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Compound Detail

CHEMBL390513

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N#Cc1ccc(N[C@@H]2CN[C@H](C(=O)N3CCSC3)C2)nc1

Basic Information

ChEMBL ID CHEMBL390513
Phase Preclinical
Structure Type MOL
InChI Key OFIKATYTXHUVBY-RYUDHWBXSA-N
4
Targets
5
Activities
1
Assay Types
2
PK Parameters
6
Publications
0
Known Names

Molecular Properties

303.4
MW (Da)
0.63
ALogP
6
HBA
2
HBD
81.0
PSA (Ų)
0.85
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H17N5OS
MW 303.39
Aromatic Rings 1
Heavy Atoms 21
NP-Likeness -1.68

Activity Summary

IC50 5 meas. best 7.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.59 7.59 25.4 2
Dipeptidyl peptidase 4
CHEMBL4653
IC50 7.52 7.52 30.4 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 5.43 5.43 3735.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 5.32 5.32 4756.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 83.9 % Rattus norvegicus
T1/2 5.27 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19217790 10.1016/j.bmc.2009.01.061 Dipeptidyl peptidase 4 2
19217790 10.1016/j.bmc.2009.01.061 Rattus norvegicus 2
17113301 10.1016/j.bmc.2006.10.059 Dipeptidyl peptidase 4 1
17113301 10.1016/j.bmc.2006.10.059 Dipeptidyl peptidase 8 1
17113301 10.1016/j.bmc.2006.10.059 Dipeptidyl peptidase 9 1
17317162 10.1016/j.bmcl.2007.01.110 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine