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Compound Detail

CHEMBL234412

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CCCC[C@H]1CN2CCc3cc(OC)c(OC)cc3[C@@H]2C[C@@H]1N

Basic Information

ChEMBL ID CHEMBL234412
Phase Preclinical
Structure Type MOL
InChI Key IYTDSNSLAQHLJL-XIRDDKMYSA-N
1
Targets
2
Activities
1
Assay Types
2
PK Parameters
9
Publications
0
Known Names

Molecular Properties

318.5
MW (Da)
3.14
ALogP
4
HBA
1
HBD
47.7
PSA (Ų)
0.91
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 C19H30N2O2
MW 318.46
Aromatic Rings 1
Heavy Atoms 23
NP-Likeness 0.89

Activity Summary

IC50 2 meas. best 6.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 6.28 6.215 520.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL - mL.min-1.g-1 Homo sapiens
CL 4700.0 mL.min-1.g-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 520.0 nM 6.28 Inhibition of human DPP4 17418568
Dipeptidyl peptidase 4 IC50 = 710.0 nM 6.15 Inhibition of human DPP4 expressed in baculovirus system 18207285

Literature References

PubMed DOI Target Context # Activities
17418568 10.1016/j.bmcl.2007.03.072 Liver microsomes 2
17418568 10.1016/j.bmcl.2007.03.072 No relevant target 2
17418568 10.1016/j.bmcl.2007.03.072 Rattus norvegicus 1
17418568 10.1016/j.bmcl.2007.03.072 Cytochrome P450 2D6 1
17418568 10.1016/j.bmcl.2007.03.072 Cytochrome P450 2C9 1
17418568 10.1016/j.bmcl.2007.03.072 Dipeptidyl peptidase 4 1
17418568 10.1016/j.bmcl.2007.03.072 ADMET 1
17418568 10.1016/j.bmcl.2007.03.072 Cytochrome P450 3A4 1
18207285 10.1016/j.ejmech.2007.11.014 Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine