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Compound Detail

CHEMBL1683128

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N[C@H](Cc1cc(F)ccc1F)[C@H]1CC[C@H](N(CCCC(F)(F)F)Cc2ccccc2)CC1

Basic Information

ChEMBL ID CHEMBL1683128
Phase Preclinical
Structure Type MOL
InChI Key SBALHHSRJPLVIC-ZFJSRUIDSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

454.5
MW (Da)
6.24
ALogP
2
HBA
1
HBD
29.3
PSA (Ų)
0.45
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H31F5N2
MW 454.53
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.28

Activity Summary

IC50 3 meas. best 6.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 6.16 6.16 690.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.64 4.64 23000.0 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 4.37 4.37 43000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 690.0 nM 6.16 Inhibition of DPP4 21320777
Dipeptidyl peptidase 2 IC50 = 23000.0 nM 4.64 Inhibition of QPP 21320777
Dipeptidyl peptidase 9 IC50 = 43000.0 nM 4.37 Inhibition of DPP9 21320777

Literature References

PubMed DOI Target Context # Activities
21320777 10.1016/j.bmcl.2010.12.060 Dipeptidyl peptidase 4 1
21320777 10.1016/j.bmcl.2010.12.060 Dipeptidyl peptidase 2 1
21320777 10.1016/j.bmcl.2010.12.060 Dipeptidyl peptidase 8 1
21320777 10.1016/j.bmcl.2010.12.060 Dipeptidyl peptidase 9 1
21320777 10.1016/j.bmcl.2010.12.060 Prolyl endopeptidase FAP 1

Data from ChEMBL 36 via Core Engine