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Assay Detail

CHEMBL2346137

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

Binding
Inhibition of rat recombinant acid ceramidase expressed in human HEK293 cells using N-lauroylceramide as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by LC/MS analysis
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acid ceramidase (CHEMBL2331070)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of a new class of highly potent inhibitors of acid ceramidase: synthesis and structure-activity relationship (SAR).
Pizzirani D, Pagliuca C, Realini N, Branduardi D, Bottegoni G, Mor M, Bertozzi F, Scarpelli R, Piomelli D, Bandiera T.
J Med Chem (2013) 56 : 3518 -3530
PubMed 23614460 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 6.88 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2333064 1 8.40
CHEMBL2333062 1 8.15
CHEMBL2333053 1 8.15
CHEMBL2333033 1 7.92
CHEMBL2333054 1 7.92
CHEMBL2333048 1 7.89
CHEMBL2333055 1 7.80
CHEMBL2333050 1 7.75
CHEMBL2333056 1 7.70
CHEMBL2333052 1 7.68
CHEMBL460499 CARMOFUR 2.0 1 7.54
CHEMBL2333060 1 7.34
CHEMBL2333042 1 7.29
CHEMBL2333049 1 7.28
CHEMBL2333051 1 7.21
CHEMBL2333032 1 7.17
CHEMBL2333041 1 6.83
CHEMBL2333040 1 6.75
CHEMBL2333061 1 6.55
CHEMBL2333059 1 6.49
CHEMBL2333035 1 6.38
CHEMBL2333065 1 6.37
CHEMBL2333063 1 6.33
CHEMBL2333034 1 6.13
CHEMBL2333038 1 6.06
CHEMBL2333036 1 5.96
CHEMBL2333039 1 5.85
CHEMBL2333031 1 5.84
CHEMBL2333058 1 5.68
CHEMBL2333044 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2333064 IC50 = 4.0 nM 8.40
CHEMBL2333062 IC50 = 7.0 nM 8.15
CHEMBL2333053 IC50 = 7.0 nM 8.15
CHEMBL2333033 IC50 = 12.0 nM 7.92
CHEMBL2333054 IC50 = 12.0 nM 7.92
CHEMBL2333048 IC50 = 13.0 nM 7.89
CHEMBL2333055 IC50 = 16.0 nM 7.80
CHEMBL2333050 IC50 = 18.0 nM 7.75
CHEMBL2333056 IC50 = 20.0 nM 7.70
CHEMBL2333052 IC50 = 21.0 nM 7.68
CHEMBL460499 CARMOFUR IC50 = 29.0 nM 7.54
CHEMBL2333060 IC50 = 46.0 nM 7.34
CHEMBL2333042 IC50 = 51.0 nM 7.29
CHEMBL2333049 IC50 = 53.0 nM 7.28
CHEMBL2333051 IC50 = 61.0 nM 7.21
CHEMBL2333032 IC50 = 67.0 nM 7.17
CHEMBL2333041 IC50 = 147.0 nM 6.83
CHEMBL2333040 IC50 = 177.0 nM 6.75
CHEMBL2333061 IC50 = 283.0 nM 6.55
CHEMBL2333059 IC50 = 325.0 nM 6.49
CHEMBL2333035 IC50 = 417.0 nM 6.38
CHEMBL2333065 IC50 = 426.0 nM 6.37
CHEMBL2333063 IC50 = 464.0 nM 6.33
CHEMBL2333034 IC50 = 733.0 nM 6.13
CHEMBL2333038 IC50 = 875.0 nM 6.06
CHEMBL2333036 IC50 = 1100.0 nM 5.96
CHEMBL2333039 IC50 = 1400.0 nM 5.85
CHEMBL2333031 IC50 = 1460.0 nM 5.84
CHEMBL2333058 IC50 = 2100.0 nM 5.68
CHEMBL2333044 IC50 = 3400.0 nM 5.47
CHEMBL2333037 IC50 = 5500.0 nM 5.26
CHEMBL2333057 IC50 = 8500.0 nM 5.07
CHEMBL2333043 IC50 - -
CHEMBL2333045 IC50 - -
CHEMBL2333046 IC50 - -
CHEMBL2333047 IC50 - -
CHEMBL2331572 IC50 - -