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Assay Detail

CHEMBL678559

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Binding
Compound was evaluated for its binding affinity towards human Endothelin A receptor
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
Murugesan N, Tellew JE, Gu Z, Kunst BL, Fadnis L, Cornelius LA, Baska RA, Yang Y, Beyer SM, Monshizadegan H, Dickinson KE, Panchal B, Valentine MT, Chong S, Morrison RA, Carlson KE, Powell JR, Moreland S, Barrish JC, Kowala MC, Macor JE.
J Med Chem (2002) 45 : 3829 -3835
PubMed 12190306 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.33 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24461 1 8.85
CHEMBL11706 BMS-248360 1 8.72
CHEMBL126755 1 7.41
CHEMBL1513 IRBESARTAN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24461 Ki = 1.4 nM 8.85
CHEMBL11706 BMS-248360 Ki = 1.9 nM 8.72
CHEMBL126755 Ki = 39.0 nM 7.41
CHEMBL1513 IRBESARTAN Ki > 0.0001 nM -