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Compound Detail

CHEMBL208901

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COc1cc(C)c(Sc2cnc(NC(=O)C3CC3)s2)cc1C(=O)N1CCN(C(=O)CN(C)C)CC1

Basic Information

ChEMBL ID CHEMBL208901
Phase Preclinical
Structure Type MOL
InChI Key AAFLHABTMIJIEE-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

517.7
MW (Da)
2.81
ALogP
8
HBA
1
HBD
95.1
PSA (Ų)
0.58
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H31N5O4S2
MW 517.68
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -1.66

Activity Summary

IC50 2 meas. best 7.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase ITK/TSK
CHEMBL2959
IC50 7.72 7.72 19.0 1
Jurkat
CHEMBL397
IC50 6.68 6.68 210.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase ITK/TSK IC50 = 19.0 nM 7.72 Inhibition of Itk 16682193
Jurkat IC50 = 210.0 nM 6.68 Inhibition of IL2 production in Jurkat T cells 16682193

Literature References

PubMed DOI Target Context # Activities
16682193 10.1016/j.bmcl.2006.04.060 Mus musculus 1
16682193 10.1016/j.bmcl.2006.04.060 Jurkat 1
16682193 10.1016/j.bmcl.2006.04.060 Tyrosine-protein kinase ITK/TSK 1

Data from ChEMBL 36 via Core Engine