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Compound Detail

CHEMBL4084295

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O=C(NCCCCc1ccccc1)n1nnc2ncccc21

Basic Information

ChEMBL ID CHEMBL4084295
Phase Preclinical
Structure Type MOL
InChI Key OBGZSFAJXABWPH-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

295.4
MW (Da)
2.41
ALogP
5
HBA
1
HBD
72.7
PSA (Ų)
0.73
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H17N5O
MW 295.35
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -1.13

Activity Summary

IC50 1 meas. best 8.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acid ceramidase
CHEMBL5463
IC50 8.89 8.89 1.3 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.03333 hr -
T1/2 2.0 hr -
T1/2 0.08333 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acid ceramidase IC50 = 1.3 nM 8.89 Inhibition of human C-terminal His-tagged acid ceramidase variant 1 expressed in... 28603987

Literature References

PubMed DOI Target Context # Activities
28603987 10.1021/acs.jmedchem.7b00472 No relevant target 2
28603987 10.1021/acs.jmedchem.7b00472 Acid ceramidase 1
28603987 10.1021/acs.jmedchem.7b00472 Plasma 1

Data from ChEMBL 36 via Core Engine