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

CHEMBL5218591

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
Cc1ccc(N2CCN(c3nc(N)nc(Nc4ccc(C)c(C)c4)n3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL5218591
Phase Preclinical
Structure Type MOL
InChI Key SHUVVOQGUDSTTM-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

389.5
MW (Da)
3.45
ALogP
7
HBA
2
HBD
83.2
PSA (Ų)
0.71
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H27N7
MW 389.51
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.77

Activity Summary

IC50 5 meas. best 6.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NADPH oxidase 5
CHEMBL1926497
IC50 6.24 6.24 570.0 1
NADPH oxidase 4
CHEMBL1250375
IC50 6.17 6.17 680.0 1
NADPH oxidase 3
CHEMBL1741216
IC50 5.5 5.5 3200.0 1
NADPH oxidase 1
CHEMBL1287628
IC50 5.16 5.16 7000.0 1
Cytochrome b-245 heavy chain
CHEMBL1287627
IC50 4.8 4.8 16000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
NADPH oxidase 5 IC50 = 570.0 nM 6.24 Inhibition of human NOX5 35981459
NADPH oxidase 4 IC50 = 680.0 nM 6.17 Inhibition of human NOX4 35981459
NADPH oxidase 3 IC50 = 3200.0 nM 5.5 Inhibition of human NOX3 35981459
NADPH oxidase 1 IC50 = 7000.0 nM 5.16 Inhibition of human NOX1 35981459
Cytochrome b-245 heavy chain IC50 = 16000.0 nM 4.8 Inhibition of human NOX2 35981459

Literature References

PubMed DOI Target Context # Activities
35981459 10.1016/j.ejmech.2022.114645 NADPH oxidase 1 1
35981459 10.1016/j.ejmech.2022.114645 Cytochrome b-245 heavy chain 1
35981459 10.1016/j.ejmech.2022.114645 NADPH oxidase 3 1
35981459 10.1016/j.ejmech.2022.114645 NADPH oxidase 4 1
35981459 10.1016/j.ejmech.2022.114645 NADPH oxidase 5 1

Data from ChEMBL 36 via Core Engine