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Compound Detail

CHEMBL288458

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COC(=O)[C@H](CC(C)C)NC(C#N)[C@@H](N)Cc1ccccc1

Basic Information

ChEMBL ID CHEMBL288458
Phase Preclinical
Structure Type MOL
InChI Key DVRZRQXKGNGTPD-KSCSMHSMSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

303.4
MW (Da)
1.63
ALogP
5
HBA
2
HBD
88.1
PSA (Ų)
0.71
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H25N3O2
MW 303.41
Aromatic Rings 1
Heavy Atoms 22
NP-Likeness -0.10

Activity Summary

IC50 2 meas. best 5.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aminopeptidase N
CHEMBL1907
IC50 5.62 5.62 2400.0 1
Aminopeptidase B
CHEMBL2836
IC50 4.3 4.3 50000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aminopeptidase N IC50 = 2400.0 nM 5.62 Inhibition of Aminopeptidase M. -
Aminopeptidase B IC50 = 50000.0 nM 4.3 Inhibition of Aminopeptidase B in murine L-cells by Aoyagi method. -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(01)80519-9 Aminopeptidase B 1
- 10.1016/S0960-894X(01)80519-9 Aminopeptidase N 1

Data from ChEMBL 36 via Core Engine