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Compound Detail

CHEMBL447132

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CN(C(=O)c1ccccc1)c1ccc2c(c1)[nH]/c(=N\C(=O)c1ccc(/C=C/c3ccccc3C(F)(F)F)s1)n2CCC(N)=O

Basic Information

ChEMBL ID CHEMBL447132
Phase Preclinical
Structure Type MOL
InChI Key NJRJGBUJDGGQDQ-ACCUITESSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

617.6
MW (Da)
6.11
ALogP
5
HBA
2
HBD
113.5
PSA (Ų)
0.22
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H26F3N5O3S
MW 617.65
Aromatic Rings 5
Heavy Atoms 44
NP-Likeness -1.54

Activity Summary

IC50 1 meas. best 6.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase ITK/TSK
CHEMBL2959
IC50 6.57 6.57 270.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase ITK/TSK IC50 = 270.0 nM 6.57 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