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Assay Detail

CHEMBL679794

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

Binding
Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells
14
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Endothelin-1 receptor (CHEMBL252)
Type SINGLE PROTEIN
Organism Homo sapiens

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 5.64 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL313984 1 6.70
CHEMBL147908 1 6.19
CHEMBL2370070 1 6.12
CHEMBL146155 1 6.03
CHEMBL327350 1 5.93
CHEMBL86814 2 5.55
CHEMBL330489 1 5.10
CHEMBL315658 1 5.04
CHEMBL289687 1 5.02
CHEMBL273391 1 4.74
CHEMBL87724 1 -
CHEMBL312916 1 -
CHEMBL432091 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL313984 IC50 = 200.0 nM 6.70
CHEMBL147908 IC50 = 650.0 nM 6.19
CHEMBL2370070 IC50 = 750.0 nM 6.12
CHEMBL146155 IC50 = 930.0 nM 6.03
CHEMBL327350 IC50 = 1180.0 nM 5.93
CHEMBL86814 IC50 = 2800.0 nM 5.55
CHEMBL330489 IC50 = 8000.0 nM 5.10
CHEMBL315658 IC50 = 9100.0 nM 5.04
CHEMBL289687 IC50 = 9500.0 nM 5.02
CHEMBL273391 IC50 = 18400.0 nM 4.74
CHEMBL87724 IC50 > 10000.0 nM -
CHEMBL312916 IC50 > 10000.0 nM -
CHEMBL86814 IC50 > 10000.0 nM -
CHEMBL432091 IC50 > 50000.0 nM -