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Assay Detail

CHEMBL1764074

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

Binding
Displacement of [3H]-naltrindole from human mu opioid receptor expressed in CHO cells after 2 hrs by scintillation counting
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor.
Del Giudice MR, Borioni A, Bastanzio G, Sbraccia M, Mustazza C, Sestili I.
Eur J Med Chem (2011) 46 : 1207 -1221
PubMed 21330016 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.64 6.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1762409 1 6.49
CHEMBL1762381 1 6.33
CHEMBL1762385 1 5.98
CHEMBL1762387 1 5.94
CHEMBL1762388 1 5.88
CHEMBL1762384 1 5.86
CHEMBL1762411 1 5.85
CHEMBL1762405 1 5.85
CHEMBL140979 1 5.82
CHEMBL1762382 1 5.80
CHEMBL1762386 1 5.72
CHEMBL1762401 1 5.70
CHEMBL1762403 1 5.66
CHEMBL1762383 1 5.60
CHEMBL1762400 1 5.59
CHEMBL1762404 1 5.56
CHEMBL1762397 1 5.48
CHEMBL1762402 1 5.36
CHEMBL1762399 1 5.35
CHEMBL1762407 1 5.31
CHEMBL1762398 1 5.29
CHEMBL1762406 1 5.27
CHEMBL1760025 1 5.22
CHEMBL1762410 1 5.15
CHEMBL1762408 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1762409 IC50 = 325.0 nM 6.49
CHEMBL1762381 IC50 = 468.0 nM 6.33
CHEMBL1762385 IC50 = 1038.0 nM 5.98
CHEMBL1762387 IC50 = 1160.0 nM 5.94
CHEMBL1762388 IC50 = 1320.0 nM 5.88
CHEMBL1762384 IC50 = 1390.0 nM 5.86
CHEMBL1762411 IC50 = 1401.0 nM 5.85
CHEMBL1762405 IC50 = 1402.0 nM 5.85
CHEMBL140979 IC50 = 1507.0 nM 5.82
CHEMBL1762382 IC50 = 1590.0 nM 5.80
CHEMBL1762386 IC50 = 1900.0 nM 5.72
CHEMBL1762401 IC50 = 1977.0 nM 5.70
CHEMBL1762403 IC50 = 2171.0 nM 5.66
CHEMBL1762383 IC50 = 2505.0 nM 5.60
CHEMBL1762400 IC50 = 2593.0 nM 5.59
CHEMBL1762404 IC50 = 2755.0 nM 5.56
CHEMBL1762397 IC50 = 3345.0 nM 5.48
CHEMBL1762402 IC50 = 4339.0 nM 5.36
CHEMBL1762399 IC50 = 4453.0 nM 5.35
CHEMBL1762407 IC50 = 4885.0 nM 5.31
CHEMBL1762398 IC50 = 5114.0 nM 5.29
CHEMBL1762406 IC50 = 5333.0 nM 5.27
CHEMBL1760025 IC50 = 5999.0 nM 5.22
CHEMBL1762410 IC50 = 7071.0 nM 5.15
CHEMBL1762408 IC50 = 9978.0 nM 5.00