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Assay Detail

CHEMBL758585

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

Binding
In vitro radioligand binding assay, for inhibition of [3H]DAMGO (Tyr-D-Ala-Gly-(Me)-Phe-Gly-ol) binding to Opioid receptor mu 1 in rat brain membranes at highest concentration of 6300 nM tested
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Probes for narcotic receptor mediated phenomena. 26. Synthesis and biological evaluation of diarylmethylpiperazines and diarylmethylpiperidines as novel, nonpeptidic delta opioid receptor ligands.
Zhang X, Rice KC, Calderon SN, Kayakiri H, Smith L, Coop A, Jacobson AE, Rothman RB, Davis P, Dersch CM, Porreca F.
J Med Chem (1999) 42 : 5455 -5463
PubMed 10639287 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 5.00 5.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL541349 1 5.00
CHEMBL545335 1 5.00
CHEMBL555570 1 5.00
CHEMBL542267 1 5.00
CHEMBL544638 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL541349 Ki = 10000.0 nM 5.00
CHEMBL545335 Ki = 10000.0 nM 5.00
CHEMBL555570 Ki = 10000.0 nM 5.00
CHEMBL542267 Ki = 10000.0 nM 5.00
CHEMBL544638 Ki = 10000.0 nM 5.00