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Compound Detail

CHEMBL457705

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CN(C(=O)c1ccccc1)c1ccc2c(c1)nc(NC(=O)c1ccc(C#N)nc1)n2CCC(N)=O

Basic Information

ChEMBL ID CHEMBL457705
Phase Preclinical
Structure Type MOL
InChI Key IFYQRVUSDKCLSD-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

467.5
MW (Da)
2.71
ALogP
7
HBA
2
HBD
147.0
PSA (Ų)
0.43
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H21N7O3
MW 467.49
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.86

Activity Summary

IC50 1 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase ITK/TSK
CHEMBL2959
IC50 7.64 7.64 23.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase ITK/TSK IC50 = 23.0 nM 7.64 Inhibition of recombinant ITK by DELFIA assay 18819794

Literature References

PubMed DOI Target Context # Activities
18819794 10.1016/j.bmcl.2008.09.017 Tyrosine-protein kinase ITK/TSK 1
18819794 10.1016/j.bmcl.2008.09.017 Insulin receptor 1

Data from ChEMBL 36 via Core Engine