Page last updated: 2024-11-13

af38469

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 CID72706115
CHEMBL ID3098745
SCHEMBL ID15903106
MeSH IDM0594209

Synonyms (26)

Synonym
CHEMBL3098745 ,
bdbm50445054
2jq ,
2-[(6-methylpyridin-2-yl)carbamoyl]-5-(trifluoromethyl)benzoic acid
SCHEMBL15903106
HY-12802
af38469 ,
4N7E
AKOS030526576
1531634-31-7
NCGC00485887-01
2-((6-methylpyridin-2-yl)carbamoyl)-5-(trifluoromethyl)benzoic acid
BCP24179
af 38469; af-38469
n-(6-methylpyridin-2-yl)-5-trifluoromethyl-phthalamic acid
EX-A2510
BS-15551
Q27453051
A883844
F85161
af-38469af-38469
AC-36108
jwcusqczmqibmr-uhfffaoysa-n
2-[(6-methyl-2-pyridyl)carbamoyl]-5-(trifluoromethyl)benzoic acid
mfcd28160694
SY342709

Research Excerpts

Bioavailability

The identification of the novel, selective, orally bioavailable Sortilin inhibitor AF38469 is described. The drug blocked GRN A-induced lung metastases and prevented cancer cell infiltration of the skin.

ExcerptReferenceRelevance
"The identification of the novel, selective, orally bioavailable Sortilin inhibitor AF38469 is described."( The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
Andersen, JL; Biilmann Rønn, LC; Bundgaard, C; Christensen, S; David, L; de Jong, IE; Egebjerg, J; Eradi, P; Eskildsen, J; Jacobsen, J; Karlsson, JJ; Kasturi, SP; Langgård, M; Lindberg, S; Malik, IJ; Maltas, PJ; Pervaram, S; Sakumudi, DR; Schrøder, TJ; Simonsen, KB; Stavenhagen, JB; Strandbygård, D; Tagmose, L; Thirup, S; Uppalanchi, S; Watson, SP, 2014
)
0.94
" Importantly, an orally bioavailable small molecule (AF38469) targeting sortilin, blocked GRN A-induced lung metastases and prevented cancer cell infiltration of the skin."( Sortilin inhibition limits secretion-induced progranulin-dependent breast cancer progression and cancer stem cell expansion.
Andersson, D; Berger, K; Fitzpatrick, P; Gregersson, P; Harrison, H; Hughes, É; Jacobsson, H; Landberg, G; Magnusson, Y; Rafnsdottir, S; Rhost, S; Ståhlberg, A, 2018
)
0.73
"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

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
SortilinHomo sapiens (human)IC50 (µMol)0.32310.23800.31110.3600AID1061998; AID1475127
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (21)

Processvia Protein(s)Taxonomy
ossificationSortilinHomo sapiens (human)
protein targeting to lysosomeSortilinHomo sapiens (human)
Golgi to endosome transportSortilinHomo sapiens (human)
endocytosisSortilinHomo sapiens (human)
G protein-coupled receptor signaling pathwaySortilinHomo sapiens (human)
neuropeptide signaling pathwaySortilinHomo sapiens (human)
endosome to lysosome transportSortilinHomo sapiens (human)
extrinsic apoptotic signaling pathway via death domain receptorsSortilinHomo sapiens (human)
regulation of gene expressionSortilinHomo sapiens (human)
myotube differentiationSortilinHomo sapiens (human)
vesicle organizationSortilinHomo sapiens (human)
endosome transport via multivesicular body sorting pathwaySortilinHomo sapiens (human)
response to insulinSortilinHomo sapiens (human)
nerve growth factor signaling pathwaySortilinHomo sapiens (human)
negative regulation of fat cell differentiationSortilinHomo sapiens (human)
glucose importSortilinHomo sapiens (human)
neurotrophin TRK receptor signaling pathwaySortilinHomo sapiens (human)
plasma membrane to endosome transportSortilinHomo sapiens (human)
negative regulation of lipoprotein lipase activitySortilinHomo sapiens (human)
Golgi to lysosome transportSortilinHomo sapiens (human)
maintenance of synapse structureSortilinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
protein bindingSortilinHomo sapiens (human)
nerve growth factor receptor activitySortilinHomo sapiens (human)
enzyme bindingSortilinHomo sapiens (human)
neurotensin receptor activity, non-G protein-coupledSortilinHomo sapiens (human)
nerve growth factor bindingSortilinHomo sapiens (human)
retromer complex bindingSortilinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (18)

Processvia Protein(s)Taxonomy
lysosomeSortilinHomo sapiens (human)
lysosomal membraneSortilinHomo sapiens (human)
early endosomeSortilinHomo sapiens (human)
endoplasmic reticulum membraneSortilinHomo sapiens (human)
Golgi apparatusSortilinHomo sapiens (human)
cytosolSortilinHomo sapiens (human)
plasma membraneSortilinHomo sapiens (human)
clathrin-coated pitSortilinHomo sapiens (human)
cell surfaceSortilinHomo sapiens (human)
endosome membraneSortilinHomo sapiens (human)
membraneSortilinHomo sapiens (human)
clathrin-coated vesicleSortilinHomo sapiens (human)
trans-Golgi network transport vesicleSortilinHomo sapiens (human)
cytoplasmic vesicleSortilinHomo sapiens (human)
nuclear membraneSortilinHomo sapiens (human)
Golgi cisterna membraneSortilinHomo sapiens (human)
perinuclear region of cytoplasmSortilinHomo sapiens (human)
cerebellar climbing fiber to Purkinje cell synapseSortilinHomo sapiens (human)
membraneSortilinHomo sapiens (human)
Golgi apparatusSortilinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (26)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
AID1061995Inhibition of PPARdelta (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1061992Inhibition of ETA receptor (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1061984Half life in rat at 1 mg/kg, iv2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1061985Blood clearance in rat at 1 mg/kg, iv2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1061986Cmax in rat at 2 mg/kg, po2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1061988Free plasma concentration in rat2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1061991Inhibition of ETB receptor (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1062000Inhibition of GPR40 (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1061987Intrinsic clearance in rat2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1061982Oral bioavailability in rat at 2 mg/kg2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1061994Inhibition of EP1 receptor (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1061993Inhibition of AT1 receptor (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1061996Inhibition of NTR1 receptor (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1475129Permeability in MDCK cells expressing human MDR1 at 0.5 uM after 150 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
The identification of novel acid isostere based inhibitors of the VPS10P family sorting receptor Sortilin.
AID1061998Displacement of [3H]-neurotensin from sortilin (unknown origin) incubated 30 mins prior to [3H]-neurotensin addition measured after 6 hrs by scintillation proximity assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1475127Displacement of [3H]-neurotensin from human His6-tagged sortilin pretreated for 30 mins followed by [3H]-neurotensin addition after 6 hrs measured for 360 secs by SPA2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
The identification of novel acid isostere based inhibitors of the VPS10P family sorting receptor Sortilin.
AID1061990Inhibition of MMP12 (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1061999Inhibition of delta opioid receptor (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1061989Solubility of the compound2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID1061983Volume of distribution at steady state in rat at 1 mg/kg, iv2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (66.67)24.3611
2020's2 (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: 23.15

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.

MetricThis Compound (vs All)
Research Demand Index23.15 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index21.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.15)

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%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]