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Compound Detail

CHEMBL474794

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Cl.NC(=O)c1ccc(C(=O)N2CCCN(C(=O)C[C@H](N)Cc3cc(F)c(F)cc3F)CC2)cc1

Basic Information

ChEMBL ID CHEMBL474794
Phase Preclinical
Structure Type MOL
InChI Key VORDXCIWIZMXCJ-UNTBIKODSA-N
Parent Compound CHEMBL1186693
Active Moiety CHEMBL1186693
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

462.5
MW (Da)
1.84
ALogP
4
HBA
2
HBD
109.7
PSA (Ų)
0.64
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26ClF3N4O3
MW 498.93
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.19

Activity Summary

IC50 1 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 6.75 6.75 180.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 180.0 nM 6.75 Inhibition of DPP4 18996694

Literature References

PubMed DOI Target Context # Activities
18996694 10.1016/j.bmcl.2008.10.076 Cytochrome P450 3A4 1
18996694 10.1016/j.bmcl.2008.10.076 Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine