Page last updated: 2024-11-13

plx7904

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID Source	ID
PubMed CID	90116945
CHEMBL ID	4206836
SCHEMBL ID	15667328
MeSH ID	M000611620

Synonyms (25)

Synonym
S7964
CS-5129
HY-18997
plx7904 ,
SCHEMBL15667328
AC-35385
n'-(3-{[5-(2-cyclopropylpyrimidin-5-yl)-1h-pyrrolo[2,3-b]pyridin-3-yl]carbonyl}-2,4-difluorophenyl)-n-ethyl-n-methylsulfuric diamide
plx-7904
pb04
5-(2-cyclopropylpyrimidin-5-yl)-3-[3-[[ethyl(methyl)sulfamoyl]amino]-2,6-difluorobenzoyl]-1h-pyrrolo[2,3-b]pyridine
1393465-84-3
AKOS030526477
({3-[5-(2-cyclopropylpyrimidin-5-yl)-1h-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluorophenyl}sulfamoyl)(ethyl)methylamine
plx7904(pb04)
BCP18248
EX-A2872
bdbm317744
us9624213, compound p-0240
CCG-269789
sulfamide, n'-[3-[[5-(2-cyclopropyl-5-pyrimidinyl)-1h-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-n-ethyl-n-methyl-
Q27456931
n'-[3-[[5-(2-cyclopropyl-5-pyrimidinyl)-1h-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-n-ethyl-n-methyl-sulfamide
A901658
MS-29512
CHEMBL4206836

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

Protein Targets (3)

Potency Measurements

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
PPM1D protein	Homo sapiens (human)	Potency	18.5569	0.0052	9.4661	32.9993	AID1347411
Interferon beta	Homo sapiens (human)	Potency	18.5569	0.0033	9.1582	39.8107	AID1347411
[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)
Serine/threonine-protein kinase B-raf	Homo sapiens (human)	IC50 (µMol)	0.0101	0.0001	0.2800	7.5890	AID1380308; AID1380310
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (72)

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)
MAPK cascade	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
myeloid progenitor cell differentiation	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
protein phosphorylation	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
epidermal growth factor receptor signaling pathway	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
visual learning	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
animal organ morphogenesis	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
positive regulation of gene expression	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
negative regulation of fibroblast migration	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
positive regulation of glucose transmembrane transport	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
synaptic vesicle exocytosis	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
thyroid gland development	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
T cell differentiation in thymus	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
substrate adhesion-dependent cell spreading	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
somatic stem cell population maintenance	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
regulation of cell population proliferation	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
negative regulation of apoptotic process	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
stress fiber assembly	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
CD4-positive, alpha-beta T cell differentiation	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
CD4-positive or CD8-positive, alpha-beta T cell lineage commitment	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
response to peptide hormone	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
negative regulation of neuron apoptotic process	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
regulation of T cell differentiation	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
thymus development	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
positive regulation of axon regeneration	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
positive regulation of axonogenesis	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
T cell receptor signaling pathway	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
positive regulation of stress fiber assembly	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
response to cAMP	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
long-term synaptic potentiation	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
head morphogenesis	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
face development	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
ERK1 and ERK2 cascade	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
cellular response to calcium ion	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
cellular response to xenobiotic stimulus	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
endothelial cell apoptotic process	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
establishment of protein localization to membrane	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreading	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
cellular response to nerve growth factor stimulus	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
negative regulation of synaptic vesicle exocytosis	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
negative regulation of endothelial cell apoptotic process	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (17)

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)
small GTPase binding	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
protein kinase activity	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
MAP kinase kinase activity	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
calcium ion binding	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
mitogen-activated protein kinase kinase binding	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
identical protein binding	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
protein-containing complex binding	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
scaffold protein binding	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
MAP kinase kinase kinase activity	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Process	via Protein(s)	Taxonomy
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
nucleus	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
plasma membrane	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
neuron projection	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
intracellular membrane-bounded organelle	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
cell body	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
presynapse	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
mitochondrion	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
plasma membrane	Serine/threonine-protein kinase B-raf	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (4)

Assay ID	Title	Year	Journal	Article
AID1380310	Inhibition of BRAF V600E mutant in human A375 cells assessed as reduction in ERK phosphorylation by AlphaScreen assay	2018	Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14	Current Insights of BRAF Inhibitors in Cancer.
AID1380308	Inhibition of N-terminal His-tagged BRAF V600E mutant (unknown origin) expressed in baculovirus infected insect cells co-expressing CDC37 using biotinylated-MEK as substrate by AlphaScreen assay	2018	Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14	Current Insights of BRAF Inhibitors in Cancer.
AID1380335	Cytotoxicity against human A375 cells harboring BRAF V600E mutant	2018	Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14	Current Insights of BRAF Inhibitors in Cancer.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

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	4 (66.67)	24.3611
2020's	2 (33.33)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.93

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 moderate demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	21.93 (24.57)
Research Supply Index	1.95 (2.92)
Research Growth Index	4.57 (4.65)
Search Engine Demand Index	18.60 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (21.93)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	2 (33.33%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	4 (66.67%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
sorafenib [no description available]	3.27	1	(trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; phenylureas; pyridinecarboxamide	angiogenesis inhibitor; anticoronaviral agent; antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; ferroptosis inducer; tyrosine kinase inhibitor
GDC-0879 [no description available]	3.27	1	indanes; ketoxime; primary alcohol; pyrazoles; pyridines	antineoplastic agent; B-Raf inhibitor
plx 4720 PLX 4720: a B-Raf(V600E) kinase inhibitor; structure in first source	3.73	2	aromatic ketone; difluorobenzene; organochlorine compound; pyrrolopyridine; sulfonamide	antineoplastic agent; B-Raf inhibitor
plx4032 [no description available]	3.95	3	aromatic ketone; difluorobenzene; monochlorobenzenes; pyrrolopyridine; sulfonamide	antineoplastic agent; B-Raf inhibitor
dabrafenib [no description available]	3.69	2	1,3-thiazoles; aminopyrimidine; organofluorine compound; sulfonamide	anticoronaviral agent; antineoplastic agent; B-Raf inhibitor
tak-632 TAK-632 : A member of the class of benzothiazoles that is 1,3-benzothiazole substituted by (cyclopropanecarbonyl)amino, 4-fluoro-3-{2-[3-(trifluoromethyl)phenyl]acetamido}phenoxy, and cyano groups at positions 2, 6 and 7, respectively. It is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAF(V600E), BRAF(WT), respectively.	2.21	1	(trifluoromethyl)benzenes; aromatic ether; benzothiazoles; cyclopropylcarboxamide; monofluorobenzenes; nitrile; secondary carboxamide	antineoplastic agent; apoptosis inducer; B-Raf inhibitor; EC 2.7.11.26 (tau-protein kinase) inhibitor; necroptosis inhibitor
ly3009120 LY3009120: a pan-RAF inhibitor; structure in first source. LY3009120 : A member of the class of pyridopyrimidines that is pyrido[2,3-d]pyrimidine substituted by methylamino, 5-{[(3,3-dimethylbutyl)carbamoyl]amino}-4-fluoro-2-methylphenyl, and methyl groups at positions 2, 6 and 7, respectively. It is a potent pan RAF inhibitor which inhibits BRAF(V600E), BRAF(WT) and CRAF(WT) (IC50 = 5.8, 9.1 and 15 nM, respectively). It also inhibits RAF homo- and heterodimers and exhibits anti-cancer properties.	3.69	2	aminotoluene; aromatic amine; biaryl; monofluorobenzenes; phenylureas; pyridopyrimidine; secondary amino compound	antineoplastic agent; apoptosis inducer; autophagy inducer; B-Raf inhibitor; necroptosis inhibitor
plx8394 PLX8394: a RAF inhibitor; structure in first source	7.58	2
sb-590885 [no description available]	3.27	1	N-{5-[2-{4-[2-(dimethylamino)ethoxy]phenyl}-4-(pyridin-4-yl)-1H-imidazol-5-yl]-2,3-dihydro-1H-inden-1-ylidene}hydroxylamine

Condition	Relationship Strength	Studies
Benign Neoplasms [description not available]	3.98	2
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.	3.98	2
Colorectal Cancer [description not available]	2.31	1
Colorectal Neoplasms Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.	2.31	1
Malignant Melanoma [description not available]	2.21	1
Melanoma A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)	2.21	1

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