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Compound Detail

CHEMBL238114

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CC(=O)Nc1ccc(OP(=O)(Oc2ccc(NC(C)=O)cc2)C2CCCN2C(=O)[C@H](CCCCN)NC(=O)OCc2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL238114
Phase Preclinical
Structure Type MOL
InChI Key NZXXSPTYMKQRAI-CYZZXXEPSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

679.7
MW (Da)
5.63
ALogP
9
HBA
4
HBD
178.4
PSA (Ų)
0.12
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H42N5O8P
MW 679.71
Aromatic Rings 3
Heavy Atoms 48
NP-Likeness -0.26

Activity Summary

IC50 3 meas. best 5.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 5.38 5.38 4200.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 4.37 4.37 43000.0 1
Dipeptidyl peptidase 2
CHEMBL3976
IC50 4.11 4.11 77000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 4200.0 nM 5.38 Inhibition of human DPP4 17958345
Dipeptidyl peptidase 8 IC50 = 43000.0 nM 4.37 Inhibition of human DPP8 17958345
Dipeptidyl peptidase 2 IC50 = 77000.0 nM 4.11 Inhibition of human DPP2 17958345

Literature References

PubMed DOI Target Context # Activities
17958345 10.1021/jm701005a Dipeptidyl peptidase 8 1
17958345 10.1021/jm701005a Dipeptidyl peptidase 4 1
17958345 10.1021/jm701005a Dipeptidyl peptidase 2 1

Data from ChEMBL 36 via Core Engine