General
Preferred name
PRT-060318
Synonyms
PRT318 ()
P142-76 ()
PRT-060318 2HCl ()
2-{[(1R,2S)-2-aminocyclohexyl]amino}-4-[(3-methylphenyl)amino]pyrimidine-5-carboxamide ()
PRT060318 ()
P&D ID
PD004470
CAS
1194961-19-7
Tags
available
drug candidate
Drug indication
Thrombosis
Drug Status
experimental
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PRICE
104
DESCRIPTION
PRT-060318, also known as PRT318 or P142-76, is a novel selective inhibitor of the tyrosine kinase Syk, as an approach to HIT treatment. PRT318 completely inhibited HIT immune complex-induced aggregation of both human and transgenic HIT mouse platelets. Transgenic HIT model mice were treated with KKO, a mouse monoclonal HIT-like antibody, and heparin. The experimental group received orally dosed PRT318, whereas the control group received vehicle. Nadir platelet counts of PRT318-treated mice were significantly higher than those of control mice. When examined with a novel thrombosis visualization technique, mice treated with PRT318 had significantly reduced thrombosis. The Syk inhibitor PRT318 thus prevented both HIT immune complex-induced thrombocytopenia and thrombosis in vivo, demonstrating its activity in HIT.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
PRT-060318 (P142-76) is a novel selective inhibitor of the Syk tyrosine kinase, as an approach to HIT treatment.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
0
Compound Sets
8
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
DrugBank
DrugMAP
MedChem Express Bioactive Compound Library
Other bioactive compounds
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
20
Molecular Weight
340.2
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
4
Rotatable Bonds
5
Ring Count
3
Aromatic Ring Count
2
cLogP
2.31
TPSA
118.95
Fraction CSP3
0.39
Chiral centers
2.0
Largest ring
6.0
QED
0.66
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
SYK
Pathway
Angiogenesis
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
Source data
