General
Preferred name
PLX51107
Synonyms
PLX-51107 ()
PLX 51107 ()
BRD4 INHIBITOR PLX51107 ()
P&D ID
PD078462
CAS
1627929-55-8
Tags
available
drug candidate
Drug indication
Haematological malignancy
Solid tumour/cancer
Drug Status
investigational
Max Phase
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
PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range).
PRICE
179
DESCRIPTION
PLX51107 is a potent and selective BET inhibitor with modest preference for bromodomain-1 (BD1) versus bromodomain-2 (BD2). It blocks the interaction mediated by the four BET family proteins.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
PLX51107 is a potent and selective BET inhibitor with Kds of 1.6, 2.1, 1.7, and 5 nM for BRD2-BD1, BRD3-BD1, BRD4-BD1, and BRDT-BD1, respectively.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
9
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Drug Repurposing Hub
DrugMAP
EUbOPEN Chemogenomics Library
MedChem Express Bioactive Compound Library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
13
Molecular Weight
438.17
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
1
Rotatable Bonds
5
Ring Count
5
Aromatic Ring Count
5
cLogP
5.68
TPSA
94.04
Fraction CSP3
0.15
Chiral centers
1.0
Largest ring
6.0
QED
0.38
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
BET
Epigenetic Reader Domain
MOA
Bromodomain inhibitor
Pathway
Epigenetics
Chromatin/Epigenetic
Recommended Cell Concentration
1 uM
Source data
