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Compound Detail

CHEMBL1650444

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Cn1c(=O)cc(N2CCC[C@@H](N)C2)n(Cc2cc(Cl)ccc2Cl)c1=O

Basic Information

ChEMBL ID CHEMBL1650444
Phase Preclinical
Structure Type MOL
InChI Key SIOPCTQIGVRHCI-CYBMUJFWSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

383.3
MW (Da)
1.83
ALogP
6
HBA
1
HBD
73.3
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 C17H20Cl2N4O2
MW 383.28
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.37

Activity Summary

IC50 2 meas. best 7.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.57 7.57 27.0 1
Dipeptidyl peptidase 8
CHEMBL4657
IC50 4.07 4.07 86000.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 2.75 hr Homo sapiens
T1/2 0.1667 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 27.0 nM 7.57 Inhibition of human DPP4 21186796
Dipeptidyl peptidase 8 IC50 = 86000.0 nM 4.07 Inhibition of human DPP8 21186796

Literature References

PubMed DOI Target Context # Activities
21186796 10.1021/jm101016w Liver microsomes 2
21186796 10.1021/jm101016w Dipeptidyl peptidase 8 1
21186796 10.1021/jm101016w Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine