3,9-bis((ethylthio)methyl)-k-252a profile

3,9-bis((ethylthio)methyl)-K-252a: RN given for (9S-(9alpha,10beta,12alpha))-isomer; mixed lineage kinase inhibitor, neuroprotective agent, and neurotrophic agent derived from K-252a; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	9917013
CHEMBL ID	290352
SCHEMBL ID	12047710
MeSH ID	M0277674

Synonym
unii-200ha2limk
200ha2limk ,
9,12-epoxy-1h-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-i)(1,6)benzodiazocine-10-carboxylic acid, 5,16-bis((ethylthio)methyl)-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, (9s-(9alpha,10beta,12alpha))-
kt 7515
kt-7515
bdbm24942
cep1347
chembl290352 ,
3,9-bis(etsm)-k-252a
kt7515
3,9-bis((ethylthio)methyl)-k-252a
cep 1347
methyl (15s,16r,18r)-10,23-bis[(ethylsulfanyl)methyl]-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxylate
156177-65-0
cep-1347
kt-1575
gtpl8173
SCHEMBL12047710
(9s,10r,12r)-5-16-bis[(ethylthio)methyl]-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1h-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester
AKOS024458422
9,12-epoxy-1h-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-i)(1,6)benzodiazocine-10-carboxylic acid, 5,16-bis((ethylthio)methyl)-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, (9s-(9.alpha.,10.beta.,12.alpha.))-
9,12-epoxy-1h-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-i)(1,6)benzodiazocine-10-carboxylic acid, 5,16-bis((ethylthio)methyl)-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, (9s,10r,12r)-
cep-1374
kt7515;kt-7515;kt 7515;cep-1347;cep 1347
BCP16748
Q27075851
methyl (15s,16r,18r)-10,23-bis(ethylsulfanylmethyl)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8(13),9,11,20(25),21,23,26-nonaene-16-carboxylate
MS-30740
methyl (5s,6r,8r)-2,11-bis((ethylthio)methyl)-6-hydroxy-5-methyl-13-oxo-5,6,7,8,14,15-hexahydro-13h-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-6-carboxylate
HY-10412
CS-0002594

Excerpt	Reference	Relevance
" Furthermore, expression of wild type MLK3 in hippocampal pyramidal neurons enhanced gp120IIIB-induced neurotoxicity, whereas expression of a dominant negative MLK3 protected neurons from the toxic effects of the glycoprotein."	( Mixed lineage kinase 3 mediates gp120IIIB-induced neurotoxicity. Bodner, A; Finn, JP; Ghadge, G; Maroney, AC; Miller, RJ; Roos, R, 2002)	0.31
" In this short-term study, CEP-1347 was safe and well tolerated."	( The safety and tolerability of a mixed lineage kinase inhibitor (CEP-1347) in PD. , 2004)	0.32
"The HIV-1 gene products Tat and gp120 are toxic to neurons and can activate cells of myeloid origin, properties that are thought to contribute to the clinical manifestations of HIV-1-associated dementia (HAD)."	( Inhibition of mixed lineage kinase 3 prevents HIV-1 Tat-mediated neurotoxicity and monocyte activation. Dewhurst, S; Fan, S; Gelbard, HA; Litzburg, A; Maggirwar, SB; Reisinger, E; Schifitto, G; Sniderhan, L; Sui, Z, 2006)	0.33

Excerpt	Reference	Relevance
" We report here URMC-099 (1) an orally bioavailable (F = 41%), potent (IC50 = 14 nM) MLK3 inhibitor with excellent brain exposure in mouse PK models and minimal interference with key human CYP450 enzymes or hERG channels."	( Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. Dewhurst, S; Gelbard, HA; Goodfellow, VS; Loweth, CJ; Marker, DF; Nguyen, T; Polesskaya, O; Pollack, S; Ravula, SB; Sheppard, D; Todd, DE; Wiemann, T; Xu, Y, 2013)	0.39

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
High affinity nerve growth factor receptor	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0002	0.5436	10.0000	AID213419
Vascular endothelial growth factor receptor 1	Homo sapiens (human)	IC50 (µMol)	0.2090	0.0001	0.2914	7.0000	AID363165
Vascular endothelial growth factor receptor 3	Homo sapiens (human)	IC50 (µMol)	0.0390	0.0001	0.2264	4.9000	AID363167
Vascular endothelial growth factor receptor 2	Homo sapiens (human)	IC50 (µMol)	0.0430	0.0000	0.4830	8.8000	AID363166
Mitogen-activated protein kinase kinase kinase 9	Homo sapiens (human)	IC50 (µMol)	0.0413	0.0005	0.2244	2.1000	AID125159; AID1384625; AID1798485; AID362969; AID363158; AID775350
Protein delta homolog 1	Homo sapiens (human)	IC50 (µMol)	0.1140	0.1140	0.1260	0.1500	AID1384628; AID363160
Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)	IC50 (µMol)	0.0412	0.0020	0.1035	0.5800	AID125160; AID1384626; AID1798485; AID775351
Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)	IC50 (µMol)	0.0364	0.0040	0.1021	1.1400	AID125162; AID1384627; AID1798485; AID362970; AID775352
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
cellular response to amyloid-beta	High affinity nerve growth factor receptor	Homo sapiens (human)
positive regulation of protein phosphorylation	High affinity nerve growth factor receptor	Homo sapiens (human)
protein phosphorylation	High affinity nerve growth factor receptor	Homo sapiens (human)
axon guidance	High affinity nerve growth factor receptor	Homo sapiens (human)
learning or memory	High affinity nerve growth factor receptor	Homo sapiens (human)
circadian rhythm	High affinity nerve growth factor receptor	Homo sapiens (human)
negative regulation of cell population proliferation	High affinity nerve growth factor receptor	Homo sapiens (human)
response to xenobiotic stimulus	High affinity nerve growth factor receptor	Homo sapiens (human)
programmed cell death involved in cell development	High affinity nerve growth factor receptor	Homo sapiens (human)
positive regulation of neuron projection development	High affinity nerve growth factor receptor	Homo sapiens (human)
peptidyl-tyrosine phosphorylation	High affinity nerve growth factor receptor	Homo sapiens (human)
olfactory nerve development	High affinity nerve growth factor receptor	Homo sapiens (human)
B cell differentiation	High affinity nerve growth factor receptor	Homo sapiens (human)
response to nutrient levels	High affinity nerve growth factor receptor	Homo sapiens (human)
peptidyl-tyrosine autophosphorylation	High affinity nerve growth factor receptor	Homo sapiens (human)
nerve growth factor signaling pathway	High affinity nerve growth factor receptor	Homo sapiens (human)
mechanoreceptor differentiation	High affinity nerve growth factor receptor	Homo sapiens (human)
negative regulation of apoptotic process	High affinity nerve growth factor receptor	Homo sapiens (human)
positive regulation of programmed cell death	High affinity nerve growth factor receptor	Homo sapiens (human)
negative regulation of neuron apoptotic process	High affinity nerve growth factor receptor	Homo sapiens (human)
positive regulation of GTPase activity	High affinity nerve growth factor receptor	Homo sapiens (human)
positive regulation of Ras protein signal transduction	High affinity nerve growth factor receptor	Homo sapiens (human)
protein autophosphorylation	High affinity nerve growth factor receptor	Homo sapiens (human)
neurotrophin TRK receptor signaling pathway	High affinity nerve growth factor receptor	Homo sapiens (human)
ephrin receptor signaling pathway	High affinity nerve growth factor receptor	Homo sapiens (human)
sympathetic nervous system development	High affinity nerve growth factor receptor	Homo sapiens (human)
response to axon injury	High affinity nerve growth factor receptor	Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain	High affinity nerve growth factor receptor	Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain	High affinity nerve growth factor receptor	Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activity	High affinity nerve growth factor receptor	Homo sapiens (human)
neuron apoptotic process	High affinity nerve growth factor receptor	Homo sapiens (human)
response to hydrostatic pressure	High affinity nerve growth factor receptor	Homo sapiens (human)
response to electrical stimulus	High affinity nerve growth factor receptor	Homo sapiens (human)
positive regulation of synapse assembly	High affinity nerve growth factor receptor	Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergic	High affinity nerve growth factor receptor	Homo sapiens (human)
Sertoli cell development	High affinity nerve growth factor receptor	Homo sapiens (human)
axonogenesis involved in innervation	High affinity nerve growth factor receptor	Homo sapiens (human)
behavioral response to formalin induced pain	High affinity nerve growth factor receptor	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	High affinity nerve growth factor receptor	Homo sapiens (human)
cellular response to nicotine	High affinity nerve growth factor receptor	Homo sapiens (human)
cellular response to nerve growth factor stimulus	High affinity nerve growth factor receptor	Homo sapiens (human)
multicellular organism development	High affinity nerve growth factor receptor	Homo sapiens (human)
positive regulation of kinase activity	High affinity nerve growth factor receptor	Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathway	High affinity nerve growth factor receptor	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	High affinity nerve growth factor receptor	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	High affinity nerve growth factor receptor	Homo sapiens (human)
angiogenesis	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
monocyte chemotaxis	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathway	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
positive regulation of cell population proliferation	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
positive regulation of phospholipase C activity	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
cell migration	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
peptidyl-tyrosine phosphorylation	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
cell differentiation	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
positive regulation of cell migration	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulus	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
vascular endothelial growth factor receptor-1 signaling pathway	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
vascular endothelial growth factor signaling pathway	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
positive regulation of MAP kinase activity	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
positive regulation of MAPK cascade	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
positive regulation of angiogenesis	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
protein autophosphorylation	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathway	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
blood vessel morphogenesis	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
embryonic morphogenesis	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
negative regulation of vascular endothelial cell proliferation	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
hyaloid vascular plexus regression	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
multicellular organism development	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
positive regulation of kinase activity	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathway	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
positive regulation of protein phosphorylation	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
positive regulation of endothelial cell proliferation	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
vasculature development	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
lymph vessel development	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
lymphangiogenesis	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
sprouting angiogenesis	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
respiratory system process	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathway	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
positive regulation of cell population proliferation	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
positive regulation of vascular endothelial growth factor production	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
positive regulation of endothelial cell migration	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
peptidyl-tyrosine phosphorylation	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulus	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
vascular endothelial growth factor signaling pathway	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
negative regulation of apoptotic process	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
positive regulation of MAPK cascade	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
positive regulation of JNK cascade	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
protein autophosphorylation	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathway	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
lung alveolus development	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
blood vessel morphogenesis	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
regulation of blood vessel remodeling	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
positive regulation of protein kinase C signaling	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
positive regulation of cell migration	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
positive regulation of kinase activity	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
multicellular organism development	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
regulation of MAPK cascade	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
angiogenesis	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
branching involved in blood vessel morphogenesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of macroautophagy	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of mitochondrial depolarization	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of mitochondrial fission	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
angiogenesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
ovarian follicle development	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
vasculogenesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of protein phosphorylation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of endothelial cell proliferation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
lymph vessel development	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cell migration involved in sprouting angiogenesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of mesenchymal cell proliferation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
epithelial cell maturation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
endocardium development	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
endothelium development	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathway	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of cell population proliferation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
regulation of cell shape	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
mesenchymal cell proliferation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of endothelial cell migration	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
negative regulation of gene expression	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
peptidyl-tyrosine phosphorylation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of cell migration	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of BMP signaling pathway	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
embryonic hemopoiesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulus	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
vascular endothelial growth factor receptor-2 signaling pathway	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
peptidyl-tyrosine autophosphorylation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
vascular endothelial growth factor signaling pathway	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
surfactant homeostasis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of MAPK cascade	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
negative regulation of neuron apoptotic process	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cell fate commitment	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of angiogenesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
protein autophosphorylation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathway	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
lung alveolus development	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
post-embryonic camera-type eye morphogenesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
epithelial cell proliferation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of positive chemotaxis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic process	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of focal adhesion assembly	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
calcium ion homeostasis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
blood vessel endothelial cell differentiation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
vascular wound healing	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
semaphorin-plexin signaling pathway	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
stem cell proliferation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
regulation of hematopoietic progenitor cell differentiation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
regulation of bone development	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cellular response to hydrogen sulfide	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
negative regulation of endothelial cell apoptotic process	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of stem cell proliferation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of endothelial cell chemotaxis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of vasculogenesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
regulation of MAPK cascade	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
multicellular organism development	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cell migration	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
endothelial cell differentiation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of kinase activity	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
MAPK cascade	Mitogen-activated protein kinase kinase kinase 9	Homo sapiens (human)
protein phosphorylation	Mitogen-activated protein kinase kinase kinase 9	Homo sapiens (human)
apoptotic process	Mitogen-activated protein kinase kinase kinase 9	Homo sapiens (human)
positive regulation of apoptotic process	Mitogen-activated protein kinase kinase kinase 9	Homo sapiens (human)
protein autophosphorylation	Mitogen-activated protein kinase kinase kinase 9	Homo sapiens (human)
cell differentiation	Protein delta homolog 1	Homo sapiens (human)
negative regulation of Notch signaling pathway	Protein delta homolog 1	Homo sapiens (human)
apoptotic process	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
signal transduction	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
smoothened signaling pathway	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
JNK cascade	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
peptidyl-serine phosphorylation	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
peptidyl-threonine phosphorylation	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
negative regulation of DNA-binding transcription factor activity	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
positive regulation of JUN kinase activity	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
negative regulation of DNA-templated transcription	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
positive regulation of JNK cascade	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
protein autophosphorylation	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
positive regulation of apoptotic process	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
MAPK cascade	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
protein phosphorylation	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
microtubule-based process	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
JNK cascade	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
positive regulation of JUN kinase activity	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
positive regulation of neuron apoptotic process	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
cell cycle G1/S phase transition	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
positive regulation of JNK cascade	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
protein autophosphorylation	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
positive regulation of apoptotic process	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
protein tyrosine kinase activity	High affinity nerve growth factor receptor	Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activity	High affinity nerve growth factor receptor	Homo sapiens (human)
GPI-linked ephrin receptor activity	High affinity nerve growth factor receptor	Homo sapiens (human)
neurotrophin p75 receptor binding	High affinity nerve growth factor receptor	Homo sapiens (human)
protein binding	High affinity nerve growth factor receptor	Homo sapiens (human)
ATP binding	High affinity nerve growth factor receptor	Homo sapiens (human)
nerve growth factor receptor activity	High affinity nerve growth factor receptor	Homo sapiens (human)
kinase binding	High affinity nerve growth factor receptor	Homo sapiens (human)
identical protein binding	High affinity nerve growth factor receptor	Homo sapiens (human)
protein homodimerization activity	High affinity nerve growth factor receptor	Homo sapiens (human)
nerve growth factor binding	High affinity nerve growth factor receptor	Homo sapiens (human)
neurotrophin binding	High affinity nerve growth factor receptor	Homo sapiens (human)
neurotrophin receptor activity	High affinity nerve growth factor receptor	Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activity	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
vascular endothelial growth factor receptor activity	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
protein binding	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
ATP binding	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
growth factor binding	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
placental growth factor receptor activity	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activity	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
vascular endothelial growth factor receptor activity	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
protein binding	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
ATP binding	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
growth factor binding	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
protein phosphatase binding	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
protein homodimerization activity	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
protein tyrosine kinase activity	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activity	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
vascular endothelial growth factor receptor activity	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
integrin binding	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
protein binding	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
ATP binding	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
coreceptor activity	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
growth factor binding	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
vascular endothelial growth factor binding	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
identical protein binding	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cadherin binding	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
Hsp90 protein binding	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
protein serine/threonine kinase activity	Mitogen-activated protein kinase kinase kinase 9	Homo sapiens (human)
JUN kinase kinase kinase activity	Mitogen-activated protein kinase kinase kinase 9	Homo sapiens (human)
MAP kinase kinase activity	Mitogen-activated protein kinase kinase kinase 9	Homo sapiens (human)
protein binding	Mitogen-activated protein kinase kinase kinase 9	Homo sapiens (human)
ATP binding	Mitogen-activated protein kinase kinase kinase 9	Homo sapiens (human)
protein homodimerization activity	Mitogen-activated protein kinase kinase kinase 9	Homo sapiens (human)
protein serine kinase activity	Mitogen-activated protein kinase kinase kinase 9	Homo sapiens (human)
molecular function activator activity	Mitogen-activated protein kinase kinase kinase 9	Homo sapiens (human)
molecular_function	Protein delta homolog 1	Homo sapiens (human)
calcium ion binding	Protein delta homolog 1	Homo sapiens (human)
protein binding	Protein delta homolog 1	Homo sapiens (human)
transcription corepressor activity	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
protein kinase activity	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
protein serine/threonine kinase activity	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
JUN kinase kinase kinase activity	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
protein binding	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
ATP binding	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
protein homodimerization activity	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
bHLH transcription factor binding	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
protein serine kinase activity	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
protein kinase activity	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
protein serine/threonine kinase activity	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
JUN kinase kinase kinase activity	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
MAP kinase kinase kinase activity	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
protein binding	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
ATP binding	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
small GTPase binding	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
mitogen-activated protein kinase kinase binding	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
mitogen-activated protein kinase kinase kinase binding	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
identical protein binding	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
protein homodimerization activity	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
protein serine kinase activity	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
early endosome	High affinity nerve growth factor receptor	Homo sapiens (human)
late endosome	High affinity nerve growth factor receptor	Homo sapiens (human)
plasma membrane	High affinity nerve growth factor receptor	Homo sapiens (human)
cell surface	High affinity nerve growth factor receptor	Homo sapiens (human)
endosome membrane	High affinity nerve growth factor receptor	Homo sapiens (human)
dendrite	High affinity nerve growth factor receptor	Homo sapiens (human)
early endosome membrane	High affinity nerve growth factor receptor	Homo sapiens (human)
late endosome membrane	High affinity nerve growth factor receptor	Homo sapiens (human)
neuronal cell body	High affinity nerve growth factor receptor	Homo sapiens (human)
recycling endosome membrane	High affinity nerve growth factor receptor	Homo sapiens (human)
protein-containing complex	High affinity nerve growth factor receptor	Homo sapiens (human)
receptor complex	High affinity nerve growth factor receptor	Homo sapiens (human)
axon	High affinity nerve growth factor receptor	Homo sapiens (human)
plasma membrane	High affinity nerve growth factor receptor	Homo sapiens (human)
extracellular space	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
endosome	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
plasma membrane	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
focal adhesion	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
actin cytoskeleton	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
receptor complex	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
plasma membrane	Vascular endothelial growth factor receptor 1	Homo sapiens (human)
extracellular region	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
nucleoplasm	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
cytosol	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
plasma membrane	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
receptor complex	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
plasma membrane	Vascular endothelial growth factor receptor 3	Homo sapiens (human)
extracellular region	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
nucleus	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
endosome	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
early endosome	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
endoplasmic reticulum	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
Golgi apparatus	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
plasma membrane	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
external side of plasma membrane	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cell junction	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
membrane raft	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
anchoring junction	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
sorting endosome	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
plasma membrane	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
receptor complex	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cellular_component	Mitogen-activated protein kinase kinase kinase 9	Homo sapiens (human)
extracellular space	Protein delta homolog 1	Homo sapiens (human)
cytoplasm	Protein delta homolog 1	Homo sapiens (human)
membrane	Protein delta homolog 1	Homo sapiens (human)
cytoplasm	Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)
centrosome	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
cytosol	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
microtubule	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
membrane	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
centrosome	Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (58)

Assay ID	Title	Year	Journal	Article
AID363167	Inhibition of human VEGFR3 expressed in baculovirus insect cell system	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
AID1384625	Inhibition of recombinant GST-tagged human MLK1 KD (1 to 500 residues) expressed in baculovirus using myelin basic protein as substrate preincubated for 15 mins measured after 30 mins in presence of [gamma-32P]ATP by scintillation counting	2018	Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18	Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration.
AID775385	Inhibition of human wild type FLT3 at 1 uM by qPCR analysis relative to control	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID165115	Inhibition of protein kinase C (PKC) from rat brain homogenate	2002	Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2	Mixed lineage kinase activity of indolocarbazole analogues.
AID775458	Drug uptake in C57BL/6 mouse brain at 10 mg/kg, iv measured at 30 mins	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775372	Inhibition of human wild type LRRK2 at 1 uM by qPCR analysis relative to control	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775349	Inhibition of human wild type CAMK1D at 1 uM by qPCR analysis relative to control	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775330	Inhibition of wild type human CAMK at 1 uM by qPCR analysis	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775343	Inhibition of human wild type CAMK2D at 1 uM by qPCR analysis relative to control	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775339	Inhibition of human wild type RSK4 at 1 uM by qPCR analysis	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775450	Ratio of drug level in brain to plasma in C57BL/6 mouse at 10 mg/kg, iv measured at 180 mins	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775347	Inhibition of human wild type Aurora kinase A at 1 uM by qPCR analysis relative to control	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID363166	Inhibition of human VEGFR2 expressed in baculovirus insect cell system	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
AID775335	Inhibition of human ABL1 mutant at 1 uM by qPCR analysis	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775350	Inhibition of MLK1 (unknown origin) after 20 mins in presence of [33P]-ATP	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID363160	Inhibition of human DLK expressed in baculovirus insect cell system	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
AID775337	Binding affinity to human MLK3	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775369	Inhibition of human LRRK2 G2019S mutant at 1 uM by qPCR analysis relative to control	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID125160	Inhibition of Mixed lineage kinase 2(MLK2)	2002	Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2	Mixed lineage kinase activity of indolocarbazole analogues.
AID775453	Plasma concentration in C57BL/6 mouse at 10 mg/kg, iv measured at 180 mins	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID363158	Inhibition of GST-fused human MLK1 expressed in CHO cells assessed as MKK4 phosphorylation	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
AID213419	Inhibition of NGF high affinity receptor tyrosine kinase TrkA	2002	Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2	Mixed lineage kinase activity of indolocarbazole analogues.
AID363196	Neuroprotective activity against human SH-SY5Y cells assessed as inhibition of MPP+-induced cell death	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
AID775328	Inhibition of human wild type ABL1 at 1 uM by qPCR analysis relative to control	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775341	Inhibition of human wild type RSK1 at 1 uM by qPCR analysis	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775329	Inhibition of wild type human AGC kinase at 1 uM by qPCR analysis	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775452	Ratio of drug level in brain to plasma in C57BL/6 mouse at 10 mg/kg, iv measured at 30 mins	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID1384628	Inhibition of DLK (unknown origin) using myelin basic protein as substrate preincubated for 15 mins measured after 30 mins in presence of [gamma-32P]ATP by scintillation counting	2018	Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18	Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration.
AID775346	Inhibition of human wild type Aurora kinase C at 1 uM by qPCR analysis relative to control	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775338	Binding affinity to human wild type TNIK at 1 uM by qPCR analysis	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID362969	Inhibition of GST-fused human MLK1	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
AID775454	Drug uptake in C57BL/6 mouse brain at 10 mg/kg, iv measured at 180 mins	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775344	Inhibition of human wild type BRSK2 at 1 uM by qPCR analysis relative to control	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775455	Drug uptake in C57BL/6 mouse brain at 10 mg/kg, iv measured at 60 mins	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775348	Inhibition of human wild type MLK1 at 1 uM by qPCR analysis relative to control	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775384	Inhibition of human wild type KIT at 1 uM by qPCR analysis relative to control	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID1384626	Inhibition of recombinant GST-tagged full length human MLK2 KD/LZ expressed in baculovirus using myelin basic protein as substrate preincubated for 15 mins measured after 30 mins in presence of [gamma-32P]ATP by scintillation counting	2018	Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18	Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration.
AID775345	Inhibition of human wild type CAMK2A at 1 uM by qPCR analysis relative to control	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775352	Inhibition of MLK3 (unknown origin) after 20 mins in presence of [33P]-ATP	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID363165	Inhibition of human VEGFR1 expressed in baculovirus insect cell system	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
AID775340	Binding affinity to human wild type MAP4K4 at 1 uM by qPCR analysis	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775457	Plasma concentration in C57BL/6 mouse at 10 mg/kg, iv measured at 30 mins	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID363199	Inhibition of MPTP-induced increase in pMKK4 levels in mouse at 1 mg/kg, po administered 2 hrs before MPTP challenge followed by 10 mg/kg, sc 2 hrs after MPTP challenge	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
AID1384627	Inhibition of recombinant GST-tagged full length human MLK3 KD expressed in baculovirus using myelin basic protein as substrate preincubated for 15 mins measured after 30 mins in presence of [gamma-32P]ATP by scintillation counting	2018	Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18	Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration.
AID362970	Inhibition of GST-fused human MLK3	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
AID775451	Ratio of drug level in brain to plasma in C57BL/6 mouse at 10 mg/kg, iv measured at 60 mins	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775342	Inhibition of human wild type AMPKalpha2 at 1 uM by qPCR analysis relative to control	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID775456	Plasma concentration in C57BL/6 mouse at 10 mg/kg, iv measured at 60 mins	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID125159	Inhibition of Mixed lineage kinase 1 (MLK1)	2002	Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2	Mixed lineage kinase activity of indolocarbazole analogues.
AID125162	Inhibition of Mixed lineage kinase 3 (MLK3)	2002	Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2	Mixed lineage kinase activity of indolocarbazole analogues.
AID775351	Inhibition of MLK2 (unknown origin) after 20 mins in presence of [33P]-ATP	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID1345776	Human mitogen-activated protein kinase kinase kinase 10 (MLK subfamily)	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID1345760	Human mitogen-activated protein kinase kinase kinase 9 (MLK subfamily)	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID1345784	Human mitogen-activated protein kinase kinase kinase 11 (MLK subfamily)	2001	The Journal of biological chemistry, Jul-06, Volume: 276, Issue:27	Cep-1347 (KT7515), a semisynthetic inhibitor of the mixed lineage kinase family.
AID1345760	Human mitogen-activated protein kinase kinase kinase 9 (MLK subfamily)	2001	The Journal of biological chemistry, Jul-06, Volume: 276, Issue:27	Cep-1347 (KT7515), a semisynthetic inhibitor of the mixed lineage kinase family.
AID1345784	Human mitogen-activated protein kinase kinase kinase 11 (MLK subfamily)	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
AID1345776	Human mitogen-activated protein kinase kinase kinase 10 (MLK subfamily)	2001	The Journal of biological chemistry, Jul-06, Volume: 276, Issue:27	Cep-1347 (KT7515), a semisynthetic inhibitor of the mixed lineage kinase family.
AID1798485	Mixed-Lineage Kinase Assay from Article 10.1021/jm8005838: \\Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo ac	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
[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	6 (8.33)	18.2507
2000's	54 (75.00)	29.6817
2010's	10 (13.89)	24.3611
2020's	2 (2.78)	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	4 (5.48%)	5.53%
Reviews	12 (16.44%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	57 (78.08%)	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
gamma-aminobutyric acid gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4.	2.02	1	0	amino acid zwitterion; gamma-amino acid; monocarboxylic acid	human metabolite; neurotransmitter; Saccharomyces cerevisiae metabolite; signalling molecule
ibotenic acid Ibotenic Acid: A neurotoxic isoxazole (similar to KAINIC ACID and MUSCIMOL) found in AMANITA mushrooms. It causes motor depression, ataxia, and changes in mood, perceptions and feelings, and is a potent excitatory amino acid agonist.	2.4	2	0	non-proteinogenic alpha-amino acid	neurotoxin
1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine: A dopaminergic neurotoxic compound which produces irreversible clinical, chemical, and pathological alterations that mimic those found in Parkinson disease.. 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine : A tetrahydropyridine that is 1,2,3,6-tetrahydropyridine substituted by a methyl group at position 1 and a phenyl group at position 4.	2.4	2	0	methylpyridines; phenylpyridine; tetrahydropyridine	neurotoxin
gentamicin Gentamicins: A complex of closely related aminoglycosides obtained from MICROMONOSPORA purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit PROTEIN BIOSYNTHESIS.	2.41	2	0
staurosporine aglycone staurosporine aglycone: metabolite from culture broth of Nocardiopsis sp.; a neurotrophin antag; inhibits BDNF TrkB receptor	4.72	5	0
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first source	2.01	1	0	chromones; morpholines; organochlorine compound	autophagy inhibitor; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; geroprotector
oxidopamine Oxidopamine: A neurotransmitter analogue that depletes noradrenergic stores in nerve endings and induces a reduction of dopamine levels in the brain. Its mechanism of action is related to the production of cytolytic free-radicals.. oxidopamine : A benzenetriol that is phenethylamine in which the hydrogens at positions 2, 4, and 5 on the phenyl ring are replaced by hydroxy groups. It occurs naturally in human urine, but is also produced as a metabolite of the drug DOPA (used for the treatment of Parkinson's disease).	2.04	1	0	benzenetriol; catecholamine; primary amino compound	drug metabolite; human metabolite; neurotoxin
pd 98059 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one: inhibits MAP kinase kinase (MEK) activity, p42 MAPK and p44 MAPK; structure in first source. 2-(2-amino-3-methoxyphenyl)chromen-4-one : A member of the class of monomethoxyflavones that is 3'-methoxyflavone bearing an additional amino substituent at position 2'.	2.41	2	0	aromatic amine; monomethoxyflavone	EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector
zonisamide Zonisamide: A benzisoxazole and sulfonamide derivative that acts as a CALCIUM CHANNEL blocker. It is used primarily as an adjunctive antiepileptic agent for the treatment of PARTIAL SEIZURES, with or without secondary generalization.. zonisamide : A 1,2-benzoxazole compound having a sulfamoylmethyl substituent at the 3-position.	3.14	1	0	1,2-benzoxazoles; sulfonamide	anticonvulsant; antioxidant; central nervous system drug; protective agent; T-type calcium channel blocker
levodopa Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease	5.72	3	1	amino acid zwitterion; dopa; L-tyrosine derivative; non-proteinogenic L-alpha-amino acid	allelochemical; antidyskinesia agent; antiparkinson drug; dopaminergic agent; hapten; human metabolite; mouse metabolite; neurotoxin; plant growth retardant; plant metabolite; prodrug
lactose Lactose: A disaccharide of GLUCOSE and GALACTOSE in human and cow milk. It is used in pharmacy for tablets, in medicine as a nutrient, and in industry.. lactose : A glycosylglucose disaccharide, found most notably in milk, that consists of D-galactose and D-glucose fragments bonded through a beta-1->4 glycosidic linkage. The glucose fragment can be in either the alpha- or beta-pyranose form, whereas the galactose fragment can only have the beta-pyranose form.. beta-lactose : The beta-anomer of lactose.	2.03	1	0	lactose
colchicine (S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions.	2.03	1	0	alkaloid; colchicine	anti-inflammatory agent; gout suppressant; mutagen
cytarabine [no description available]	2.01	1	0	beta-D-arabinoside; monosaccharide derivative; pyrimidine nucleoside	antimetabolite; antineoplastic agent; antiviral agent; immunosuppressive agent
pyrroles 1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.	2.08	1	0	pyrrole; secondary amine
framycetin Framycetin: A component of NEOMYCIN that is produced by Streptomyces fradiae. On hydrolysis it yields neamine and neobiosamine B. (From Merck Index, 11th ed). framycetin : A tetracyclic antibacterial agent derived from neomycin, being a glycoside ester of neamine and neobiosamine B.	2.41	2	0	aminoglycoside	allergen; antibacterial drug; Escherichia coli metabolite
pyrazolanthrone pyrazolanthrone: JNK (c-Jun N-terminal kinase) inhibitor; structure in first source. anthra[1,9-cd]pyrazol-6(2H)-one : A member of the class of anthrapyrazoles that is anthra[1,9-cd]pyrazole substituted at position 6 by an oxo group. An inhibitor of c-Jun N-terminal kinase.	4.32	3	0	anthrapyrazole; aromatic ketone; cyclic ketone	antineoplastic agent; c-Jun N-terminal kinase inhibitor; geroprotector
isoxazoles Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent.	3.14	1	0	isoxazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
thiazoles [no description available]	3.53	2	0	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
methamphetamine Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.. methamphetamine : A member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent.	2.02	1	0	amphetamines; secondary amine	central nervous system stimulant; environmental contaminant; neurotoxin; psychotropic drug; xenobiotic
acetylcysteine N-acetyl-L-cysteine : An N-acetyl-L-amino acid that is the N-acetylated derivative of the natural amino acid L-cysteine.	2	1	0	acetylcysteine; L-cysteine derivative; N-acetyl-L-amino acid	antidote to paracetamol poisoning; antiinfective agent; antioxidant; antiviral drug; ferroptosis inhibitor; geroprotector; human metabolite; mucolytic; radical scavenger; vulnerary
ferrous chloride ferrous chloride: induces convulsions; RN given refers to parent cpd	2.02	1	0	iron coordination entity
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	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).	2.17	1	0	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent
etoposide [no description available]	2.01	1	0	beta-D-glucoside; furonaphthodioxole; organic heterotetracyclic compound	antineoplastic agent; DNA synthesis inhibitor
1-methyl-4-phenylpyridinium 1-Methyl-4-phenylpyridinium: An active neurotoxic metabolite of 1-METHYL-4-PHENYL-1,2,3,6-TETRAHYDROPYRIDINE. The compound reduces dopamine levels, inhibits the biosynthesis of catecholamines, depletes cardiac norepinephrine and inactivates tyrosine hydroxylase. These and other toxic effects lead to cessation of oxidative phosphorylation, ATP depletion, and cell death. The compound, which is related to PARAQUAT, has also been used as an herbicide.. N-methyl-4-phenylpyridinium : A pyridinium ion that is N-methylpyridinium having a phenyl substituent at the 4-position.	2.02	1	0	pyridinium ion	apoptosis inducer; herbicide; human xenobiotic metabolite; neurotoxin
staurosporine [no description available]	2.08	1	0	indolocarbazole alkaloid; organic heterooctacyclic compound	apoptosis inducer; bacterial metabolite; EC 2.7.11.13 (protein kinase C) inhibitor; geroprotector
thiazolyl blue thiazolyl blue: RN & II refers to bromide. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide : The bromide salt of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium.	2.03	1	0	organic bromide salt	colorimetric reagent; dye
lestaurtinib [no description available]	2.08	1	0	indolocarbazole
atazanavir sulfate Atazanavir Sulfate: An azapeptide and HIV-PROTEASE INHIBITOR that is used in the treatment of HIV INFECTIONS and AIDS in combination with other ANTI-HIV AGENTS.	2.08	1	0	organic sulfate salt
sb 203580 [no description available]	2.92	4	0	imidazoles; monofluorobenzenes; pyridines; sulfoxide	EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector; Hsp90 inhibitor; neuroprotective agent
ritonavir Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.	2.08	1	0	1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas	antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic
cocaine Cocaine: An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.. cocaine : A tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca.	3.48	1	1	benzoate ester; methyl ester; tertiary amino compound; tropane alkaloid	adrenergic uptake inhibitor; central nervous system stimulant; dopamine uptake inhibitor; environmental contaminant; local anaesthetic; mouse metabolite; plant metabolite; serotonin uptake inhibitor; sodium channel blocker; sympathomimetic agent; vasoconstrictor agent; xenobiotic
pd 173955 PD 173955: inhibits src family-selective tyrosine kinase; structure in first source	2.08	1	0	aryl sulfide; dichlorobenzene; methyl sulfide; pyridopyrimidine	tyrosine kinase inhibitor
cystine [no description available]	2.02	1	0
su 11248 [no description available]	3.27	1	0	monocarboxylic acid amide; pyrroles	angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; immunomodulator; neuroprotective agent; vascular endothelial growth factor receptor antagonist
pregabalin Pregabalin: A gamma-aminobutyric acid (GABA) derivative that functions as a CALCIUM CHANNEL BLOCKER and is used as an ANTICONVULSANT as well as an ANTI-ANXIETY AGENT. It is also used as an ANALGESIC in the treatment of NEUROPATHIC PAIN and FIBROMYALGIA.. pregabalin : A gamma-amino acid that is gamma-aminobutyric acid (GABA) carrying an isobutyl substitutent at the beta-position (the S-enantiomer). Binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues.	2.02	1	0	gamma-amino acid	anticonvulsant; calcium channel blocker
vx680 [no description available]	3.62	2	0	N-arylpiperazine
gw-5074 [no description available]	3.12	1	0
oxepins Oxepins: Compounds based on a 7-membered heterocyclic ring including an oxygen. They can be considered a medium ring ether. A natural source is the MONTANOA plant genus. Some dibenzo-dioxepins, called depsidones, are found in GARCINIA plants.	3.14	1	0
midostaurin midostaurin : An organic heterooctacyclic compound that is the N-benzoyl derivative of staurosporine.	2.08	1	0	benzamides; gamma-lactam; indolocarbazole; organic heterooctacyclic compound	antineoplastic agent; EC 2.7.11.13 (protein kinase C) inhibitor
flag peptide FLAG peptide: engineered as a tag for immunoaffinity purification of genetically-engineered proteins; amino acid sequence given in first source; a polar octapeptide. FLAG peptide : An eight amino acid peptide consisting of L-aspartic acid, L-tyrosine, L-lysine, four L-aspartic acid residues, and L-lysine joined in sequence by peptide linkages. It is widely used as a fusion tag for the purification and detection of a wide variety of recombinant proteins.	2.04	1	0	peptide
as 601245 1,3-benzothiazol-2-yl(2-((2-(3-pyridinyl)ethyl)amino)-4-pyrimidinyl)acetonitrile: a c-Jun NH2-terminal protein kinase inhibitor with neuroprotective activity; also an NSAID	3.12	1	0	benzothiazoles
pazopanib pazopanib: a protein kinase inhibitor. pazopanib : A pyrimidine that is 5-(pyrimidin-2-yl}amino-2-methylbenzenesulfonamide substituted at position 4 by a (2,3-dimethylindazol-6-yl)(methyl)amino group. Used as its hydrochloride salt for treatment of kidney cancer.	2.08	1	0	aminopyrimidine; indazoles; sulfonamide	angiogenesis modulating agent; antineoplastic agent; tyrosine kinase inhibitor; vascular endothelial growth factor receptor antagonist
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one [no description available]	2.08	1	0	methoxybenzenes; substituted aniline
kw 2449 KW 2449: has both multikinase inhibitory activity and antineoplastic activity; structure in first source	2.08	1	0
nvp-tae684 [no description available]	2.08	1	0	piperidines
ceruletide Ceruletide: A specific decapeptide obtained from the skin of Hila caerulea, an Australian amphibian. Caerulein is similar in action and composition to CHOLECYSTOKININ. It stimulates gastric, biliary, and pancreatic secretion; and certain smooth muscle. It is used in paralytic ileus and as diagnostic aid in pancreatic malfunction.. ceruletide : A decapeptide comprising 5-oxoprolyl, glutamyl, aspartyl, O-sulfotyrosyl, threonyl, glycyl, tryptopyl, methionyl, aspartyl and phenylalaninamide residues in sequence. Found in the skins of certain Australian amphibians, it is an analogue of the gastrointestinal peptide hormone cholecystokinin and stimulates gastric, biliary, and pancreatic secretion. It is used in cases of paralysis of the intestine (paralytic ileus) and as a diagnostic aid in pancreatic malfunction.	2.41	2	0	oligopeptide	diagnostic agent; gastrointestinal drug
calpain Calpain: Cysteine proteinase found in many tissues. Hydrolyzes a variety of endogenous proteins including NEUROPEPTIDES; CYTOSKELETAL PROTEINS; proteins from SMOOTH MUSCLE; CARDIAC MUSCLE; liver; platelets; and erythrocytes. Two subclasses having high and low calcium sensitivity are known. Removes Z-discs and M-lines from myofibrils. Activates phosphorylase kinase and cyclic nucleotide-independent protein kinase. This enzyme was formerly listed as EC 3.4.22.4.	2	1	0
gsk 1363089 GSK 1363089: a multikinase inhibitor that acts on Met, RON, Axl, and VEGFR; structure in first source	2.08	1	0	aromatic ether
urmc-099 URMC-099: inhibits mixed lineage kinase 3	2.08	1	0
transforming growth factor beta Transforming Growth Factor beta: A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.	2	1	0
cyclin d1 Cyclin D1: Protein encoded by the bcl-1 gene which plays a critical role in regulating the cell cycle. Overexpression of cyclin D1 is the result of bcl-1 rearrangement, a t(11;14) translocation, and is implicated in various neoplasms.	2.02	1	0
didanosine Didanosine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase; ddI is then metabolized to dideoxyadenosine triphosphate, its putative active metabolite.. didanosine : A purine 2',3'-dideoxyribonucleoside that is inosine in which the hydroxy groups at both the 2' and the 3' positions on the sugar moiety have been replaced by hydrogen. An antiviral drug, it is used as a medication to treat HIV/AIDS.	2.02	1	0	purine 2',3'-dideoxyribonucleoside	antimetabolite; antiviral drug; EC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor; geroprotector; HIV-1 reverse transcriptase inhibitor
nintedanib nintedanib : A member of the class of oxindoles that is a kinase inhibitor used (in the form of its ethylsulfonate salt) for the treatment of idiopathic pulmonary fibrosis and cancer.	2.08	1	0
cep-11004 CEP-11004: inhibitors of the c-Jun N-terminal kinase (JNK) signaling pathway	2.95	4	0

Condition	Indicated	Relationship Strength	Studies	Trials
Cognition Disorders Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment.	0	2.08	1	0
HIV Coinfection [description not available]	0	2.49	2	0
HIV Infections Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).	0	2.49	2	0
Degenerative Diseases, Central Nervous System [description not available]	0	4.9	4	0
Neurodegenerative Diseases Hereditary and sporadic conditions which are characterized by progressive nervous system dysfunction. These disorders are often associated with atrophy of the affected central or peripheral nervous system structures.	0	4.9	4	0
Cancer of the Retina [description not available]	0	2.41	1	0
Glial Cell Tumors [description not available]	0	2.41	1	0
Eye Cancer, Retinoblastoma [description not available]	0	2.72	2	0
Glioma Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)	0	2.41	1	0
Retinoblastoma A malignant tumor arising from the nuclear layer of the retina that is the most common primary tumor of the eye in children. The tumor tends to occur in early childhood or infancy and may be present at birth. The majority are sporadic, but the condition may be transmitted as an autosomal dominant trait. Histologic features include dense cellularity, small round polygonal cells, and areas of calcification and necrosis. An abnormal pupil reflex (leukokoria); NYSTAGMUS, PATHOLOGIC; STRABISMUS; and visual loss represent common clinical characteristics of this condition. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, p2104)	0	2.72	2	0
Cancer of Ovary [description not available]	0	2.17	1	0
Local Neoplasm Recurrence [description not available]	0	2.17	1	0
Ovarian Neoplasms Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.	0	2.17	1	0
Breast Cancer [description not available]	0	2.08	1	0
Breast Neoplasms Tumors or cancer of the human BREAST.	0	2.08	1	0
Idiopathic Parkinson Disease [description not available]	0	11.51	16	7
Parkinson Disease A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)	1	13.51	16	7
Disease Exacerbation [description not available]	0	8.14	7	5
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	4.2	6	0
Akinetic-Rigid Variant of Huntington Disease [description not available]	0	2.44	2	0
Huntington Disease A familial disorder inherited as an autosomal dominant trait and characterized by the onset of progressive CHOREA and DEMENTIA in the fourth or fifth decade of life. Common initial manifestations include paranoia; poor impulse control; DEPRESSION; HALLUCINATIONS; and DELUSIONS. Eventually intellectual impairment; loss of fine motor control; ATHETOSIS; and diffuse chorea involving axial and limb musculature develops, leading to a vegetative state within 10-15 years of disease onset. The juvenile variant has a more fulminant course including SEIZURES; ATAXIA; dementia; and chorea. (From Adams et al., Principles of Neurology, 6th ed, pp1060-4)	0	2.44	2	0
Anoxia-Ischemia, Brain [description not available]	0	2.05	1	0
Innate Inflammatory Response [description not available]	0	2.73	3	0
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	0	2.73	3	0
Hypoxia-Ischemia, Brain A disorder characterized by a reduction of oxygen in the blood combined with reduced blood flow (ISCHEMIA) to the brain from a localized obstruction of a cerebral artery or from systemic hypoperfusion. Prolonged hypoxia-ischemia is associated with ISCHEMIC ATTACK, TRANSIENT; BRAIN INFARCTION; BRAIN EDEMA; COMA; and other conditions.	0	2.05	1	0
Astrocytosis [description not available]	0	2.44	2	0
Acquired-Immune Deficiency Syndrome Dementia Complex [description not available]	0	2.05	1	0
AIDS Dementia Complex A neurologic condition associated with the ACQUIRED IMMUNODEFICIENCY SYNDROME and characterized by impaired concentration and memory, slowness of hand movements, ATAXIA, incontinence, apathy, and gait difficulties associated with HIV-1 viral infection of the central nervous system. Pathologic examination of the brain reveals white matter rarefaction, perivascular infiltrates of lymphocytes, foamy macrophages, and multinucleated giant cells. (From Adams et al., Principles of Neurology, 6th ed, pp760-1; N Engl J Med, 1995 Apr 6;332(14):934-40)	0	2.05	1	0
Benign Neoplasms [description not available]	0	3.44	1	1
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	3.44	1	1
Autosomal Dominant Juvenile Parkinson Disease [description not available]	0	2.43	2	0
Parkinsonian Disorders A group of disorders which feature impaired motor control characterized by bradykinesia, MUSCLE RIGIDITY; TREMOR; and postural instability. Parkinsonian diseases are generally divided into primary parkinsonism (see PARKINSON DISEASE), secondary parkinsonism (see PARKINSON DISEASE, SECONDARY) and inherited forms. These conditions are associated with dysfunction of dopaminergic or closely related motor integration neuronal pathways in the BASAL GANGLIA.	0	2.43	2	0
Deafness, Transitory [description not available]	0	2.93	1	0
Acute Confusional Senile Dementia [description not available]	0	3.33	2	0
Alzheimer Disease A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)	0	3.33	2	0
Hearing Loss A general term for the complete or partial loss of the ability to hear from one or both ears.	0	2.93	1	0
Diarrhea An increased liquidity or decreased consistency of FECES, such as running stool. Fecal consistency is related to the ratio of water-holding capacity of insoluble solids to total water, rather than the amount of water present. Diarrhea is not hyperdefecation or increased fecal weight.	0	3.4	1	1
Apoplexy [description not available]	0	2.02	1	0
Ache [description not available]	0	2.02	1	0
Peripheral Nerve Diseases [description not available]	0	2.02	1	0
Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.	0	2.02	1	0
Peripheral Nervous System Diseases Diseases of the peripheral nerves external to the brain and spinal cord, which includes diseases of the nerve roots, ganglia, plexi, autonomic nerves, sensory nerves, and motor nerves.	0	2.02	1	0
Stroke A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)	0	2.02	1	0
Benign Neoplasms, Brain [description not available]	0	2.94	1	0
Brain Neoplasms Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.	0	2.94	1	0
Nerve Degeneration Loss of functional activity and trophic degeneration of nerve axons and their terminal arborizations following the destruction of their cells of origin or interruption of their continuity with these cells. The pathology is characteristic of neurodegenerative diseases. Often the process of nerve degeneration is studied in research on neuroanatomical localization and correlation of the neurophysiology of neural pathways.	0	9.06	9	4
Brain Inflammation [description not available]	0	2.02	1	0
Encephalitis Inflammation of the BRAIN due to infection, autoimmune processes, toxins, and other conditions. Viral infections (see ENCEPHALITIS, VIRAL) are a relatively frequent cause of this condition.	0	2.02	1	0
MPTP Neurotoxicity Syndrome [description not available]	0	2	1	0
Acoustic Trauma Usually refer to hearing loss due to a single noise event such as an explosion or shotgun blast.	0	2	1	0
Hearing Loss, Noise-Induced Hearing loss due to exposure to explosive loud noise or chronic exposure to sound level greater than 85 dB. The hearing loss is often in the frequency range 4000-6000 hertz.	0	2	1	0
Anasarca [description not available]	0	2	1	0
Pancreatic Diseases Pathological processes of the PANCREAS.	0	2	1	0
Acute Edematous Pancreatitis [description not available]	0	2.41	2	0
Edema Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.	0	2	1	0
Pancreatitis INFLAMMATION of the PANCREAS. Pancreatitis is classified as acute unless there are computed tomographic or endoscopic retrograde cholangiopancreatographic findings of CHRONIC PANCREATITIS (International Symposium on Acute Pancreatitis, Atlanta, 1992). The two most common forms of acute pancreatitis are ALCOHOLIC PANCREATITIS and gallstone pancreatitis.	0	2.41	2	0
Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.	0	2	1	0
Acute Disease Disease having a short and relatively severe course.	0	2	1	0
Necrosis The death of cells in an organ or tissue due to disease, injury or failure of the blood supply.	0	2	1	0

3,9-bis((ethylthio)methyl)-k-252a

Description

Cross-References

Synonyms (31)

Research Excerpts

Toxicity

Bioavailability

Protein Targets (8)

Inhibition Measurements

Biological Processes (130)

Molecular Functions (36)

Ceullar Components (33)

Bioassays (58)

Research

Studies (72)

Market Indicators

Research Demand Index: 10.47

Study Types

3,9-bis((ethylthio)methyl)-k-252a

Description

Cross-References

Synonyms (31)

Research Excerpts

Toxicity

Bioavailability

Protein Targets (8)

Inhibition Measurements

Biological Processes (130)

Molecular Functions (36)

Ceullar Components (33)

Bioassays (58)

Research

Studies (72)

Market Indicators

Research Demand Index: 10.47

Study Types

Related Drugs (55)

Related Conditions (59)