General
Preferred name
AFURESERTIB
Synonyms
GSK 2110183B ()
GSK2110183B, Afuresertib, GSK2110183, GSK2110183C, Afuresertib HCl ()
GSK-2110183 ()
GSK2110183C ()
GSK2110183 ()
GSK 2110183 hydrochloride ()
Afuresertib (hydrochloride) ()
GSK2110183 (hydrochloride) ()
LAE002 (hydrochloride) ()
LAE002 ()
Afuresertib (GSK2110183) ()
AFURESERTIB HYDROCHLORIDE ()
ASB-183 ()
ASB183 ()
GSK-2110183C ()
GSK2110183B ()
GSK-2110183B ()
P&D ID
PD012538
CAS
1047644-62-1
1047645-82-8
Tags
available
drug candidate
Drug indication
Neoplasm
Multiple myeloma
leukaemia
Solid tumour/cancer
Drug Status
investigational
Max Phase
3.0
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
Afuresertib (GSK2110183) is an inhibitor of the AKT family of protein kinases in clincal trials for cancer. Note that in previous releases we had mistakenly linked the structure of GSK2141795 characterised in the same paper (PubChem CID 57826797) that has an extra fluorine in the terminal ring (n.b. several vendors in PubChem still have this name-to-structure error)
(GtoPdb)
DESCRIPTION
Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively[1][2].
PRICE
90
DESCRIPTION
Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively[1][2].
PRICE
91
DESCRIPTION
Afuresertib, also known as GSK2110183, is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor GSK2110183 binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Afuresertib hydrochloride is an inhibitor of Akt kinase (Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively)
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
17
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Clinical kinase drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
JUMP-Target 1 Compound Set
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
41
Molecular Weight
426.05
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
2
Rotatable Bonds
6
Ring Count
3
Aromatic Ring Count
3
cLogP
3.89
TPSA
72.94
Fraction CSP3
0.22
Chiral centers
1.0
Largest ring
6.0
QED
0.63
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Targets
AKT1,AKT2,AKT3
Target
Akt
AKT1
AKT2
AKT3
PKC
ROCK
AKT1, AKT2, AKT3
MOA
Akt inhibitor
Pathway
Cell Cycle/Checkpoint
Chromatin/Epigenetic
Cytoskeletal Signaling
PI3K/Akt/mTOR signaling
Stem Cells
Cell Cycle/DNA Damage
cytoskeleton
Epigenetics
PI3K/Akt/mTOR
Stem Cell/Wnt
TGF-beta/Smad
Source data
