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Assay Detail

CHEMBL4013053

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

Binding
Inhibition of human C-terminal His-tagged acid ceramidase variant 1 expressed in HEK293 cells using fluorogenic substrate Rbm-14-12 preincubated for 30 mins followed by substrate addition measured after 1 hr by fluorogenic assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
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 31 8.17 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4093029 1 9.05
CHEMBL4103207 1 9.00
CHEMBL4084295 1 8.89
CHEMBL4092051 1 8.68
CHEMBL4062592 1 8.66
CHEMBL4075447 1 8.62
CHEMBL4065362 1 8.62
CHEMBL4100744 1 8.60
CHEMBL4071239 1 8.39
CHEMBL4075028 1 8.33
CHEMBL66205 1 8.18
CHEMBL4096883 1 8.15
CHEMBL4089655 1 8.15
CHEMBL4076230 1 8.08
CHEMBL4101140 1 8.07
CHEMBL4095461 1 8.00
CHEMBL4094489 1 7.86
CHEMBL4075846 1 7.83
CHEMBL460499 CARMOFUR 2.0 1 7.68
CHEMBL4099796 1 7.68
CHEMBL4076865 1 7.65
CHEMBL4075647 1 7.53
CHEMBL4077199 1 7.25
CHEMBL4090927 1 7.17
CHEMBL4081779 1 -
CHEMBL4067955 1 -
CHEMBL4092056 1 -
CHEMBL4075570 1 -
CHEMBL4084302 1 -
CHEMBL4103996 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4093029 IC50 = 0.9 nM 9.05
CHEMBL4103207 IC50 = 1.0 nM 9.00
CHEMBL4084295 IC50 = 1.3 nM 8.89
CHEMBL4092051 IC50 = 2.1 nM 8.68
CHEMBL4062592 IC50 = 2.2 nM 8.66
CHEMBL4075447 IC50 = 2.4 nM 8.62
CHEMBL4065362 IC50 = 2.4 nM 8.62
CHEMBL4100744 IC50 = 2.5 nM 8.60
CHEMBL4071239 IC50 = 4.1 nM 8.39
CHEMBL4075028 IC50 = 4.7 nM 8.33
CHEMBL66205 IC50 = 6.6 nM 8.18
CHEMBL4096883 IC50 = 7.0 nM 8.15
CHEMBL4089655 IC50 = 7.0 nM 8.15
CHEMBL4076230 IC50 = 8.3 nM 8.08
CHEMBL4101140 IC50 = 8.5 nM 8.07
CHEMBL4095461 IC50 = 9.9 nM 8.00
CHEMBL4094489 IC50 = 13.9 nM 7.86
CHEMBL4075846 IC50 = 14.8 nM 7.83
CHEMBL460499 CARMOFUR IC50 = 20.7 nM 7.68
CHEMBL4099796 IC50 = 21.0 nM 7.68
CHEMBL4076865 IC50 = 22.5 nM 7.65
CHEMBL4075647 IC50 = 29.3 nM 7.53
CHEMBL4077199 IC50 = 55.9 nM 7.25
CHEMBL4090927 IC50 = 68.4 nM 7.17
CHEMBL4081779 IC50 > 10000.0 nM -
CHEMBL4067955 IC50 > 10000.0 nM -
CHEMBL4092056 IC50 > 10000.0 nM -
CHEMBL4075570 IC50 > 10000.0 nM -
CHEMBL4084302 IC50 > 10000.0 nM -
CHEMBL4103996 IC50 > 10000.0 nM -
CHEMBL4086076 IC50 > 10000.0 nM -