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Compound Detail

CHEMBL4753194

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Cc1cccc(Oc2ccc(Nc3ncnc4ccc(NC(=O)CNCCO)cc34)cc2Cl)c1

Basic Information

ChEMBL ID CHEMBL4753194
Phase Preclinical
Structure Type MOL
InChI Key UWOVJYYCKNJHNU-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

477.9
MW (Da)
4.65
ALogP
7
HBA
4
HBD
108.4
PSA (Ų)
0.26
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24ClN5O3
MW 477.95
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.48

Activity Summary

IC50 4 meas. best 6.88

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
BT-474
CHEMBL614529
IC50 6.88 6.88 132.0 1
AU565
CHEMBL1075393
IC50 6.52 6.52 304.0 1
MDA-MB-231
CHEMBL400
IC50 5.11 5.11 7833.0 1
MCF7
CHEMBL387
IC50 4.97 4.97 10778.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33314925 10.1021/acs.jmedchem.0c01647 Tyrosine-protein kinase JAK2 1
33314925 10.1021/acs.jmedchem.0c01647 AU565 1
33314925 10.1021/acs.jmedchem.0c01647 Mast/stem cell growth factor receptor Kit 1
33314925 10.1021/acs.jmedchem.0c01647 Epidermal growth factor receptor 1
33314925 10.1021/acs.jmedchem.0c01647 Mitogen-activated protein kinase 3 1
33314925 10.1021/acs.jmedchem.0c01647 Mitogen-activated protein kinase 1 1
33314925 10.1021/acs.jmedchem.0c01647 Focal adhesion kinase 1 1
33314925 10.1021/acs.jmedchem.0c01647 Vascular endothelial growth factor receptor 1 1
33314925 10.1021/acs.jmedchem.0c01647 Vascular endothelial growth factor receptor 3 1
33314925 10.1021/acs.jmedchem.0c01647 Receptor tyrosine-protein kinase erbB-2 1
33314925 10.1021/acs.jmedchem.0c01647 Receptor tyrosine-protein kinase erbB-4 1
33314925 10.1021/acs.jmedchem.0c01647 MDA-MB-231 1
33314925 10.1021/acs.jmedchem.0c01647 Vascular endothelial growth factor receptor 2 1
33314925 10.1021/acs.jmedchem.0c01647 MAP kinase-activated protein kinase 2 1
33314925 10.1021/acs.jmedchem.0c01647 Tyrosine-protein kinase SYK 1
33314925 10.1021/acs.jmedchem.0c01647 Unchecked 1
33314925 10.1021/acs.jmedchem.0c01647 Proto-oncogene tyrosine-protein kinase Src 1
33314925 10.1021/acs.jmedchem.0c01647 Mitogen-activated protein kinase 14 1
33314925 10.1021/acs.jmedchem.0c01647 Platelet-derived growth factor receptor alpha 1
33314925 10.1021/acs.jmedchem.0c01647 Rho-associated protein kinase 2 1

Data from ChEMBL 36 via Core Engine