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Assay Detail

CHEMBL753543

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Functional
Antagonistic activity against human cloned Opioid receptor delta 1 using DPDPE in [35S]GTP-gamma-S, assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.
Thomas JB, Atkinson RN, Vinson NA, Catanzaro JL, Perretta CL, Fix SE, Mascarella SW, Rothman RB, Xu H, Dersch CM, Cantrell BE, Zimmerman DM, Carroll FI.
J Med Chem (2003) 46 : 3127 -3137
PubMed 12825951 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 7.81 7.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL485832 GUANIDINONALTRINDOLE 1 7.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL485832 GUANIDINONALTRINDOLE Kd = 15.49 nM 7.81