Page last updated: 2024-11-13

sklb1002

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

Description

SKLB1002: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	71461003
CHEMBL ID	2180603
MeSH ID	M0591431

Synonyms (32)

Synonym
bdbm50399536
CHEMBL2180603 ,
S7258
1225451-84-2
sklb1002
HY-13944
CS-1807
K0060
c13h12n4o2s2
2-((6,7-dimethoxyquinazolin-4-yl)thio)-5-methyl-1,3,4-thiadiazole
AC-33004
J-004821
AKOS026750477
EX-A319
HMS3653M04
sklb1002, >=98% (hplc)
SW220084-1
mfcd27938707
FT-0700126
BS-14631
2-[(6,7-dimethoxyquinazolin-4-yl)thio]-5-methyl-1,3,4-thiadiazole
6,7-dimethoxy-4-[(5-methyl-1,3,4-thiadiazol-2-yl)thio]quinazoline
BCP09480
sklb-1002
SB19354
2-(6,7-dimethoxyquinazolin-4-yl)sulfanyl-5-methyl-1,3,4-thiadiazole
CCG-267711
H11010
NCGC00378568-07
A891099
AZB45184
6,7-dimethoxy-4-[(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]quinazoline

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 (1)

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Vascular endothelial growth factor receptor 2	Homo sapiens (human)	IC50 (µMol)	0.0320	0.0000	0.4830	8.8000	AID710632
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (63)

Process	via Protein(s)	Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Process	via Protein(s)	Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Process	via Protein(s)	Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (7)

Assay ID	Title	Year	Journal	Article
AID710558	Antitumor activity against human HepG2 cells xenografted mouse assessed as inhibition of tumor growth at 100 mg/kg qd for 18 days	2012	Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24	Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.
AID710619	Antiangiogenic activity in HUVEC assessed as inhibition of tube formation at 10 uM	2012	Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24	Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.
AID710632	Inhibition of VEGFR2	2012	Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24	Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.
AID710618	Antiangiogenic activity in zebrafish embryos assessed as inhibition of intersegmental vessel growth at 2.5 uM	2012	Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24	Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.
AID710617	Antitumor activity against human SW620 cells xenografted mouse assessed as inhibition of tumor growth at 100 mg/kg qd for 18 days	2012	Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24	Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.
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.
[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	5 (83.33)	24.3611
2020's	1 (16.67)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.02

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	16.02 (24.57)
Research Supply Index	1.95 (2.92)
Research Growth Index	4.51 (4.65)
Search Engine Demand Index	10.37 (26.88)
Search Engine Supply Index	3.00 (0.95)

This Compound (16.02)

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	6 (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
quinazolines Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.	3.02	4	azaarene; mancude organic heterobicyclic parent; ortho-fused heteroarene; quinazolines
vatalanib [no description available]	2.07	1	monochlorobenzenes; phthalazines; pyridines; secondary amino compound	angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; vascular endothelial growth factor receptor antagonist
telatinib [no description available]	2.07	1
cp 547632 3-(4-bromo-2,6-difluorobenzyloxy)-5-(3-(4-pyrrolidin-1-ylbutyl)ureido)isothiazole-4-carboxylic acid amide: inhibits vascular endothelial growth factor receptor-2 tyrosine kinase; structure in first source	2.07	1
lenvatinib lenvatinib : A member of the class of quinolines that is the carboxamide of 4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxylic acid. A multi-kinase inhibitor and orphan drug used (as its mesylate salt) for the treatment of various types of thyroid cancer that do not respond to radioiodine.	2.07	1	aromatic amide; aromatic ether; cyclopropanes; monocarboxylic acid amide; monochlorobenzenes; phenylureas; quinolines	antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; fibroblast growth factor receptor antagonist; orphan drug; vascular endothelial growth factor receptor antagonist
ki23057 Ki23057: K-samII/FGF-R2 phosphorylation inhibitor for treatment of scirrhous gastric cancer; structure in first source	2.07	1
osi 930 OSI 930: inhibits both receptor tyrosine kinase Kit and kinase insert domain receptor; structure in first source	2.07	1	aromatic amide
tivozanib N-(2-chloro-4-((6,7-dimethoxy-4-quinolyl)oxy)phenyl)-N'-(5-methyl-3-isoxazolyl)urea: KNR-951 is the HCl, monohydrate salt; an antineoplastic agent; structure in first source	2.07	1	aromatic ether
cediranib [no description available]	2.07	1	aromatic ether
aee 788 AEE 788: structure in first source	2.07	1	6-{4-[(4-ethylpiperazin-1-yl)methyl]phenyl}-N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine	angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; epidermal growth factor receptor antagonist; trypanocidal drug
motesanib [no description available]	2.07	1	pyridinecarboxamide
tak 593 TAK 593: structure in first source	2.07	1
gsk 1363089 GSK 1363089: a multikinase inhibitor that acts on Met, RON, Axl, and VEGFR; structure in first source	2.07	1	aromatic ether

Condition	Relationship Strength	Studies
Benign Neoplasms [description not available]	2.47	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.	2.47	2
Burns, Chemical Burns caused by contact with or exposure to CAUSTICS or strong ACIDS.	2.25	1
Corneal Diseases Diseases of the cornea.	2.25	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.81	3
Innate Inflammatory Response [description not available]	2.08	1
Angiogenesis, Pathologic [description not available]	2.48	2
Palmoplantaris Pustulosis [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
Psoriasis A common genetically determined, chronic, inflammatory skin disease characterized by rounded erythematous, dry, scaling patches. The lesions have a predilection for nails, scalp, genitalia, extensor surfaces, and the lumbosacral region. Accelerated epidermopoiesis is considered to be the fundamental pathologic feature in psoriasis.	2.08	1
B16 Melanoma [description not available]	2.06	1
Invasiveness, Neoplasm [description not available]	2.06	1
Breast Cancer [description not available]	2.1	1
Cancer of Colon [description not available]	2.1	1
Breast Neoplasms Tumors or cancer of the human BREAST.	2.1	1
Colonic Neoplasms Tumors or cancer of the COLON.	2.1	1
Necrosis The death of cells in an organ or tissue due to disease, injury or failure of the blood supply.	2.1	1

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