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Assay Detail

CHEMBL752677

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

Binding
Binding affinity to Opioid receptor mu 1 by using [3H]DAMGO 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

Mu-type opioid receptor (CHEMBL4354)
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 7.15 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL172529 1 8.09
CHEMBL172493 1 7.79
CHEMBL368522 1 7.78
CHEMBL368421 1 7.73
CHEMBL170399 1 7.68
CHEMBL367497 1 7.66
CHEMBL567175 NALTRINDOLE 1 7.56
CHEMBL435898 1 7.52
CHEMBL367962 1 7.50
CHEMBL176537 1 7.44
CHEMBL477154 1 7.41
CHEMBL173749 1 7.15
CHEMBL173874 1 7.04
CHEMBL368600 1 6.90
CHEMBL353930 1 6.67
CHEMBL174263 1 6.17
CHEMBL367290 1 5.29
CHEMBL173319 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL172529 Ki = 8.11 nM 8.09
CHEMBL172493 Ki = 16.4 nM 7.79
CHEMBL368522 Ki = 16.7 nM 7.78
CHEMBL368421 Ki = 18.7 nM 7.73
CHEMBL170399 Ki = 20.9 nM 7.68
CHEMBL367497 Ki = 22.0 nM 7.66
CHEMBL567175 NALTRINDOLE Ki = 27.5 nM 7.56
CHEMBL435898 Ki = 30.0 nM 7.52
CHEMBL367962 Ki = 32.0 nM 7.50
CHEMBL176537 Ki = 36.2 nM 7.44
CHEMBL477154 Ki = 39.2 nM 7.41
CHEMBL173749 Ki = 70.7 nM 7.15
CHEMBL173874 Ki = 90.3 nM 7.04
CHEMBL368600 Ki = 124.9 nM 6.90
CHEMBL353930 Ki = 213.7 nM 6.67
CHEMBL174263 Ki = 671.2 nM 6.17
CHEMBL367290 Ki = 5191.0 nM 5.29
CHEMBL173319 Ki = 5127.0 nM 5.29