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Compound Detail

CHEMBL499345

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Nc1nc(Nc2cccc(Br)c2)c2cc(Cc3ccccc3Cl)[nH]c2n1

Basic Information

ChEMBL ID CHEMBL499345
Phase Preclinical
Structure Type MOL
InChI Key ISXTVMIMVFTRIL-UHFFFAOYSA-N
5
Targets
8
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

428.7
MW (Da)
5.29
ALogP
4
HBA
3
HBD
79.6
PSA (Ų)
0.41
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 C19H15BrClN5
MW 428.72
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -1.26

Activity Summary

IC50 8 meas. best 5.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gallus gallus
CHEMBL613109
IC50 5.77 5.77 1700.0 1
Epidermal growth factor receptor
CHEMBL203
IC50 5.37 5.37 4310.0 2
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 5.25 5.25 5580.0 2
Insulin-like growth factor 1 receptor
CHEMBL5381
IC50 5.13 5.13 7400.0 1
Vascular endothelial growth factor receptor 1
CHEMBL1868
IC50 4.57 4.57 26800.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18467105 10.1016/j.bmc.2008.04.019 Epidermal growth factor receptor 1
18467105 10.1016/j.bmc.2008.04.019 Vascular endothelial growth factor receptor 1 1
18467105 10.1016/j.bmc.2008.04.019 Vascular endothelial growth factor receptor 2 1
18467105 10.1016/j.bmc.2008.04.019 Platelet-derived growth factor receptor beta 1
18467105 10.1016/j.bmc.2008.04.019 A-431 1
18467105 10.1016/j.bmc.2008.04.019 Gallus gallus 1
19610618 10.1021/jm9002395 Insulin-like growth factor 1 receptor 1
19610618 10.1021/jm9002395 Insulin receptor 1
22370340 10.1016/j.bmc.2012.01.029 Epidermal growth factor receptor 1
22370340 10.1016/j.bmc.2012.01.029 Vascular endothelial growth factor receptor 1 1
22370340 10.1016/j.bmc.2012.01.029 Vascular endothelial growth factor receptor 2 1
22370340 10.1016/j.bmc.2012.01.029 Platelet-derived growth factor receptor beta 1
22370340 10.1016/j.bmc.2012.01.029 A-431 1

Data from ChEMBL 36 via Core Engine