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Assay Detail

CHEMBL923552

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

Binding
Displacement of [125I]IOXY from human recombinant kappa opioid receptor expressed in CHO cells
24
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Herkinorin analogues with differential beta-arrestin-2 interactions.
Tidgewell K, Groer CE, Harding WW, Lozama A, Schmidt M, Marquam A, Hiemstra J, Partilla JS, Dersch CM, Rothman RB, Bohn LM, Prisinzano TE.
J Med Chem (2008) 51 : 2421 -2431
PubMed 18380425 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 6.57 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445332 SALVINORIN A 1.0 2 8.72
CHEMBL213155 1 7.52
CHEMBL261024 1 7.16
CHEMBL260121 1 7.16
CHEMBL410436 1 7.10
CHEMBL363324 HERKINORIN 1 7.05
CHEMBL407155 1 7.05
CHEMBL429685 1 6.64
CHEMBL409414 1 6.58
CHEMBL264967 1 6.58
CHEMBL424698 SALVINORIN B 1 6.55
CHEMBL408900 1 6.39
CHEMBL260286 1 6.27
CHEMBL260485 1 6.26
CHEMBL265195 1 6.24
CHEMBL259299 1 6.13
CHEMBL260809 1 6.10
CHEMBL408775 1 6.05
CHEMBL438561 1 5.85
CHEMBL262346 1 5.85
CHEMBL258754 1 5.70
CHEMBL261807 1 5.26
CHEMBL259658 1 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445332 SALVINORIN A Ki = 1.9 nM 8.72
CHEMBL445332 SALVINORIN A Ki = 5.7 nM 8.24
CHEMBL213155 Ki = 30.0 nM 7.52
CHEMBL261024 Ki = 70.0 nM 7.16
CHEMBL260121 Ki = 70.0 nM 7.16
CHEMBL410436 Ki = 80.0 nM 7.10
CHEMBL363324 HERKINORIN Ki = 90.0 nM 7.05
CHEMBL407155 Ki = 90.0 nM 7.05
CHEMBL429685 Ki = 230.0 nM 6.64
CHEMBL409414 Ki = 260.0 nM 6.58
CHEMBL264967 Ki = 260.0 nM 6.58
CHEMBL424698 SALVINORIN B Ki = 280.0 nM 6.55
CHEMBL408900 Ki = 410.0 nM 6.39
CHEMBL260286 Ki = 540.0 nM 6.27
CHEMBL260485 Ki = 550.0 nM 6.26
CHEMBL265195 Ki = 570.0 nM 6.24
CHEMBL259299 Ki = 740.0 nM 6.13
CHEMBL260809 Ki = 800.0 nM 6.10
CHEMBL408775 Ki = 900.0 nM 6.05
CHEMBL438561 Ki = 1400.0 nM 5.85
CHEMBL262346 Ki = 1410.0 nM 5.85
CHEMBL258754 Ki = 2010.0 nM 5.70
CHEMBL261807 Ki = 5490.0 nM 5.26
CHEMBL259658 Ki = 7430.0 nM 5.13