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Compound Detail

CHEMBL3093902

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N#C[C@@H]1C[C@H](F)CN1C(=O)[C@@H](N)Cc1ccccc1

Basic Information

ChEMBL ID CHEMBL3093902
Phase Preclinical
Structure Type MOL
InChI Key DKYVWDSJKVMXJP-AVGNSLFASA-N
5
Targets
6
Activities
1
Assay Types
17
PK Parameters
11
Publications
0
Known Names

Molecular Properties

261.3
MW (Da)
1.02
ALogP
3
HBA
1
HBD
70.1
PSA (Ų)
0.88
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H16FN3O
MW 261.30
Aromatic Rings 1
Heavy Atoms 19
NP-Likeness -0.20

Activity Summary

IC50 6 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.77 7.77 17.0 2
Prolyl endopeptidase FAP
CHEMBL4683
IC50 5.82 5.82 1530.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.84 4.84 14520.0 1
Dipeptidyl peptidase 9
CHEMBL4793
IC50 4.7 4.7 19790.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 4.65 4.65 22510.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 2083.0 ng.hr.mL-1 Rattus norvegicus
AUC 458.0 ng.hr.mL-1 Rattus norvegicus
AUC 2082.0 ng.hr.mL-1 Rattus norvegicus
AUC 455.0 ng.hr.mL-1 Rattus norvegicus
AUC 6684054.0 ng.hr.mL-1 Mus musculus
AUC 7339917.0 ng.hr.mL-1 Mus musculus
AUC 4661592.0 ng.hr.mL-1 Mus musculus
AUC 4619784.0 ng.hr.mL-1 Mus musculus
AUC 4538781.0 ng.hr.mL-1 Mus musculus
AUC 5139771.0 ng.hr.mL-1 Mus musculus
Cmax 1691.54 nM Rattus norvegicus
F 21.8 % Rattus norvegicus
F 21.8 % Mus musculus
T1/2 5.4 hr Rattus norvegicus
T1/2 5.4 hr Rattus norvegicus
T1/2 5.4 hr Mus musculus
Tmax 0.5 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24153396 10.1016/j.bmc.2013.09.048 Mus musculus 34
24153396 10.1016/j.bmc.2013.09.048 Rattus norvegicus 9
34428715 10.1016/j.bmc.2021.116354 Mus musculus 6
24153396 10.1016/j.bmc.2013.09.048 Unchecked 2
34428715 10.1016/j.bmc.2021.116354 ADMET 2
24153396 10.1016/j.bmc.2013.09.048 Prolyl endopeptidase FAP 1
24153396 10.1016/j.bmc.2013.09.048 Dipeptidyl peptidase 2 1
24153396 10.1016/j.bmc.2013.09.048 Dipeptidyl peptidase 9 1
24153396 10.1016/j.bmc.2013.09.048 Dipeptidyl peptidase 4 1
24153396 10.1016/j.bmc.2013.09.048 Dipeptidyl peptidase 8 1
34428715 10.1016/j.bmc.2021.116354 Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine