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Assay Detail

CHEMBL751037

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

Binding
Binding affinity against cloned human Opioid receptor kappa 1 transfected into chinese hamster ovary cells using [3H]U-69593 as radioligand
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type ovary
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.
Black SL, Chauvignac C, Grundt P, Miller CN, Wood S, Traynor JR, Lewis JW, Husbands SM.
J Med Chem (2003) 46 : 5505 -5511
PubMed 14640558 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 8.85 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112374 1 9.74
CHEMBL573214 NORBINALTORPHIMINE 1 9.70
CHEMBL2112373 1 9.31
CHEMBL610044 1 9.20
CHEMBL610045 1 9.18
CHEMBL610043 1 9.07
CHEMBL610038 1 9.02
CHEMBL610042 1 8.85
CHEMBL610032 1 8.79
CHEMBL610033 1 8.67
CHEMBL610799 1 8.62
CHEMBL610041 1 8.62
CHEMBL610035 1 8.56
CHEMBL610040 1 8.56
CHEMBL610036 1 8.49
CHEMBL610037 1 8.41
CHEMBL610039 1 8.32
CHEMBL610034 1 8.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112374 Ki = 0.18 nM 9.74
CHEMBL573214 NORBINALTORPHIMINE Ki = 0.2 nM 9.70
CHEMBL2112373 Ki = 0.49 nM 9.31
CHEMBL610044 Ki = 0.63 nM 9.20
CHEMBL610045 Ki = 0.66 nM 9.18
CHEMBL610043 Ki = 0.86 nM 9.07
CHEMBL610038 Ki = 0.95 nM 9.02
CHEMBL610042 Ki = 1.42 nM 8.85
CHEMBL610032 Ki = 1.61 nM 8.79
CHEMBL610033 Ki = 2.14 nM 8.67
CHEMBL610799 Ki = 2.38 nM 8.62
CHEMBL610041 Ki = 2.41 nM 8.62
CHEMBL610035 Ki = 2.72 nM 8.56
CHEMBL610040 Ki = 2.74 nM 8.56
CHEMBL610036 Ki = 3.26 nM 8.49
CHEMBL610037 Ki = 3.91 nM 8.41
CHEMBL610039 Ki = 4.8 nM 8.32
CHEMBL610034 Ki = 6.96 nM 8.16