Page last updated: 2024-11-13
amg 511
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
AMG 511: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
ID Source | ID |
---|---|
PubMed CID | 56947516 |
CHEMBL ID | 2170081 |
SCHEMBL ID | 116429 |
MeSH ID | M000607845 |
Synonyms (24)
Synonym |
---|
14K , |
4-(2-[(5-fluoro-6-methoxypyridin-3-yl)amino]-5-{(1r)-1-[4-(methylsulfonyl)piperazin-1-yl]ethyl}pyridin-3-yl)-6-methyl-1,3,5-triazin-2-amine |
chembl2170081 , |
us8772480, 148 |
bdbm50396808 |
SCHEMBL116429 |
amg-511 |
1253573-53-3 |
amg511 |
4-[2-[(5-fluoro-6-methoxypyridin-3-yl)amino]-5-[(1r)-1-(4-methylsulfonylpiperazin-1-yl)ethyl]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine |
NCGC00387802-01 |
BCP28993 |
amg 511; amg511 |
EX-A1575 |
amg 511 |
nsc782122 |
nsc-782122 |
Q27451683 |
CS-0006892 |
HY-13440 |
(r)-4-[2-[(5-fluoro-6-methoxypyridin-3-yl)amino]-5-[1-(4-methylsulfonylpiperazin-1-yl)ethyl]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine |
(r)-4-(2-((5-fluoro-6-methoxypyridin-3-yl)amino)-5-(1-(4-(methylsulfonyl)piperazin-1-yl)ethyl)pyridin-3-yl)-6-methyl-1,3,5-triazin-2-amine |
(r)-4-(2-(5-fluoro-6-methoxypyridin-3-ylamino)-5-(1-(4-(methylsulfonyl)piperazin-1-yl)ethyl)pyridin-3-yl)-6-methyl-1,3,5-triazin-2-amine |
AKOS040741104 |
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 (7)
Inhibition Measurements
Biological Processes (236)
Molecular Functions (36)
Ceullar Components (41)
Bioassays (44)
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. |
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. |
AID1347157 | Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS | 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. |
AID1347161 | Confirmatory 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. |
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. |
AID1347169 | Tertiary RLuc qRT-PCR qHTS assay 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. |
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. |
AID701197 | Mean residence time in Sprague-Dawley rat at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID1175283 | Intrinsic clearance in rat liver microsomes at 1 uM after 30 mins | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511. |
AID701193 | Inhibition of PI3K in po dosed CD1 nude mouse assessed as plasma concentration for inhibition of HGF-induced AKT Ser473 phosphorylation administered 6 hrs prior to HGF-stimulation measured after 5 mins by electrochemiluminescence immunoassay | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID701205 | Inhibition of human N-terminal polyHis-tagged PI3K p110delta/p85alpha expressed in baculovirus infected Sf9 cells using phosphatidylinositol-4,5-bisphosphate as substrate after 20 mins by spectrophotometric analysis | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID701191 | Antitumor activity against human U87MG cells xenografted in CD1 nude mouse assessed as tumor stasis at 3 mg/kg, po administered QD for 12 days relative to vehicle-treated control | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID1175288 | Fraction unbound in Sprague-Dawley rat plasma at 1 mg/kg, iv and 2 mg/kg, po | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511. |
AID1175286 | Terminal half life in Sprague-Dawley rat at 1 mg/kg, iv and 2 mg/kg, po | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511. |
AID701201 | Inhibition of mTOR | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID1175287 | Oral bioavailability in Sprague-Dawley rat at 2 mg/kg | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511. |
AID701198 | Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID701202 | Intrinsic clearance in human liver microsomes assessed per mg of protein at 1 uM after 30 mins | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID701206 | Inhibition of human N-terminal polyHis-tagged PI3K p110gamma expressed in baculovirus infected Hi5 cells using ATP as substrate after 20 mins by spectrophotometric analysis | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID1175284 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv and 2 mg/kg, po | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511. |
AID701203 | Intrinsic clearance in rat liver microsomes assessed per mg of protein at 1 uM after 30 mins | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID701194 | Inhibition of PI3K in po dosed CD1 nude mouse liver assessed as inhibition of HGF-induced AKT Ser473 phosphorylation administered 6 hrs prior to HGF-stimulation measured after 5 mins by electrochemiluminescence immunoassay | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID701200 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID1175279 | Inhibition of human N-terminal poly-His tagged p110 alpha/ p85alpha expressed in Sf9 Baculovirus system after 20 mins by AlphaScreen assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511. |
AID701207 | Inhibition of human N-terminal polyHis-tagged PI3K p110beta/p85alpha expressed in baculovirus infected Sf9 cells using phosphatidylinositol-4,5-bisphosphate as substrate after 20 mins by spectrophotometric analysis | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID1175281 | Inhibition of PI3K-mediated Akt S473 phosphorylation in human U87MG cells after 2 hrs by cell-based assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511. |
AID701187 | Inhibition of human PI4K | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID701195 | AUC in Sprague-Dawley rat at 2 mg/kg, po | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID1175282 | Intrinsic clearance in human liver microsomes at 1 uM after 30 mins | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511. |
AID1175289 | Efflux ratio of permeability across pig LLC-PK1 cells stably over-expressing rat P-gp at 5 uM | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511. |
AID701199 | Inhibition of human VPS34 | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID1175292 | Inhibition of human N-terminal poly-His tagged p110beta/p85alpha expressed in Sf9 Baculovirus system after 20 mins by AlphaScreen assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511. |
AID1175293 | Inhibition of human N-terminal poly-His tagged p110delta/p85alpha expressed in Sf9 Baculovirus system after 20 mins by AlphaScreen assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511. |
AID701208 | Inhibition of human N-terminal polyHis-tagged PI3K p110alpha/p85alpha expressed in baculovirus infected Sf9 cells using phosphatidylinositol-4,5-bisphosphate as substrate after 20 mins by spectrophotometric analysis | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID701196 | Oral bioavailability in Sprague-Dawley rat at 2 mg/kg | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID1175280 | Inhibition of recombinant N-terminally GST-tagged mTOR (1360 to 2549 aa) (unknown origin) assessed as inhibition of 27BP1 phosphorylation after 90 mins by TR-FRET assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511. |
AID701192 | Antitumor activity against human U87MG cells xenografted in CD1 nude mouse assessed as tumor growth inhibition at 1 mg/kg, po administered QD for 12 days relative to vehicle-treated control | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID701190 | Antitumor activity against human U87MG cells xenografted in CD1 nude mouse assessed as tumor regression at 10 mg/kg, po administered QD for 12 days relative to vehicle-treated control | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID1175294 | Inhibition of human N-terminal poly-His tagged p110gamma (114 to 1102 aa)/p85alpha expressed in Sf9 Baculovirus system after 20 mins by AlphaScreen assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511. |
AID1175285 | Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv and 2 mg/kg, po | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511. |
AID701188 | AUC in CD1 nude mouse xenografted with human U87MG cells at 0.6 mg/kg, po administered QD for 12 days | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID701204 | Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human U87MG cells after 2 hrs | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
AID701189 | Antitumor activity against human U87MG cells xenografted in po dosed CD1 nude mouse administered QD for 12 days | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (5)
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 (60.00) | 24.3611 |
2020's | 2 (40.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Market Indicators
Research Demand Index: 17.90
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.
| This Compound (17.90) 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 | 5 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |