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Assay Detail

CHEMBL749999

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

Binding
Binding affinity at delta opioid receptor in guinea pig brain by [3H]c[D-Pen2, p-Cl-Phe4, D-Pen5]-enkephalin displacement.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.
Meyer JP, Collins N, Lung FD, Davis P, Zalewska T, Porreca F, Yamamura HI, Hruby VJ.
J Med Chem (1994) 37 : 3910 -3917
PubMed 7966152 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.43 7.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112652 1 7.86
CHEMBL2370618 1 7.80
CHEMBL411338 1 7.73
CHEMBL216640 1 7.59
CHEMBL2370627 1 6.63
CHEMBL2370629 1 6.62
CHEMBL2370622 1 6.61
CHEMBL2370611 1 6.50
CHEMBL404929 1 6.41
CHEMBL2370612 1 6.14
CHEMBL2370626 1 6.00
CHEMBL2111843 1 5.99
CHEMBL2370610 1 5.87
CHEMBL414713 1 5.86
CHEMBL374268 1 5.76
CHEMBL263509 1 5.72
CHEMBL2370628 1 5.70
CHEMBL2369128 1 5.66
CHEMBL2370631 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112652 IC50 = 13.9 nM 7.86
CHEMBL2370618 IC50 = 15.9 nM 7.80
CHEMBL411338 IC50 = 18.6 nM 7.73
CHEMBL216640 IC50 = 25.5 nM 7.59
CHEMBL2370627 IC50 = 232.0 nM 6.63
CHEMBL2370629 IC50 = 242.0 nM 6.62
CHEMBL2370622 IC50 = 245.0 nM 6.61
CHEMBL2370611 IC50 = 319.0 nM 6.50
CHEMBL404929 IC50 = 390.0 nM 6.41
CHEMBL2370612 IC50 = 717.0 nM 6.14
CHEMBL2370626 IC50 = 1000.0 nM 6.00
CHEMBL2111843 IC50 = 1030.0 nM 5.99
CHEMBL2370610 IC50 = 1360.0 nM 5.87
CHEMBL414713 IC50 = 1370.0 nM 5.86
CHEMBL374268 IC50 = 1740.0 nM 5.76
CHEMBL263509 IC50 = 1908.0 nM 5.72
CHEMBL2370628 IC50 = 2000.0 nM 5.70
CHEMBL2369128 IC50 = 2190.0 nM 5.66
CHEMBL2370631 IC50 = 2340.0 nM 5.63