General
Preferred name
molibresib
Synonyms
GSK525762A ()
I-BET-762 ()
I-BET 762 besylate ()
GSK 525762A ()
I-BET ()
GSK525762 ()
I-BET 762 ()
GSK-525762A ()
GSK-525762 ()
Molibresib (besylate) ()
GSK 525762C ()
I-BET 762 (besylate) ()
I-BET762 ()
GSK525762, GSK525762A ()
Molibresib (I-BET-762) ()
Molibresib besylate ()
Bet inhibitor gsk525762 ()
GSK525762C ()
GSK-525762C ()
P&D ID
PD003552
CAS
1260907-17-2
1895049-20-3
Tags
available
drug candidate
Drug indication
Haematological malignancy
Carcinoma
Solid tumour/cancer
Drug Status
investigational
Max Phase
2.0
1.0
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
I-BET compounds are acetyl histone mimetics.
DESCRIPTION
I-BET compounds such as molibresib are acetyl histone mimetics.
According to GSK's pipeline web resource they have terminated development of molibresib in cancer, as their emerging data did not support progression. (GtoPdb)
According to GSK's pipeline web resource they have terminated development of molibresib in cancer, as their emerging data did not support progression. (GtoPdb)
DESCRIPTION
Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
PRICE
114
DESCRIPTION
Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
PRICE
1000
DESCRIPTION
Molibresib besylate (GSK 525762C) is a selective and potent inhibitor of the bromodomain and extra-terminal (BET) family of proteins with potential anticancer activity for the study of refractory hematologic malignant diseases.Molibresib besylate generates reactive oxygen species (ROS), which potentiate ATM activation.
DESCRIPTION
inhibitor of bromodomain (BRD) and extra-C terminal domain (BET) proteins
(Informer Set)
DESCRIPTION
Inhibitor of Hedgehog (Hh) signaling; inhibits cytoplasmic dynein
(Tocris Bioactive Compound Library)
DESCRIPTION
Molibresib (GSK525762) is an inhibitor of BET proteins (IC50: about 35 nM).
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
11
Organisms
1
Compound Sets
19
ChEMBL Drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
Informer Set
IPPI - DB
LINCS compound set
Mcule NIBR MoA Box Subset
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Welcome Trust Cancer Drugs
ZINC Tool Compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
38
Molecular Weight
423.15
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
1
Rotatable Bonds
5
Ring Count
4
Aromatic Ring Count
3
cLogP
3.66
TPSA
81.4
Fraction CSP3
0.27
Chiral centers
1.0
Largest ring
7.0
QED
0.68
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
BRD2
BRD3
BRD4
BRD2, BRD3, BRD4
BET proteins
Epigenetic Reader Domain
Compound status
probe
Pathway
chromatin other
Epigenetics
Chromatin/Epigenetic
Primary Target
Bromodomains
MOA
Inhibitor
BRD2/3/4/T BET familiy inhibitor
Bromodomain inhibitor
Member status
virtual
Source data
