General
Preferred name
UNC1215
Synonyms
UNC 1215 ()
P&D ID
PD000005
CAS
1415800-43-9
Tags
available
probe
drug candidate
Drug indication
Discovery agent
Probe info
Probe type
calculated probe
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
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)
COMMENT
As of June 2016, this is the first and only potent and selective inhibitor of L3MBTL3 with activity in cells. This looks like a good compound to probe this target's disease relevance and biology. The authors have characterized its off target activities as comprehensively as can be expected, including kinases, secondary pharmacology, epigenetic enzyme panels and cellular target pull-down experiments, and the data supports UNC1215 as a potent and selective inhibitor. Jun 30 2016 - 4:40am; This probe seems to have a very nice selectivity towards L3MBTL3. UNC1215 is nontoxic at concentration well above the EC50. Jun 30 2016 - 4:40am
DESCRIPTION
UNC1215 was delevoped in a collaboration between the SGC (Structural Genomics Consortium) and the Center for Integrative Chemical Biology and Drug Discovery (CICBDD) at The University of North Carolina. It is the first chemical probe for a Kme (methyl-lysine recognition domain)-binding protein. UNC1215 is reported to be a potent and selective modulator of the Kme reading function of L3MBTL3, a member of the malignant brain tumor (MBT) family of chromatin interacting transcriptional repressors . Click here to link to the SGC's full list of epigenetics probes.
(GtoPdb)
DESCRIPTION
UNC1215 is a potent and selective inhibitor for the methyllysine (Kme) reading domain function of L3MBTL3 with a Kd value of 120 nM and an IC50 of 40 nM. UNC1215 has the potential to treat malignant brain tumor.
PRICE
101
MOA
Inhibitor
(Chemical Probes.org)
DESCRIPTION
UNC1215, an effective and specific MBT (malignant brain tumor) antagonist, binds L3MBTL3 (IC50/Kd: 40/120 nM). The selectivity of UNC1215 for L3MBTL3 is 50-fold higher versus other members of the human MBT family.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
26
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
Chemical Probes.org
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
High-quality chemical probes
IPPI - DB
LINCS compound set
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
Nature Chemical Biology Probes
Novartis Chemogenetic Library (NIBR MoA Box)
Selleckchem Bioactive Compound Library
SGC Probes
TargetMol Bioactive Compound Library
Tool Compound Set
Welcome Trust Cancer Drugs
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
18
Molecular Weight
529.34
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
6
Ring Count
6
Aromatic Ring Count
2
cLogP
4.83
TPSA
59.13
Fraction CSP3
0.56
Chiral centers
0.0
Largest ring
6.0
QED
0.58
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
L3MBTL3
Lethal(3)malignant brain tumor-like protein 3
Apoptosis
Histone methyltransferase
L3MBTL3-D274A
Epigenetic Reader Domain
Member status
member
MOA
L3MBTL3 inhibitor
L3MBTL3 reader domain inhibitor
L3MBTL antagonist
Target class
Epigenetics
Epigenetic
Pathway
Chromatin/Epigenetic
Protein Family
Methyl Lysine Binder
Target subclass
Malignant brain tumor Reader
Control
UNC1079
Recommended Cell Concentration
1 uM
Source data
