General
Preferred name
BI-7273
Synonyms
BI 7273 ()
P&D ID
PD049397
CAS
1883429-21-7
Tags
available
free of charge
probe
drug candidate
Drug indication
Acute myeloid leukaemia
Probe info
Probe type
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Orthogonal probes
4
No orthogonal probes found
Similar probes
3
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
BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM.
PRICE
100
DESCRIPTION
BI-7273 (compound 1 in PMID: 26914985}, is a selective BRD9 inhibitor tool compound .
(GtoPdb)
DESCRIPTION
BI-7273 was developed in collaboration with the Structural Genomics Consortium (SGC). The potent dual BRD7/BRD9 inhibitor shows 30-fold better potency in the BRD7 AlphaScreen assay compared to our more selective BRD9 inhibitor BI-9564.
BI-7273 binds with high affinity to BRD9 and BRD7 (IC50(BRD9, AlphaScreen) = 19 nM; IC50(BRD7, AlphaScreen) = 117 nM) and is selective versus other BET family members (> 100 µM AlphaScreen). Binding affinity to CECR2 as the only off-target (IC50 (ITC) = 187 nM).
It shows good ADME parameters which make it a suitable probe compound for in vitro and in vivo experiments.1 The negative control BI-6354 is recommended for in vitro experiments.
(opnMe Portal)
DESCRIPTION
BI-7273 is a potent BRD9 bromodomain inhibitor (Ki = 15.4 nM; IC50 = 19 nM). BI-7273 structurally related BRD7 bromodomain (IC50 = 117 nM) without effect against the BRD2 and BRD4 bromodomain or a panel of kinases. BI-7273 has potential for use in treating acute myeloid leukemia according to a study in vitro (EC50 = 1.4 µM).
(BOC Sciences Bioactive Compounds)
DESCRIPTION
BI-7273 is an effective, specific, BRD9 BD Inhibitor, which can infiltrate cell.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
3
Organisms
0
Compound Sets
13
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
CZ-OPENSCREEN Bioactive Library
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
High-quality chemical probes
MedChem Express Bioactive Compound Library
opnMe Portal
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
14
Molecular Weight
353.17
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
0
Rotatable Bonds
5
Ring Count
3
Aromatic Ring Count
3
cLogP
2.68
TPSA
56.59
Fraction CSP3
0.3
Chiral centers
0.0
Largest ring
6.0
QED
0.71
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
BRD7
BRD9
Epigenetic Reader Domain
BRD7/BRD9
Pathway
Epigenetics
Chromatin/Epigenetic
Solubility
Soluble in DMSO, Ethanol
Recommended Cell Concentration
None
Source data
