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Assay Detail

CHEMBL752841

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Binding
Agonist potency was measured using GTP gamma-[35S] binding assay
22
Total Activities
22
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

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
EC50 22 7.45 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25230 1 9.92
CHEMBL13470 SNC-80 1 8.44
CHEMBL129420 1 8.44
CHEMBL126819 1 8.16
CHEMBL127761 1 8.15
CHEMBL127434 1 7.98
CHEMBL125734 1 7.75
CHEMBL24035 1 7.48
CHEMBL338980 1 7.44
CHEMBL125742 1 7.38
CHEMBL2112649 1 7.35
CHEMBL126223 1 7.30
CHEMBL340834 1 7.27
CHEMBL126366 1 7.26
CHEMBL128005 1 7.11
CHEMBL128006 1 6.95
CHEMBL126382 1 6.92
CHEMBL127638 1 6.73
CHEMBL124642 1 6.68
CHEMBL434817 1 6.56
CHEMBL127507 1 6.52
CHEMBL339621 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25230 EC50 = 0.12 nM 9.92
CHEMBL13470 SNC-80 EC50 = 3.67 nM 8.44
CHEMBL129420 EC50 = 3.6 nM 8.44
CHEMBL126819 EC50 = 6.86 nM 8.16
CHEMBL127761 EC50 = 7.1 nM 8.15
CHEMBL127434 EC50 = 10.4 nM 7.98
CHEMBL125734 EC50 = 18.0 nM 7.75
CHEMBL24035 EC50 = 33.0 nM 7.48
CHEMBL338980 EC50 = 36.5 nM 7.44
CHEMBL125742 EC50 = 42.0 nM 7.38
CHEMBL2112649 EC50 = 44.9 nM 7.35
CHEMBL126223 EC50 = 50.0 nM 7.30
CHEMBL340834 EC50 = 53.3 nM 7.27
CHEMBL126366 EC50 = 54.6 nM 7.26
CHEMBL128005 EC50 = 78.1 nM 7.11
CHEMBL128006 EC50 = 113.0 nM 6.95
CHEMBL126382 EC50 = 121.0 nM 6.92
CHEMBL127638 EC50 = 187.0 nM 6.73
CHEMBL124642 EC50 = 211.0 nM 6.68
CHEMBL434817 EC50 = 273.0 nM 6.56
CHEMBL127507 EC50 = 303.0 nM 6.52
CHEMBL339621 EC50 = 635.0 nM 6.20