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Assay Detail

CHEMBL671685

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Binding
Inhibitory concentration was evaluated by measuring the binding affinity at the Endothelin B receptor in rat cerebellar membranes
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebellum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Endothelin receptor type B (CHEMBL4631)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design of a potent combined pseudopeptide endothelin-A/endothelin-B receptor antagonist, Ac-DBhg16-Leu-Asp-Ile-[NMe]Ile-Trp21 (PD 156252): examination of its pharmacokinetic and spectral properties.
Cody WL, He JX, Reily MD, Haleen SJ, Walker DM, Reyner EL, Stewart BH, Doherty AM.
J Med Chem (1997) 40 : 2228 -2240
PubMed 9216842 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.36 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL262993 1 7.82
CHEMBL328942 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL262993 IC50 = 15.0 nM 7.82
CHEMBL328942 IC50 = 130.0 nM 6.89