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Compound Detail

CHEMBL444394

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COc1ccc(/C=C/c2ccc(C(=O)/N=c3\[nH]c4cc(N(C)C(=O)c5ccccc5)ccc4n3CCC(N)=O)s2)cc1

Basic Information

ChEMBL ID CHEMBL444394
Phase Preclinical
Structure Type MOL
InChI Key WZSMWQDFBNKCKK-GXDHUFHOSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

579.7
MW (Da)
5.10
ALogP
6
HBA
2
HBD
122.8
PSA (Ų)
0.25
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H29N5O4S
MW 579.68
Aromatic Rings 5
Heavy Atoms 42
NP-Likeness -1.36

Activity Summary

IC50 1 meas. best 7.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase ITK/TSK
CHEMBL2959
IC50 7.24 7.24 58.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase ITK/TSK IC50 = 58.0 nM 7.24 Inhibition of ITK by DELPHIA 18930400

Literature References

PubMed DOI Target Context # Activities
18930400 10.1016/j.bmcl.2008.09.098 Tyrosine-protein kinase ITK/TSK 2
18930400 10.1016/j.bmcl.2008.09.098 Insulin receptor 1

Data from ChEMBL 36 via Core Engine