General
Preferred name
Onvansertib
Synonyms
NMS-P937 ()
NMS-1286937 ()
NMS1286937 ()
PCM-075 ()
PCM-075, NMS1286937 ()
Onvansertib (NMS-P937) ()
ONVANSERTIB FUMARATE ()
Nms-p937 fumarate ()
PMS-075H ()
Nms-p937 fumarate salt ()
Pcm-075 fumarate ()
P&D ID
PD012524
CAS
1034616-18-6
Tags
available
probe
drug candidate
Drug indication
Acute myeloid leukaemia
Neoplasm
Prostate cancer
Solid tumour/cancer
Drug Status
investigational
Max Phase
2.0
1.0
Probe info
Probe type
calculated probe
Probe selectivity
protein-selective
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
49
No orthogonal probes found
Similar probes
24
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
Onvansertib (NMS-P937) is an orally available, selective polo-like kinase 1 (PLK1) inhibitor. Its discovery is described in , where it is compound 7g.
(GtoPdb)
DESCRIPTION
NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC50 of 2 nM.
PRICE
91
DESCRIPTION
NMS1286937, also know as NMS-P937, is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor NMS-1286937 selectively inhibits PLK1, inducing selective G2/M cell-cycle arrest followed by apoptosis in a variety of tumor cells while causing reversible cell-cycle arrest at the G1 and G2 stages without apoptosis in normal cells. PLK1 inhibition may result in the inhibition of proliferation in PLK1-overexpressing tumor cells. PLK1 is a serine/threonine protein kinase crucial in the regulation of mitosis.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Onvansertib (NMS-1286937) is a PLK1 inhibitor (IC50=2 nM) with high selectivity and oral activity. Onvansertib has antitumor activity and inhibits tumor growth.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
159
Organisms
0
Compound Sets
16
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
LINCS compound set
MedChem Express Bioactive Compound Library
PKIDB
Probe Miner (suitable probes)
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
28
Molecular Weight
532.22
Hydrogen Bond Acceptors
10
Hydrogen Bond Donors
3
Rotatable Bonds
7
Ring Count
5
Aromatic Ring Count
3
cLogP
1.92
TPSA
134.66
Fraction CSP3
0.42
Chiral centers
0.0
Largest ring
6.0
QED
0.42
Structural alerts
1
anil_di_alk_C(246)
c:1:c:c(:c:c:c:1-[#8]-[#6;X4])-[#7;$([#7!H0]-[#6;X4]),$([#7](-[#6;X4])-[#6;X4])]
PAINS Family A
Related compounds
Custom attributes
(extracted from source data)
Target
Apoptosis
PLK
PLK1
PLK2
PLK3
FLT3, PLK1, PLK2, PLK3
Polo-like Kinase (PLK)
Apoptosis related,PLK
MOA
PLK inhibitor
Pathway
Cell Cycle/DNA Damage
Cell Cycle/Checkpoint
Recommended Cell Concentration
100 nM
Source data
