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Compound Detail

CHEMBL37281

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COC(=O)C1CCCN1C(=O)[C@H](CC(C)C)N[C@H](C#N)[C@@H](N)Cc1ccccc1

Basic Information

ChEMBL ID CHEMBL37281
Phase Preclinical
Structure Type MOL
InChI Key XFIFYSDGOLDFKE-GURQWTFNSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

400.5
MW (Da)
1.62
ALogP
6
HBA
2
HBD
108.5
PSA (Ų)
0.61
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H32N4O3
MW 400.52
Aromatic Rings 1
Heavy Atoms 29
NP-Likeness -0.29

Activity Summary

IC50 2 meas. best 5.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aminopeptidase N
CHEMBL1907
IC50 5.47 5.47 3400.0 1
Aminopeptidase B
CHEMBL2836
IC50 4.85 4.85 14000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aminopeptidase N IC50 = 3400.0 nM 5.47 Inhibition of Aminopeptidase M. -
Aminopeptidase B IC50 = 14000.0 nM 4.85 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