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Assay Detail

CHEMBL845237

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

Binding
Inhibition of delta-selective antagonist binding to opioid receptor of mouse vas dferens
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Delta-type opioid receptor (CHEMBL3222)
Type SINGLE PROTEIN
Organism Mus musculus

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 14 6.85 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL405618 ANALOG OF DYNORPHIN A 1 8.04
CHEMBL438274 1 8.04
CHEMBL409793 1 7.60
CHEMBL438223 DYNORPHIN A (1-11) 1 7.54
CHEMBL411557 DYNORPHIN A (1-17) 1 7.40
CHEMBL265241 1 7.03
CHEMBL411196 1 5.39
CHEMBL2371443 1 5.38
CHEMBL415406 1 5.20
CHEMBL384566 1 -
CHEMBL386722 1 -
CHEMBL408497 1 -
CHEMBL414494 1 -
CHEMBL444626 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL405618 ANALOG OF DYNORPHIN A IC50 = 9.1 nM 8.04
CHEMBL438274 IC50 = 9.17 nM 8.04
CHEMBL409793 IC50 = 25.3 nM 7.60
CHEMBL438223 DYNORPHIN A (1-11) IC50 = 28.93 nM 7.54
CHEMBL411557 DYNORPHIN A (1-17) IC50 = 39.7 nM 7.40
CHEMBL265241 IC50 = 92.6 nM 7.03
CHEMBL411196 IC50 = 4100.0 nM 5.39
CHEMBL2371443 IC50 = 4180.0 nM 5.38
CHEMBL415406 IC50 = 6262.0 nM 5.20
CHEMBL384566 IC50 > 6000.0 nM -
CHEMBL386722 IC50 > 3000.0 nM -
CHEMBL408497 IC50 > 3000.0 nM -
CHEMBL414494 IC50 > 6000.0 nM -
CHEMBL444626 IC50 > 3000.0 nM -