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Assay Detail

CHEMBL682967

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

Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Endothelin-1 receptor (CHEMBL252)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bis-sulfonamides as endothelin receptor antagonists.
Boss C, Bolli MH, Weller T, Fischli W, Clozel M.
Bioorg Med Chem Lett (2003) 13 : 951 -954
PubMed 12617928 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 6.48 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL172297 1 7.85
CHEMBL367958 1 7.72
CHEMBL367444 1 7.66
CHEMBL177802 1 7.35
CHEMBL368617 1 7.32
CHEMBL172071 1 7.30
CHEMBL368738 1 7.29
CHEMBL172030 1 7.19
CHEMBL367443 1 7.11
CHEMBL171950 1 7.10
CHEMBL177538 1 7.09
CHEMBL276949 1 7.07
CHEMBL368107 1 6.94
CHEMBL176749 1 6.92
CHEMBL369676 1 6.85
CHEMBL174413 1 6.73
CHEMBL176997 1 6.58
CHEMBL172029 1 6.31
CHEMBL368528 1 6.24
CHEMBL172759 1 6.23
CHEMBL367275 1 6.14
CHEMBL175268 1 5.98
CHEMBL174781 1 5.88
CHEMBL277275 1 5.88
CHEMBL367274 1 5.86
CHEMBL366872 1 5.80
CHEMBL174547 1 5.73
CHEMBL366628 1 5.66
CHEMBL368945 1 5.66
CHEMBL366627 1 5.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL172297 IC50 = 14.0 nM 7.85
CHEMBL367958 IC50 = 19.0 nM 7.72
CHEMBL367444 IC50 = 22.0 nM 7.66
CHEMBL177802 IC50 = 45.0 nM 7.35
CHEMBL368617 IC50 = 48.0 nM 7.32
CHEMBL172071 IC50 = 50.0 nM 7.30
CHEMBL368738 IC50 = 51.0 nM 7.29
CHEMBL172030 IC50 = 64.0 nM 7.19
CHEMBL367443 IC50 = 77.0 nM 7.11
CHEMBL171950 IC50 = 80.0 nM 7.10
CHEMBL177538 IC50 = 82.0 nM 7.09
CHEMBL276949 IC50 = 86.0 nM 7.07
CHEMBL368107 IC50 = 116.0 nM 6.94
CHEMBL176749 IC50 = 119.0 nM 6.92
CHEMBL369676 IC50 = 140.0 nM 6.85
CHEMBL174413 IC50 = 185.0 nM 6.73
CHEMBL176997 IC50 = 261.0 nM 6.58
CHEMBL172029 IC50 = 487.0 nM 6.31
CHEMBL368528 IC50 = 582.0 nM 6.24
CHEMBL172759 IC50 = 587.0 nM 6.23
CHEMBL367275 IC50 = 724.0 nM 6.14
CHEMBL175268 IC50 = 1050.0 nM 5.98
CHEMBL174781 IC50 = 1320.0 nM 5.88
CHEMBL277275 IC50 = 1317.0 nM 5.88
CHEMBL367274 IC50 = 1385.0 nM 5.86
CHEMBL366872 IC50 = 1591.0 nM 5.80
CHEMBL174547 IC50 = 1850.0 nM 5.73
CHEMBL366628 IC50 = 2193.0 nM 5.66
CHEMBL368945 IC50 = 2190.0 nM 5.66
CHEMBL366627 IC50 = 2770.0 nM 5.56
CHEMBL367017 IC50 = 2838.0 nM 5.55
CHEMBL176418 IC50 = 4900.0 nM 5.31
CHEMBL173201 IC50 = 5115.0 nM 5.29
CHEMBL172441 IC50 = 8390.0 nM 5.08