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Compound Detail

CHEMBL4856337

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CC#CCn1c(N2CCC[C@@H](N)C2)cc(=O)n(Cc2ccc(Br)c(C(=O)O)c2)c1=O

Basic Information

ChEMBL ID CHEMBL4856337
Phase Preclinical
Structure Type MOL
InChI Key HHPODXPOWPNFMI-OAHLLOKOSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
5
Publications
0
Known Names

Molecular Properties

475.3
MW (Da)
1.47
ALogP
7
HBA
2
HBD
110.6
PSA (Ų)
0.63
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23BrN4O4
MW 475.34
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.77

Activity Summary

IC50 1 meas. best 9.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 9.1 9.1 0.8 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 5684.67 ng.hr.mL-1 Rattus norvegicus
CL 115.33 mL.min-1.kg-1 Rattus norvegicus
Cmax 51710.35 nM Rattus norvegicus
T1/2 0.59 hr Rattus norvegicus
Tmax 0.83 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34399391 10.1016/j.ejmech.2021.113765 ADMET 7
34399391 10.1016/j.ejmech.2021.113765 Dipeptidyl peptidase 9 1
34399391 10.1016/j.ejmech.2021.113765 L02 1
34399391 10.1016/j.ejmech.2021.113765 Dipeptidyl peptidase 8 1
34399391 10.1016/j.ejmech.2021.113765 Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine