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Assay Detail

CHEMBL754444

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

Binding
Compound was evaluated for the inhibition of [3H]DSLET([[3H]D-Ser2,Leu5,Thr6]enkephalin binding to Opioid receptor delta 1 in rat brain homogenates.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL269)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological activities of dynorphin A analogues with opioid antagonist properties.
Gairin JE, Mazarguil H, Alvinerie P, Saint-Pierre S, Meunier JC, Cros J.
J Med Chem (1986) 29 : 1913 -1917
PubMed 2876099 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.16 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2373009 1 8.27
CHEMBL2028997 1 8.20
CHEMBL384584 1 8.13
CHEMBL438223 DYNORPHIN A (1-11) 1 7.97
CHEMBL2373013 1 6.87
CHEMBL2373014 1 6.52
CHEMBL2373012 1 6.25
CHEMBL2373008 1 6.20
CHEMBL3037891 1 5.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2373009 Ki = 5.43 nM 8.27
CHEMBL2028997 Ki = 6.3 nM 8.20
CHEMBL384584 Ki = 7.47 nM 8.13
CHEMBL438223 DYNORPHIN A (1-11) Ki = 10.66 nM 7.97
CHEMBL2373013 Ki = 134.0 nM 6.87
CHEMBL2373014 Ki = 303.0 nM 6.52
CHEMBL2373012 Ki = 561.0 nM 6.25
CHEMBL2373008 Ki = 631.0 nM 6.20
CHEMBL3037891 Ki = 1035.0 nM 5.99