General
Preferred name
TAK-715
Synonyms
KIN001-201 ()
TPKI-107 ()
TAK715 ()
TAK 715 ()
P&D ID
PD010510
CAS
303162-79-0
Tags
available
drug candidate
Drug indication
Rheumatoid arthritis
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
TAK-715 was developed as a p38 MAP kinase inhibitor, with anti-TNFα activity of potential clinical use as an anti-rheumatoid arthritis (RA) agent . TAK-715 is now available for repurposing via the MRC-Industry Asset Sharing Initiative 2016 (full compound list).
(GtoPdb)
DESCRIPTION
TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38¦Á and p38¦Â, respectively. TAK-715 inhibits casein kinase I (CK1¦Ä/¦Å) to regulate activation of Wnt/¦Â-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model[1][2].
PRICE
91
DESCRIPTION
TAK-715 is a p38 MAPK inhibitor for p38??.
DESCRIPTION
TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
TAK-715 is a p38 MAPK inhibitor for p38α.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
0
Compound Sets
20
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
Kinase Chemogenomic Set (KCGS 08/2017, in progress)
LINCS compound set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Welcome Trust Cancer Drugs
ZINC Tool Compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
28
Molecular Weight
399.14
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
1
Rotatable Bonds
5
Ring Count
4
Aromatic Ring Count
4
cLogP
6.0
TPSA
54.88
Fraction CSP3
0.12
Chiral centers
0.0
Largest ring
6.0
QED
0.45
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
JNK and p38 signaling
MAPK
Metabolism
Stem Cells
Cell Cycle/DNA Damage
MAPK/ERK Pathway
Stem Cell/Wnt
Target
p38a
Autophagy
Casein kinase
JNK1
p38 MAPK
p38α
p38β
p38γ
p38δ
MAPK14
Wnt
MOA
p38 MAPK inhibitor
Recommended Cell Concentration
None
Source data
