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Assay Detail

CHEMBL670634

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

Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

1-benzyl-3-thioaryl-2-carboxyindoles as potent non-peptide endothelin antagonists
Bunker AM, Edmunds JJ, Berryman KA, Walker DM, Flynn MA, Welch KM, Doherty AM
Bioorg Med Chem Lett (1996) 6 : 1367 -1370
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.92 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28563 1 6.77
CHEMBL28920 1 6.64
CHEMBL27732 1 6.55
CHEMBL287169 1 6.42
CHEMBL283598 1 6.38
CHEMBL283858 1 6.38
CHEMBL29147 1 6.31
CHEMBL281451 1 6.16
CHEMBL27617 1 6.12
CHEMBL28188 1 6.06
CHEMBL285368 1 5.96
CHEMBL416570 1 5.96
CHEMBL285380 1 5.80
CHEMBL28779 1 5.35
CHEMBL282398 1 5.17
CHEMBL283648 1 5.13
CHEMBL28948 1 4.82
CHEMBL282426 1 4.54
CHEMBL27911 1 -
CHEMBL435568 1 -
CHEMBL10143 1 -
CHEMBL416019 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28563 IC50 = 170.0 nM 6.77
CHEMBL28920 IC50 = 230.0 nM 6.64
CHEMBL27732 IC50 = 280.0 nM 6.55
CHEMBL287169 IC50 = 380.0 nM 6.42
CHEMBL283598 IC50 = 420.0 nM 6.38
CHEMBL283858 IC50 = 420.0 nM 6.38
CHEMBL29147 IC50 = 490.0 nM 6.31
CHEMBL281451 IC50 = 690.0 nM 6.16
CHEMBL27617 IC50 = 760.0 nM 6.12
CHEMBL28188 IC50 = 870.0 nM 6.06
CHEMBL285368 IC50 = 1100.0 nM 5.96
CHEMBL416570 IC50 = 1100.0 nM 5.96
CHEMBL285380 IC50 = 1600.0 nM 5.80
CHEMBL28779 IC50 = 4500.0 nM 5.35
CHEMBL282398 IC50 = 6700.0 nM 5.17
CHEMBL283648 IC50 = 7400.0 nM 5.13
CHEMBL28948 IC50 = 15000.0 nM 4.82
CHEMBL282426 IC50 = 29000.0 nM 4.54
CHEMBL27911 IC50 > 25000.0 nM -
CHEMBL435568 IC50 > 2500.0 nM -
CHEMBL10143 IC50 > 100000.0 nM -
CHEMBL416019 IC50 > 25000.0 nM -