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Assay Detail

CHEMBL5381577

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

Toxicity
Inhibition of human ERG tail current by plate-based planar patch clamp method
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Toxicity
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery of a Potent and Orally Bioavailable Zwitterionic Series of Selective Estrogen Receptor Degrader-Antagonists.
Scott JS, Stead D, Barlaam B, Breed J, Carbajo RJ, Chiarparin E, Cureton N, Davey PRJ, Fisher DI, Gangl ET, Grebe T, Greenwood RD, Hande S, Hatoum-Mokdad H, Hughes SJ, Hunt TA, Johnson T, Kavanagh SL, Klinowska TCM, Larner CJB, Lawson M, Lister AS, Longmire D, Marden S, McGuire TM, McMillan C, McMurray L, Morrow CJ, Nissink JWM, Moss TA, O'Donovan DH, Polanski R, Stokes S, Thakur K, Trueman D, Truman C, Tucker MJ, Wang H, Whalley N, Wu D, Wu Y, Yang B, Yang W.
J Med Chem (2023) 66 : 2918 -2945
PubMed 36727211 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.27 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5400637 1 5.82
CHEMBL5398790 1 5.44
CHEMBL5423660 1 5.42
CHEMBL5424734 1 5.39
CHEMBL5407684 1 5.35
CHEMBL5432698 1 5.34
CHEMBL5421791 1 5.29
CHEMBL5413311 1 5.28
CHEMBL5399407 1 5.27
CHEMBL5427353 1 5.24
CHEMBL5424508 1 5.17
CHEMBL5427839 1 5.16
CHEMBL5424726 1 5.00
CHEMBL5394023 1 4.92
CHEMBL4868243 1 4.89
CHEMBL5436976 1 -
CHEMBL5432663 1 -
CHEMBL5404810 1 -
CHEMBL5430566 1 -
CHEMBL5440088 1 -
CHEMBL5426983 1 -
CHEMBL5426160 1 -
CHEMBL5420450 1 -
CHEMBL5408358 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5400637 IC50 = 1500.0 nM 5.82
CHEMBL5398790 IC50 = 3600.0 nM 5.44
CHEMBL5423660 IC50 = 3800.0 nM 5.42
CHEMBL5424734 IC50 = 4100.0 nM 5.39
CHEMBL5407684 IC50 = 4500.0 nM 5.35
CHEMBL5432698 IC50 = 4600.0 nM 5.34
CHEMBL5421791 IC50 = 5100.0 nM 5.29
CHEMBL5413311 IC50 = 5300.0 nM 5.28
CHEMBL5399407 IC50 = 5400.0 nM 5.27
CHEMBL5427353 IC50 = 5700.0 nM 5.24
CHEMBL5424508 IC50 = 6700.0 nM 5.17
CHEMBL5427839 IC50 = 7000.0 nM 5.16
CHEMBL5424726 IC50 = 10000.0 nM 5.00
CHEMBL5394023 IC50 = 12000.0 nM 4.92
CHEMBL4868243 IC50 = 13000.0 nM 4.89
CHEMBL5436976 IC50 > 40000.0 nM -
CHEMBL5432663 IC50 > 40000.0 nM -
CHEMBL5404810 IC50 > 40000.0 nM -
CHEMBL5430566 IC50 > 40000.0 nM -
CHEMBL5440088 IC50 > 40000.0 nM -
CHEMBL5426983 IC50 > 40000.0 nM -
CHEMBL5426160 IC50 > 40000.0 nM -
CHEMBL5420450 IC50 > 40000.0 nM -
CHEMBL5408358 IC50 > 40000.0 nM -