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Compound Detail

CHEMBL98798

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COc1cc2ncnc(Oc3cccc(Br)c3)c2cc1OC

Basic Information

ChEMBL ID CHEMBL98798
Phase Preclinical
Structure Type MOL
InChI Key BRHOGFZRGDIAMT-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

361.2
MW (Da)
4.20
ALogP
5
HBA
0
HBD
53.5
PSA (Ų)
0.70
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H13BrN2O3
MW 361.20
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -0.98

Activity Summary

IC50 4 meas. best 7.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 7.16 6.14 70.0 2
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 5.01 5.01 9800.0 1
Platelet-derived growth factor receptor beta
CHEMBL4125
IC50 4.83 4.83 14800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(97)10117-2 Platelet-derived growth factor receptor beta 1
- 10.1016/S0960-894X(97)10117-2 Epidermal growth factor receptor 1
21033670 10.1021/jm1009605 Calf thymus DNA 1
21033670 10.1021/jm1009605 Nucleic Acid 1
21353546 10.1016/j.bmcl.2011.01.137 Epidermal growth factor receptor 1
21353546 10.1016/j.bmcl.2011.01.137 Vascular endothelial growth factor receptor 2 1
21353546 10.1016/j.bmcl.2011.01.137 PC-3 1
21353546 10.1016/j.bmcl.2011.01.137 HT-29 1
21353546 10.1016/j.bmcl.2011.01.137 MCF7 1
21353546 10.1016/j.bmcl.2011.01.137 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine