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Assay Detail

CHEMBL674514

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

Binding
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
14
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebellum
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design of C-terminal peptide antagonists of endothelin: structure-activity relationships of ET-[1621, D-His16]
Doherty A, Cody W, He J, DePue P, Leonard D, Dunbar J, Hill K, Flynn M, Reynolds E
Bioorg Med Chem Lett (1993) 3 : 497 -502
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.07 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL146155 1 7.52
CHEMBL327350 1 7.46
CHEMBL313984 1 7.30
CHEMBL86814 2 6.85
CHEMBL147908 1 5.89
CHEMBL2370070 1 5.40
CHEMBL315658 1 5.03
CHEMBL289687 1 5.00
CHEMBL273391 1 4.73
CHEMBL87724 1 -
CHEMBL312916 1 -
CHEMBL330489 1 -
CHEMBL432091 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL146155 IC50 = 30.0 nM 7.52
CHEMBL327350 IC50 = 35.0 nM 7.46
CHEMBL313984 IC50 = 50.0 nM 7.30
CHEMBL86814 IC50 = 140.0 nM 6.85
CHEMBL147908 IC50 = 1300.0 nM 5.89
CHEMBL86814 IC50 = 3300.0 nM 5.48
CHEMBL2370070 IC50 = 4000.0 nM 5.40
CHEMBL315658 IC50 = 9300.0 nM 5.03
CHEMBL289687 IC50 = 10000.0 nM 5.00
CHEMBL273391 IC50 = 18500.0 nM 4.73
CHEMBL87724 IC50 > 10000.0 nM -
CHEMBL312916 IC50 > 10000.0 nM -
CHEMBL330489 IC50 > 10000.0 nM -
CHEMBL432091 IC50 > 50000.0 nM -