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Compound Detail

CHEMBL1243372

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N#C[C@@H]1CCCN1C(=O)[C@@H](N)CCCN1Cc2ccccc2C1=O

Basic Information

ChEMBL ID CHEMBL1243372
Phase Preclinical
Structure Type MOL
InChI Key HGEQTKWTBCNJEW-HOCLYGCPSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

326.4
MW (Da)
1.26
ALogP
4
HBA
1
HBD
90.4
PSA (Ų)
0.88
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 C18H22N4O2
MW 326.40
Aromatic Rings 1
Heavy Atoms 24
NP-Likeness -0.30

Activity Summary

IC50 5 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 8.0 8.0 10.0 1
Prolyl endopeptidase FAP
CHEMBL4683
IC50 7.27 7.27 54.0 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 7.05 7.05 89.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 6.44 6.44 360.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 5.58 5.58 2600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20718420 10.1021/jm1002556 Prolyl endopeptidase FAP 1
20718420 10.1021/jm1002556 Dipeptidyl peptidase 8 1
20718420 10.1021/jm1002556 Dipeptidyl peptidase 9 1
20718420 10.1021/jm1002556 Dipeptidyl peptidase 2 1
20718420 10.1021/jm1002556 Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine