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Assay Detail

CHEMBL677309

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

Functional
Functional inhibition of ET-1 induced [Ca2+] increase in human neuroblastoma-derived SK-N-MC cells, which express Endothelin A receptor
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type SK-N-MC
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis of 2-substituted d-tryptophan-containing peptide derivatives with endothelin receptor antagonist activity
Fukami T, Yamakawa T, Kojima H, Amano Y, Ihara M, Yano M, Ishikawa K
Bioorg Med Chem Lett (1995) 5 : 1483 -1488
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.51 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284250 1 7.80
CHEMBL431124 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284250 IC50 = 16.0 nM 7.80
CHEMBL431124 IC50 = 6100.0 nM 5.21