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Compound Detail

CHEMBL5266987

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CO[C@@H]1CCCN1C(=O)CC(C)(C)[C@H](N)C(=O)N1CCC[C@H]1C#N.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL5266987
Phase Preclinical
Structure Type MOL
InChI Key JYAFNTLJDGYONR-SQFLUBDYSA-N
Parent Compound CHEMBL5315589
Active Moiety CHEMBL5315589
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

336.4
MW (Da)
0.84
ALogP
5
HBA
1
HBD
99.7
PSA (Ų)
0.80
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H29F3N4O5
MW 450.46
Aromatic Rings 0
Heavy Atoms 24
NP-Likeness 0.13

Activity Summary

IC50 1 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.85 7.85 14.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 168.0 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 14.0 nM 7.85 Inhibition of DPP-4 (unknown origin) 34428715

Literature References

PubMed DOI Target Context # Activities
34428715 10.1016/j.bmc.2021.116354 Dipeptidyl peptidase 4 1
34428715 10.1016/j.bmc.2021.116354 No relevant target 1

Data from ChEMBL 36 via Core Engine