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Compound Detail

CHEMBL1681802

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N[C@H](Cc1cc(F)ccc1F)[C@H]1CC[C@H](N2CCn3c(nnc3C(F)(F)F)C2)CC1

Basic Information

ChEMBL ID CHEMBL1681802
Phase Preclinical
Structure Type MOL
InChI Key DMNMXJKWEZEVSV-SRCQZFHVSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

429.4
MW (Da)
3.52
ALogP
5
HBA
1
HBD
60.0
PSA (Ų)
0.76
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 C20H24F5N5
MW 429.44
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.24

Activity Summary

IC50 3 meas. best 6.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 6.48 6.48 330.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.75 4.75 18000.0 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 4.03 4.03 93000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 330.0 nM 6.48 Inhibition of DPP4 21320777
Dipeptidyl peptidase 2 IC50 = 18000.0 nM 4.75 Inhibition of QPP 21320777
Dipeptidyl peptidase 9 IC50 = 93000.0 nM 4.03 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