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Assay Detail

CHEMBL755191

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

Binding
Binding affinity of compound for Opioid receptor mu 1 was determined using [3H]DAMGO as radioligand from rat brain tissue
6
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Importance of phenolic address groups in opioid kappa receptor selective antagonists.
Thomas JB, Fix SE, Rothman RB, Mascarella SW, Dersch CM, Cantrell BE, Zimmerman DM, Carroll FI.
J Med Chem (2004) 47 : 1070 -1073
PubMed 14761209 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.10 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415247 JDTIC 1.0 1 8.43
CHEMBL573214 NORBINALTORPHIMINE 2 8.08
CHEMBL10986 1 6.77
CHEMBL10872 1 6.11
CHEMBL11285 1 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415247 JDTIC Ki = 3.73 nM 8.43
CHEMBL573214 NORBINALTORPHIMINE Ki = 8.3 nM 8.08
CHEMBL573214 NORBINALTORPHIMINE Ki = 65.0 nM 7.19
CHEMBL10986 Ki = 171.0 nM 6.77
CHEMBL10872 Ki = 775.0 nM 6.11
CHEMBL11285 Ki = 946.0 nM 6.02