC50 = 7.9 nM 8.10
CHEMBL4467644 EC50 = 12.0 nM 7.92
CHEMBL4462000 EC50 = 17.0 nM 7.77
CHEMBL4561040 EC50 = 33.0 nM 7.48
CHEMBL4483681 EC50 = 42.0 nM 7.38
CHEMBL4463652 EC50 = 43.0 nM 7.37
CHEMBL4555496 EC50 = 227.0 nM 6.64
CHEMBL4438714 EC50 = 247.0 nM 6.61