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Assay Detail

CHEMBL844035

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

Binding
Inhibition of [3H]DPDPE binding to delta opioid receptor of guinea pig brain homogenate
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.
Kawasaki AM, Knapp RJ, Kramer TH, Walton A, Wire WS, Hashimoto S, Yamamura HI, Porreca F, Burks TF, Hruby VJ.
J Med Chem (1993) 36 : 750 -757
PubMed 8096246 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.78 9.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265241 1 9.32
CHEMBL438274 1 8.71
CHEMBL411557 DYNORPHIN A (1-17) 1 8.60
CHEMBL405618 ANALOG OF DYNORPHIN A 1 8.39
CHEMBL409793 1 8.18
CHEMBL438223 DYNORPHIN A (1-11) 1 8.16
CHEMBL411196 1 8.02
CHEMBL386722 1 7.51
CHEMBL444626 1 7.08
CHEMBL414494 1 7.06
CHEMBL384566 1 6.97
CHEMBL2371443 1 6.74
CHEMBL408497 1 6.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265241 IC50 = 0.475 nM 9.32
CHEMBL438274 IC50 = 1.93 nM 8.71
CHEMBL411557 DYNORPHIN A (1-17) IC50 = 2.54 nM 8.60
CHEMBL405618 ANALOG OF DYNORPHIN A IC50 = 4.07 nM 8.39
CHEMBL409793 IC50 = 6.54 nM 8.18
CHEMBL438223 DYNORPHIN A (1-11) IC50 = 6.99 nM 8.16
CHEMBL411196 IC50 = 9.6 nM 8.02
CHEMBL386722 IC50 = 31.2 nM 7.51
CHEMBL444626 IC50 = 82.5 nM 7.08
CHEMBL414494 IC50 = 86.3 nM 7.06
CHEMBL384566 IC50 = 107.0 nM 6.97
CHEMBL2371443 IC50 = 181.0 nM 6.74
CHEMBL408497 IC50 = 389.0 nM 6.41