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Assay Detail

CHEMBL678455

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

Binding
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.
13
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

-Carbamate butenolide analogues as potent ETA selective endothelin receptor antagonists and prodrugs
Patt WC, Reisdorph BR, Repine JT, Doherty AM, Haleen SJ, Walker DM, Welch KM, Flynn MA, Hallak H, Reyner EL, Stewart BH
Bioorg Med Chem Lett (1997) 7 : 297 -302
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.78 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8981 PD-156707 1 6.32
CHEMBL103846 1 5.89
CHEMBL319452 1 5.75
CHEMBL316523 1 5.60
CHEMBL51530 1 5.34
CHEMBL320839 1 -
CHEMBL276173 1 -
CHEMBL450337 1 -
CHEMBL322920 3 -
CHEMBL103501 1 -
CHEMBL320183 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8981 PD-156707 IC50 = 480.0 nM 6.32
CHEMBL103846 IC50 = 1300.0 nM 5.89
CHEMBL319452 IC50 = 1800.0 nM 5.75
CHEMBL316523 IC50 = 2500.0 nM 5.60
CHEMBL51530 IC50 = 4550.0 nM 5.34
CHEMBL320839 IC50 > 2500.0 nM -
CHEMBL276173 IC50 > 25000.0 nM -
CHEMBL450337 IC50 > 2500.0 nM -
CHEMBL322920 IC50 > 2500.0 nM -
CHEMBL103501 IC50 > 2500.0 nM -
CHEMBL322920 IC50 > 2500.0 nM -
CHEMBL320183 IC50 > 2500.0 nM -
CHEMBL322920 IC50 > 2500.0 nM -