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Compound Detail

CHEMBL2105754

TRELAGLIPTIN SUCCINATE
💊 Approved Drug
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💊 Approved Drug
Cn1c(=O)cc(N2CCC[C@@H](N)C2)n(Cc2cc(F)ccc2C#N)c1=O.O=C(O)CCC(=O)O

Basic Information

ChEMBL ID CHEMBL2105754
Name TRELAGLIPTIN SUCCINATE
Phase Approved
Structure Type MOL
InChI Key OGCNTTUPLQTBJI-XFULWGLBSA-N
Parent Compound CHEMBL1650443
Active Moiety CHEMBL1650443

Known Names

SYR-111472 SUCCINATE SYR-472 SYR111472 SUCCINATE Trelagliptin succinate Zafatek
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
5
Known Names
2
Indications
1
Mechanisms

Molecular Properties

357.4
MW (Da)
0.53
ALogP
7
HBA
1
HBD
97.0
PSA (Ų)
0.86
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2015
Availability Unknown
Chirality Single Enantiomer
USAN Stem -gliptin
USAN Year 2011

Extended Properties

Molecular Formula C22H26FN5O6
MW 475.48
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.59

Mechanism of Action

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

Indications

Diabetes Mellitus Diabetes Mellitus, Type 2

Activity Summary

IC50 1 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 8.4 8.4 4.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 4.0 nM 8.4 Inhibition of DPP4 (unknown origin) 38704940

Literature References

PubMed DOI Target Context # Activities
38704940 10.1016/j.ejmech.2024.116464 Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine