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Compound Detail

CHEMBL472478

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COc1cc(Nc2nccc(-c3nccs3)n2)cc(OC)c1

Basic Information

ChEMBL ID CHEMBL472478
Phase Preclinical
Structure Type MOL
InChI Key GQUIEPYFROOKLV-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

314.4
MW (Da)
3.36
ALogP
7
HBA
1
HBD
69.2
PSA (Ų)
0.78
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H14N4O2S
MW 314.37
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -1.49

Activity Summary

Ki 3 meas. best 7.85
IC50 1 meas. best 7.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase SYK
CHEMBL2599
Ki 7.85 7.85 14.0 1
Tyrosine-protein kinase SYK
CHEMBL2599
IC50 7.16 7.16 70.0 1
Tyrosine-protein kinase ZAP-70
CHEMBL2803
Ki 6.5 6.5 318.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
Ki 6.06 6.06 862.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18938080 10.1016/j.bmcl.2008.09.106 Tyrosine-protein kinase SYK 2
18938080 10.1016/j.bmcl.2008.09.106 Tyrosine-protein kinase ZAP-70 1
18938080 10.1016/j.bmcl.2008.09.106 Proto-oncogene tyrosine-protein kinase Src 1
18938080 10.1016/j.bmcl.2008.09.106 Unchecked 1
18938080 10.1016/j.bmcl.2008.09.106 Cyclin-dependent kinase 2 1
18938080 10.1016/j.bmcl.2008.09.106 Liver microsomes 1

Data from ChEMBL 36 via Core Engine