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Compound Detail

CHEMBL474211

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N#C[C@@H]1CCCN1C(=O)[C@@H](N)CCC(=O)N1CCSC1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL474211
Phase Preclinical
Structure Type MOL
InChI Key BAVYYROUIZXLMI-ACMTZBLWSA-N
Parent Compound CHEMBL1186670
Active Moiety CHEMBL1186670
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

296.4
MW (Da)
0.14
ALogP
5
HBA
1
HBD
90.4
PSA (Ų)
0.80
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H21F3N4O4S
MW 410.42
Aromatic Rings 0
Heavy Atoms 20
NP-Likeness -0.74

Activity Summary

IC50 3 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 8.0 8.0 10.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 5.41 5.41 3900.0 1
Unchecked
CHEMBL612545
IC50 5.08 5.08 8300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 10.0 nM 8.0 Inhibition of DPP4 19269819
Dipeptidyl peptidase 8 IC50 = 3900.0 nM 5.41 Inhibition of DPP8 19269819
Unchecked IC50 = 8300.0 nM 5.08 Inhibition of FAP 19269819

Literature References

PubMed DOI Target Context # Activities
19269819 10.1016/j.bmcl.2009.02.061 Unchecked 2
19269819 10.1016/j.bmcl.2009.02.061 Dipeptidyl peptidase 4 1
19269819 10.1016/j.bmcl.2009.02.061 Dipeptidyl peptidase 8 1
19269819 10.1016/j.bmcl.2009.02.061 Dipeptidyl peptidase 2 1

Data from ChEMBL 36 via Core Engine