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Assay Detail

CHEMBL884719

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

Binding
Inhibitory concentration against endothelin receptor type A
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 Expert

Target

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

Publication

Designed multiple ligands. An emerging drug discovery paradigm.
Morphy R, Rankovic Z.
J Med Chem (2005) 48 : 6523 -6543
PubMed 16220969 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.25 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11706 BMS-248360 1 8.72
CHEMBL539423 SPARSENTAN 4.0 1 8.03
CHEMBL383581 EDONENTAN 2.0 1 8.00
CHEMBL1513 IRBESARTAN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11706 BMS-248360 Ki = 1.9 nM 8.72
CHEMBL539423 SPARSENTAN Ki = 9.3 nM 8.03
CHEMBL383581 EDONENTAN Ki = 10.0 nM 8.00
CHEMBL1513 IRBESARTAN Ki > 10000.0 nM -