General
Preferred name
TALMAPIMOD
Synonyms
SCIO 469 hydrochloride ()
SCIO-469 ()
SCIO 469 ()
Talmapimod hydrochloride ()
P&D ID
PD016638
CAS
309913-83-5
Tags
available
drug candidate
Drug indication
Discovery agent
Multiple myeloma
Drug Status
investigational
Max Phase
2.0
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)
DESCRIPTION
Talmapimod is an orally bioavailable, investigational small-molecule p38 mitogen-activated protein kinase (MAPK) inhibitor with potential immunomodulating, anti-inflammatory, and antineoplastic activities.
(GtoPdb)
DESCRIPTION
Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38¦Á inhibitor with an IC50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38¦Â, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs[1][2][3].
PRICE
190
DESCRIPTION
Talmapimod (SCIO-469) is a selective, orally active, ATP-competitive p38?? inhibitor with IC50 values of 9 nM for p38?? and 90 nM for p38??. Talmapimod exhibits at least 2000-fold selectivity over a panel of 20 kinases, including other MAPKs.
DESCRIPTION
Investigated for use/treatment in pain (acute or chronic) and rheumatoid arthritis.
(PKIDB)
DESCRIPTION
Talmapimod, also known as SCIO-469, is an orally bioavailable, small-molecule, p38 mitogen-activated protein kinase (MAPK) inhibitor with potential immunomodulating, anti-inflammatory, and antineoplastic activities. Talmapimod specifically binds to and inhibits the phosphorylation of p38 MAPK, which may result in the induction of tumor cell apoptosis, the inhibition of tumor cell proliferation, and the inhibition of tumor angiogenesis. This agent may also enhance proteasome inhibitor-induced apoptosis. p38 MAPK is a serine/threonine protein kinase involved in a MAPK signaling cascade that controls cellular responses to various environmental stresses, cytokines, and endotoxins.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Talmapimod (SCIO-469) is a selective, orally active, ATP-competitive p38α inhibitor with IC50 values of 9 nM for p38α and 90 nM for p38β. Talmapimod exhibits at least 2000-fold selectivity over a panel of 20 kinases, including other MAPKs.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Human hematopoietic prostaglandin D synthase (H-PGDS) inhibitor
(Tocris Bioactive Compound Library)
DESCRIPTION
Selective p38 MAPK inhibitor
(Tocriscreen Plus)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
0
Compound Sets
18
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Clinical kinase drugs
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
PKIDB
ReFrame library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
39
Molecular Weight
512.2
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
0
Rotatable Bonds
5
Ring Count
4
Aromatic Ring Count
3
cLogP
3.98
TPSA
65.86
Fraction CSP3
0.37
Chiral centers
2.0
Largest ring
6.0
QED
0.38
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Enzymes
Target
Autophagy
p38 MAPK
p38α
p38β
IL1B, MAPK11, MAPK14, MT-CO2, TNF
p38a MAPK inhibitor
MAPK14
Targets
MAPK14,MAPK11,MAPK12,MAPK13
MOA
Inhibitor
p38 MAPK inhibitor
Pathway
MAPK/ERK Pathway
MAPK
Source data
