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Assay Detail

CHEMBL3614737

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

Binding
Inhibition of sphingomyelin synthase-1 (unknown origin) expressed in HeLa cells using C6-NBD-Cer and DMPC as substrate after 2 hrs by fluorescent HPLC-based analysis
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Discovery, synthesis and biological evaluation of 2-(4-(N-phenethylsulfamoyl)phenoxy)acetamides (SAPAs) as novel sphingomyelin synthase 1 inhibitors.
Li YL, Qi XY, Jiang H, Deng XD, Dong YP, Ding TB, Zhou L, Men P, Chu Y, Wang RX, Jiang XC, Ye DY.
Bioorg Med Chem (2015) 23 : 6173 -6184
PubMed 26314925 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.06 5.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3613983 1 5.68
CHEMBL3613975 1 5.28
CHEMBL3612087 1 5.23
CHEMBL3613987 1 5.18
CHEMBL3613984 1 5.09
CHEMBL3613995 1 5.04
CHEMBL3613988 1 4.98
CHEMBL3613990 1 4.85
CHEMBL3613986 1 4.83
CHEMBL3613985 1 4.81
CHEMBL3613982 1 4.64
CHEMBL3613976 1 -
CHEMBL3613977 1 -
CHEMBL3613978 1 -
CHEMBL3613979 1 -
CHEMBL3613980 1 -
CHEMBL3613981 1 -
CHEMBL3613989 1 -
CHEMBL3613991 1 -
CHEMBL3613996 1 -
CHEMBL3613997 1 -
CHEMBL3613992 1 -
CHEMBL3613993 1 -
CHEMBL3613994 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3613983 IC50 = 2100.0 nM 5.68
CHEMBL3613975 IC50 = 5200.0 nM 5.28
CHEMBL3612087 IC50 = 5900.0 nM 5.23
CHEMBL3613987 IC50 = 6600.0 nM 5.18
CHEMBL3613984 IC50 = 8100.0 nM 5.09
CHEMBL3613995 IC50 = 9200.0 nM 5.04
CHEMBL3613988 IC50 = 10500.0 nM 4.98
CHEMBL3613990 IC50 = 14200.0 nM 4.85
CHEMBL3613986 IC50 = 14700.0 nM 4.83
CHEMBL3613985 IC50 = 15600.0 nM 4.81
CHEMBL3613982 IC50 = 23100.0 nM 4.64
CHEMBL3613976 IC50 > 100000.0 nM -
CHEMBL3613977 IC50 > 100000.0 nM -
CHEMBL3613978 IC50 > 100000.0 nM -
CHEMBL3613979 IC50 > 50000.0 nM -
CHEMBL3613980 IC50 > 100000.0 nM -
CHEMBL3613981 IC50 > 50000.0 nM -
CHEMBL3613989 IC50 > 50000.0 nM -
CHEMBL3613991 IC50 > 100000.0 nM -
CHEMBL3613996 IC50 > 100000.0 nM -
CHEMBL3613997 IC50 = 219000.0 nM -
CHEMBL3613992 IC50 > 100000.0 nM -
CHEMBL3613993 IC50 > 100000.0 nM -
CHEMBL3613994 IC50 > 100000.0 nM -