Page last updated: 2024-11-12

bx 517

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Description

BX 517: a phosphoinositide-dependent kinase-1 inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	11161844
CHEMBL ID	228654
SCHEMBL ID	5567818
MeSH ID	M0513672

Synonyms (35)

Synonym
bx-517
indolinone based inhibitor, 4i
[(3z)-2-oxo-3-[1-(1h-pyrrol-2-yl)ethylidene]-2,3-dihydro-1h-indol-5-yl]urea
bdbm17004
bx 517
CHEMBL228654
S6504
850717-64-5
urea, n-(2,3-dihydro-2-oxo-3-((3z)-1-(1h-pyrrol-2-yl)ethylidene)-1h-indol-5-yl)-
syv8vn8w5k ,
unii-syv8vn8w5k
5-ureido-3-(1-(pyrrol-2-yl)ethylidene)indolin-2-one
946843-63-6
urea, n-(2,3-dihydro-2-oxo-3-(1-(1h-pyrrol-2-yl)ethylidene)-1h-indol-5-yl)-
urea, (2,3-dihydro-2-oxo-3-(1-(1h-pyrrol-2-yl)ethylidene)-1h-indol-5-yl)-
SCHEMBL5567818
bx517 ,
HY-13842
CS-6066
{2-oxo-3-[1-(1h-pyrrol-2-yl)ethylidene]-2,3-dihydro-1h-indol-5-yl}urea
pdk-1 inhibitors
AKOS032945106
pdk1 inhibitor2
pdk1 inhibitor ii;bx-517;bx517;bx 517
BCP16225
(z)-1-(3-(1-(1h-pyrrol-2-yl)ethylidene)-2-oxoindolin-5-yl)urea
EX-A2243
pdk1 inhibitor 2
[(3z)-2-oxo-3-[1-(1h-pyrrol-2-yl)ethylidene]-1h-indol-5-yl]urea
NCGC00486863-01
urea, [2,3-dihydro-2-oxo-3-[1-(1h-pyrrol-2-yl)ethylidene]-1h-indol-5-yl]-
Q27289467
F85475
MS-24008
(z)-n-(3-(1-(1h-pyrrol-2-yl)ethylidene)-2-hydroxy-3h-indol-5-yl)carbamimidic acid

Research Excerpts

Bioavailability

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

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)	IC50 (µMol)	0.0178	0.0025	1.4513	9.0000	AID1388455; AID1797575; AID1797577; AID1797578; AID291127; AID299513; AID299515; AID729480
RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)	IC50 (µMol)	0.1000	0.0002	0.7387	10.0000	AID299516
RAC-beta serine/threonine-protein kinase	Homo sapiens (human)	IC50 (µMol)	0.0050	0.0005	0.5013	7.6000	AID291126
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (164)

Process	via Protein(s)	Taxonomy
intracellular signal transduction	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
type B pancreatic cell development	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
protein phosphorylation	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
negative regulation of protein kinase activity	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
hyperosmotic response	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
epidermal growth factor receptor signaling pathway	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
insulin receptor signaling pathway	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
positive regulation of phospholipase activity	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
negative regulation of cardiac muscle cell apoptotic process	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
cell migration	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
peptidyl-threonine phosphorylation	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
calcium-mediated signaling	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
actin cytoskeleton organization	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathway	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
T cell costimulation	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
activation of protein kinase B activity	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
cellular response to insulin stimulus	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
negative regulation of toll-like receptor signaling pathway	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
regulation of canonical NF-kappaB signal transduction	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
regulation of mast cell degranulation	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
positive regulation of angiogenesis	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
protein autophosphorylation	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
insulin-like growth factor receptor signaling pathway	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosol	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
cellular response to epidermal growth factor stimulus	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
extrinsic apoptotic signaling pathway	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
positive regulation of protein localization to plasma membrane	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
positive regulation of sprouting angiogenesis	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
positive regulation of vascular endothelial cell proliferation	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
negative regulation of endothelial cell apoptotic process	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
peptidyl-serine phosphorylation	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
intracellular signal transduction	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
protein phosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
activation-induced cell death of T cells	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
intracellular signal transduction	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
osteoblast differentiation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
maternal placenta development	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of protein phosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of endothelial cell proliferation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cell migration involved in sprouting angiogenesis	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
glycogen biosynthetic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of glycogen biosynthetic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
glucose metabolic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of translation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein phosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of protein kinase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein import into nucleus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
nitric oxide biosynthetic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
inflammatory response	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
response to oxidative stress	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
signal transduction	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
epidermal growth factor receptor signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
G protein-coupled receptor signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
canonical NF-kappaB signal transduction	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cell population proliferation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
insulin receptor signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
apoptotic mitochondrial changes	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
response to heat	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
gene expression	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of autophagy	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of endothelial cell migration	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of gene expression	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of gene expression	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of long-chain fatty acid import across plasma membrane	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
fibroblast migration	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of fibroblast migration	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of sodium ion transport	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of glucose metabolic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of endopeptidase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of neuron projection development	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of macroautophagy	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
phosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein ubiquitination	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
peptidyl-serine phosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
peptidyl-threonine phosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
virus-mediated perturbation of host defense response	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cytokine-mediated signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
mammalian oogenesis stage	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cell differentiation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of cell growth	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of cell migration	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of cell migration	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
T cell costimulation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of protein ubiquitination	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of myelination	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
lipopolysaccharide-mediated signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
TOR signaling	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of fatty acid beta-oxidation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of endodeoxyribonuclease activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of protein binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
response to food	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
peripheral nervous system myelin maintenance	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to insulin stimulus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
response to fluid shear stress	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to reactive oxygen species	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
interleukin-18-mediated signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to decreased oxygen levels	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
non-canonical NF-kappaB signal transduction	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
glucose homeostasis	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of apoptotic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of apoptotic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
anoikis	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of mRNA stability	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of nitric oxide biosynthetic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of fat cell differentiation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of glycogen biosynthetic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of Notch signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of proteolysis	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of DNA-templated transcription	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of glucose import	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of organ growth	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein autophosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of lipid biosynthetic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
insulin-like growth factor receptor signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
behavioral response to pain	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of smooth muscle cell proliferation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of nitric-oxide synthase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of DNA-binding transcription factor activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
striated muscle cell differentiation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of protein metabolic process	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
excitatory postsynaptic potential	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
response to growth hormone	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
mammary gland epithelial cell differentiation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
labyrinthine layer blood vessel development	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
response to UV-A	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
response to growth factor	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to cadmium ion	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to tumor necrosis factor	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to epidermal growth factor stimulus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to prostaglandin E stimulus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of protein serine/threonine kinase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
establishment of protein localization to mitochondrion	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
maintenance of protein location in mitochondrion	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of release of cytochrome c from mitochondria	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to granulocyte macrophage colony-stimulating factor stimulus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
execution phase of apoptosis	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of postsynapse organization	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of tRNA methylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to oxidised low-density lipoprotein particle stimulus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of protein localization to lysosome	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of cGAS/STING signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycle	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of protein localization to nucleus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to peptide	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of signal transduction by p53 class mediator	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of cilium assembly	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of oxidative stress-induced intrinsic apoptotic signaling pathway	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of leukocyte cell-cell adhesion	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of protein localization to plasma membrane	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of I-kappaB phosphorylation	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of TORC1 signaling	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of protein localization to endoplasmic reticulum	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cellular response to nerve growth factor stimulus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
response to insulin-like growth factor stimulus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of protein localization to cell surface	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
regulation of type B pancreatic cell development	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of lymphocyte migration	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligand	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
intracellular signal transduction	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
glycogen biosynthetic process	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
glucose metabolic process	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
regulation of translation	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
signal transduction	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
insulin receptor signaling pathway	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
negative regulation of long-chain fatty acid import across plasma membrane	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of glucose metabolic process	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
regulation of cell migration	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of cell migration	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of fatty acid beta-oxidation	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
peripheral nervous system myelin maintenance	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
cellular response to insulin stimulus	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
protein modification process	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
fat cell differentiation	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of glycogen biosynthetic process	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of glucose import	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
regulation of cell cycle	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
mammary gland epithelial cell differentiation	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
cellular response to high light intensity	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
organic substance transport	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
protein localization to plasma membrane	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of protein targeting to membrane	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
retinal rod cell apoptotic process	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
positive regulation of cell motility	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
intracellular signal transduction	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
peptidyl-serine phosphorylation	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Process	via Protein(s)	Taxonomy
protein serine/threonine kinase activity	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
3-phosphoinositide-dependent protein kinase activity	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
protein binding	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
ATP binding	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
phospholipase activator activity	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
phospholipase binding	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
protein serine kinase activity	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
protein kinase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein serine/threonine kinase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein serine/threonine/tyrosine kinase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
calmodulin binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
ATP binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
phosphatidylinositol-3,4,5-trisphosphate binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
kinase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
enzyme binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein kinase binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
nitric-oxide synthase regulator activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein serine/threonine kinase inhibitor activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
identical protein binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein homodimerization activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
phosphatidylinositol-3,4-bisphosphate binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
14-3-3 protein binding	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
potassium channel activator activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein serine kinase activity	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein serine/threonine kinase activity	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
protein binding	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
ATP binding	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
metal ion binding	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
protein serine kinase activity	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
molecular function activator activity	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (24)

Process	via Protein(s)	Taxonomy
nucleus	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
cytoplasm	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
cytosol	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
plasma membrane	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
focal adhesion	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
postsynaptic density	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
cytoplasmic vesicle	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
cell projection	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
cytoplasm	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
mitochondrial intermembrane space	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
membrane	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
nucleus	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
nucleoplasm	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cytoplasm	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
spindle	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cytosol	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
plasma membrane	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cell-cell junction	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
cell cortex	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
microtubule cytoskeleton	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
lamellipodium	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
vesicle	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
ciliary basal body	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
postsynapse	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
glutamatergic synapse	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
protein-containing complex	RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)
nucleus	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
nucleoplasm	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
early endosome	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
cytosol	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
plasma membrane	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
cell cortex	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
ruffle membrane	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
intracellular membrane-bounded organelle	RAC-beta serine/threonine-protein kinase	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (23)

Assay ID	Title	Year	Journal	Article
AID299522	Selectivity for PDK1 over PKA	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.
AID291131	Stability in human liver microsomes after 1 hr	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517.
AID299516	Inhibition of Akt phosphorylation in PC3 cells	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.
AID291126	Inhibition of AKT2	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517.
AID291130	Volume of distribution at steady state in rat 5 mg/kg, iv	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517.
AID299517	Inhibition of PKA	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.
AID291127	Inhibition of AKT phosphorylation in PC3 cells	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517.
AID729480	Inhibition of PDK1 (unknown origin)	2013	Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7	Selective 3-phosphoinositide-dependent kinase 1 (PDK1) inhibitors: dissecting the function and pharmacology of PDK1.
AID291128	Half life in rat at 5 mg/kg, iv	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517.
AID291132	Solubility in PBS	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517.
AID299521	Oral bioavailability in rat at 10 mg/kg	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.
AID1388455	Inhibition of PDK1 (unknown origin) after 1 hr in presence of Ser/Thr-07 by fluorometric assay	2017	Bioorganic & medicinal chemistry letters, 12-15, Volume: 27, Issue:24	Fragment-based design, synthesis, biological evaluation, and SAR of 1H-benzo[d]imidazol-2-yl)-1H-indazol derivatives as potent PDK1 inhibitors.
AID299513	Inhibition of PDK1 mediated cAKT2 phosphorylation by AKT2 activation assay	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.
AID291129	Clearance in rat at 5 mg/kg, iv	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517.
AID299518	Solubility in phosphate buffered saline	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.
AID299520	Clearance in rat at 2 mg/kg, iv	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.
AID299515	Inhibition of PDK1	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.
AID299519	Half life in rat at 2 mg/kg, iv	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.
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.
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.
AID1797578	PDK1 Activity Assay (33P-filter paper) from Article 10.1016/j.bmcl.2007.04.071: \\Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.\\	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.
AID1797577	PDK1-mediated AKT2 Activation Assay (cAKT2 33P-SPA) from Article 10.1016/j.bmcl.2007.04.071: \\Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.\\	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.
AID1797575	PDK1-mediated AKT2 Activation Assay (cAKT2 33P-SPA) from Article 10.1016/j.bmcl.2007.05.060: \\Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517.\\	2007	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	2 (40.00)	29.6817
2010's	3 (60.00)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.84

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	12.84 (24.57)
Research Supply Index	1.79 (2.92)
Research Growth Index	4.63 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (12.84)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	5 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
urea pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.	2.03	1	isourea; monocarboxylic acid amide; one-carbon compound	Daphnia magna metabolite; Escherichia coli metabolite; fertilizer; flour treatment agent; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
osu 03012 OSU 03012: a PDK-1 inhibitor; structure in first source	2.08	1	antibiotic antifungal drug; aromatic amide; glycine derivative; organofluorine compound; phenanthrenes; pyrazoles	antineoplastic agent; apoptosis inducer; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
gsk 2334470 GSK 2334470: a PDK1 inhibitor; structure in first source	2.08	1	indazoles
1-[(3,4-difluorophenyl)methyl]-2-oxo-N-[(1R)-2-[(2-oxo-1,3-dihydrobenzimidazol-5-yl)oxy]-1-phenylethyl]-3-pyridinecarboxamide [no description available]	2.08	1	benzimidazoles

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