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Assay Detail

CHEMBL5133256

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

Toxicity
Inhibition of human ERG expressed in HEK cells by voltage clamp assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors.
Taoka BM, Wu WL, Hao J, Dolmaski M, Wang H, Levorse D, Orth P, Hyde LA, Smith B, Michener MS, Kennedy ME, Parker EM, Cumming JN.
Bioorg Med Chem Lett (2022) 56 : 128463 -128463
PubMed 34838652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.09 5.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3301601 VERUBECESTAT 3.0 1 5.66
CHEMBL5174392 1 5.24
CHEMBL3937515 1 5.09
CHEMBL5198665 1 4.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3301601 VERUBECESTAT IC50 = 2200.0 nM 5.66
CHEMBL5174392 IC50 = 5800.0 nM 5.24
CHEMBL3937515 IC50 = 8100.0 nM 5.09
CHEMBL5198665 IC50 = 44000.0 nM 4.36