General
Preferred name
PIK-75
Synonyms
PIK-75 Hydrochloride ()
PIK 75 hydrochloride ()
PIK-75 (hydrochloride) ()
PIK-75 HCl ()
P&D ID
PD016738
CAS
372196-77-5
945619-31-8
372196-67-3
Tags
available
drug candidate
Drug indication
Discovery agent
Drug Status
investigational
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 PIK-75 hydrochloride is a reversible DNA-PK and p110¦Á-selective inhibitor, which inhibits DNA-PK, p110¦Á and p110¦Ã with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110¦Á >200-fold more potently than p110¦Â (IC50=1.3 ¦ÌM)[1][2]. PIK-75 hydrochloride induces apoptosis[3].
DESCRIPTION The discovery of PIK-75 is described by Hayakawa et al. (2007) , where it is compound 8c. (GtoPdb)
DESCRIPTION PIK-75 is a reversible DNA-PK and p110¦Á-selective inhibitor, which inhibits DNA-PK, p110¦Á and p110¦Ã with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110¦Á >200-fold more potently than p110¦Â (IC50=1.3 ¦ÌM)[1][2]. PIK-75 induces apoptosis[3].
PRICE 49
DESCRIPTION PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110??(IC50=5.8 nM) and p110??(IC50=76 nM).
DESCRIPTION PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM). (TargetMol Bioactive Compound Library)
Cell lines
7
Organisms
1
Compound Sets
16
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
MedChem Express Bioactive Compound Library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
ZINC Tool Compounds
External IDs
33
Properties
(calculated by RDKit )
Molecular Weight
450.99
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
0
Rotatable Bonds
5
Ring Count
3
Aromatic Ring Count
3
cLogP
2.97
TPSA
110.18
Fraction CSP3
0.12
Chiral centers
0.0
Largest ring
6.0
QED
0.34
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
Apoptosis
DNA-PK
p110α
p110β
p110γ
p110δ
PI3K
p110¦Á
p110¦Â
p110¦Ã
p110¦Ä
PIK3CA, PIK3CB, PIK3CD, PIK3CG, PRKDC
PI3K p110a inhibitor
DNA-PK,PI3K
MOA
DNA-PK inhibitor
PI3K inhibitor
DNA protein kinase inhibitor, PI3K inhibitor
Pathway
Cell Cycle/DNA Damage
PI3K/Akt/mTOR
DNA Damage/DNA Repair
PI3K/Akt/mTOR signaling
Source data