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Compound Detail

CHEMBL403408

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CC#CCn1c(NC[C@H](C)N)nc2cnn(Cc3nc(C)c4ccccc4n3)c(=O)c21

Basic Information

ChEMBL ID CHEMBL403408
Phase Preclinical
Structure Type MOL
InChI Key HYBQECPBYZXFJO-AWEZNQCLSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

416.5
MW (Da)
1.68
ALogP
9
HBA
2
HBD
116.5
PSA (Ų)
0.46
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H24N8O
MW 416.49
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.24

Activity Summary

IC50 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 8.7 8.7 2.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 2.0 nM 8.7 Inhibition of DPP4 in human Caco-2 cells after 1 hr 18485703

Literature References

PubMed DOI Target Context # Activities
18485703 10.1016/j.bmcl.2008.04.075 Dipeptidyl peptidase 4 1
18485703 10.1016/j.bmcl.2008.04.075 Muscarinic acetylcholine receptor M1 1
18485703 10.1016/j.bmcl.2008.04.075 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine