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Compound Detail

CHEMBL217198

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COc1ccc(NC(=O)CC(C)(C)NCC(=O)N2CCC[C@H]2C#N)cc1OC

Basic Information

ChEMBL ID CHEMBL217198
Phase Preclinical
Structure Type MOL
InChI Key WREGAGBMMHFZHU-HNNXBMFYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

388.5
MW (Da)
1.92
ALogP
6
HBA
2
HBD
103.7
PSA (Ų)
0.71
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H28N4O4
MW 388.47
Aromatic Rings 1
Heavy Atoms 28
NP-Likeness -0.98

Activity Summary

IC50 2 meas. best 6.94

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 6.94 6.94 116.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 116.0 nM 6.94 In vitro inhibition of DPP-4 17194587
Dipeptidyl peptidase 4 IC50 = 116.0 nM 6.94 Inhibition of DPP4 20483603

Literature References

PubMed DOI Target Context # Activities
17194587 10.1016/j.bmcl.2006.12.019 Dipeptidyl peptidase 4 3
17194587 10.1016/j.bmcl.2006.12.019 Dipeptidyl peptidase 2 1
17194587 10.1016/j.bmcl.2006.12.019 Dipeptidyl peptidase 8 1
17194587 10.1016/j.bmcl.2006.12.019 Rattus norvegicus 1
17194587 10.1016/j.bmcl.2006.12.019 Prolyl endopeptidase FAP 1
20483603 10.1016/j.bmcl.2010.04.124 Prolyl endopeptidase FAP 1
20483603 10.1016/j.bmcl.2010.04.124 Dipeptidyl peptidase 2 1
20483603 10.1016/j.bmcl.2010.04.124 Dipeptidyl peptidase 9 1
20483603 10.1016/j.bmcl.2010.04.124 Dipeptidyl peptidase 8 1
20483603 10.1016/j.bmcl.2010.04.124 Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine