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Compound Detail

CHEMBL519388

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C/C(=C\C#N)c1ccc(C(=O)/N=c2\[nH]c3cc(N(C)C(=O)c4ccccc4)ccc3n2CCC(N)=O)s1

Basic Information

ChEMBL ID CHEMBL519388
Phase Preclinical
Structure Type MOL
InChI Key CVIBKQQGYYKXTR-SFQUDFHCSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

512.6
MW (Da)
3.85
ALogP
6
HBA
2
HBD
137.3
PSA (Ų)
0.36
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H24N6O3S
MW 512.60
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.38

Activity Summary

IC50 3 meas. best 7.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase ITK/TSK
CHEMBL2959
IC50 7.2 6.87 63.0 2
Insulin receptor
CHEMBL1981
IC50 5.35 5.35 4500.0 1

Activity Data Samples

Top measurements by pChEMBL value

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