General
Preferred name
LGH-447
Synonyms
cpd 8 ()
5HZ ()
LGH447 ()
LGH447 dihydrochloride ()
PIM447 ()
PIM-447 (dihydrochloride) ()
NVP-LGH477 ()
PIM 447 ()
PIM-447 ()
PIM KINASE INHIBITOR LGH447 ()
P&D ID
PD076541
CAS
1210608-43-7
1820565-69-2
Tags
available
probe
drug candidate
Drug indication
Multiple myeloma
Myelofibrosis
Drug Status
investigational
Max Phase
1.0
Probe info
Probe type
experimental probe
calculated probe
Probe sources
Chemical Probes.org
High-quality chemical probes
Probe Miner (suitable probes)
Probe targets
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION PIM447 is a potent and selective pan PIM kinase inhibitor , that is being investigated for clinical efficacy against hematological malignancies. (GtoPdb)
COMMENT PIM-447 is a pan-PIM 1, 2 and 3 kinase inhibitor that demonstrates potent biochemical activity and good selectivity in a 442 kinase panel. There is a large drop off to cellular activity in both antiproliferative and biomarker assays and the contribution of each isoform to the response in the cellular environment is unknown. The cellular biomarker used, pS6RP, is indirect which should be considered when interpreting this data. PIM-447 shows a strong effect in a mouse xenograft study, with a pharmacodynamic response consistent with the in vitro data. Apart from the kinase selectivity and hERG activity, no broad pharmacological profiling data has been provided to further validate use of PIM-447 in vivo. Apr 10 2021 - 1:32pm
MOA Inhibitor (Chemical Probes.org)
Cell lines
4
Organisms
0
Compound Sets
12
ChEMBL Drugs
CHEMBL3651966
Chemical Probes.org
pim-447
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB14943
DrugMAP
DMQN9ME
DMU26OE
EUbOPEN Chemogenomics Library
EUB0001581
Guide to Pharmacology
9790
High-quality chemical probes
PD076541
MedChem Express Bioactive Compound Library
HY-19322
HY-19322B
Novartis Chemogenetic Library (NIBR MoA Box)
Probe Miner (suitable probes)
P11309/474134
External IDs
23
Properties
(calculated by RDKit )
Molecular Weight
440.18
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
2
Rotatable Bonds
4
Ring Count
4
Aromatic Ring Count
3
cLogP
5.04
TPSA
80.9
Fraction CSP3
0.29
Chiral centers
3.0
Largest ring
6.0
QED
0.6
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Member status
virtual
MOA
Pim-1 Kinase Inhibitors
Pim-2 Kinase Inhibitors
Pim-3 Kinase Inhibitors
PIM kinase inhibitor
Target subclass
CAMK
CAMK, CAMK, CAMK
Target class
Protein kinase
Kinase, Kinase, Kinase
Orthogonal probe
SGI-1776,
Pathway
Apoptosis
JAK/STAT Signaling
Target
Pim
PIM1, PIM2, PIM3
Control
cpd 1
Recommended Cell Concentration
1 µM
Source data