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Assay Detail

CHEMBL677447

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

Binding
Binding affinity towards Endothelin B receptor in human girardi heart cell membranes
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Heart
Cell Type heart
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Endothelin receptor type B (CHEMBL1785)
Type SINGLE PROTEIN
Organism Homo sapiens

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 6 7.94 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL73925 1 8.96
CHEMBL307936 1 8.40
CHEMBL306123 1 8.30
CHEMBL2304017 1 7.54
CHEMBL2304006 1 7.54
CHEMBL2304015 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL73925 IC50 = 1.1 nM 8.96
CHEMBL307936 IC50 = 4.0 nM 8.40
CHEMBL306123 IC50 = 5.0 nM 8.30
CHEMBL2304017 IC50 = 29.0 nM 7.54
CHEMBL2304006 IC50 = 29.0 nM 7.54
CHEMBL2304015 IC50 = 130.0 nM 6.89