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Assay Detail

CHEMBL5246773

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

Binding
Binding affinity to recombinant human ETA
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Targeted Drugs for Treatment of Pulmonary Arterial Hypertension: Past, Present, and Future Perspectives.
Zheng W, Wang Z, Jiang X, Zhao Q, Shen J.
J Med Chem (2020) 63 : 15153 -15186
PubMed 33314936 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.94 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL957 BOSENTAN 4.0 1 7.10
CHEMBL4438132 1 6.10
CHEMBL4525321 1 5.82
CHEMBL5272983 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL957 BOSENTAN IC50 = 80.0 nM 7.10
CHEMBL4438132 IC50 = 800.0 nM 6.10
CHEMBL4525321 IC50 = 1500.0 nM 5.82
CHEMBL5272983 IC50 = 18000.0 nM 4.75