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Compound Detail

CHEMBL513985

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c1ccc(Oc2cccc(Nc3nccc(-c4nccs4)n3)c2)cc1

Basic Information

ChEMBL ID CHEMBL513985
Phase Preclinical
Structure Type MOL
InChI Key JDMSPHKFVGVCKN-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

346.4
MW (Da)
5.14
ALogP
6
HBA
1
HBD
59.9
PSA (Ų)
0.54
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H14N4OS
MW 346.42
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -1.58

Activity Summary

IC50 1 meas. best 6.0
Ki 1 meas. best 6.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase SYK
CHEMBL2599
Ki 6.2 6.2 630.0 1
Tyrosine-protein kinase SYK
CHEMBL2599
IC50 6.0 6.0 1000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase SYK Ki = 630.0 nM 6.2 Inhibition of SYK 18938080
Tyrosine-protein kinase SYK IC50 = 1000.0 nM 6.0 Inhibition of recombinant Syk 19254842

Literature References

PubMed DOI Target Context # Activities
18938080 10.1016/j.bmcl.2008.09.106 Tyrosine-protein kinase SYK 1
19254842 10.1016/j.bmcl.2009.02.049 Tyrosine-protein kinase SYK 1

Data from ChEMBL 36 via Core Engine