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Compound Detail

CHEMBL3616917

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CC#CCn1c(N2CCNC(=O)C2)nc2c1c(=O)n(Cc1nc(OC)c3ccccc3n1)c(=O)n2C

Basic Information

ChEMBL ID CHEMBL3616917
Phase Preclinical
Structure Type MOL
InChI Key SHWBAHDKEFNAPF-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

488.5
MW (Da)
-0.14
ALogP
11
HBA
1
HBD
129.2
PSA (Ų)
0.38
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H24N8O4
MW 488.51
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.38

Activity Summary

IC50 1 meas. best 5.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prolyl endopeptidase FAP
CHEMBL4683
IC50 5.24 5.24 5800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prolyl endopeptidase FAP IC50 = 5800.0 nM 5.24 Binding affinity to FAP (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