gsk2879552 profile

GSK2879552: inhibits lysine demethylase 1; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

GSK2879552 : A member of the class of piperidines that is piperidine substituted by (4-carboxyphenyl)methyl and {[(1R,2S)-2-phenylcyclopropyl]amino}methyl groups at positions 1 and 4, respectively. It is a potent and irreversible inhibitor of lysine specific demethylase 1 (LSD1, also known as KDM1A). It was under clinical investigation for the treatment of acute myeloid leukaemia and small cell lung carcinoma. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

ID Source	ID
PubMed CID	66571643
CHEMBL ID	3786182
CHEBI ID	176334
SCHEMBL ID	12813936
MeSH ID	M000610780

Synonym
4-{[4-({[(1r,2s)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}benzoic acid
CHEBI:176334
gsk-2879552
gsk 2879552
1401966-69-5
gsk2879552
SCHEMBL12813936
LRULVYSBRWUVGR-FCHUYYIVSA-N
4-((4-(((trans-2-phenylcyclopropyl)amino)methyl)piperidin-1-yl)methyl)benzoic acid
CS-3997
1401966-63-9
gsk 2879552 [who-dd]
benzoic acid, 4-((4-((((1r,2s)-2-phenylcyclopropyl)amino)methyl)-1-piperidinyl)methyl)-
unii-gt77z6y09z
4-((4-((((1r,2s)-2-phenylcyclopropyl)amino)methyl)piperidin-1-yl)methyl)benzoic acid
gt77z6y09z ,
HY-18632
gtpl9116
4-[[4-[[[(1r,2s)-2-phenylcyclopropyl]amino]methyl]piperidin-1-yl]methyl]benzoic acid
example 26 [wo2012135113]
3,5,7-trihydroxy-8-(3-methyl-2-buten-1-yl)-2-[4-(trifluoromethyl)phenyl]-4h-chromen-4-one
J-690161
CHEMBL3786182 ,
EX-A1181
AKOS027324406
NCGC00387878-01
bdbm50158869
4-[[4-[[((1r,2s)-2-phenylcyclopropyl)amino]methyl]piperidin-1-yl]methyl]benzoic acid
mfcd28411435
Q27077894
gsk2879522
AMY42178
AS-56180
AC-35762
gsk-2879552 hcl
gsk2879552 hcl
nsc-783917
gsk 2879552 hcl
nsc783917
benzoic acid, 4-[[4-[[[(1r,2s)-2-phenylcyclopropyl]amino]methyl]-1-piperidinyl]methyl]-, rel-
BG170574

Excerpt	Reference	Relevance
"GSK2879552 is a potent, selective inhibitor of lysine demethylase 1A and has demonstrated favorable PK properties but provided poor disease control and a high AE rate in patients with SCLC. "	( Phase I, Open-Label, Dose-Escalation Study of the Safety, Pharmacokinetics, Pharmacodynamics, and Efficacy of GSK2879552 in Relapsed/Refractory SCLC. Ballas, MS; Bauer, TM; Besse, B; Collingwood, T; Dhar, A; Ferron-Brady, G; Garrido, P; Govindan, R; Kruger, RG; Martinez-Marti, A; Mohammad, HP; Moreno, V; Park, J; Trigo, JM; Wu, Y, 2019)	2.17

Excerpt	Reference	Relevance
" In all, 22 patients completed the study; 7 withdrew, primarily owing to adverse events (AEs)."	( Phase I, Open-Label, Dose-Escalation Study of the Safety, Pharmacokinetics, Pharmacodynamics, and Efficacy of GSK2879552 in Relapsed/Refractory SCLC. Ballas, MS; Bauer, TM; Besse, B; Collingwood, T; Dhar, A; Ferron-Brady, G; Garrido, P; Govindan, R; Kruger, RG; Martinez-Marti, A; Mohammad, HP; Moreno, V; Park, J; Trigo, JM; Wu, Y, 2019)	0.73

Excerpt	Reference	Relevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Role	Description
EC 1.14.99.66 (lysine-specific histone demethylase 1A) inhibitor	An EC 1.14.99.* (miscellaneous oxidoreductase acting on paired donors, with incorporation or reduction of molecular oxygen) inhibitor that interferes with the action of lysine-specific histone demethylase 1A (EC 1.14.99.66).
antineoplastic agent	A substance that inhibits or prevents the proliferation of neoplasms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
benzoic acids	Any aromatic carboxylic acid that consists of benzene in which at least a single hydrogen has been substituted by a carboxy group.
monocarboxylic acid	An oxoacid containing a single carboxy group.
piperidines
cyclopropanes	Cyclopropane and its derivatives formed by substitution.
tertiary amino compound	A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
secondary amino compound	A compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
benzenes	Any benzenoid aromatic compound consisting of the benzene skeleton and its substituted derivatives.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Lysine-specific histone demethylase 1A	Homo sapiens (human)	IC50 (µMol)	50.6981	0.0031	2.1602	9.6000	AID1427607; AID1459729; AID1532695; AID1572509; AID1669136; AID1755599; AID1903136; AID1903171
Lysine-specific histone demethylase 1A	Homo sapiens (human)	Ki	1.1365	0.0096	2.5442	5.6000	AID1289333; AID1669149; AID1755599
Cytochrome P450 2C9	Homo sapiens (human)	IC50 (µMol)	100.0000	0.0000	2.8005	10.0000	AID1572512
Amine oxidase [flavin-containing] A	Homo sapiens (human)	IC50 (µMol)	100.0000	0.0000	2.3789	9.7700	AID1572511; AID1903138; AID1903169
Amine oxidase [flavin-containing] B	Homo sapiens (human)	IC50 (µMol)	100.0000	0.0000	1.8914	9.5700	AID1572512; AID1903139; AID1903170
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Lysine-specific histone demethylase 1A	Homo sapiens (human)	EC50 (µMol)	0.0540	0.0540	0.0540	0.0540	AID1669135
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
regulation of double-strand break repair via homologous recombination	Lysine-specific histone demethylase 1A	Homo sapiens (human)
positive regulation of protein ubiquitination	Lysine-specific histone demethylase 1A	Homo sapiens (human)
regulation of protein localization	Lysine-specific histone demethylase 1A	Homo sapiens (human)
cellular response to UV	Lysine-specific histone demethylase 1A	Homo sapiens (human)
cellular response to gamma radiation	Lysine-specific histone demethylase 1A	Homo sapiens (human)
DNA repair-dependent chromatin remodeling	Lysine-specific histone demethylase 1A	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Lysine-specific histone demethylase 1A	Homo sapiens (human)
positive regulation of neuroblast proliferation	Lysine-specific histone demethylase 1A	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Lysine-specific histone demethylase 1A	Homo sapiens (human)
protein demethylation	Lysine-specific histone demethylase 1A	Homo sapiens (human)
positive regulation of epithelial to mesenchymal transition	Lysine-specific histone demethylase 1A	Homo sapiens (human)
positive regulation of neuron projection development	Lysine-specific histone demethylase 1A	Homo sapiens (human)
cerebral cortex development	Lysine-specific histone demethylase 1A	Homo sapiens (human)
negative regulation of protein binding	Lysine-specific histone demethylase 1A	Homo sapiens (human)
neuron maturation	Lysine-specific histone demethylase 1A	Homo sapiens (human)
negative regulation of DNA binding	Lysine-specific histone demethylase 1A	Homo sapiens (human)
negative regulation of DNA-binding transcription factor activity	Lysine-specific histone demethylase 1A	Homo sapiens (human)
negative regulation of DNA damage response, signal transduction by p53 class mediator	Lysine-specific histone demethylase 1A	Homo sapiens (human)
positive regulation of cell size	Lysine-specific histone demethylase 1A	Homo sapiens (human)
negative regulation of DNA-templated transcription	Lysine-specific histone demethylase 1A	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Lysine-specific histone demethylase 1A	Homo sapiens (human)
guanine metabolic process	Lysine-specific histone demethylase 1A	Homo sapiens (human)
muscle cell development	Lysine-specific histone demethylase 1A	Homo sapiens (human)
regulation of androgen receptor signaling pathway	Lysine-specific histone demethylase 1A	Homo sapiens (human)
response to fungicide	Lysine-specific histone demethylase 1A	Homo sapiens (human)
cellular response to cAMP	Lysine-specific histone demethylase 1A	Homo sapiens (human)
regulation of DNA methylation-dependent heterochromatin formation	Lysine-specific histone demethylase 1A	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	Lysine-specific histone demethylase 1A	Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediator	Lysine-specific histone demethylase 1A	Homo sapiens (human)
positive regulation of neural precursor cell proliferation	Lysine-specific histone demethylase 1A	Homo sapiens (human)
positive regulation of stem cell proliferation	Lysine-specific histone demethylase 1A	Homo sapiens (human)
chromatin remodeling	Lysine-specific histone demethylase 1A	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
urea metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
amide metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
icosanoid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2C9	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
biogenic amine metabolic process	Amine oxidase [flavin-containing] A	Homo sapiens (human)
positive regulation of signal transduction	Amine oxidase [flavin-containing] A	Homo sapiens (human)
dopamine catabolic process	Amine oxidase [flavin-containing] A	Homo sapiens (human)
response to xenobiotic stimulus	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to toxic substance	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to aluminum ion	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to selenium ion	Amine oxidase [flavin-containing] B	Homo sapiens (human)
negative regulation of serotonin secretion	Amine oxidase [flavin-containing] B	Homo sapiens (human)
phenylethylamine catabolic process	Amine oxidase [flavin-containing] B	Homo sapiens (human)
substantia nigra development	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to lipopolysaccharide	Amine oxidase [flavin-containing] B	Homo sapiens (human)
dopamine catabolic process	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to ethanol	Amine oxidase [flavin-containing] B	Homo sapiens (human)
positive regulation of dopamine metabolic process	Amine oxidase [flavin-containing] B	Homo sapiens (human)
hydrogen peroxide biosynthetic process	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to corticosterone	Amine oxidase [flavin-containing] B	Homo sapiens (human)
epigenetic programing of female pronucleus	Lysine-specific histone demethylase 1B	Homo sapiens (human)
genomic imprinting	Lysine-specific histone demethylase 1B	Homo sapiens (human)
chromatin remodeling	Lysine-specific histone demethylase 1B	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
telomeric DNA binding	Lysine-specific histone demethylase 1A	Homo sapiens (human)
p53 binding	Lysine-specific histone demethylase 1A	Homo sapiens (human)
chromatin binding	Lysine-specific histone demethylase 1A	Homo sapiens (human)
transcription coactivator activity	Lysine-specific histone demethylase 1A	Homo sapiens (human)
protein binding	Lysine-specific histone demethylase 1A	Homo sapiens (human)
oxidoreductase activity	Lysine-specific histone demethylase 1A	Homo sapiens (human)
enzyme binding	Lysine-specific histone demethylase 1A	Homo sapiens (human)
nuclear receptor coactivator activity	Lysine-specific histone demethylase 1A	Homo sapiens (human)
demethylase activity	Lysine-specific histone demethylase 1A	Homo sapiens (human)
histone demethylase activity	Lysine-specific histone demethylase 1A	Homo sapiens (human)
histone H3K4 demethylase activity	Lysine-specific histone demethylase 1A	Homo sapiens (human)
histone H3K9 demethylase activity	Lysine-specific histone demethylase 1A	Homo sapiens (human)
identical protein binding	Lysine-specific histone demethylase 1A	Homo sapiens (human)
MRF binding	Lysine-specific histone demethylase 1A	Homo sapiens (human)
flavin adenine dinucleotide binding	Lysine-specific histone demethylase 1A	Homo sapiens (human)
nuclear androgen receptor binding	Lysine-specific histone demethylase 1A	Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor binding	Lysine-specific histone demethylase 1A	Homo sapiens (human)
telomeric repeat-containing RNA binding	Lysine-specific histone demethylase 1A	Homo sapiens (human)
DNA-binding transcription factor binding	Lysine-specific histone demethylase 1A	Homo sapiens (human)
FAD-dependent H3K4me/H3K4me3 demethylase activity	Lysine-specific histone demethylase 1A	Homo sapiens (human)
promoter-specific chromatin binding	Lysine-specific histone demethylase 1A	Homo sapiens (human)
transcription factor binding	Lysine-specific histone demethylase 1A	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 2C9	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C9	Homo sapiens (human)
heme binding	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2C9	Homo sapiens (human)
protein binding	Amine oxidase [flavin-containing] A	Homo sapiens (human)
primary amine oxidase activity	Amine oxidase [flavin-containing] A	Homo sapiens (human)
aliphatic amine oxidase activity	Amine oxidase [flavin-containing] A	Homo sapiens (human)
monoamine oxidase activity	Amine oxidase [flavin-containing] A	Homo sapiens (human)
flavin adenine dinucleotide binding	Amine oxidase [flavin-containing] A	Homo sapiens (human)
protein binding	Amine oxidase [flavin-containing] B	Homo sapiens (human)
primary amine oxidase activity	Amine oxidase [flavin-containing] B	Homo sapiens (human)
electron transfer activity	Amine oxidase [flavin-containing] B	Homo sapiens (human)
identical protein binding	Amine oxidase [flavin-containing] B	Homo sapiens (human)
aliphatic amine oxidase activity	Amine oxidase [flavin-containing] B	Homo sapiens (human)
monoamine oxidase activity	Amine oxidase [flavin-containing] B	Homo sapiens (human)
flavin adenine dinucleotide binding	Amine oxidase [flavin-containing] B	Homo sapiens (human)
protein binding	Lysine-specific histone demethylase 1B	Homo sapiens (human)
zinc ion binding	Lysine-specific histone demethylase 1B	Homo sapiens (human)
histone demethylase activity	Lysine-specific histone demethylase 1B	Homo sapiens (human)
histone binding	Lysine-specific histone demethylase 1B	Homo sapiens (human)
FAD binding	Lysine-specific histone demethylase 1B	Homo sapiens (human)
FAD-dependent H3K4me/H3K4me3 demethylase activity	Lysine-specific histone demethylase 1B	Homo sapiens (human)
transcription factor binding	Lysine-specific histone demethylase 1B	Homo sapiens (human)
oxidoreductase activity	Lysine-specific histone demethylase 1B	Homo sapiens (human)
flavin adenine dinucleotide binding	Lysine-specific histone demethylase 1B	Homo sapiens (human)
chromatin binding	Lysine-specific histone demethylase 1B	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
chromatin	Lysine-specific histone demethylase 1A	Homo sapiens (human)
nucleus	Lysine-specific histone demethylase 1A	Homo sapiens (human)
chromosome, telomeric region	Lysine-specific histone demethylase 1A	Homo sapiens (human)
nucleus	Lysine-specific histone demethylase 1A	Homo sapiens (human)
nucleoplasm	Lysine-specific histone demethylase 1A	Homo sapiens (human)
transcription regulator complex	Lysine-specific histone demethylase 1A	Homo sapiens (human)
protein-containing complex	Lysine-specific histone demethylase 1A	Homo sapiens (human)
DNA repair complex	Lysine-specific histone demethylase 1A	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C9	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
mitochondrion	Amine oxidase [flavin-containing] A	Homo sapiens (human)
mitochondrial outer membrane	Amine oxidase [flavin-containing] A	Homo sapiens (human)
cytosol	Amine oxidase [flavin-containing] A	Homo sapiens (human)
mitochondrion	Amine oxidase [flavin-containing] A	Homo sapiens (human)
mitochondrion	Amine oxidase [flavin-containing] B	Homo sapiens (human)
mitochondrial envelope	Amine oxidase [flavin-containing] B	Homo sapiens (human)
mitochondrial outer membrane	Amine oxidase [flavin-containing] B	Homo sapiens (human)
dendrite	Amine oxidase [flavin-containing] B	Homo sapiens (human)
neuronal cell body	Amine oxidase [flavin-containing] B	Homo sapiens (human)
mitochondrion	Amine oxidase [flavin-containing] B	Homo sapiens (human)
nucleus	Lysine-specific histone demethylase 1B	Homo sapiens (human)
nucleoplasm	Lysine-specific histone demethylase 1B	Homo sapiens (human)
nucleosome	Lysine-specific histone demethylase 1B	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (60)

Assay ID	Title	Year	Journal	Article
AID1755599	Inhibition of LSD1 (unknown origin) using H3K4(diMe) peptide as substrate measured after 60 mins by amplex red dye based HRP-coupled assay	2020	Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23	Tranylcypromine Based Lysine-Specific Demethylase 1 Inhibitor: Summary and Perspective.
AID1459726	Cytotoxicity against human A549 cells assessed as growth inhibition by MTT assay	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Design, synthesis and biological evaluation of [1,2,4]triazolo[1,5-a]pyrimidines as potent lysine specific demethylase 1 (LSD1/KDM1A) inhibitors.
AID1903142	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay
AID1572512	Inhibition of MAOB (unknown origin) by Promega MAO-Glo assay	2019	Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6	Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor.
AID1669139	Metabolic stability in rat liver microsomes assessed as intrinsic clearance	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.
AID1903171	Inhibition of human LSD1 using H3K4Me2 peptide as substrate incubated for 60 min by horseradish peroxidase coupled assay
AID1669136	Inhibition of recombinant N-terminal His-tagged LSD1 (unknown origin) expressed in Escherichia coli expression system using ART-K(Me1)-QTARKSTGGKAPRKQLAGGK(Biotin) as substrate incubated for 60 mins by TR-FRET assay	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.
AID1572515	Inhibition of LSD1 in human MV4-11 cells assessed as increase in CD86 mRNA expression at 1000 nM by SYBR Green dye-bsed RT-qPCR analysis relative to control	2019	Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6	Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor.
AID1903138	Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI insect cells using luminogenic MAO substrate incubated for 1 hr by luciferin-based luminescence assay
AID1847831	Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	2021	Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24	Installation of Pargyline, a LSD1 Inhibitor, in the HDAC Inhibitory Template Culminated in the Identification of a Tractable Antiprostate Cancer Agent.
AID1572511	Inhibition of MAOA (unknown origin) by Promega MAO-Glo assay	2019	Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6	Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor.
AID1854422	Antiproliferative activity against human SCLC cell	2022	European journal of medicinal chemistry, Oct-05, Volume: 240	A comprehensive comparative study on LSD1 in different cancers and tumor specific LSD1 inhibitors.
AID1459727	Cytotoxicity against human PC9 cells assessed as growth inhibition by MTT assay	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Design, synthesis and biological evaluation of [1,2,4]triazolo[1,5-a]pyrimidines as potent lysine specific demethylase 1 (LSD1/KDM1A) inhibitors.
AID1427613	Reversible inhibition of full length recombinant LSD1 (unknown origin) expressed in Escherichia coli BL21(DE) assessed as recovery of enzyme activity at 600 uM preincubated for 1 hr followed by compound dilution and subsequent H3K4me2 substrate addition b
AID1903177	Induction of differentiation of human MV4-11 cells assessed as morphological changes by measuring reduction in nuclear to cytoplasmic ratio at 5 uM incubated for 240 hrs by Wright-Giemsa staining based microscopy
AID1903146	Irreversible inhibition of recombinant human LSD1 at 300 nM incubated for 1 hr by jump dilution method
AID1903170	Inhibition of human MAOB
AID1903143	Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay
AID1903136	Inhibition of N-terminal His/GST-tagged human LSD1 (172 to 852 residues) expressed in expressed in baculovirus infected insect cells using biotinylated H3K4Me2 peptide as substrate by TR-FRET assay
AID1435569	Reversible inhibition of recombinant full length LSD1 (unknown origin) expressed in Escherichia coli BL21 (DE) assessed as recovery of enzyme activity using H3K4me2 substrate preincubated followed by compound dilution by 80-fold by fluorescence assay	2017	European journal of medicinal chemistry, Jan-27, Volume: 126	Discovery of resveratrol derivatives as novel LSD1 inhibitors: Design, synthesis and their biological evaluation.
AID1669138	Metabolic stability in mouse liver microsomes assessed as intrinsic clearance	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.
AID1847828	Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	2021	Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24	Installation of Pargyline, a LSD1 Inhibitor, in the HDAC Inhibitory Template Culminated in the Identification of a Tractable Antiprostate Cancer Agent.
AID1903178	Induction of differentiation of human MV4-11 cells assessed as morphological changes by measuring segmented nucleus at 5 uM incubated for 240 hrs by Wright-Giemsa staining based microscopy
AID1572510	Inhibition of full length human menin/FAM-tagged MLL1 (unknown origin) protein-protein interaction after 15 mins by fluorescence polarization assay	2019	Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6	Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor.
AID1459724	Cytotoxicity against human MGC803 cells assessed as growth inhibition by MTT assay	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Design, synthesis and biological evaluation of [1,2,4]triazolo[1,5-a]pyrimidines as potent lysine specific demethylase 1 (LSD1/KDM1A) inhibitors.
AID1903139	Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI insect cells using luminogenic MAO substrate incubated for 1 hr by luciferin-based luminescence assay
AID1903141	Upregulation of CD86 expression in human MV4-11 cells assessed as fold change in CD86 expression at IC50 incubated for 24 hrs by qRT-PCR analysis relative to control
AID1602252	Irreversible inhibition of recombinant LSD1 (unknown origin) assessed as recovery of enzyme activity at 1.6 uM measured 1 hr after 80-fold dilution	2019	European journal of medicinal chemistry, Mar-15, Volume: 166	Experience-based discovery (EBD) of aryl hydrazines as new scaffolds for the development of LSD1/KDM1A inhibitors.
AID1903137	Inhibition of recombinant human full length LSD2 using biotinylated H3K4Me2 peptide as substrate by TR-FRET assay
AID1459725	Cytotoxicity against human EC109 cells assessed as growth inhibition by MTT assay	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Design, synthesis and biological evaluation of [1,2,4]triazolo[1,5-a]pyrimidines as potent lysine specific demethylase 1 (LSD1/KDM1A) inhibitors.
AID1289333	Inhibition of KDM1A (unknown origin) by peroxidase coupled assay	2016	Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4	Recent Progress in Histone Demethylase Inhibitors.
AID1669137	Growth inhibition on human Kasumi-1 cells measured upto 12 days by Cell Titer-Glo luminescent cell viability assay	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.
AID1459729	Inhibition of recombinant human LSD1 (157 to 852 residues) expressed in Escherichia coli BL21(DE3) using H3K4me2 as substrate preincubated for 1 hr followed by substrate addition by fluorescence assay	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Design, synthesis and biological evaluation of [1,2,4]triazolo[1,5-a]pyrimidines as potent lysine specific demethylase 1 (LSD1/KDM1A) inhibitors.
AID1719019	Antitumour activity against human MM1.S cells xenografted in SCID mouse assessed as tumour growth inhibition at 25 mg/kg, po for 12 days relative to control	2021	Bioorganic & medicinal chemistry letters, 02-15, Volume: 34	Novel dual LSD1/HDAC6 inhibitors for the treatment of multiple myeloma.
AID1903140	Selectivity index, ratio of IC50 for inhibition of recombinant human full length LSD2 to IC50 for inhibition of N-terminal His/GST-tagged human LSD1 (172 to 852 residues) expressed in baculovirus infected insect cells
AID1427607	Inhibition of full length recombinant LSD1 (unknown origin) expressed in Escherichia coli BL21(DE) using H3K4me2 as substrate by fluorescence assay
AID1903144	Activation of CD86 expression in human MV4-11 cells incubated for 24 hrs by qRT-PCR analysis
AID1903168	Inhibition of human LSD2
AID1592293	Irreversible inhibition of recombinant LSD1 (unknown origin) expressed in Escherichia coli BL21(DE) assessed as recovery of enzyme activity at 1.6 uM using H3K4me2 substrate incubated for 1 hr followed by 80 fold dilution by dilution assay
AID1903169	Inhibition of human MAOA
AID1669135	Inhibition of LSD1 in human MV4-11 cells assessed as induction of LY96 mRNA expression incubated for 16 hrs by chemiluminescent method	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.
AID1572509	Inhibition of recombinant human LSD1 (172 to 852 residues) using biotin-labelled H3K4me2 (1 to 24 residues) after 1 hr by TR-FRET assay	2019	Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6	Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor.
AID1669140	Metabolic stability in dog liver microsomes assessed as intrinsic clearance	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.
AID1427625	Antiproliferative activity against human MGC803 cells after 5 days by MTT assay
AID1572514	Antiproliferative activity against human MV4-11 cells after 240 hrs by MTS assay	2019	Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6	Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor.
AID1669148	Time dependant inhibition of recombinant N-terminal His-tagged LSD1 (unknown origin) expressed in Escherichia coli expression system assessed as inactivation constant using ART-K(Me1)-QTARKSTGGKAPRKQLAGGK(Biotin) as substrate incubated for 60 mins by TR-F	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.
AID1669141	Metabolic stability in human liver microsomes assessed as intrinsic clearance	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.
AID1669149	Time dependant inhibition of recombinant N-terminal His-tagged LSD1 (unknown origin) expressed in Escherichia coli expression system assessed as inhibitory constant using ART-K(Me1)-QTARKSTGGKAPRKQLAGGK(Biotin) as substrate incubated for 60 mins by TR-FRE	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.
AID1854421	Antiproliferative activity against human AML cell	2022	European journal of medicinal chemistry, Oct-05, Volume: 240	A comprehensive comparative study on LSD1 in different cancers and tumor specific LSD1 inhibitors.
AID1514387	Irreversible inhibition of full length LSD1 (unknown origin) expressed in Escherichia coli BL21 (DE) using H3K4me2 peptide as substrate assessed as enzyme activity recovery preincubated for 1 hr followed by 80 fold compound dilution by fluorescence assay	2018	Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24	Design, synthesis and in vitro evaluation of stilbene derivatives as novel LSD1 inhibitors for AML therapy.
AID1903172	Selectivity ratio of Kinact for human LSD1 to Ki(app) for human LSD1
AID1532695	Inhibition of full length recombinant LSD1 (unknown origin) expressed in Escherichia coli BL21(DE3) using H3K4me2 as substrate after 30 mins in presence of FAD by amplex red reagent based fluorescence assay	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Ligand-based design, synthesis and biological evaluation of xanthine derivatives as LSD1/KDM1A inhibitors.
AID1903147	Irreversible inhibition of recombinant human LSD1 at 2 uM incubated for 1 hr by jump dilution method
AID1669150	Time dependant inhibition of recombinant N-terminal His-tagged LSD1 (unknown origin) expressed in Escherichia coli expression system assessed as ratio of inactivation constant to inhibitory constant using ART-K(Me1)-QTARKSTGGKAPRKQLAGGK(Biotin) as substra	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	18 (62.07)	24.3611
2020's	11 (37.93)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	2 (6.90%)	5.53%
Reviews	5 (17.24%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	22 (75.86%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
niacinamide nicotinamide : A pyridinecarboxamide that is pyridine in which the hydrogen at position 3 is replaced by a carboxamide group.	2.15	1	0	pyridine alkaloid; pyridinecarboxamide; vitamin B3	anti-inflammatory agent; antioxidant; cofactor; EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor; EC 3.5.1.98 (histone deacetylase) inhibitor; Escherichia coli metabolite; geroprotector; human urinary metabolite; metabolite; mouse metabolite; neuroprotective agent; Saccharomyces cerevisiae metabolite; Sir2 inhibitor
fluorouracil Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.	2.15	1	0	nucleobase analogue; organofluorine compound	antimetabolite; antineoplastic agent; environmental contaminant; immunosuppressive agent; radiosensitizing agent; xenobiotic
phenelzine Phenelzine: One of the MONOAMINE OXIDASE INHIBITORS used to treat DEPRESSION; PHOBIC DISORDERS; and PANIC.	2.15	1	0	primary amine
clorgyline Clorgyline: An antidepressive agent and monoamine oxidase inhibitor related to PARGYLINE.. clorgyline : An aromatic ether that is the 2,4-dichlorophenyl ether of 3-aminopropan-1-ol in which the nitrogen is substituted by a methyl group and a prop-1-yn-3-yl group. A monoamine oxidase inhibitor, it was formerly used as an antidepressant.	2.63	2	0	aromatic ether; dichlorobenzene; terminal acetylenic compound; tertiary amino compound	antidepressant; EC 1.4.3.4 (monoamine oxidase) inhibitor
pargyline Pargyline: A monoamine oxidase inhibitor with antihypertensive properties.	2.61	2	0	aromatic amine
lysine Lysine: An essential amino acid. It is often added to animal feed.. lysine : A diamino acid that is caproic (hexanoic) acid bearing two amino substituents at positions 2 and 6.. L-lysine : An L-alpha-amino acid; the L-isomer of lysine.	9.28	2	1	aspartate family amino acid; L-alpha-amino acid zwitterion; L-alpha-amino acid; lysine; organic molecular entity; proteinogenic amino acid	algal metabolite; anticonvulsant; Escherichia coli metabolite; human metabolite; micronutrient; mouse metabolite; nutraceutical; plant metabolite; Saccharomyces cerevisiae metabolite
tranylcypromine Tranylcypromine: A propylamine formed from the cyclization of the side chain of amphetamine. This monoamine oxidase inhibitor is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It also is useful in panic and phobic disorders. (From AMA Drug Evaluations Annual, 1994, p311). tranylcypromine : A racemate comprising equal amounts of (1R,2S)- and (1S,2R)-2-phenylcyclopropan-1-amine. An irreversible monoamine oxidase inhibitor that is used as an antidepressant (INN tranylcypromine).. (1R,2S)-tranylcypromine : A 2-phenylcyclopropan-1-amine that is the (1R,2S)-enantiomer of tranylcypromine.	4.79	4	0	2-phenylcyclopropan-1-amine
selegiline Selegiline: A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl.	2.17	1	0	selegiline; terminal acetylenic compound	geroprotector
paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).	2.31	1	0	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent
di-n-desethylamiodarone di-N-desethylamiodarone: amiodarone metabolite in dogs; structure given in first source	3.23	1	0
abiraterone [no description available]	2.31	1	0	3beta-hydroxy-Delta(5)-steroid; 3beta-sterol; pyridines	antineoplastic agent; EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor
epiberberine epiberberine: isolated in plants of Coptis from China	3.51	1	0
sorafenib [no description available]	2.15	1	0	(trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; phenylureas; pyridinecarboxamide	angiogenesis inhibitor; anticoronaviral agent; antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; ferroptosis inducer; tyrosine kinase inhibitor
tretinoin Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry.	2.21	1	0	retinoic acid; vitamin A	anti-inflammatory agent; antineoplastic agent; antioxidant; AP-1 antagonist; human metabolite; keratolytic drug; retinoic acid receptor agonist; retinoid X receptor agonist; signalling molecule
farnesol Farnesol: A colorless liquid extracted from oils of plants such as citronella, neroli, cyclamen, and tuberose. It is an intermediate step in the biological synthesis of cholesterol from mevalonic acid in vertebrates. It has a delicate odor and is used in perfumery. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed). (2-trans,6-trans)-farnesol : The (2-trans,6-trans)-stereoisomer of farnesol.. farnesol : A farnesane sesquiterpenoid that is dodeca-2,6,10-triene substituted by methyl groups at positions 3, 7 and 11 and a hydroxy group at position 1.	3.23	1	0	farnesol	plant metabolite
resveratrol trans-resveratrol : A resveratrol in which the double bond has E configuration.	3.73	2	0	resveratrol	antioxidant; phytoalexin; plant metabolite; quorum sensing inhibitor; radical scavenger
5-carboxy-8-hydroxyquinoline 5-carboxy-8-hydroxyquinoline: a JmjC histone demethylase inhibitor; structure in first source	3.23	1	0	quinolines
capsaicin ALGRX-4975: an injectable capsaicin (TRPV1 receptor agonist) formulation for longlasting pain relief. capsaicinoid : A family of aromatic fatty amides produced as secondary metabolites by chilli peppers.	3.51	1	0	capsaicinoid	non-narcotic analgesic; TRPV1 agonist; voltage-gated sodium channel blocker
biochanin a [no description available]	3.51	1	0	4'-methoxyisoflavones; 7-hydroxyisoflavones	antineoplastic agent; EC 3.5.1.99 (fatty acid amide hydrolase) inhibitor; phytoestrogen; plant metabolite; tyrosine kinase inhibitor
salvianolic acid B salvianolic acid B: isolated from Salvia miltiorrhiza. salvianolic acid B : A member of the class of 1-benzofurans that is an antioxidant and free radical scavenging compound extracted from S. miltiorrhiza	3.51	1	0	1-benzofurans; catechols; dicarboxylic acid; enoate ester; polyphenol	anti-inflammatory agent; antidepressant; antineoplastic agent; antioxidant; apoptosis inducer; autophagy inhibitor; cardioprotective agent; hepatoprotective agent; hypoglycemic agent; neuroprotective agent; osteogenesis regulator; plant metabolite
mdv 3100 [no description available]	2.31	1	0	(trifluoromethyl)benzenes; benzamides; imidazolidinone; monofluorobenzenes; nitrile; thiocarbonyl compound	androgen antagonist; antineoplastic agent
1-(4-methyl-1-piperazinyl)-2-[[(1R,2S)-2-(4-phenylmethoxyphenyl)cyclopropyl]amino]ethanone [no description available]	3.35	1	0	amino acid amide
acy-1215 ricolinostat: an HDAC6 inhibitor; structure in first source	2.31	1	0	pyrimidinecarboxylic acid

Condition	Indicated	Relationship Strength	Studies	Trials
Acute Myelogenous Leukemia [description not available]	0	4.31	3	1
Leukemia, Myeloid, Acute Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.	0	4.31	3	1
Congenital Zika Syndrome [description not available]	0	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.25	1	0
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	0	2.25	1	0
Kahler Disease [description not available]	0	2.31	1	0
Experimental Neoplasms [description not available]	0	2.31	1	0
Multiple Myeloma A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.	0	2.31	1	0
Cancer of Prostate [description not available]	0	2.31	1	0
Prostatic Neoplasms Tumors or cancer of the PROSTATE.	0	2.31	1	0
Carcinogenesis The origin, production or development of cancer through genotypic and phenotypic changes which upset the normal balance between cell proliferation and cell death. Carcinogenesis generally requires a constellation of steps, which may occur quickly or over a period of many years.	0	3.33	1	0
Benign Neoplasms [description not available]	0	3.98	2	0
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	0	3.98	2	0
Dysmyelopoietic Syndromes [description not available]	0	3.8	1	1
Myelodysplastic Syndromes Clonal hematopoietic stem cell disorders characterized by dysplasia in one or more hematopoietic cell lineages. They predominantly affect patients over 60, are considered preleukemic conditions, and have high probability of transformation into ACUTE MYELOID LEUKEMIA.	1	10.8	1	1
Bone Loss, Osteoclastic [description not available]	0	2.6	1	0
Age-Related Osteoporosis [description not available]	0	2.6	1	0
Osteoporosis Reduction of bone mass without alteration in the composition of bone, leading to fractures. Primary osteoporosis can be of two major types: postmenopausal osteoporosis (OSTEOPOROSIS, POSTMENOPAUSAL) and age-related or senile osteoporosis.	0	2.6	1	0
Hepatocellular Carcinoma [description not available]	0	2.15	1	0
Cancer of Liver [description not available]	0	2.15	1	0
Carcinoma, Hepatocellular A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.	0	2.15	1	0
Liver Neoplasms Tumors or cancer of the LIVER.	0	2.15	1	0
Carcinoma, Small Cell Lung [description not available]	0	4.86	2	1
Cancer of Lung [description not available]	0	4.86	2	1
Local Neoplasm Recurrence [description not available]	0	4.51	1	1
Lung Neoplasms Tumors or cancer of the LUNG.	0	4.86	2	1
Small Cell Lung Carcinoma A form of highly malignant lung cancer that is composed of small ovoid cells (SMALL CELL CARCINOMA).	1	6.86	2	1
Leukemia, Lymphoblastic, Acute, T Cell [description not available]	0	2.15	1	0
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma A leukemia/lymphoma found predominately in children and young adults and characterized LYMPHADENOPATHY and THYMUS GLAND involvement. It most frequently presents as a lymphoma, but a leukemic progression in the bone marrow is common.	0	2.15	1	0

gsk2879552

Description

Cross-References

Synonyms (41)

Research Excerpts

Overview

Toxicity

Bioavailability

Roles (2)

Drug Classes (7)

Protein Targets (5)

Inhibition Measurements

Activation Measurements

Biological Processes (63)

Molecular Functions (42)

Ceullar Components (18)

Bioassays (60)

Research

Studies (29)

Market Indicators

Research Demand Index: 29.47

Study Types

gsk2879552

Description

Cross-References

Synonyms (41)

Research Excerpts

Overview

Toxicity

Bioavailability

Roles (2)

Drug Classes (7)

Protein Targets (5)

Inhibition Measurements

Activation Measurements

Biological Processes (63)

Molecular Functions (42)

Ceullar Components (18)

Bioassays (60)

Research

Studies (29)

Market Indicators

Research Demand Index: 29.47

Study Types

Related Drugs (23)

Related Conditions (29)