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Assay Detail

CHEMBL4381549

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

Binding
Inhibition of recombinant human acid sphingomyelinase (His62 to Pro628 residues) using NBD-sphingomyelin as substrate after 30 mins by fluorescence based assay
10
Total Activities
10
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

Target

Sphingomyelin phosphodiesterase (CHEMBL2760)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Potent, Selective, and Direct Acid Sphingomyelinase Inhibitors with Antidepressant Activity.
Yang K, Yu J, Nong K, Wang Y, Niu A, Chen W, Dong J, Wang J.
J Med Chem (2020) 63 : 961 -974
PubMed 31944697 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.57 6.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4517596 1 6.44
CHEMBL4167681 1 6.05
CHEMBL4464068 1 5.66
CHEMBL4465034 1 5.47
CHEMBL4551503 1 5.47
CHEMBL4462822 1 5.42
CHEMBL4471880 1 5.39
CHEMBL4449978 1 5.37
CHEMBL4464771 1 5.31
CHEMBL4464117 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4517596 IC50 = 360.0 nM 6.44
CHEMBL4167681 IC50 = 890.0 nM 6.05
CHEMBL4464068 IC50 = 2200.0 nM 5.66
CHEMBL4465034 IC50 = 3380.0 nM 5.47
CHEMBL4551503 IC50 = 3370.0 nM 5.47
CHEMBL4462822 IC50 = 3830.0 nM 5.42
CHEMBL4471880 IC50 = 4090.0 nM 5.39
CHEMBL4449978 IC50 = 4250.0 nM 5.37
CHEMBL4464771 IC50 = 4930.0 nM 5.31
CHEMBL4464117 IC50 = 8070.0 nM 5.09