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Compound Detail

CHEMBL2180561

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COc1ccc(CNC(=O)c2nc(Br)c3cccnc3c2N[C@H]2CC[C@H](N)CC2)cc1

Basic Information

ChEMBL ID CHEMBL2180561
Phase Preclinical
Structure Type MOL
InChI Key WITSYZLHKBGMMR-WKILWMFISA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

484.4
MW (Da)
4.01
ALogP
6
HBA
3
HBD
102.2
PSA (Ų)
0.46
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26BrN5O2
MW 484.40
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.02

Activity Summary

IC50 4 meas. best 5.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HCT-116
CHEMBL394
IC50 5.52 5.52 3000.0 1
HEY
CHEMBL613869
IC50 5.4 5.4 4000.0 1
SK-BR-3
CHEMBL613834
IC50 5.3 5.3 5000.0 1
MDA-MB-435
CHEMBL614697
IC50 5.3 5.3 5000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23098137 10.1021/jm300667v Vascular endothelial growth factor receptor 2 2
23098137 10.1021/jm300667v Angiopoietin-1 receptor 1
23098137 10.1021/jm300667v Hepatocyte growth factor receptor 1
23098137 10.1021/jm300667v Fibroblast growth factor receptor 1 1
23098137 10.1021/jm300667v Insulin-like growth factor 1 receptor 1
23098137 10.1021/jm300667v Proto-oncogene tyrosine-protein kinase Src 1
23098137 10.1021/jm300667v Receptor tyrosine-protein kinase erbB-2 1
23098137 10.1021/jm300667v Epidermal growth factor receptor 1
23098137 10.1021/jm300667v HEY 1
23098137 10.1021/jm300667v SK-BR-3 1
23098137 10.1021/jm300667v MCF7 1
23098137 10.1021/jm300667v HCT-116 1
23098137 10.1021/jm300667v MDA-MB-435 1

Data from ChEMBL 36 via Core Engine