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Assay Detail

CHEMBL4667908

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

Binding
Inhibition of SPP in human U2OS cells cotransfected with EGFP-labeled EnvSigSeq-SEAP incubated for 24 hrs by Hoechst staining based Cellomics ArrayScan analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.
Velcicky J,Mathison CJN,Nikulin V,Pflieger D,Epple R,Azimioara M,Cow C,Michellys PY,Rigollier P,Beisner DR,Bodendorf U,Guerini D,Liu B,Wen B,Zaharevitz S,Brandl T
ACS Med Chem Lett (2019) 10 : 887 -892
PubMed 31223443 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.50 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4759048 1 6.19
CHEMBL4753654 1 5.82
CHEMBL4740837 1 5.75
CHEMBL4762492 1 5.70
CHEMBL4789381 1 5.50
CHEMBL4759943 1 5.48
CHEMBL4792187 1 5.41
CHEMBL4762370 1 5.09
CHEMBL4741014 1 4.58
CHEMBL4798232 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4759048 IC50 = 650.0 nM 6.19
CHEMBL4753654 IC50 = 1500.0 nM 5.82
CHEMBL4740837 IC50 = 1800.0 nM 5.75
CHEMBL4762492 IC50 = 2000.0 nM 5.70
CHEMBL4789381 IC50 = 3200.0 nM 5.50
CHEMBL4759943 IC50 = 3300.0 nM 5.48
CHEMBL4792187 IC50 = 3900.0 nM 5.41
CHEMBL4762370 IC50 = 8100.0 nM 5.09
CHEMBL4741014 IC50 = 26000.0 nM 4.58
CHEMBL4798232 IC50 > 32000.0 nM -