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Assay Detail

CHEMBL679121

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Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL ↗
59
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Endothelin-1 receptor (CHEMBL4566) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722.
Winn M, von Geldern TW, Opgenorth TJ, Jae HS, Tasker AS, Boyd SA, Kester JA, Mantei RA, Bal R, Sorensen BK, Wu-Wong JR, Chiou WJ, Dixon DB, Novosad EI, Hernandez L, Marsh KC.
J Med Chem (1996) 39 : 1039 -1048
PubMed 8676339 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 59 7.19 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9334 — — 1 9.66
CHEMBL9194 ATRASENTAN 3.0 1 9.51
CHEMBL8923 — — 1 9.44
CHEMBL269141 — — 1 9.37
CHEMBL9488 — — 1 9.34
CHEMBL9313 — — 1 9.25
CHEMBL9283 — — 1 9.09
CHEMBL9502 — — 1 9.07
CHEMBL9139 — — 1 8.91
CHEMBL9119 — — 1 8.73
CHEMBL9223 — — 1 8.35
CHEMBL9162 — — 1 8.34
CHEMBL267695 — — 1 8.33
CHEMBL9050 — — 1 8.24
CHEMBL266594 — — 1 8.18
CHEMBL267279 — — 1 8.12
CHEMBL266337 — — 1 8.09
CHEMBL268864 — — 1 7.79
CHEMBL266354 — — 1 7.79
CHEMBL9141 — — 1 7.76
CHEMBL8736 — — 1 7.62
CHEMBL9212 — — 1 7.48
CHEMBL9342 — — 1 7.47
CHEMBL8911 — — 1 7.43
CHEMBL267761 — — 1 7.37
CHEMBL417972 — — 1 7.36
CHEMBL273476 — — 1 7.30
CHEMBL430084 — — 1 7.24
CHEMBL268433 — — 1 7.07
CHEMBL275306 — — 1 6.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9334 — IC50 = 0.22 nM 9.66
CHEMBL9194 ATRASENTAN IC50 = 0.31 nM 9.51
CHEMBL8923 — IC50 = 0.36 nM 9.44
CHEMBL269141 — IC50 = 0.43 nM 9.37
CHEMBL9488 — IC50 = 0.46 nM 9.34
CHEMBL9313 — IC50 = 0.56 nM 9.25
CHEMBL9283 — IC50 = 0.81 nM 9.09
CHEMBL9502 — IC50 = 0.85 nM 9.07
CHEMBL9139 — IC50 = 1.23 nM 8.91
CHEMBL9119 — IC50 = 1.88 nM 8.73
CHEMBL9223 — IC50 = 4.45 nM 8.35
CHEMBL9162 — IC50 = 4.62 nM 8.34
CHEMBL267695 — IC50 = 4.71 nM 8.33
CHEMBL9050 — IC50 = 5.78 nM 8.24
CHEMBL266594 — IC50 = 6.63 nM 8.18
CHEMBL267279 — IC50 = 7.61 nM 8.12
CHEMBL266337 — IC50 = 8.2 nM 8.09
CHEMBL268864 — IC50 = 16.2 nM 7.79
CHEMBL266354 — IC50 = 16.2 nM 7.79
CHEMBL9141 — IC50 = 17.2 nM 7.76
CHEMBL8736 — IC50 = 23.8 nM 7.62
CHEMBL9212 — IC50 = 32.9 nM 7.48
CHEMBL9342 — IC50 = 34.2 nM 7.47
CHEMBL8911 — IC50 = 37.0 nM 7.43
CHEMBL267761 — IC50 = 43.0 nM 7.37
CHEMBL417972 — IC50 = 44.0 nM 7.36
CHEMBL273476 — IC50 = 50.2 nM 7.30
CHEMBL430084 — IC50 = 58.0 nM 7.24
CHEMBL268433 — IC50 = 85.0 nM 7.07
CHEMBL275306 — IC50 = 108.0 nM 6.97
CHEMBL9040 — IC50 = 106.0 nM 6.97
CHEMBL9495 — IC50 = 112.0 nM 6.95
CHEMBL9132 — IC50 = 121.0 nM 6.92
CHEMBL9082 — IC50 = 163.0 nM 6.79
CHEMBL428504 — IC50 = 171.0 nM 6.77
CHEMBL9147 — IC50 = 178.0 nM 6.75
CHEMBL8878 — IC50 = 220.0 nM 6.66
CHEMBL428644 — IC50 = 350.0 nM 6.46
CHEMBL8925 — IC50 = 396.0 nM 6.40
CHEMBL268902 — IC50 = 437.0 nM 6.36
CHEMBL9189 — IC50 = 520.0 nM 6.28
CHEMBL267483 — IC50 = 684.0 nM 6.17
CHEMBL9183 — IC50 = 682.0 nM 6.17
CHEMBL266144 — IC50 = 765.0 nM 6.12
CHEMBL269108 — IC50 = 769.0 nM 6.11
CHEMBL8671 — IC50 = 781.0 nM 6.11
CHEMBL268432 — IC50 = 794.0 nM 6.10
CHEMBL266143 — IC50 = 900.0 nM 6.05
CHEMBL8677 — IC50 = 885.0 nM 6.05
CHEMBL8776 — IC50 = 1080.0 nM 5.97