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Assay Detail

CHEMBL755867

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

Binding
Binding affinity to Opioid receptor kappa 1 by using [3H]U-69593 as a radioligand from guinea pig
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole.
Clayson J, Jales A, Tyacke RJ, Hudson AL, Nutt DJ, Lewis JW, Husbands SM.
Bioorg Med Chem Lett (2001) 11 : 939 -943
PubMed 11294396 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.22 8.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL477154 1 8.08
CHEMBL368522 1 8.08
CHEMBL368421 1 8.01
CHEMBL172493 1 7.92
CHEMBL367497 1 7.85
CHEMBL567175 NALTRINDOLE 1 7.84
CHEMBL172529 1 7.84
CHEMBL367962 1 7.75
CHEMBL170399 1 7.74
CHEMBL176537 1 7.57
CHEMBL368600 1 7.26
CHEMBL173874 1 7.24
CHEMBL435898 1 6.93
CHEMBL173749 1 6.70
CHEMBL353930 1 6.29
CHEMBL367290 1 5.75
CHEMBL174263 1 5.57
CHEMBL173319 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL477154 Ki = 8.33 nM 8.08
CHEMBL368522 Ki = 8.3 nM 8.08
CHEMBL368421 Ki = 9.84 nM 8.01
CHEMBL172493 Ki = 11.9 nM 7.92
CHEMBL367497 Ki = 14.0 nM 7.85
CHEMBL567175 NALTRINDOLE Ki = 14.3 nM 7.84
CHEMBL172529 Ki = 14.5 nM 7.84
CHEMBL367962 Ki = 18.0 nM 7.75
CHEMBL170399 Ki = 18.3 nM 7.74
CHEMBL176537 Ki = 26.7 nM 7.57
CHEMBL368600 Ki = 54.8 nM 7.26
CHEMBL173874 Ki = 57.3 nM 7.24
CHEMBL435898 Ki = 116.7 nM 6.93
CHEMBL173749 Ki = 200.4 nM 6.70
CHEMBL353930 Ki = 515.0 nM 6.29
CHEMBL367290 Ki = 1784.0 nM 5.75
CHEMBL174263 Ki = 2679.0 nM 5.57
CHEMBL173319 Ki = 3105.0 nM 5.51