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Compound Detail

CHEMBL3084938

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CN(C)C(=O)Nc1ccc(S(=O)(=O)N[C@H]2CC[C@H]([C@H](N)C(=O)N3CCCC3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL3084938
Phase Preclinical
Structure Type MOL
InChI Key PEBCJHONXDFPDD-IEZWGBDMSA-N
2
Targets
2
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

451.6
MW (Da)
1.57
ALogP
5
HBA
3
HBD
124.8
PSA (Ų)
0.61
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 C21H33N5O4S
MW 451.59
Aromatic Rings 1
Heavy Atoms 31
NP-Likeness -1.44

Activity Summary

IC50 2 meas. best 7.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.58 7.58 26.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.92 4.92 12000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 21.0 mL.min-1.kg-1 Rattus norvegicus
F 1.0 % Rattus norvegicus
T1/2 2.4 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14684294 10.1016/j.bmcl.2003.10.016 Rattus norvegicus 3
14684294 10.1016/j.bmcl.2003.10.016 Dipeptidyl peptidase 4 1
14684294 10.1016/j.bmcl.2003.10.016 Dipeptidyl peptidase 2 1
14684294 10.1016/j.bmcl.2003.10.016 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine