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Assay Detail

CHEMBL674890

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Binding
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Endothelin receptor type B (CHEMBL1785)
Type SINGLE PROTEIN
Organism Homo sapiens

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
Ki 3 7.04 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1627022 1 7.39
CHEMBL112531 1 6.89
CHEMBL175616 BOSENTAN SODIUM 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1627022 Ki = 41.0 nM 7.39
CHEMBL112531 Ki = 130.0 nM 6.89
CHEMBL175616 BOSENTAN SODIUM Ki = 140.0 nM 6.85