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Compound Detail

CHEMBL210932

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CCN1CCN(C(=O)c2cc(Sc3cnc(NC(=O)C4CC4)s3)c(C)cc2OC)CC1

Basic Information

ChEMBL ID CHEMBL210932
Phase Preclinical
Structure Type MOL
InChI Key ICLTWMGTAQDABY-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

460.6
MW (Da)
3.74
ALogP
7
HBA
1
HBD
74.8
PSA (Ų)
0.68
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 C22H28N4O3S2
MW 460.63
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.78

Activity Summary

IC50 2 meas. best 6.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase ITK/TSK
CHEMBL2959
IC50 6.58 6.58 260.0 1
Jurkat
CHEMBL397
IC50 6.0 6.0 1000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase ITK/TSK IC50 = 260.0 nM 6.58 Inhibition of Itk 16682193
Jurkat IC50 = 1000.0 nM 6.0 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