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Compound Detail

CHEMBL1683143

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COC(=O)C1CCCC(N2CCC([C@H](N)Cc3cc(F)ccc3F)CC2)C1

Basic Information

ChEMBL ID CHEMBL1683143
Phase Preclinical
Structure Type MOL
InChI Key ULGNQMQAXLOXHB-PKUWUEBNSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

380.5
MW (Da)
3.28
ALogP
4
HBA
1
HBD
55.6
PSA (Ų)
0.80
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H30F2N2O2
MW 380.48
Aromatic Rings 1
Heavy Atoms 27
NP-Likeness -0.73

Activity Summary

IC50 4 meas. best 7.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.27 7.27 54.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.89 4.89 13000.0 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 4.55 4.55 28000.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 4.41 4.41 39000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 54.0 nM 7.27 Inhibition of DPP4 21320777
Dipeptidyl peptidase 2 IC50 = 13000.0 nM 4.89 Inhibition of QPP 21320777
Dipeptidyl peptidase 9 IC50 = 28000.0 nM 4.55 Inhibition of DPP9 21320777
Dipeptidyl peptidase 8 IC50 = 39000.0 nM 4.41 Inhibition of DPP8 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