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Assay Detail

CHEMBL1912403

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

Binding
Inhibition of GCS activity in human A549 cells assessed as amount of GM1 on the cell membrane after 72 hrs by FL-CTB-based fluorescent microscopy
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A549
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Ceramide glucosyltransferase (CHEMBL2063)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a new class of glucosylceramide synthase inhibitors.
Koltun E, Richards S, Chan V, Nachtigall J, Du H, Noson K, Galan A, Aay N, Hanel A, Harrison A, Zhang J, Won KA, Tam D, Qian F, Wang T, Finn P, Ogilvie K, Rosen J, Mohan R, Larson C, Lamb P, Nuss J, Kearney P.
Bioorg Med Chem Lett (2011) 21 : 6773 -6777
PubMed 21974949 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.02 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1911818 1 9.52
CHEMBL1911678 1 8.70
CHEMBL1911679 1 8.70
CHEMBL1911817 1 8.70
CHEMBL1911829 1 8.40
CHEMBL1911827 1 8.30
CHEMBL1911830 1 7.92
CHEMBL1911819 1 7.89
CHEMBL1911820 1 7.30
CHEMBL574645 1 4.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1911818 IC50 = 0.3 nM 9.52
CHEMBL1911678 IC50 = 2.0 nM 8.70
CHEMBL1911679 IC50 = 2.0 nM 8.70
CHEMBL1911817 IC50 = 2.0 nM 8.70
CHEMBL1911829 IC50 = 4.0 nM 8.40
CHEMBL1911827 IC50 = 5.0 nM 8.30
CHEMBL1911830 IC50 = 12.0 nM 7.92
CHEMBL1911819 IC50 = 13.0 nM 7.89
CHEMBL1911820 IC50 = 50.0 nM 7.30
CHEMBL574645 IC50 = 16500.0 nM 4.78