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Assay Detail

CHEMBL675450

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Functional
pA2 value towards endothelin receptor A was determined as functional ETA antagonism
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Endothelin antagonists: evaluation of 2,1,3-benzothiadiazole as a methylendioxyphenyl bioisoster.
Mederski WW, Osswald M, Dorsch D, Anzali S, Christadler M, Schmitges CJ, Wilm C.
Bioorg Med Chem Lett (1998) 8 : 17 -22
PubMed 9871621 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 7.87 8.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL48907 1 8.50
CHEMBL25438 PD-156707 SODIUM 1 7.60
CHEMBL303902 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL48907 Kd = 3.162 nM 8.50
CHEMBL25438 PD-156707 SODIUM Kd = 25.12 nM 7.60
CHEMBL303902 Kd = 31.62 nM 7.50