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Compound Detail

CHEMBL474982

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N#C[C@@H]1CCCN1C(=O)[C@@H](N)CCC(=O)N1CCN(c2ccncc2)CC1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL474982
Phase Preclinical
Structure Type MOL
InChI Key MOGMHBOZKKGMRX-QJHJCNPRSA-N
Parent Compound CHEMBL1186707
Active Moiety CHEMBL1186707
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

370.5
MW (Da)
0.35
ALogP
6
HBA
1
HBD
106.6
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 C21H27F3N6O4
MW 484.48
Aromatic Rings 1
Heavy Atoms 27
NP-Likeness -0.99

Activity Summary

IC50 4 meas. best 7.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.72 7.72 19.0 1
Unchecked
CHEMBL612545
IC50 6.33 6.33 470.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 6.01 6.01 980.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.77 4.77 17000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 19.0 nM 7.72 Inhibition of DPP4 19269819
Unchecked IC50 = 470.0 nM 6.33 Inhibition of FAP 19269819
Dipeptidyl peptidase 8 IC50 = 980.0 nM 6.01 Inhibition of DPP8 19269819
Dipeptidyl peptidase 2 IC50 = 17000.0 nM 4.77 Inhibition of DPP2 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