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Assay Detail

CHEMBL671389

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Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL ↗
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebellum
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Endothelin receptor type B (CHEMBL3949) ↗
Type SINGLE PROTEIN
Organism Sus scrofa

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 58 5.74 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9334 — — 1 7.40
CHEMBL269141 — — 1 7.39
CHEMBL266337 — — 1 6.74
CHEMBL9194 ATRASENTAN 3.0 1 6.72
CHEMBL268433 — — 1 6.55
CHEMBL9283 — — 1 6.51
CHEMBL268864 — — 1 6.51
CHEMBL9488 — — 1 6.50
CHEMBL9313 — — 1 6.50
CHEMBL9141 — — 1 6.40
CHEMBL267279 — — 1 6.39
CHEMBL8923 — — 1 6.29
CHEMBL9502 — — 1 6.28
CHEMBL9139 — — 1 6.22
CHEMBL9050 — — 1 6.21
CHEMBL8911 — — 1 6.12
CHEMBL8736 — — 1 6.09
CHEMBL417972 — — 1 6.08
CHEMBL9342 — — 1 6.05
CHEMBL9119 — — 1 5.98
CHEMBL9223 — — 1 5.97
CHEMBL273476 — — 1 5.93
CHEMBL267761 — — 1 5.90
CHEMBL267695 — — 1 5.86
CHEMBL8925 — — 1 5.83
CHEMBL268432 — — 1 5.80
CHEMBL269108 — — 1 5.78
CHEMBL428504 — — 1 5.75
CHEMBL9495 — — 1 5.75
CHEMBL266354 — — 1 5.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9334 — IC50 = 40.0 nM 7.40
CHEMBL269141 — IC50 = 41.0 nM 7.39
CHEMBL266337 — IC50 = 184.0 nM 6.74
CHEMBL9194 ATRASENTAN IC50 = 191.0 nM 6.72
CHEMBL268433 — IC50 = 283.0 nM 6.55
CHEMBL9283 — IC50 = 306.0 nM 6.51
CHEMBL268864 — IC50 = 307.0 nM 6.51
CHEMBL9488 — IC50 = 315.0 nM 6.50
CHEMBL9313 — IC50 = 313.0 nM 6.50
CHEMBL9141 — IC50 = 398.0 nM 6.40
CHEMBL267279 — IC50 = 404.0 nM 6.39
CHEMBL8923 — IC50 = 515.0 nM 6.29
CHEMBL9502 — IC50 = 531.0 nM 6.28
CHEMBL9139 — IC50 = 598.0 nM 6.22
CHEMBL9050 — IC50 = 624.0 nM 6.21
CHEMBL8911 — IC50 = 750.0 nM 6.12
CHEMBL8736 — IC50 = 806.0 nM 6.09
CHEMBL417972 — IC50 = 834.0 nM 6.08
CHEMBL9342 — IC50 = 889.0 nM 6.05
CHEMBL9119 — IC50 = 1050.0 nM 5.98
CHEMBL9223 — IC50 = 1070.0 nM 5.97
CHEMBL273476 — IC50 = 1180.0 nM 5.93
CHEMBL267761 — IC50 = 1259.0 nM 5.90
CHEMBL267695 — IC50 = 1390.0 nM 5.86
CHEMBL8925 — IC50 = 1470.0 nM 5.83
CHEMBL268432 — IC50 = 1590.0 nM 5.80
CHEMBL269108 — IC50 = 1680.0 nM 5.78
CHEMBL428504 — IC50 = 1770.0 nM 5.75
CHEMBL9495 — IC50 = 1800.0 nM 5.75
CHEMBL266354 — IC50 = 1820.0 nM 5.74
CHEMBL266143 — IC50 = 2360.0 nM 5.63
CHEMBL9082 — IC50 = 2430.0 nM 5.61
CHEMBL266594 — IC50 = 2900.0 nM 5.54
CHEMBL428644 — IC50 = 3040.0 nM 5.52
CHEMBL427935 — IC50 = 3274.0 nM 5.49
CHEMBL9183 — IC50 = 3390.0 nM 5.47
CHEMBL8677 — IC50 = 3400.0 nM 5.47
CHEMBL266336 — IC50 = 3510.0 nM 5.46
CHEMBL266144 — IC50 = 3590.0 nM 5.45
CHEMBL9147 — IC50 = 3730.0 nM 5.43
CHEMBL8671 — IC50 = 3790.0 nM 5.42
CHEMBL8878 — IC50 = 3830.0 nM 5.42
CHEMBL9040 — IC50 = 4000.0 nM 5.40
CHEMBL9132 — IC50 = 4200.0 nM 5.38
CHEMBL8776 — IC50 = 5020.0 nM 5.30
CHEMBL275306 — IC50 = 4970.0 nM 5.30
CHEMBL9212 — IC50 = 5250.0 nM 5.28
CHEMBL417971 — IC50 = 6180.0 nM 5.21
CHEMBL9012 — IC50 = 7930.0 nM 5.10
CHEMBL268902 — IC50 = 8380.0 nM 5.08