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Compound Detail

CHEMBL400841

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CN(C)C(=O)[C@@H]([C@H]1CC[C@H](c2cccc3ncnn32)CC1)[C@H](N)C(=O)N1CC[C@H](F)C1

Basic Information

ChEMBL ID CHEMBL400841
Phase Preclinical
Structure Type MOL
InChI Key ZPWDKZWKUOYOHA-UKSSEWCLSA-N
3
Targets
5
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

430.5
MW (Da)
1.61
ALogP
6
HBA
1
HBD
96.8
PSA (Ų)
0.78
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 C22H31FN6O2
MW 430.53
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.11

Activity Summary

IC50 5 meas. best 8.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 8.64 8.2867 2.3 3
Dipeptidyl peptidase 9
CHEMBL4793
IC50 4.55 4.55 28000.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 4.28 4.28 53000.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 31.0 % Rattus norvegicus
T1/2 0.54 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17851076 10.1016/j.bmcl.2007.08.049 Dipeptidyl peptidase 4 2
17851076 10.1016/j.bmcl.2007.08.049 Rattus norvegicus 2
17851076 10.1016/j.bmcl.2007.08.049 Dipeptidyl peptidase 8 1
17851076 10.1016/j.bmcl.2007.08.049 Dipeptidyl peptidase 9 1
- 10.1007/s00044-012-0455-6 Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine