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Assay Detail

CHEMBL674070

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

Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Endothelin-1 receptor (CHEMBL4566)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Potent and selective ET-A antagonists. 2. Discovery and evaluation of potent and water soluble N-(6-(2-(aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide derivatives.
Morimoto H, Ohashi N, Shimadzu H, Kushiyama E, Kawanishi H, Hosaka T, Kawase Y, Yasuda K, Kikkawa K, Yamauchi-Kohno R, Yamada K.
J Med Chem (2001) 44 : 3369 -3377
PubMed 11585442 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.98 10.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1627023 1 10.47
CHEMBL1627022 1 9.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1627023 IC50 = 0.034 nM 10.47
CHEMBL1627022 IC50 = 0.33 nM 9.48