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Assay Detail

CHEMBL749744

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Binding
Binding affinity against cloned human Opioid receptor mu 1 using [125I]FK33824 as radioligand
25
Total Activities
25
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

New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability.
Plobeck N, Delorme D, Wei ZY, Yang H, Zhou F, Schwarz P, Gawell L, Gagnon H, Pelcman B, Schmidt R, Yue SY, Walpole C, Brown W, Zhou E, Labarre M, Payza K, St-Onge S, Kamassah A, Morin PE, Projean D, Ducharme J, Roberts E.
J Med Chem (2000) 43 : 3878 -3894
PubMed 11052793 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.89 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25230 1 8.68
CHEMBL340724 1 6.73
CHEMBL434817 1 6.55
CHEMBL13470 SNC-80 1 6.50
CHEMBL123679 1 6.31
CHEMBL127434 1 6.21
CHEMBL129420 1 6.20
CHEMBL125734 1 6.11
CHEMBL127761 1 6.11
CHEMBL126819 1 5.99
CHEMBL126366 1 5.83
CHEMBL2112649 1 5.65
CHEMBL127507 1 5.64
CHEMBL125248 1 5.62
CHEMBL126223 1 5.57
CHEMBL127638 1 5.34
CHEMBL24035 1 5.30
CHEMBL125742 1 5.28
CHEMBL128006 1 5.27
CHEMBL340834 1 5.25
CHEMBL338436 1 5.16
CHEMBL128005 1 5.15
CHEMBL338980 1 5.09
CHEMBL124642 1 -
CHEMBL126382 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25230 IC50 = 2.1 nM 8.68
CHEMBL340724 IC50 = 185.0 nM 6.73
CHEMBL434817 IC50 = 284.0 nM 6.55
CHEMBL13470 SNC-80 IC50 = 320.0 nM 6.50
CHEMBL123679 IC50 = 486.0 nM 6.31
CHEMBL127434 IC50 = 620.0 nM 6.21
CHEMBL129420 IC50 = 632.0 nM 6.20
CHEMBL125734 IC50 = 777.0 nM 6.11
CHEMBL127761 IC50 = 785.0 nM 6.11
CHEMBL126819 IC50 = 1016.0 nM 5.99
CHEMBL126366 IC50 = 1477.0 nM 5.83
CHEMBL2112649 IC50 = 2222.0 nM 5.65
CHEMBL127507 IC50 = 2290.0 nM 5.64
CHEMBL125248 IC50 = 2398.0 nM 5.62
CHEMBL126223 IC50 = 2677.0 nM 5.57
CHEMBL127638 IC50 = 4538.0 nM 5.34
CHEMBL24035 IC50 = 5064.0 nM 5.30
CHEMBL125742 IC50 = 5290.0 nM 5.28
CHEMBL128006 IC50 = 5330.0 nM 5.27
CHEMBL340834 IC50 = 5647.0 nM 5.25
CHEMBL338436 IC50 = 6970.0 nM 5.16
CHEMBL128005 IC50 = 7092.0 nM 5.15
CHEMBL338980 IC50 = 8150.0 nM 5.09
CHEMBL124642 IC50 > 10000.0 nM -
CHEMBL126382 IC50 > 10000.0 nM -