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Compound Detail

CHEMBL227670

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COc1ccc2nc(N3CCC[C@@H](N)C3)n(Cc3ccccc3C#N)c(=O)c2c1

Basic Information

ChEMBL ID CHEMBL227670
Phase Preclinical
Structure Type MOL
InChI Key KEHDIZISMAQBKX-QGZVFWFLSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

389.5
MW (Da)
2.25
ALogP
7
HBA
1
HBD
97.2
PSA (Ų)
0.74
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23N5O2
MW 389.46
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.44

Activity Summary

IC50 2 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 8.1 8.1 8.0 1
Cytochrome P450 3A4
CHEMBL340
IC50 6.7 6.7 200.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.1667 hr Rattus norvegicus
T1/2 1.367 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 8.0 nM 8.1 Inhibition of human DPP4 17441705
Cytochrome P450 3A4 IC50 = 200.0 nM 6.7 Inhibition of human CYP3A4 17441705

Literature References

PubMed DOI Target Context # Activities
17441705 10.1021/jm070104l Liver microsomes 2
17441705 10.1021/jm070104l Dipeptidyl peptidase 4 1
17441705 10.1021/jm070104l Dipeptidyl peptidase 8 1
17441705 10.1021/jm070104l Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine