General
Preferred name
Lck Inhibitor
Synonyms
TC-S 7003 ()
P&D ID
PD013011
CAS
847950-09-8
Tags
available
drug candidate
Drug indication
Discovery agent
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis[1].
PRICE 195
DESCRIPTION Serum- and glucocorticoid-regulated kinase (SGK) inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Potent Lck inhibitor (Tocriscreen Plus)
DESCRIPTION Lck Inhibitor is a small-molecule inhibitor. It takes participate in the T-cell receptor (TCR) signal transduction and affects the expression of genes associated with cell proliferation, cytokine release and T-cell survival. It has been designed and developed as therapeutic agents for the treatment for T-cell-mediated autoimmune and organ transplant rejection. It showed high selectivity against Lck over another Src family kinase Src and the kinases. It also showed more than 1000-fold greater selectivity over CDK, MAPK and the RSK family. (BOC Sciences Bioactive Compounds)
DESCRIPTION TC-S 7003 (Lck Inhibitor) is an orally active, selective and potent lymphocyte kinase (Lck) inhibitor with anti-inflammatory activity, inhibition of Lck, Lyn, Src, and Syk kinases, and inhibition of T-cell proliferation, and may be useful in the study of arthritis. (TargetMol Bioactive Compound Library)
Cell lines
3
Organisms
0
Compound Sets
7
BOC Sciences Bioactive Compounds
Drug Repurposing Hub
DrugMAP
MedChem Express Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
External IDs
14
Properties
(calculated by RDKit )
Molecular Weight
530.25
Hydrogen Bond Acceptors
9
Hydrogen Bond Donors
1
Rotatable Bonds
4
Ring Count
7
Aromatic Ring Count
6
cLogP
4.69
TPSA
83.59
Fraction CSP3
0.23
Chiral centers
0.0
Largest ring
6.0
QED
0.35
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
SRC
LCK
Lyn
SYK
Target Type
Enzymes
Primary Target
Src Kinases
MOA
Inhibitor
Src inhibitor
Pathway
Angiogenesis
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
Source data