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Assay Detail

CHEMBL4138413

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

Binding
Displacement of [125I]BNtxA from mouse MOR expressed in CHO cell membranes after 90 mins by filter binding assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL2858)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and pharmacological evaluation of novel selective MOR agonist 6β-pyridinyl amidomorphines exhibiting long-lasting antinociception.
Urai Á, Váradi A, Szőcs L, Komjáti B, Le Rouzic V, Hunkele A, Pasternak GW, Majumdar S, Hosztafi S.
Medchemcomm (2017) 8 : 152 -157
PubMed 28603600 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.32 8.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4165157 1 8.90
CHEMBL4159603 1 8.70
CHEMBL4168572 1 8.48
CHEMBL4173059 1 8.43
CHEMBL70 MORPHINE 4.0 1 8.34
CHEMBL4167519 1 8.16
CHEMBL4167929 1 8.15
CHEMBL4176436 1 7.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4165157 Ki = 1.25 nM 8.90
CHEMBL4159603 Ki = 2.0 nM 8.70
CHEMBL4168572 Ki = 3.29 nM 8.48
CHEMBL4173059 Ki = 3.73 nM 8.43
CHEMBL70 MORPHINE Ki = 4.6 nM 8.34
CHEMBL4167519 Ki = 6.91 nM 8.16
CHEMBL4167929 Ki = 7.02 nM 8.15
CHEMBL4176436 Ki = 40.59 nM 7.39