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Compound Detail

CHEMBL427233

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CNc1ncc2cc(-c3cc(C(=O)Nc4cccc5c4CCC5)ccc3C)ccc2n1

Basic Information

ChEMBL ID CHEMBL427233
Phase Preclinical
Structure Type MOL
InChI Key ZYDVIGWWZRPSHL-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

408.5
MW (Da)
5.39
ALogP
4
HBA
2
HBD
66.9
PSA (Ų)
0.48
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H24N4O
MW 408.51
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.19

Activity Summary

IC50 5 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase Lck
CHEMBL258
IC50 9.52 9.52 0.3 1
Mitogen-activated protein kinase 14
CHEMBL260
IC50 7.68 7.68 21.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.32 7.32 48.0 1
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 5.87 5.87 1339.0 1
T-cell
CHEMBL614309
IC50 5.78 5.78 1664.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16970394 10.1021/jm0605482 Tyrosine-protein kinase Lck 1
16970394 10.1021/jm0605482 T-cell 1
16970394 10.1021/jm0605482 Vascular endothelial growth factor receptor 2 1
16970394 10.1021/jm0605482 Mitogen-activated protein kinase 14 1
16970394 10.1021/jm0605482 Tyrosine-protein kinase JAK3 1

Data from ChEMBL 36 via Core Engine