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Assay Detail

CHEMBL4013057

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

Binding
Inhibition of acid ceramidase in human A375 cells using fluorogenic substrate Rbm-14-12 preincubated for 2 hrs followed by substrate addition measured after 3 hrs by fluorogenic assay
5
Total Activities
5
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

Acid ceramidase (CHEMBL5463)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pharmacophore Identification and Scaffold Exploration to Discover Novel, Potent, and Chemically Stable Inhibitors of Acid Ceramidase in Melanoma Cells.
Ortega JA, Arencibia JM, La Sala G, Borgogno M, Bauer I, Bono L, Braccia C, Armirotti A, Girotto S, Ganesan A, De Vivo M.
J Med Chem (2017) 60 : 5800 -5815
PubMed 28603987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.42 7.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4100744 1 7.12
CHEMBL460499 CARMOFUR 2.0 1 6.72
CHEMBL4075846 1 6.30
CHEMBL4094489 1 6.01
CHEMBL4076865 1 5.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4100744 IC50 = 75.6 nM 7.12
CHEMBL460499 CARMOFUR IC50 = 190.8 nM 6.72
CHEMBL4075846 IC50 = 505.3 nM 6.30
CHEMBL4094489 IC50 = 966.9 nM 6.01
CHEMBL4076865 IC50 = 1061.5 nM 5.97