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Assay Detail

CHEMBL4048266

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ADMET
Inhibition of human SPP expressed in human U2OS cells using EGFP-labeled EnvSigSeq-SEAP as substrate after 24 hrs by Hoechst staining based high content imaging assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of the First Potent, Selective, and Orally Bioavailable Signal Peptide Peptidase-Like 2a (SPPL2a) Inhibitor Displaying Pronounced Immunomodulatory Effects In Vivo.
Velcicky J, Bodendorf U, Rigollier P, Epple R, Beisner DR, Guerini D, Smith P, Liu B, Feifel R, Wipfli P, Aichholz R, Couttet P, Dix I, Widmer T, Wen B, Brandl T.
J Med Chem (2018) 61 : 865 -880
PubMed 29359565 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.37 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL392068 1 7.30
CHEMBL4069936 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL392068 IC50 = 50.0 nM 7.30
CHEMBL4069936 IC50 = 3730.0 nM 5.43