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Compound Detail

CHEMBL474543

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Clc1ccc2c(Nc3ccc(-c4nc5ccccc5s4)cc3)ccnc2c1

Basic Information

ChEMBL ID CHEMBL474543
Phase Preclinical
Structure Type MOL
InChI Key IFTCXKUSJMWVRD-UHFFFAOYSA-N
9
Targets
9
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

387.9
MW (Da)
6.91
ALogP
4
HBA
1
HBD
37.8
PSA (Ų)
0.37
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 C22H14ClN3S
MW 387.90
Aromatic Rings 5
Heavy Atoms 27
NP-Likeness -1.80

Activity Summary

IC50 9 meas. best 6.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 6.2 6.2 630.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.19 6.19 640.0 1
Aurora kinase B
CHEMBL2185
IC50 6.12 6.12 750.0 1
Insulin-like growth factor 1 receptor
CHEMBL1957
IC50 6.07 6.07 860.0 1
Ephrin type-B receptor 4
CHEMBL5147
IC50 5.85 5.85 1400.0 1
Insulin receptor
CHEMBL1981
IC50 5.57 5.57 2700.0 1
Epidermal growth factor receptor
CHEMBL203
IC50 5.28 5.28 5300.0 1
Aurora kinase A
CHEMBL4722
IC50 5.24 5.24 5700.0 1
Angiopoietin-1 receptor
CHEMBL4128
IC50 5.16 5.16 7000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19211246 10.1016/j.bmcl.2009.01.054 Angiopoietin-1 receptor 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 Insulin receptor 1
19211246 10.1016/j.bmcl.2009.01.054 Ephrin type-B receptor 4 1
19211246 10.1016/j.bmcl.2009.01.054 Insulin-like growth factor 1 receptor 1
19211246 10.1016/j.bmcl.2009.01.054 Aurora kinase B 1
19211246 10.1016/j.bmcl.2009.01.054 Vascular endothelial growth factor receptor 2 1
19211246 10.1016/j.bmcl.2009.01.054 Proto-oncogene tyrosine-protein kinase Src 1

Data from ChEMBL 36 via Core Engine