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Compound Detail

CHEMBL474346

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Clc1cc(Nc2ncnc3ccsc23)ccc1-c1nc2ccccc2s1

Basic Information

ChEMBL ID CHEMBL474346
Phase Preclinical
Structure Type MOL
InChI Key LRLIJRSPYLLOIV-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

394.9
MW (Da)
6.37
ALogP
6
HBA
1
HBD
50.7
PSA (Ų)
0.39
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H11ClN4S2
MW 394.91
Aromatic Rings 5
Heavy Atoms 26
NP-Likeness -2.36

Activity Summary

IC50 1 meas. best 5.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiopoietin-1 receptor
CHEMBL4128
IC50 5.36 5.36 4400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Angiopoietin-1 receptor IC50 = 4400.0 nM 5.36 Inhibition of TIE2 by virtual HTS assay 19211246

Literature References

PubMed DOI Target Context # Activities
19211246 10.1016/j.bmcl.2009.01.054 Aurora kinase B 1
19211246 10.1016/j.bmcl.2009.01.054 Aurora kinase A 1
19211246 10.1016/j.bmcl.2009.01.054 Epidermal growth factor receptor 1
19211246 10.1016/j.bmcl.2009.01.054 Receptor tyrosine-protein kinase erbB-2 1
19211246 10.1016/j.bmcl.2009.01.054 Insulin receptor 1
19211246 10.1016/j.bmcl.2009.01.054 Proto-oncogene tyrosine-protein kinase Src 1
19211246 10.1016/j.bmcl.2009.01.054 Vascular endothelial growth factor receptor 3 1
19211246 10.1016/j.bmcl.2009.01.054 Vascular endothelial growth factor receptor 2 1
19211246 10.1016/j.bmcl.2009.01.054 Insulin-like growth factor 1 receptor 1
19211246 10.1016/j.bmcl.2009.01.054 Angiopoietin-1 receptor 1

Data from ChEMBL 36 via Core Engine