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Compound Detail

CHEMBL427261

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N[C@@H](CC(=O)N1CCn2c(nnc2C(F)(F)F)C1)Cc1cc(Cl)ccc1F

Basic Information

ChEMBL ID CHEMBL427261
Phase Preclinical
Structure Type MOL
InChI Key MUMFFVRFHUQYEC-LLVKDONJSA-N
2
Targets
3
Activities
1
Assay Types
4
PK Parameters
5
Publications
0
Known Names

Molecular Properties

405.8
MW (Da)
2.39
ALogP
5
HBA
1
HBD
77.0
PSA (Ų)
0.79
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H16ClF4N5O
MW 405.78
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -1.73

Activity Summary

IC50 3 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.68 7.68 21.0 2
Dipeptidyl peptidase 9
CHEMBL4793
IC50 4.01 4.01 98000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 0.18 uM.hr.Kg/mg Rattus norvegicus
CL 99.0 mL.min-1.kg-1 Rattus norvegicus
F 43.0 % Rattus norvegicus
T1/2 1.7 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 21.0 nM 7.68 Inhibition of DPP4 17337342
Dipeptidyl peptidase 4 IC50 = 21.0 nM 7.68 Inhibition of DPP4 activity 17434732
Dipeptidyl peptidase 9 IC50 = 98000.0 nM 4.01 Inhibition of DPP9 activity 17434732

Literature References

PubMed DOI Target Context # Activities
17434732 10.1016/j.bmcl.2007.03.098 Rattus norvegicus 4
17337342 10.1016/j.bmcl.2007.02.040 Dipeptidyl peptidase 4 1
17434732 10.1016/j.bmcl.2007.03.098 Dipeptidyl peptidase 4 1
17434732 10.1016/j.bmcl.2007.03.098 Dipeptidyl peptidase 9 1
17434732 10.1016/j.bmcl.2007.03.098 Dipeptidyl peptidase 8 1

Data from ChEMBL 36 via Core Engine