Page last updated: 2024-11-13

al8697

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

Cross-References

ID SourceID
PubMed CID25060093
CHEMBL ID2087742
SCHEMBL ID3610415
MeSH IDM0577804

Synonyms (18)

Synonym
SCHEMBL3610415
CHEMBL2087742 ,
bdbm50420740
n-cyclopropyl-3-[3-(1,1-dimethylethyl)-6,8-difluoro-1,2,4-triazolo[4,3-a]pyridin-7-yl]-5-fluoro-4-methylbenzamide
al 8697
1057394-06-5
AKOS024458328
NCGC00387189-01
CS-0029380
AC9480
al8697
MS-26852
al-8697
HY-108645
SY263536
3-[3-(tert-butyl)-6,8-difluoro-[1,2,4]triazolo[4,3-a]pyridin-7-yl]-n-cyclopropyl-5-fluoro-4-methylbenzamide
mfcd28133371
3-(3-tert-butyl-6,8-difluoro-[1,2,4]triazolo[4,3-a]pyridin-7-yl)-n-cyclopropyl-5-fluoro-4-methylbenzamide

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"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 (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Mitogen-activated protein kinase 13Homo sapiens (human)IC50 (µMol)0.00620.00070.45956.3000AID685461
Proto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)IC50 (µMol)2.00000.00010.34843.5970AID685492
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (52)

Processvia Protein(s)Taxonomy
response to osmotic stressMitogen-activated protein kinase 13Homo sapiens (human)
peptidyl-serine phosphorylationMitogen-activated protein kinase 13Homo sapiens (human)
positive regulation of interleukin-6 productionMitogen-activated protein kinase 13Homo sapiens (human)
cellular response to UVMitogen-activated protein kinase 13Homo sapiens (human)
positive regulation of inflammatory responseMitogen-activated protein kinase 13Homo sapiens (human)
stress-activated MAPK cascadeMitogen-activated protein kinase 13Homo sapiens (human)
cellular response to hydrogen peroxideMitogen-activated protein kinase 13Homo sapiens (human)
cellular response to interleukin-1Mitogen-activated protein kinase 13Homo sapiens (human)
cellular response to sorbitolMitogen-activated protein kinase 13Homo sapiens (human)
cellular response to anisomycinMitogen-activated protein kinase 13Homo sapiens (human)
cellular response to sodium arseniteMitogen-activated protein kinase 13Homo sapiens (human)
intracellular signal transductionMitogen-activated protein kinase 13Homo sapiens (human)
MAPK cascadeProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
ureteric bud developmentProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
neural crest cell migrationProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
embryonic epithelial tube formationProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
protein phosphorylationProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
homophilic cell adhesion via plasma membrane adhesion moleculesProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
neuron cell-cell adhesionProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
signal transductionProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
axon guidanceProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
posterior midgut developmentProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
response to xenobiotic stimulusProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of gene expressionProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of neuron projection developmentProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of neuron maturationProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
regulation of cell adhesionProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of cell migrationProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
membrane protein proteolysisProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of cell adhesion mediated by integrinProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
ureter maturationProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
glial cell-derived neurotrophic factor receptor signaling pathwayProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
neuron maturationProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of MAPK cascadeProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of cell sizeProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of DNA-templated transcriptionProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
response to painProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
enteric nervous system developmentProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
regulation of axonogenesisProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
retina development in camera-type eyeProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
innervationProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
Peyer's patch morphogenesisProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
cellular response to retinoic acidProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of metanephric glomerulus developmentProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
lymphocyte migration into lymphoid organsProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
GDF15-GFRAL signaling pathwayProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of extrinsic apoptotic signaling pathway in absence of ligandProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of kinase activityProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
multicellular organism developmentProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
protein serine/threonine kinase activityMitogen-activated protein kinase 13Homo sapiens (human)
MAP kinase activityMitogen-activated protein kinase 13Homo sapiens (human)
protein bindingMitogen-activated protein kinase 13Homo sapiens (human)
ATP bindingMitogen-activated protein kinase 13Homo sapiens (human)
protein serine kinase activityMitogen-activated protein kinase 13Homo sapiens (human)
protein tyrosine kinase activityProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
calcium ion bindingProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
protein bindingProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
ATP bindingProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
signaling receptor activityProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
cytosolMitogen-activated protein kinase 13Homo sapiens (human)
cytoplasmMitogen-activated protein kinase 13Homo sapiens (human)
nucleusMitogen-activated protein kinase 13Homo sapiens (human)
plasma membraneProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
early endosomeProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
plasma membraneProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
endosome membraneProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
dendriteProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
neuronal cell bodyProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
receptor complexProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
plasma membrane protein complexProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
axonProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (38)

Assay IDTitleYearJournalArticle
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings 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.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347411qHTS 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) Libary2020ACS 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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID685468Cytotoxicity against CHO cells at 200 uM2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685474Volume of distribution at steady state in Wistar rat at 1 mg/kg, iv2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685461Inhibition of p38alpha2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685472AUC in Wistar rat at 1 mg/kg, iv2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685477Oral bioavailability in Wistar rat at 10 mg/kg2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685489Inhibition of CYP2C19 at < 25 uM2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685486Inhibition of CYP1A2 at < 25 uM2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685478AUC in beagle dog at 1 mg/kg, iv2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685475Cmax in Wistar rat at 10 mg/kg, po2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685464Stability in human hepatic microsomes assessed as compound turnover at 5 uM incubated for 30 mins in presence of NADPH2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685466Passive permeability from basolateral to apical side in human Caco2 cells at 12.5 uM2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685469Protein binding in rat plasma2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685483Oral bioavailability in beagle dog at 1 mg/kg2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685479Clearance in beagle dog at 1 mg/kg, iv2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685462Inhibition of LPS-induced TNFalpha production in human whole blood2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685476AUC in Wistar rat at 10 mg/kg, po2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685471Half life in Wistar rat at 1 mg/kg, iv2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685480Volume of distribution at steady state in beagle dog at 1 mg/kg, iv2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685465Passive permeability from apical to basolateral side in human Caco2 cells at 12.5 uM2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685487Inhibition of CYP3A4 at < 25 uM2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685481Cmax in beagle dog at 1 mg/kg, po2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685496Antiarthritic effect in rat adjuvant-induced arthritis model assessed as inhibition of right paw edema at 3 mg/kg, po dosed daily during last 10 days of test2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685482AUC in beagle dog at 1 mg/kg, po2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685490Inhibition of CYP2D6 at < 25 uM2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685485Toxicity against CHO cells2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685484Half life in beagle dog at 1 mg/kg, iv2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685470Protein binding in human plasma2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685492Inhibition of RET2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685473Clearance in Wistar rat at 1 mg/kg, iv2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685495Inhibition of TNFalpha release in rat LPS-induced endotoxemia model dosed orally 1 hr prior to LPS challenge and measured 1.5 hrs post LPS challenge2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685463Stability in rat hepatic microsomes assessed as compound turnover at 5 uM incubated for 30 mins in presence of NADPH2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
AID685488Inhibition of CYP2C9 at < 25 uM2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's2 (40.00)24.3611
2020's3 (60.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.72

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.

MetricThis Compound (vs All)
Research Demand Index12.72 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.72)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]