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Assay Detail

CHEMBL677270

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

Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type GH
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
IC50 3 7.67 8.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1627022 1 8.08
CHEMBL1627023 1 7.51
CHEMBL112531 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1627022 IC50 = 8.3 nM 8.08
CHEMBL1627023 IC50 = 31.0 nM 7.51
CHEMBL112531 IC50 = 38.0 nM 7.42