plx647 profile

ID Source	ID
PubMed CID	11545419
CHEMBL ID	4224714
SCHEMBL ID	1268018
MeSH ID	M0585427

Synonym
5-(1h-pyrrolo[2,3-b]pyridin-3-ylmethyl)-n-[4-(trifluoromethyl)benzyl]pyridin-2-amine
4HVS
[5-(1h-pyrrolo[2,3-b]pyridin-3-ylmethyl)-pyridin-2-yl]-(4-trifluoromethyl-benzyl)-amine
CS-3984
SCHEMBL1268018
5-((1h-pyrrolo[2,3-b]pyridin-3-yl)methyl)-n-(4-(trifluoromethyl)benzyl)pyridin-2-amine
873786-09-5
plx647
AC-35285
5-(1h-pyrrolo[2,3-b]pyridin-3-ylmethyl)-n-[[4-(trifluoromethyl)phenyl]methyl]pyridin-2-amine
HY-13838
J-690377
AKOS026750267
EX-A586
5-(1h-pyrrolo[2,3-b]pyridin-3-ylmethyl)-n-[[4-(trifluoromethyl)phenyl]methyl]-2-pyridinamine
mfcd28100808
NCGC00371004-04
plx-647
FT-0700390
AS-16576
BCP15182
NCGC00481596-01
Q27456207
CHEMBL4224714 ,
bdbm50460038
A857023
5-({1h-pyrrolo[2,3-b]pyridin-3-yl}methyl)-n-{[4-(trifluoromethyl)phenyl]methyl}pyridin-2-amine

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

Protein Targets (10)

Potency Measurements

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
PPM1D protein	Homo sapiens (human)	Potency	16.5388	0.0052	9.4661	32.9993	AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	6.7412	0.0123	7.9835	43.2770	AID1645841
G	Vesicular stomatitis virus	Potency	1.1988	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2D6	Homo sapiens (human)	Potency	0.1900	0.0010	8.3798	61.1304	AID1645840
Interferon beta	Homo sapiens (human)	Potency	12.7038	0.0033	9.1582	39.8107	AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	1.1988	0.0123	8.9648	39.8107	AID1645842
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	1.1988	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	1.1988	0.0123	8.9648	39.8107	AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)	IC50 (µMol)	0.0280	0.0006	0.5676	5.5450	AID1388792
Mast/stem cell growth factor receptor Kit	Homo sapiens (human)	IC50 (µMol)	0.0160	0.0007	0.4708	10.0000	AID1388793
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (147)

Process	via Protein(s)	Taxonomy
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell activation involved in immune response	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to virus	Interferon beta	Homo sapiens (human)
positive regulation of autophagy	Interferon beta	Homo sapiens (human)
cytokine-mediated signaling pathway	Interferon beta	Homo sapiens (human)
natural killer cell activation	Interferon beta	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT protein	Interferon beta	Homo sapiens (human)
cellular response to interferon-beta	Interferon beta	Homo sapiens (human)
B cell proliferation	Interferon beta	Homo sapiens (human)
negative regulation of viral genome replication	Interferon beta	Homo sapiens (human)
innate immune response	Interferon beta	Homo sapiens (human)
positive regulation of innate immune response	Interferon beta	Homo sapiens (human)
regulation of MHC class I biosynthetic process	Interferon beta	Homo sapiens (human)
negative regulation of T cell differentiation	Interferon beta	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Interferon beta	Homo sapiens (human)
defense response to virus	Interferon beta	Homo sapiens (human)
type I interferon-mediated signaling pathway	Interferon beta	Homo sapiens (human)
neuron cellular homeostasis	Interferon beta	Homo sapiens (human)
cellular response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
cellular response to virus	Interferon beta	Homo sapiens (human)
negative regulation of Lewy body formation	Interferon beta	Homo sapiens (human)
negative regulation of T-helper 2 cell cytokine production	Interferon beta	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell differentiation	Interferon beta	Homo sapiens (human)
natural killer cell activation involved in immune response	Interferon beta	Homo sapiens (human)
adaptive immune response	Interferon beta	Homo sapiens (human)
T cell activation involved in immune response	Interferon beta	Homo sapiens (human)
humoral immune response	Interferon beta	Homo sapiens (human)
positive regulation of T cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
adaptive immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independent	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of T cell anergy	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
defense response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
detection of bacterium	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-12 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-6 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protection from natural killer cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
innate immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of dendritic cell differentiation	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class Ib	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
positive regulation of macrophage chemotaxis	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
positive regulation of macrophage proliferation	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
positive regulation of protein phosphorylation	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
response to ischemia	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
inflammatory response	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
signal transduction	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathway	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
axon guidance	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
cell population proliferation	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
positive regulation of cell population proliferation	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
negative regulation of cell population proliferation	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
regulation of cell shape	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
peptidyl-tyrosine phosphorylation	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
cytokine-mediated signaling pathway	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
olfactory bulb development	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
forebrain neuron differentiation	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
hemopoiesis	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
monocyte differentiation	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
macrophage differentiation	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
osteoclast differentiation	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
ruffle organization	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
positive regulation of chemokine production	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
regulation of actin cytoskeleton organization	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
cellular response to macrophage colony-stimulating factor stimulus	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
macrophage colony-stimulating factor signaling pathway	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT protein	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
negative regulation of apoptotic process	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
positive regulation by host of viral process	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
innate immune response	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
regulation of bone resorption	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
cell-cell junction maintenance	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
protein autophosphorylation	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
mammary gland duct morphogenesis	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
positive regulation of protein tyrosine kinase activity	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
microglial cell proliferation	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
cellular response to cytokine stimulus	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
regulation of macrophage migration	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
positive regulation of cell motility	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
positive regulation of cell migration	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
regulation of MAPK cascade	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
positive regulation of kinase activity	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
multicellular organism development	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
ovarian follicle development	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
myeloid progenitor cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
lymphoid progenitor cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
immature B cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
mast cell chemotaxis	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of dendritic cell cytokine production	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
glycosphingolipid metabolic process	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
inflammatory response	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
signal transduction	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
spermatogenesis	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
spermatid development	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
germ cell migration	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
regulation of cell shape	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
visual learning	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
male gonad development	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of phospholipase C activity	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
cytokine-mediated signaling pathway	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
stem cell population maintenance	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
lamellipodium assembly	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
actin cytoskeleton organization	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
hemopoiesis	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
T cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
erythrocyte differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
melanocyte differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of pseudopodium assembly	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of mast cell cytokine production	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
somatic stem cell population maintenance	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
embryonic hemopoiesis	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
ectopic germ cell programmed cell death	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
intracellular signal transduction	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
hematopoietic stem cell migration	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
megakaryocyte development	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
Fc receptor signaling pathway	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
Kit signaling pathway	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
erythropoietin-mediated signaling pathway	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
regulation of cell population proliferation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT protein	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
negative regulation of programmed cell death	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
mast cell degranulation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of MAPK cascade	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
pigmentation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
tongue development	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of Notch signaling pathway	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STAT	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
response to cadmium ion	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
protein autophosphorylation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of long-term neuronal synaptic plasticity	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
digestive tract development	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
stem cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
epithelial cell proliferation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of sound	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of DNA-binding transcription factor activity	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
negative regulation of developmental process	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
cell chemotaxis	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
mast cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
mast cell proliferation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of mast cell proliferation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
melanocyte migration	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
melanocyte adhesion	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of pyloric antrum smooth muscle contraction	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
regulation of bile acid metabolic process	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of colon smooth muscle contraction	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of small intestine smooth muscle contraction	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
negative regulation of reproductive process	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of cell migration	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of MAP kinase activity	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
multicellular organism development	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
B cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
hematopoietic progenitor cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
inositol phosphate metabolic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
negative regulation of cold-induced thermogenesis	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (29)

Process	via Protein(s)	Taxonomy
cytokine activity	Interferon beta	Homo sapiens (human)
cytokine receptor binding	Interferon beta	Homo sapiens (human)
type I interferon receptor binding	Interferon beta	Homo sapiens (human)
protein binding	Interferon beta	Homo sapiens (human)
chloramphenicol O-acetyltransferase activity	Interferon beta	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
signaling receptor binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
peptide antigen binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein-folding chaperone binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein tyrosine kinase activity	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
macrophage colony-stimulating factor receptor activity	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
protein binding	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
ATP binding	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
protein phosphatase binding	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
cytokine binding	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
protein homodimerization activity	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
growth factor binding	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
protease binding	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
protein tyrosine kinase activity	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activity	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
stem cell factor receptor activity	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
protein binding	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
ATP binding	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
cytokine binding	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
SH2 domain binding	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
protein homodimerization activity	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
metal ion binding	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
growth factor binding	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol heptakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
protein binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
ATP binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 1-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 3-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (28)

Process	via Protein(s)	Taxonomy
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
Golgi membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
endoplasmic reticulum	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
Golgi apparatus	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
cell surface	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
ER to Golgi transport vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
secretory granule membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
phagocytic vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
early endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
recycling endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular exosome	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
lumenal side of endoplasmic reticulum membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
MHC class I protein complex	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular space	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
external side of plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
nucleoplasm	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
plasma membrane	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
cell surface	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
intracellular membrane-bounded organelle	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
CSF1-CSF1R complex	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
receptor complex	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
plasma membrane	Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)
fibrillar center	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
acrosomal vesicle	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
extracellular space	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
plasma membrane	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
cell-cell junction	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
external side of plasma membrane	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
cytoplasmic side of plasma membrane	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
plasma membrane	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
receptor complex	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
fibrillar center	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytosol	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleus	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (13)

Assay ID	Title	Year	Journal	Article
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.
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1388792	Inhibition of CSF1R (unknown origin) using biotinylated peptide substrate	2018	Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13	Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors.
AID1388796	Inhibition of LPS-induced IL-6 level in serum of Swiss Webster mouse at 40 mg/kg, po via gavage pretreated for 4.15 hrs followed by LPS stimulation measured after 1.5 hrs by ELISA relative to control	2018	Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13	Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors.
AID1388794	Aqueous solubility of the compound by turbidity-based assay	2018	Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13	Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors.
AID1388797	Anti-inflammatory activity in unilateral ureter obstruction-induced C57BL/6 mouse renal inflammation model assessed as reduction in F4/80+ macrophage accumulation in kidney at 40 mg/kg, po via gavage administered at 12 hrs time interval for 7 days startin	2018	Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13	Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors.
AID1388793	Inhibition of KIT (unknown origin) using biotinylated peptide substrate	2018	Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13	Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors.
AID1388795	Inhibition of LPS-induced TNFalpha level in serum of Swiss Webster mouse at 40 mg/kg, po via gavage pretreated for 4.15 hrs followed by LPS stimulation measured after 1.5 hrs by ELISA relative to control	2018	Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13	Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors.
AID977608	Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB	2013	Proceedings of the National Academy of Sciences of the United States of America, Apr-02, Volume: 110, Issue:14	Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	3 (50.00)	24.3611
2020's	3 (50.00)	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	0 (0.00%)	5.53%
Reviews	1 (16.67%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	5 (83.33%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
gw 2580 5-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)pyrimidine-2,4-diamine: a cFMS kinase inhibitor; structure in first source	3.27	1
enmd 2076 ENMD 2076: an antiangiogenic agent with aurora kinase inhibitory and antineoplastic activities	3.27	1
pexidartinib pexidartinib: inhibits both CSF1R and c-kit receptor tyrosine kinase; structure in first source. pexidartinib : A pyrrolopyridine that is 5-chloro-1H-pyrrolo[2,3-b]pyridine which is substituted by a [6-({[6-(trifluoromethyl)pyridin-3-yl]methyl}amino)pyridin-3-yl]methyl group at position 3. It is a potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, KIT, and FLT3 (IC50 of 20 nM, 10 nM and 160 nM, respectively). Approved by the FDA for the treatment of adult patients with symptomatic tenosynovial giant cell tumor (TGCT).	3.27	1	aminopyridine; organochlorine compound; organofluorine compound; pyrrolopyridine; secondary amino compound	antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
jnj-40346527 JNJ-40346527: inhibits colony-stimulating factor-1 receptor kinase	3.27	1
blz 945 [no description available]	3.27	1

Condition	Relationship Strength	Studies
Innate Inflammatory Response [description not available]	2.08	1
Metastase [description not available]	2.08	1
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.	2.08	1
Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.	2.08	1
Congenital Zika Syndrome [description not available]	2.25	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.25	1
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	2.25	1

plx647

Cross-References

Synonyms (27)

Research Excerpts

Bioavailability

Protein Targets (10)

Potency Measurements

Inhibition Measurements

Biological Processes (147)

Molecular Functions (29)

Ceullar Components (28)

Bioassays (13)

Research

Studies (6)

Market Indicators

Research Demand Index: 17.74

Study Types

plx647

Cross-References

Synonyms (27)

Research Excerpts

Bioavailability

Protein Targets (10)

Potency Measurements

Inhibition Measurements

Biological Processes (147)

Molecular Functions (29)

Ceullar Components (28)

Bioassays (13)

Research

Studies (6)

Market Indicators

Research Demand Index: 17.74

Study Types

Related Drugs (5)

Related Conditions (7)