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Compound Detail

CHEMBL1082462

DBPR-108
🧪 Phase III
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🧪 Phase III
CC(C)(CC(=O)N1CCCC1)NCC(=O)N1C[C@@H](F)C[C@H]1C#N
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL1082462
Name DBPR-108
Phase Phase III
Structure Type MOL
InChI Key VQKSCYBKUIDZEI-STQMWFEESA-N

Known Names

Dbpr-108 Prusogliptin
1
Targets
3
Activities
1
Assay Types
2
PK Parameters
19
Publications
2
Known Names
3
Indications
1
Mechanisms

Molecular Properties

324.4
MW (Da)
0.83
ALogP
4
HBA
1
HBD
76.4
PSA (Ų)
0.81
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer

Extended Properties

Molecular Formula C16H25FN4O2
MW 324.40
Aromatic Rings 0
Heavy Atoms 23
NP-Likeness -0.80

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Dipeptidyl peptidase IV inhibitor INHIBITOR Dipeptidyl peptidase 4 ✓ ✓

Indications

Diabetes Mellitus, Type 2 Kidney Diseases Liver Diseases

Activity Summary

IC50 3 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
 IC50 8.3 8.04 5.0 3

Pharmacokinetic Data

Parameter Value Units Species
F 19.0 % Rattus norvegicus
F 68.0 % Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 5.0 nM 8.3 Inhibition of DPP4 in presence of 50% human serum 20483603
Dipeptidyl peptidase 4 IC50 = 10.0 nM 8.0 Inhibition of DPP4 in presence of 50% rat serum 20483603
Dipeptidyl peptidase 4 IC50 = 15.0 nM 7.82 Inhibition of DPP4 20483603

Literature References

PubMed DOI Target Context # Activities
20483603 10.1016/j.bmcl.2010.04.124 Dipeptidyl peptidase 4 3
20483603 10.1016/j.bmcl.2010.04.124 Unchecked 3
20483603 10.1016/j.bmcl.2010.04.124 Rattus norvegicus 3
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
20483603 10.1016/j.bmcl.2010.04.124 Cathepsin B 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
20483603 10.1016/j.bmcl.2010.04.124 Voltage-gated inwardly rectifying potassium channel KCNH2 1
20483603 10.1016/j.bmcl.2010.04.124 Prothrombin 1
20483603 10.1016/j.bmcl.2010.04.124 Coagulation factor X 1
20483603 10.1016/j.bmcl.2010.04.124 Pro-cathepsin H 1
20483603 10.1016/j.bmcl.2010.04.124 Caspase-10 1
20483603 10.1016/j.bmcl.2010.04.124 Caspase-1 1
20483603 10.1016/j.bmcl.2010.04.124 Beta-secretase 1 1
20483603 10.1016/j.bmcl.2010.04.124 Canis familiaris 1
20483603 10.1016/j.bmcl.2010.04.124 Mus musculus 1
20483603 10.1016/j.bmcl.2010.04.124 Dipeptidyl peptidase 8 1
20483603 10.1016/j.bmcl.2010.04.124 Dipeptidyl peptidase 9 1

Data from ChEMBL 36 via Core Engine