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Compound Detail

CHEMBL470780

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Cc1cc(C)cc(Nc2nccc(-c3ncc(C)s3)n2)c1

Basic Information

ChEMBL ID CHEMBL470780
Phase Preclinical
Structure Type MOL
InChI Key LZQTVVQZQUWSAI-UHFFFAOYSA-N
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

296.4
MW (Da)
4.27
ALogP
5
HBA
1
HBD
50.7
PSA (Ų)
0.78
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H16N4S
MW 296.40
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -1.63

Activity Summary

Ki 4 meas. best 7.64
IC50 1 meas. best 6.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase SYK
CHEMBL2599
Ki 7.64 7.64 23.0 1
Tyrosine-protein kinase SYK
CHEMBL2599
IC50 6.7 6.7 200.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
Ki 6.46 6.46 348.0 1
Tyrosine-protein kinase ZAP-70
CHEMBL2803
Ki 6.39 6.39 410.0 1
Cyclin-dependent kinase 2
CHEMBL301
Ki 5.96 5.96 1100.0 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