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Compound Detail

CHEMBL3616896

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CC#CCn1c(N2CC(=O)N[C@H](CO)C2)nc2c1c(=O)n(Cc1nc(C)c3ccccc3n1)c(=O)n2C

Basic Information

ChEMBL ID CHEMBL3616896
Phase Preclinical
Structure Type MOL
InChI Key QQSHPPSZQGKKKZ-INIZCTEOSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

502.5
MW (Da)
-0.48
ALogP
11
HBA
2
HBD
140.2
PSA (Ų)
0.35
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H26N8O4
MW 502.54
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.04

Activity Summary

IC50 2 meas. best 5.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prolyl endopeptidase FAP
CHEMBL4683
IC50 5.48 5.48 3300.0 1
Dipeptidyl peptidase 4
CHEMBL284
IC50 4.74 4.74 18100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prolyl endopeptidase FAP IC50 = 3300.0 nM 5.48 Binding affinity to FAP (unknown origin) -
Dipeptidyl peptidase 4 IC50 = 18100.0 nM 4.74 Binding affinity to DPP4 (unknown origin) -

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C4MD00167B Prolyl endopeptidase FAP 1
- 10.1039/C4MD00167B Dipeptidyl peptidase 4 1
- 10.1039/C4MD00167B Prolyl endopeptidase 1
- 10.1039/C4MD00167B Dipeptidyl peptidase 9 1
- 10.1039/C4MD00167B Dipeptidyl peptidase 2 1

Data from ChEMBL 36 via Core Engine