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Assay Detail

CHEMBL670642

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

Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous 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. 1. Syntheses and structure-activity relationships of N-(6-(2-(aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide derivatives.
Morimoto H, Shimadzu H, Kushiyama E, Kawanishi H, Hosaka T, Kawase Y, Yasuda K, Kikkawa K, Yamauchi-Kohno R, Yamada K.
J Med Chem (2001) 44 : 3355 -3368
PubMed 11585441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.47 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL367445 1 8.42
CHEMBL175501 1 8.15
CHEMBL176272 1 7.55
CHEMBL369489 1 7.42
CHEMBL177979 1 6.66
CHEMBL368796 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL367445 IC50 = 3.8 nM 8.42
CHEMBL175501 IC50 = 7.0 nM 8.15
CHEMBL176272 IC50 = 28.0 nM 7.55
CHEMBL369489 IC50 = 38.0 nM 7.42
CHEMBL177979 IC50 = 220.0 nM 6.66
CHEMBL368796 IC50 = 240.0 nM 6.62