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Compound Detail

CHEMBL4297435

RETAGLIPTIN
🧪 Phase III
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🧪 Phase III
COC(=O)c1nc(C(F)(F)F)n2c1CN(C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F)CC2

Basic Information

ChEMBL ID CHEMBL4297435
Name RETAGLIPTIN
Phase Phase III
Structure Type MOL
InChI Key WIIAMRXFUJLYEF-SNVBAGLBSA-N

Known Names

Retagliptin SP-2086 Sp2086
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
3
Known Names
2
Indications

Molecular Properties

464.4
MW (Da)
2.41
ALogP
6
HBA
1
HBD
90.5
PSA (Ų)
0.42
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer
USAN Stem -gliptin

Extended Properties

Molecular Formula C19H18F6N4O3
MW 464.37
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.13

Indications

Diabetes Mellitus, Type 2 Renal Insufficiency

Activity Summary

IC50 1 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.92 7.92 12.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 12.0 nM 7.92 Inhibition of DPP-4 (unknown origin) 37647598

Literature References

PubMed DOI Target Context # Activities
37647598 10.1021/acs.jmedchem.3c00412 Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine