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Assay Detail

CHEMBL673047

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Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Tissue Kidney
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Benzofuro[3,2-b]pyridines as mixed ET(A)/ET(B) and selective ET(B) endothelin receptor antagonists.
Mederski WW, Osswald M, Dorsch D, Christadler M, Schmitges CJ, Wilm C.
Bioorg Med Chem Lett (1999) 9 : 619 -622
PubMed 10098676 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.44 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL433700 1 8.44
CHEMBL155708 1 8.07
CHEMBL160768 1 7.89
CHEMBL349556 1 7.57
CHEMBL348407 1 7.39
CHEMBL156194 1 6.92
CHEMBL157742 1 6.92
CHEMBL347680 1 6.77
CHEMBL352241 1 6.70
CHEMBL156453 1 6.52
CHEMBL156404 1 6.37
CHEMBL422002 1 6.18
CHEMBL157827 1 5.89
CHEMBL158239 1 5.80
CHEMBL156539 1 5.72
CHEMBL158204 1 5.57
CHEMBL345380 1 5.52
CHEMBL155973 1 5.46
CHEMBL157763 1 5.28
CHEMBL156532 1 5.19
CHEMBL155937 1 5.17
CHEMBL160828 1 -
CHEMBL346926 1 -
CHEMBL280096 1 -
CHEMBL158123 1 -
CHEMBL156269 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL433700 IC50 = 3.6 nM 8.44
CHEMBL155708 IC50 = 8.6 nM 8.07
CHEMBL160768 IC50 = 13.0 nM 7.89
CHEMBL349556 IC50 = 27.0 nM 7.57
CHEMBL348407 IC50 = 41.0 nM 7.39
CHEMBL156194 IC50 = 120.0 nM 6.92
CHEMBL157742 IC50 = 120.0 nM 6.92
CHEMBL347680 IC50 = 170.0 nM 6.77
CHEMBL352241 IC50 = 200.0 nM 6.70
CHEMBL156453 IC50 = 300.0 nM 6.52
CHEMBL156404 IC50 = 430.0 nM 6.37
CHEMBL422002 IC50 = 660.0 nM 6.18
CHEMBL157827 IC50 = 1300.0 nM 5.89
CHEMBL158239 IC50 = 1600.0 nM 5.80
CHEMBL156539 IC50 = 1900.0 nM 5.72
CHEMBL158204 IC50 = 2700.0 nM 5.57
CHEMBL345380 IC50 = 3000.0 nM 5.52
CHEMBL155973 IC50 = 3500.0 nM 5.46
CHEMBL157763 IC50 = 5200.0 nM 5.28
CHEMBL156532 IC50 = 6400.0 nM 5.19
CHEMBL155937 IC50 = 6800.0 nM 5.17
CHEMBL160828 IC50 > 10000.0 nM -
CHEMBL346926 IC50 > 10000.0 nM -
CHEMBL280096 IC50 > 10000.0 nM -
CHEMBL158123 IC50 > 10000.0 nM -
CHEMBL156269 IC50 > 10000.0 nM -