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Assay Detail

CHEMBL756699

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

Binding
Binding affinity to mu-opioid receptor of rat brain using [3H]DAMGO as radioligand
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
Thomas JB, Atkinson RN, Rothman RB, Fix SE, Mascarella SW, Vinson NA, Xu H, Dersch CM, Lu Y, Cantrell BE, Zimmerman DM, Carroll FI.
J Med Chem (2001) 44 : 2687 -2690
PubMed 11495579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 6.98 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573214 NORBINALTORPHIMINE 1 7.19
CHEMBL10986 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573214 NORBINALTORPHIMINE Ki = 65.06 nM 7.19
CHEMBL10986 Ki = 171.0 nM 6.77