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Compound Detail

CHEMBL473188

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O=C([C@@H]1C[C@H](N2CCN(c3ncccn3)CC2)CN1)N1CC(F)C1

Basic Information

ChEMBL ID CHEMBL473188
Phase Preclinical
Structure Type MOL
InChI Key SQYBOLCVZXHFPW-KBPBESRZSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
6
Publications
0
Known Names

Molecular Properties

334.4
MW (Da)
-0.49
ALogP
6
HBA
1
HBD
64.6
PSA (Ų)
0.80
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 C16H23FN6O
MW 334.40
Aromatic Rings 1
Heavy Atoms 24
NP-Likeness -1.23

Activity Summary

IC50 1 meas. best 7.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.39 7.39 41.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1073.0 ng.hr.mL-1 Rattus norvegicus
CL 16.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 5137.56 nM Rattus norvegicus
F 91.0 % Rattus norvegicus
T1/2 3.6 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 41.0 nM 7.39 Inhibition of human recombinant DPP4 19275964

Literature References

PubMed DOI Target Context # Activities
19275964 10.1016/j.bmcl.2009.02.041 Rattus norvegicus 6
19275964 10.1016/j.bmcl.2009.02.041 MDCK 2
19275964 10.1016/j.bmcl.2009.02.041 Voltage-gated inwardly rectifying potassium channel KCNH2 1
19275964 10.1016/j.bmcl.2009.02.041 Dipeptidyl peptidase 4 1
19275964 10.1016/j.bmcl.2009.02.041 Dipeptidyl peptidase 2 1
19275964 10.1016/j.bmcl.2009.02.041 Dipeptidyl peptidase 8 1

Data from ChEMBL 36 via Core Engine