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Compound Detail

CHEMBL440982

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CC(=O)Nc1ccc(OP(=O)(Oc2ccc(NC(C)=O)cc2)C2c3ccccc3CN2C(=O)[C@@H](N)CCCCN)cc1

Basic Information

ChEMBL ID CHEMBL440982
Phase Preclinical
Structure Type MOL
InChI Key MKKBABAOGFLBRQ-MBCWZBCWSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

593.6
MW (Da)
4.75
ALogP
8
HBA
4
HBD
166.1
PSA (Ų)
0.17
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H36N5O6P
MW 593.62
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness -0.16

Activity Summary

IC50 1 meas. best 6.28
Kd 1 meas. best 6.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 8
CHEMBL4657
IC50 6.28 6.28 530.0 1
Dipeptidyl peptidase 8
CHEMBL4657
Kd 6.11 6.11 770.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 8 IC50 = 530.0 nM 6.28 Inhibition of human DPP8 17958345
Dipeptidyl peptidase 8 Kd = 770.0 nM 6.11 Inhibition of human DPP8 17958345

Literature References

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

Data from ChEMBL 36 via Core Engine