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Compound Detail

CHEMBL1779710

EVOGLIPTIN
💊 Approved Drug
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💊 Approved Drug
CC(C)(C)OC[C@@H]1C(=O)NCCN1C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL1779710
Name EVOGLIPTIN
Phase Approved
Structure Type MOL
InChI Key LCDDAGSJHKEABN-MLGOLLRUSA-N

Known Names

Da-1229 DA1229 Evogliptin Evogliptina Evogliptine
2
Targets
2
Activities
1
Assay Types
5
PK Parameters
11
Publications
5
Known Names
5
Indications
1
Mechanisms

Molecular Properties

401.4
MW (Da)
1.51
ALogP
4
HBA
2
HBD
84.7
PSA (Ų)
0.71
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2015
Availability Unknown
Chirality Single Enantiomer

Routes of Administration

Oral
USAN Stem -gliptin

Extended Properties

Molecular Formula C19H26F3N3O3
MW 401.43
Aromatic Rings 1
Heavy Atoms 28
NP-Likeness -0.77

Mechanism of Action

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

Indications

Diabetes Mellitus Diabetes Mellitus, Type 2 Aortic Valve Disease Kidney Diseases Liver Diseases

ATC Classification

A10BH07
evogliptin
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: DRUGS USED IN DIABETES

Activity Summary

IC50 2 meas. best 9.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
 IC50 9.05 9.05 0.9 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
 IC50 4.1 4.1 79600.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 60.5 mL.min-1.kg-1 Rattus norvegicus
F 74.8 % Rattus norvegicus
T1/2 1.5 hr Homo sapiens
T1/2 6.1 hr Rattus norvegicus
T1/2 32.5 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 0.9 nM 9.05 Inhibition of recombinant human DPP-4 assessed as H-Gly-Pro-AMC cleavage after 1... 21570283
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 79600.0 nM 4.1 Inhibition of human ERG by patch clamp method 21570283

Literature References

PubMed DOI Target Context # Activities
21570283 10.1016/j.bmcl.2011.04.029 Rattus norvegicus 8
21570283 10.1016/j.bmcl.2011.04.029 Mus musculus 3
21570283 10.1016/j.bmcl.2011.04.029 Dipeptidyl peptidase 4 1
21570283 10.1016/j.bmcl.2011.04.029 Cytochrome P450 3A4 1
21570283 10.1016/j.bmcl.2011.04.029 Cytochrome P450 2D6 1
21570283 10.1016/j.bmcl.2011.04.029 Cytochrome P450 2C9 1
21570283 10.1016/j.bmcl.2011.04.029 Cytochrome P450 2C19 1
21570283 10.1016/j.bmcl.2011.04.029 Cytochrome P450 1A2 1
21570283 10.1016/j.bmcl.2011.04.029 Liver 1
21570283 10.1016/j.bmcl.2011.04.029 Voltage-gated inwardly rectifying potassium channel KCNH2 1
29609120 10.1016/j.ejmech.2018.03.041 Homo sapiens 1

Data from ChEMBL 36 via Core Engine