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Assay Detail

CHEMBL750412

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Binding
Binding affinity against delta-opiate receptor (human) using [3H]-DPDPE radioligand
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands.
Poulain R, Horvath D, Bonnet B, Eckhoff C, Chapelain B, Bodinier MC, Déprez B.
J Med Chem (2001) 44 : 3378 -3390
PubMed 11585443 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 6.36 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2368861 BUPRENORPHINE HYDROCHLORIDE 4.0 1 9.05
CHEMBL115222 1 7.94
CHEMBL114379 1 7.43
CHEMBL420863 1 6.93
CHEMBL1707 LOPERAMIDE HYDROCHLORIDE 4.0 1 6.91
CHEMBL115652 1 6.86
CHEMBL80 NALOXONE 4.0 1 6.82
CHEMBL2096625 1 6.62
CHEMBL324297 1 6.58
CHEMBL895 NALBUPHINE 4.0 1 6.45
CHEMBL596 FENTANYL 4.0 1 6.37
CHEMBL325842 1 6.21
CHEMBL115229 1 5.98
CHEMBL651 METHADONE 4.0 1 5.96
CHEMBL326962 1 5.92
CHEMBL112191 1 5.85
CHEMBL114825 1 5.75
CHEMBL115280 1 5.74
CHEMBL115444 1 5.60
CHEMBL114280 1 5.48
CHEMBL325750 1 5.38
CHEMBL326320 1 5.25
CHEMBL419214 1 5.15
CHEMBL324142 1 -
CHEMBL332697 1 -
CHEMBL324170 1 -
CHEMBL324257 1 -
CHEMBL326538 1 -
CHEMBL325874 1 -
CHEMBL115076 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2368861 BUPRENORPHINE HYDROCHLORIDE IC50 = 0.9 nM 9.05
CHEMBL115222 IC50 = 11.4 nM 7.94
CHEMBL114379 IC50 = 37.4 nM 7.43
CHEMBL420863 IC50 = 117.0 nM 6.93
CHEMBL1707 LOPERAMIDE HYDROCHLORIDE IC50 = 123.0 nM 6.91
CHEMBL115652 IC50 = 138.0 nM 6.86
CHEMBL80 NALOXONE IC50 = 151.0 nM 6.82
CHEMBL2096625 IC50 = 242.0 nM 6.62
CHEMBL324297 IC50 = 264.0 nM 6.58
CHEMBL895 NALBUPHINE IC50 = 353.0 nM 6.45
CHEMBL596 FENTANYL IC50 = 431.0 nM 6.37
CHEMBL325842 IC50 = 620.0 nM 6.21
CHEMBL115229 IC50 = 1040.0 nM 5.98
CHEMBL651 METHADONE IC50 = 1090.0 nM 5.96
CHEMBL326962 IC50 = 1190.0 nM 5.92
CHEMBL112191 IC50 = 1410.0 nM 5.85
CHEMBL114825 IC50 = 1765.0 nM 5.75
CHEMBL115280 IC50 = 1840.0 nM 5.74
CHEMBL115444 IC50 = 2530.0 nM 5.60
CHEMBL114280 IC50 = 3330.0 nM 5.48
CHEMBL325750 IC50 = 4120.0 nM 5.38
CHEMBL326320 IC50 = 5640.0 nM 5.25
CHEMBL419214 IC50 = 7130.0 nM 5.15
CHEMBL115284 IC50 > 10000.0 nM -
CHEMBL325697 IC50 > 10000.0 nM -
CHEMBL114204 IC50 > 10000.0 nM -
CHEMBL114824 IC50 > 10000.0 nM -
CHEMBL114940 IC50 > 10000.0 nM -
CHEMBL111918 IC50 > 10000.0 nM -
CHEMBL325674 IC50 > 10000.0 nM -
CHEMBL324479 IC50 > 10000.0 nM -
CHEMBL607 MEPERIDINE IC50 > 10000.0 nM -
CHEMBL333843 IC50 > 10000.0 nM -
CHEMBL114327 IC50 > 10000.0 nM -
CHEMBL115549 IC50 > 10000.0 nM -
CHEMBL324471 IC50 > 10000.0 nM -
CHEMBL420500 IC50 > 10000.0 nM -
CHEMBL113811 IC50 > 10000.0 nM -
CHEMBL369475 CODEINE MONOHYDRATE IC50 > 10000.0 nM -
CHEMBL115076 IC50 > 10000.0 nM -
CHEMBL325874 IC50 > 10000.0 nM -
CHEMBL326538 IC50 > 10000.0 nM -
CHEMBL324257 IC50 > 10000.0 nM -
CHEMBL324170 IC50 > 10000.0 nM -
CHEMBL332697 IC50 > 10000.0 nM -
CHEMBL324142 IC50 > 10000.0 nM -