Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL227954

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
N#Cc1ccccc1Cn1c(N2CCC[C@@H](N)C2)nc2ccccc2c1=O

Basic Information

ChEMBL ID CHEMBL227954
Phase Preclinical
Structure Type MOL
InChI Key OYNURZXTLNNKAP-QGZVFWFLSA-N
2
Targets
3
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

359.4
MW (Da)
2.24
ALogP
6
HBA
1
HBD
87.9
PSA (Ų)
0.77
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C21H21N5O
MW 359.43
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.49

Activity Summary

IC50 3 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.89 7.89 13.0 2
Cytochrome P450 3A4
CHEMBL340
IC50 5.7 5.7 2000.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.04167 hr Rattus norvegicus
T1/2 3.333 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 13.0 nM 7.89 Inhibition of human DPP4 17441705
Dipeptidyl peptidase 4 IC50 = 13.0 nM 7.89 Inhibition of dipeptidyl peptidase 4 (unknown origin) -
Cytochrome P450 3A4 IC50 = 2000.0 nM 5.7 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
- 10.1007/s00044-012-0455-6 Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine