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Assay Detail

CHEMBL757059

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

Binding
Binding affinity against mu opiate receptor
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

From hit to lead. Analyzing structure-profile relationships.
Poulain R, Horvath D, Bonnet B, Eckhoff C, Chapelain B, Bodinier MC, Déprez B.
J Med Chem (2001) 44 : 3391 -3401
PubMed 11585444 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.55 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL115222 1 9.05
CHEMBL114379 1 8.92
CHEMBL324297 1 8.82
CHEMBL115652 1 8.70
CHEMBL420863 1 8.62
CHEMBL325945 1 8.20
CHEMBL114484 1 7.80
CHEMBL326962 1 7.78
CHEMBL115229 1 7.71
CHEMBL325750 1 7.53
CHEMBL115280 1 7.08
CHEMBL115444 1 6.83
CHEMBL114825 1 6.75
CHEMBL115709 1 6.71
CHEMBL114280 1 6.63
CHEMBL111918 1 6.13
CHEMBL325258 1 6.10
CHEMBL332697 1 6.02
CHEMBL115549 1 5.98
CHEMBL326320 1 5.91
CHEMBL326263 1 5.83
CHEMBL325674 1 5.83
CHEMBL115249 1 5.77
CHEMBL115076 1 5.76
CHEMBL420500 1 5.64
CHEMBL325697 1 5.64
CHEMBL333843 1 5.61
CHEMBL114299 1 5.59
CHEMBL419214 1 5.54
CHEMBL116735 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL115222 IC50 = 0.9 nM 9.05
CHEMBL114379 IC50 = 1.2 nM 8.92
CHEMBL324297 IC50 = 1.5 nM 8.82
CHEMBL115652 IC50 = 2.0 nM 8.70
CHEMBL420863 IC50 = 2.4 nM 8.62
CHEMBL325945 IC50 = 6.3 nM 8.20
CHEMBL114484 IC50 = 16.0 nM 7.80
CHEMBL326962 IC50 = 16.7 nM 7.78
CHEMBL115229 IC50 = 19.3 nM 7.71
CHEMBL325750 IC50 = 29.4 nM 7.53
CHEMBL115280 IC50 = 83.5 nM 7.08
CHEMBL115444 IC50 = 147.0 nM 6.83
CHEMBL114825 IC50 = 179.0 nM 6.75
CHEMBL115709 IC50 = 197.0 nM 6.71
CHEMBL114280 IC50 = 235.0 nM 6.63
CHEMBL111918 IC50 = 735.0 nM 6.13
CHEMBL325258 IC50 = 800.0 nM 6.10
CHEMBL332697 IC50 = 960.0 nM 6.02
CHEMBL115549 IC50 = 1050.0 nM 5.98
CHEMBL326320 IC50 = 1235.0 nM 5.91
CHEMBL326263 IC50 = 1470.0 nM 5.83
CHEMBL325674 IC50 = 1470.0 nM 5.83
CHEMBL115249 IC50 = 1690.0 nM 5.77
CHEMBL115076 IC50 = 1730.0 nM 5.76
CHEMBL420500 IC50 = 2285.0 nM 5.64
CHEMBL325697 IC50 = 2285.0 nM 5.64
CHEMBL333843 IC50 = 2480.0 nM 5.61
CHEMBL114299 IC50 = 2590.0 nM 5.59
CHEMBL419214 IC50 = 2890.0 nM 5.54
CHEMBL116735 IC50 = 3660.0 nM 5.44
CHEMBL117537 IC50 = 3810.0 nM 5.42
CHEMBL420499 IC50 = 3950.0 nM 5.40
CHEMBL325516 IC50 = 4015.0 nM 5.40
CHEMBL113956 IC50 = 4545.0 nM 5.34
CHEMBL324479 IC50 = 4955.0 nM 5.30
CHEMBL116463 IC50 = 6545.0 nM 5.18