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Assay Detail

CHEMBL4684593

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

Binding
Displacement of [3H]-DAMGO from rat mu opioid receptor expressed in CHO cells incubated for 30 mins by liquid scintillation counting method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic.
Huang H,Wang W,Xu X,Zhu C,Wang Y,Liu J,Li W,Fu W
Eur J Med Chem (2020) 189 : 112070 -112070
PubMed 31982651 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.29 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4786173 1 8.92
CHEMBL38874 DAMGO 1 8.64
CHEMBL4756256 1 8.14
CHEMBL1400 O-DESMETHYL TRAMADOL 1 7.89
CHEMBL4800532 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4786173 Ki = 1.2 nM 8.92
CHEMBL38874 DAMGO Ki = 2.3 nM 8.64
CHEMBL4756256 Ki = 7.3 nM 8.14
CHEMBL1400 O-DESMETHYL TRAMADOL Ki = 13.0 nM 7.89
CHEMBL4800532 Ki = 14.1 nM 7.85