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Assay Detail

CHEMBL4200192

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

Binding
Inhibition of human SMS2 using C6-NBD-ceramide and DMPC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by HPLC analysis
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Discovery of 4-Benzyloxybenzo[ d]isoxazole-3-amine Derivatives as Highly Selective and Orally Efficacious Human Sphingomyelin Synthase 2 Inhibitors that Reduce Chronic Inflammation in db/ db Mice.
Mo M, Yang J, Jiang XC, Cao Y, Fei J, Chen Y, Qi X, Chu Y, Zhou L, Ye D.
J Med Chem (2018) 61 : 8241 -8254
PubMed 30074791 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 6.33 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4203399 1 7.05
CHEMBL4204352 1 7.00
CHEMBL4214637 1 7.00
CHEMBL4207944 1 6.96
CHEMBL4202436 1 6.82
CHEMBL4206801 1 6.80
CHEMBL4205965 1 6.72
CHEMBL4211357 1 6.62
CHEMBL4217275 1 6.62
CHEMBL4202973 1 6.57
CHEMBL4212291 1 6.47
CHEMBL4217676 1 6.33
CHEMBL4216327 1 6.28
CHEMBL4211679 1 6.17
CHEMBL4210244 1 6.13
CHEMBL4203583 1 6.02
CHEMBL4217259 1 5.92
CHEMBL4212845 1 5.89
CHEMBL4205041 1 5.82
CHEMBL4215175 1 5.77
CHEMBL4204126 1 5.36
CHEMBL4207927 1 5.04
CHEMBL4208270 1 -
CHEMBL4215792 1 -
CHEMBL4207322 1 -
CHEMBL4208469 1 -
CHEMBL4208447 1 -
CHEMBL4212831 1 -
CHEMBL4212313 1 -
CHEMBL4216023 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4203399 IC50 = 90.0 nM 7.05
CHEMBL4204352 IC50 = 100.0 nM 7.00
CHEMBL4214637 IC50 = 100.0 nM 7.00
CHEMBL4207944 IC50 = 110.0 nM 6.96
CHEMBL4202436 IC50 = 150.0 nM 6.82
CHEMBL4206801 IC50 = 160.0 nM 6.80
CHEMBL4205965 IC50 = 190.0 nM 6.72
CHEMBL4211357 IC50 = 240.0 nM 6.62
CHEMBL4217275 IC50 = 240.0 nM 6.62
CHEMBL4202973 IC50 = 270.0 nM 6.57
CHEMBL4212291 IC50 = 340.0 nM 6.47
CHEMBL4217676 IC50 = 470.0 nM 6.33
CHEMBL4216327 IC50 = 520.0 nM 6.28
CHEMBL4211679 IC50 = 670.0 nM 6.17
CHEMBL4210244 IC50 = 740.0 nM 6.13
CHEMBL4203583 IC50 = 960.0 nM 6.02
CHEMBL4217259 IC50 = 1200.0 nM 5.92
CHEMBL4212845 IC50 = 1300.0 nM 5.89
CHEMBL4205041 IC50 = 1500.0 nM 5.82
CHEMBL4215175 IC50 = 1700.0 nM 5.77
CHEMBL4204126 IC50 = 4400.0 nM 5.36
CHEMBL4207927 IC50 = 9100.0 nM 5.04
CHEMBL4208270 IC50 > 10000.0 nM -
CHEMBL4215792 IC50 > 10000.0 nM -
CHEMBL4207322 IC50 > 10000.0 nM -
CHEMBL4208469 IC50 > 10000.0 nM -
CHEMBL4208447 IC50 > 10000.0 nM -
CHEMBL4212831 IC50 > 10000.0 nM -
CHEMBL4212313 IC50 > 10000.0 nM -
CHEMBL4216023 IC50 > 10000.0 nM -
CHEMBL4216548 IC50 > 10000.0 nM -