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Compound Detail

CHEMBL5289984

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CC#CCn1c(N2CCC[C@@H](N)C2)cc(=O)n(Cc2cn(C/C=C/C(=O)O)nn2)c1=O

Basic Information

ChEMBL ID CHEMBL5289984
Phase Preclinical
Structure Type MOL
InChI Key PDYFFDPMFVTJCH-KEDPEKRHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

427.5
MW (Da)
-0.76
ALogP
10
HBA
2
HBD
141.3
PSA (Ų)
0.43
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H25N7O4
MW 427.47
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -0.77

Activity Summary

IC50 1 meas. best 8.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 8.02 8.02 9.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 9.56 nM 8.02 Inhibition of human recombinant DPP-4 using (H-Gly-Pro-AMC as substrate 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 Mus musculus 1

Data from ChEMBL 36 via Core Engine