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Assay Detail

CHEMBL4409275

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor (unknown origin) expressed in HEK293 cells after 1 hr by liquid scintillation counting
10
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL233)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Progress in the development of more effective and safer analgesics for pain management.
Turnaturi R, Chiechio S, Salerno L, Rescifina A, Pittalà V, Cantarella G, Tomarchio E, Parenti C, Pasquinucci L.
Eur J Med Chem (2019) 183 : 111701 -111701
PubMed 31550662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 8.62 8.84
Ki 4 10.96 10.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4550234 2 10.96
CHEMBL4521879 2 10.96
CHEMBL4439415 2 10.96
CHEMBL4450250 2 10.96
CHEMBL4577301 1 8.84
CHEMBL4544686 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4550234 Ki = 0.0109 nM 10.96
CHEMBL4521879 Ki = 0.0109 nM 10.96
CHEMBL4439415 Ki = 0.0109 nM 10.96
CHEMBL4450250 Ki = 0.0109 nM 10.96
CHEMBL4577301 EC50 = 1.45 nM 8.84
CHEMBL4544686 EC50 = 4.0 nM 8.40
CHEMBL4550234 EC50 = 0.00177 nM -
CHEMBL4521879 EC50 = 0.00177 nM -
CHEMBL4439415 EC50 = 0.00177 nM -
CHEMBL4450250 EC50 = 0.00177 nM -