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Compound Detail

CHEMBL470175

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Oc1cc(Nc2nccc(-c3nccs3)n2)cc(C(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL470175
Phase Preclinical
Structure Type MOL
InChI Key LDMSFYNGFVTKRW-UHFFFAOYSA-N
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

338.3
MW (Da)
4.07
ALogP
6
HBA
2
HBD
70.9
PSA (Ų)
0.75
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 C14H9F3N4OS
MW 338.31
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -1.47

Activity Summary

Ki 4 meas. best 7.36
IC50 1 meas. best 6.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase SYK
CHEMBL2599
Ki 7.36 7.36 44.0 1
Tyrosine-protein kinase SYK
CHEMBL2599
IC50 6.39 6.39 410.0 1
Tyrosine-protein kinase ZAP-70
CHEMBL2803
Ki 6.12 6.12 754.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
Ki 6.0 6.0 991.0 1
Cyclin-dependent kinase 2
CHEMBL301
Ki 5.78 5.78 1652.0 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