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Assay Detail

CHEMBL679705

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Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL ↗
63
Total Activities
63
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Endothelin-1 receptor (CHEMBL4130) ↗
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Potent and selective ET-A antagonists. 1. Syntheses and structure-activity relationships of N-(6-(2-(aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide derivatives.
Morimoto H, Shimadzu H, Kushiyama E, Kawanishi H, Hosaka T, Kawase Y, Yasuda K, Kikkawa K, Yamauchi-Kohno R, Yamada K.
J Med Chem (2001) 44 : 3355 -3368
PubMed 11585441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 63 8.70 10.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL332922 — — 1 10.89
CHEMBL114380 — — 1 10.82
CHEMBL115724 — — 1 10.74
CHEMBL115333 — — 1 10.55
CHEMBL177173 — — 1 10.44
CHEMBL114700 — — 1 10.29
CHEMBL114964 — — 1 10.23
CHEMBL321242 — — 1 9.96
CHEMBL112141 — — 1 9.80
CHEMBL177924 — — 1 9.80
CHEMBL116281 — — 1 9.54
CHEMBL114660 — — 1 9.43
CHEMBL112162 — — 1 9.19
CHEMBL111934 — — 1 9.12
CHEMBL114933 — — 1 9.07
CHEMBL441277 — — 1 9.05
CHEMBL116220 — — 1 9.00
CHEMBL112134 — — 1 9.00
CHEMBL324246 — — 1 8.92
CHEMBL115230 — — 1 8.92
CHEMBL115017 — — 1 8.85
CHEMBL175931 — — 1 8.72
CHEMBL114201 — — 1 8.72
CHEMBL334263 — — 1 8.55
CHEMBL112502 — — 1 8.54
CHEMBL114683 — — 1 8.51
CHEMBL116002 — — 1 8.47
CHEMBL442031 — — 1 8.21
CHEMBL175616 BOSENTAN SODIUM — 1 8.12
CHEMBL114105 — — 1 8.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL332922 — IC50 = 0.013 nM 10.89
CHEMBL114380 — IC50 = 0.015 nM 10.82
CHEMBL115724 — IC50 = 0.018 nM 10.74
CHEMBL115333 — IC50 = 0.028 nM 10.55
CHEMBL177173 — IC50 = 0.036 nM 10.44
CHEMBL114700 — IC50 = 0.051 nM 10.29
CHEMBL114964 — IC50 = 0.059 nM 10.23
CHEMBL321242 — IC50 = 0.11 nM 9.96
CHEMBL112141 — IC50 = 0.16 nM 9.80
CHEMBL177924 — IC50 = 0.16 nM 9.80
CHEMBL116281 — IC50 = 0.29 nM 9.54
CHEMBL114660 — IC50 = 0.37 nM 9.43
CHEMBL112162 — IC50 = 0.64 nM 9.19
CHEMBL111934 — IC50 = 0.76 nM 9.12
CHEMBL114933 — IC50 = 0.86 nM 9.07
CHEMBL441277 — IC50 = 0.89 nM 9.05
CHEMBL116220 — IC50 = 1.0 nM 9.00
CHEMBL112134 — IC50 = 1.0 nM 9.00
CHEMBL324246 — IC50 = 1.2 nM 8.92
CHEMBL115230 — IC50 = 1.2 nM 8.92
CHEMBL115017 — IC50 = 1.4 nM 8.85
CHEMBL175931 — IC50 = 1.9 nM 8.72
CHEMBL114201 — IC50 = 1.9 nM 8.72
CHEMBL334263 — IC50 = 2.8 nM 8.55
CHEMBL112502 — IC50 = 2.9 nM 8.54
CHEMBL114683 — IC50 = 3.1 nM 8.51
CHEMBL116002 — IC50 = 3.4 nM 8.47
CHEMBL442031 — IC50 = 6.2 nM 8.21
CHEMBL175616 BOSENTAN SODIUM IC50 = 7.5 nM 8.12
CHEMBL114105 — IC50 = 8.8 nM 8.06
CHEMBL420501 — IC50 = 9.9 nM 8.00
CHEMBL331580 — IC50 = 12.0 nM 7.92
CHEMBL326160 — IC50 = 15.2 nM 7.82
CHEMBL177373 — IC50 = 22.0 nM 7.66
CHEMBL324943 — IC50 = 24.5 nM 7.61
CHEMBL326105 — IC50 = 25.8 nM 7.59
CHEMBL113927 — IC50 = 39.4 nM 7.41
CHEMBL114704 — IC50 = 45.4 nM 7.34
CHEMBL113888 — IC50 = 51.4 nM 7.29
CHEMBL111876 — IC50 = 65.0 nM 7.19
CHEMBL114985 — IC50 = 92.0 nM 7.04
CHEMBL430515 — IC50 = 93.5 nM 7.03
CHEMBL115951 — IC50 = 160.0 nM 6.80
CHEMBL321226 — IC50 = 170.0 nM 6.77
CHEMBL175523 — IC50 = 0.0085 nM -
CHEMBL115133 — IC50 > 100.0 nM -
CHEMBL353317 — IC50 < 0.001 nM -
CHEMBL112531 — IC50 < 0.001 nM -
CHEMBL116046 — IC50 < 0.001 nM -
CHEMBL116108 — IC50 < 0.001 nM -