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Assay Detail

CHEMBL3270913

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

Binding
Displacement of [3H]U69,593 from human kappa opioid receptor transfected in CHO cell membranes after 60 mins
13
Total Activities
13
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

Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.
Journigan VB, Polgar WE, Khroyan TV, Zaveri NT.
Bioorg Med Chem (2014) 22 : 2508 -2516
PubMed 24657054 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.88 8.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL440765 U-69593 1 8.98
CHEMBL3262548 1 7.89
CHEMBL3262547 1 7.82
CHEMBL3262546 1 7.25
CHEMBL3262549 1 7.05
CHEMBL3262544 1 6.82
CHEMBL3262545 1 6.74
CHEMBL3262551 1 6.33
CHEMBL3262542 1 6.29
CHEMBL3262543 1 6.09
CHEMBL3262552 1 5.86
CHEMBL3262550 1 5.38
CHEMBL3262553 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL440765 U-69593 Ki = 1.05 nM 8.98
CHEMBL3262548 Ki = 12.82 nM 7.89
CHEMBL3262547 Ki = 15.13 nM 7.82
CHEMBL3262546 Ki = 56.3 nM 7.25
CHEMBL3262549 Ki = 88.4 nM 7.05
CHEMBL3262544 Ki = 152.0 nM 6.82
CHEMBL3262545 Ki = 184.0 nM 6.74
CHEMBL3262551 Ki = 467.7 nM 6.33
CHEMBL3262542 Ki = 516.0 nM 6.29
CHEMBL3262543 Ki = 814.0 nM 6.09
CHEMBL3262552 Ki = 1367.0 nM 5.86
CHEMBL3262550 Ki = 4171.0 nM 5.38
CHEMBL3262553 Ki > 10000.0 nM -