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Assay Detail

CHEMBL693384

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

Functional
Inhibitory activity against ET 1 induced calcium increase in human Girardi heart cells
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type heart
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and structure-activity relationships of 2-substituted D-tryptophan-containing peptidic endothelin receptor antagonists: importance of the C-2 substituent of the D-tryptophan residue for endothelin A and B receptor subtype selectivity.
Fukami T, Yamakawa T, Niiyama K, Kojima H, Amano Y, Kanda F, Ozaki S, Fukuroda T, Ihara M, Yano M, Ishikawa K.
J Med Chem (1996) 39 : 2313 -2330
PubMed 8691426 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.93 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL306123 1 8.40
CHEMBL2304015 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL306123 IC50 = 4.0 nM 8.40
CHEMBL2304015 IC50 = 35.0 nM 7.46