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Assay Detail

CHEMBL2167350

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

Binding
Inhibition of GCS assessed as amount of UDP glucose after 3 hrs by Fluorometry analysis
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Ceramide glucosyltransferase (CHEMBL2063)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and characterization of an inhibitor of glucosylceramide synthase.
Richards S, Larson CJ, Koltun ES, Hanel A, Chan V, Nachtigall J, Harrison A, Aay N, Du H, Arcalas A, Galan A, Zhang J, Zhang W, Won KA, Tam D, Qian F, Wang T, Finn P, Ogilvie K, Rosen J, Aoyama R, Plonowski A, Cancilla B, Bentzien F, Yakes M, Mohan R, Lamb P, Nuss J, Kearney P.
J Med Chem (2012) 55 : 4322 -4335
PubMed 22497444 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.72 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2163838 1 8.70
CHEMBL2163828 1 8.70
CHEMBL2163821 1 8.70
CHEMBL2163827 1 8.52
CHEMBL2163826 1 8.52
CHEMBL2163823 1 8.52
CHEMBL2163825 1 8.40
CHEMBL2163839 1 8.40
CHEMBL2163834 1 8.15
CHEMBL1911678 1 8.05
CHEMBL2163829 1 8.00
CHEMBL2163833 1 8.00
CHEMBL2163832 1 7.92
CHEMBL2163824 1 7.80
CHEMBL1911679 1 7.80
CHEMBL2163836 1 7.70
CHEMBL574645 1 7.05
CHEMBL2163830 1 7.05
CHEMBL2163835 1 6.82
CHEMBL2163831 1 6.80
CHEMBL2163837 1 6.72
CHEMBL2163822 1 6.58
CHEMBL1029 MIGLUSTAT 4.0 1 4.66
CHEMBL2163819 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2163838 IC50 = 2.0 nM 8.70
CHEMBL2163828 IC50 = 2.0 nM 8.70
CHEMBL2163821 IC50 = 2.0 nM 8.70
CHEMBL2163827 IC50 = 3.0 nM 8.52
CHEMBL2163826 IC50 = 3.0 nM 8.52
CHEMBL2163823 IC50 = 3.0 nM 8.52
CHEMBL2163825 IC50 = 4.0 nM 8.40
CHEMBL2163839 IC50 = 4.0 nM 8.40
CHEMBL2163834 IC50 = 7.0 nM 8.15
CHEMBL1911678 IC50 = 9.0 nM 8.05
CHEMBL2163829 IC50 = 10.0 nM 8.00
CHEMBL2163833 IC50 = 10.0 nM 8.00
CHEMBL2163832 IC50 = 12.0 nM 7.92
CHEMBL2163824 IC50 = 16.0 nM 7.80
CHEMBL1911679 IC50 = 16.0 nM 7.80
CHEMBL2163836 IC50 = 20.0 nM 7.70
CHEMBL574645 IC50 = 90.0 nM 7.05
CHEMBL2163830 IC50 = 90.0 nM 7.05
CHEMBL2163835 IC50 = 150.0 nM 6.82
CHEMBL2163831 IC50 = 160.0 nM 6.80
CHEMBL2163837 IC50 = 190.0 nM 6.72
CHEMBL2163822 IC50 = 260.0 nM 6.58
CHEMBL1029 MIGLUSTAT IC50 = 22000.0 nM 4.66
CHEMBL2163819 IC50 > 4000.0 nM -