General
Preferred name
OF-1
Synonyms
OF 1 ()
OF1 ()
P&D ID
PD000014
CAS
919973-83-4
Tags
available
probe
drug candidate
Drug indication
Discovery agent
Probe info
Probe type
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
5
No orthogonal probes found
Similar probes
2
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
OF-1 is a small molecule inhibitor of the bromodomain proteins BRPF1/2/3 and is one of the chemical tools in the Structural Genomics Consortium's Epigenetic Probes Library. BRPF1/2/3 provide the scaffold for the formation of MYST complexes which play essential functions in DNA repair, recombination, replication and activation of transcription.
(GtoPdb)
DESCRIPTION
Selective BRPF1B and BRPF2 inhibitor
(Tocriscreen Plus)
DESCRIPTION
Deoxyadenosine analog; pro-apoptotic
(Tocris Bioactive Compound Library)
DESCRIPTION
OF-1 is the potent and selective BRPF (BRomodomain and PHD Finger containing) inhibitor with Kd values 100 nM, 500 nM, and 2.4 μM for BRPF1B, BRPF2, and BRPF3, respectively. Selectivity against other bromodomains is very good, in general >100-fold. OF-1 increases thermal stability in the cellular thermal shift assay (CETSA) of full length BRPF1B at 1 µM and also demonstrates accelerated FRAP recovery at 5 µM in the BRPF2 FRAP assay.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
19
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Bromodomains chemical toolbox
Cayman Chemical Bioactives
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
High-quality chemical probes
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
Selleckchem Bioactive Compound Library
SGC Probes
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
15
Molecular Weight
439.02
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
1
Rotatable Bonds
4
Ring Count
3
Aromatic Ring Count
3
cLogP
2.76
TPSA
82.33
Fraction CSP3
0.24
Chiral centers
0.0
Largest ring
6.0
QED
0.68
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Cell Biology
Pathway
Chromatin/Epigenetic
Epigenetics
Target
BRPF1B
BRPF2
BRD1
BRPF inhibitor
Epigenetic Reader Domain
BRPF1
BRPF3
Primary Target
Bromodomains
MOA
Inhibitor
BRPF1B and BRPF2 inhibitor
Bromodomain inhibitor
Member status
member
Recommended Cell Concentration
1 µM
Source data
