General
Preferred name
AZD-6482
Synonyms
AZD6482 ()
AZD 6482 ()
KIN001-193 ()
WO2009093972 ()
KIN 193 ()
4urk ()
KIN-193 ()
Azd 6482 ()
P&D ID
PD003410
CAS
1173900-33-8
173900-33-8
Tags
available
drug candidate
probe
Drug indication
Thrombosis
Drug Status
investigational
Max Phase
Phase 2
Probe info
Probe selectivity
family-selective
Probe type
P&D approved
experimental probe
Probe sources
Chemical Probes.org
High-quality chemical probes
Probe targets
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 AZD6482 is an inhibitor of phosphatidylinositol-3 kinase activity with selectivity for the β isozyme . (GtoPdb)
COMMENT Given that the profiling data available at this point uses an in vitro affinity binding assay that does not use ATP, it is difficult to assess the intracellular selectivity profile (which may very well be even better). That said, the probe appears to have decent selectivity within and outside the PI3K family. The fact that the probe appears to be selectively active against tumours driven by PTEN loss, only when they do not also have a p110 alpha activating mutation, adds to the promise and utility of this probe. Highest utility is likely to be in systems with low expression of, and biological process dependence on, the delta and gamma isoforms. Nov 23 2020 - 8:53am; AZ6482 is a highly selective and potent chemical probe for PI3Kbeta. It is suitable for study the role of the target in model cell systems and animal studies. Dec 8 2020 - 10:10am; AZD-6482 is a suitable chemical probe for assessing PIK3CB (PI3Kbeta) function. The compound is 8-fold selective over PI3Kdelta in in vitro assays and so care should be taken when used in cellular studies to differentiate PI3Kbeta from PI3Kdelta activity in certain contexts. Dec 18 2020 - 10:17am
MOA Inhibitor, ATP competitive (Chemical Probes.org)
DESCRIPTION inhibitor of PI3K catalytic subunits beta and delta (Informer Set)
DESCRIPTION Potent and selective PI 3-Kbeta inhibitor (Tocriscreen Plus)
DESCRIPTION Dual DNA-PK and PI 3-K inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION AZD6482 is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ. Phase 1. (BOC Sciences Bioactive Compounds)
Cell lines
583
Organisms
0
Compound Sets
28
AdooQ Bioactive Compound Library
A10112
Axon Medchem Screening Library
2926
BOC Sciences Bioactive Compounds
azd6482-cas-1173900-33-8-item-84-161512
Cayman Chemical Bioactives
15250
ChEMBL Drugs
CHEMBL2165191
Chemical Probes.org
azd-6482
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
8059
Concise Guide to Pharmacology 2019/20
8059
Concise Guide to Pharmacology 2021/22
8059
Concise Guide to Pharmacology 2023/24
8059
Drug Repurposing Hub
DrugBank
DB14980
DrugMAP
DMVP4E5
EU-OPENSCREEN Bioactive Compound Library
EOS101483
Guide to Pharmacology
8059
High-quality chemical probes
PD003410
Informer Set
639390
Kinase Inhibitors (best-in-class)
LINCS compound set
10059-101
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL2165191
MedChem Express Bioactive Compound Library
HY-10344
ReFrame library
Selleckchem Bioactive Compound Library
azd6482
TargetMol Bioactive Compound Library
T6087
Tocris Bioactive Compound Library
4839
Tocriscreen Plus
4839
Welcome Trust Cancer Drugs
1066
156
External IDs
27
Properties
(calculated by RDKit )
Molecular Weight
408.18
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
4
Aromatic Ring Count
3
cLogP
2.71
TPSA
96.17
Fraction CSP3
0.32
Chiral centers
1.0
Largest ring
6.0
QED
0.67
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
PIK3CB
PIK3CD
PI3K beta (P3C2B)
PI3Kβ
DNA-PK
PI3K??
PIK3CA, PIK3CB, PIK3CD, PIK3CG
PI3K p110ß inhibitor
PI3K
Compound status
clinical
Target Type
Enzymes
Pathway
PI3K signaling
DNA Damage/DNA Repair
PI3K/Akt/mTOR signaling
Autophagy
PI3K/Akt/mTOR
Kinase group
Lipid
Primary Target
PI 3-kinase
MOA
Inhibitor
PI3K inhibitor
Target class
Lipid kinase
Target subclass
Class I
Source data