General
Preferred name
BIRABRESIB
Synonyms
OTX-015 ()
OTX015 (MK 8628/Birabresib) ()
MK-8628 ()
OTX 015 ()
OTX015 £¨MK 8628/Birabresib£© ()
OTX015 ()
MK 8628 ()
Birabresib (OTX015) ()
Y-803 anhydrous ()
OTX015 ANHYDROUS ()
OTX-015 ANHYDROUS ()
P&D ID
PD012534
CAS
202590-98-5
Tags
available
drug candidate
Drug indication
Solid tumour/cancer
Acute myeloid leukaemia
Glioblastoma multiforme
Myelodysplastic syndrome
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
Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM.
PRICE
86
DESCRIPTION
OTX015 inhibits interaction between bromodomain and extra-terminal (BET) family of bromodomain-containing proteins (BRDs) BET domains and acetylated histone 4 (AcH4). It is an orally available novel BRD2/3/4 inhibitor with potent preclinical anti-tumour activity . OTX015 is an analogue of .
(GtoPdb)
DESCRIPTION
Birabresib (MK-8628) is a synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic activity.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Potent and selective BRPF1 inhibitor
(Tocris Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
31
Organisms
0
Compound Sets
14
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
MedChem Express Bioactive Compound Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
26
Molecular Weight
491.12
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
2
Rotatable Bonds
4
Ring Count
5
Aromatic Ring Count
4
cLogP
5.53
TPSA
92.4
Fraction CSP3
0.2
Chiral centers
1.0
Largest ring
7.0
QED
0.37
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
BRDs
Epigenetic Reader Domain
BRD2, BRD3, BRD4
BET-BRD inhibitor
Epigenetic Reader Domain,NSD
Primary Target
Bromodomains
MOA
Inhibitor
Bromodomain inhibitor
Pathway
Epigenetics
Chromatin/Epigenetic
Source data
