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Compound Detail

CHEMBL362018

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N#C[C@@H]1CCCN1C(=O)[C@@H](N)CC(=O)N1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1

Basic Information

ChEMBL ID CHEMBL362018
Phase Preclinical
Structure Type MOL
InChI Key BLQSJTWUUQHVBT-GOTSBHOMSA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

481.6
MW (Da)
2.43
ALogP
5
HBA
1
HBD
93.7
PSA (Ų)
0.68
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H29F2N5O2
MW 481.55
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.96

Activity Summary

IC50 6 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 8
CHEMBL4657
IC50 7.85 7.8167 14.0 3
Dipeptidyl peptidase 9
CHEMBL4793
IC50 7.28 7.28 53.0 1
Dipeptidyl peptidase 4
CHEMBL284
IC50 6.64 6.6 227.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15664838 10.1016/j.bmcl.2004.11.023 Dipeptidyl peptidase 4 1
15664838 10.1016/j.bmcl.2004.11.023 Dipeptidyl peptidase 8 1
15664838 10.1016/j.bmcl.2004.11.023 Dipeptidyl peptidase 2 1
15927466 10.1016/j.bmcl.2005.04.051 Dipeptidyl peptidase 4 1
15927466 10.1016/j.bmcl.2005.04.051 Dipeptidyl peptidase 8 1
15927466 10.1016/j.bmcl.2005.04.051 Dipeptidyl peptidase 2 1
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