Compounds > pf 8380
Page last updated: 2024-08-03 13:09:47

pf 8380

Description

Cross-References

ID SourceID
PubMed CID25265312
CHEMBL ID3186509
SCHEMBL ID3054811
MeSH IDM0548126

Synonyms (42)

Synonym
HY-13344
pf 8380
pf-8380
AKOS016011387
NCGC00346939-01
CS-0591
S8218
1144035-53-9
smr004701264
MLS006010144
SCHEMBL3054811
3,5-dichlorobenzyl 4-(3-oxo-3-(2-oxo-2,3-dihydrobenzo[d]oxazol-6-yl)propyl)piperazine-1-carboxylate
3,5-dichlorobenzyl-[4-[3-oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]]piperazine-1-carboxylate
AC-32916
CHEMBL3186509 ,
6zo ,
DTXSID50649524
(3,5-dichlorophenyl)methyl 4-[3-oxo-3-(2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)propyl]piperazine-1-carboxylate
gtpl9142
compound 21 [pmid: 26745766]
pf8380
compound 4 [pmid: 23300119]
J-003089
EX-A137
mfcd20527274
3,5-dichlorobenzyl 4-[3-oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylate
NCGC00346939-05
bdbm50187693
unii-t582dim5a4
3,5-dichlorobenzyl 4-(3-oxo-3-(2-oxo-2,3-dihydrobenzo-[d]oxazol-6-yl)propyl)piperazine-1-carboxylate
2(3h)-benzoxazolone, 6-(1-oxo-3-(1-piperazinyl)propyl)-
T582DIM5A4 ,
BCP06651
6-(3-(piperazin-1-yl)propanoyl)-benzo[d]oxazol-2(3h)-one
atx inhibitor iii
AS-40376
HMS3740G07
CCG-269523
1-piperazinecarboxylic acid, 4-[3-(2,3-dihydro-2-oxo-6-benzoxazolyl)-3-oxopropyl]-, (3,5-dichlorophenyl)methyl ester
Q27456612
(3,5-dichlorophenyl)methyl 4-[3-oxo-3-(2-oxo-3h-1,3-benzoxazol-6-yl)propyl]piperazine-1-carboxylate
4-[3-oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester

Protein Targets (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency4.7724AID1645841
GVesicular stomatitis virusPotency7.5637AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency15.0916AID1645840
Interferon betaHomo sapiens (human)Potency7.5637AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency7.5637AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency7.5637AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency7.5637AID1645842

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Acyl-CoA desaturase 1Rattus norvegicus (Norway rat)IC500.0084AID1633000
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC501.5900AID1349341; AID1497191
Ectonucleotide pyrophosphatase/phosphodiesterase family member 2Homo sapiens (human)IC500.0096AID1312303; AID1325587; AID1349372; AID1433834; AID1438632; AID1480296; AID1488986; AID1488987; AID1497192; AID1632555; AID1633000; AID1656151; AID1656153; AID1739783; AID1908642
Ectonucleotide pyrophosphatase/phosphodiesterase family member 2Rattus norvegicus (Norway rat)IC501.0366AID1312303; AID1349340; AID1908948
Acyl-CoA Rattus norvegicus (Norway rat)IC500.0084AID1633000
Ectonucleotide pyrophosphatase/phosphodiesterase family member 2Mus musculus (house mouse)IC500.0022AID1480294; AID1480295

Bioassays (82)

Assay IDTitleYearJournalArticle
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
ISSN: 1554-8937		High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490		Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
ISSN: 2472-5560		Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111		A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1745845Primary qHTS for Inhibitors of ATXN expression2022The Journal of biological chemistry, 08, Volume: 298, Issue:8
ISSN: 1083-351X
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
ISSN: 2211-1247		A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173ISSN: 1872-9096A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173ISSN: 1872-9096A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173ISSN: 1872-9096A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111		A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1312305Clearance in Lewis rat at 1 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
ISSN: 1520-4804		Development of Autotaxin Inhibitors: An Overview of the Patent and Primary Literature.
AID1908645Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jun-05, Volume: 236ISSN: 1768-3254Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors.
AID1497190Equilibrium solubility of compound at pH 6.8 by high-throughput screening method2018Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13
ISSN: 1464-3405		Development of autotaxin inhibitors: A series of zinc binding triazoles.
AID1633001Inhibition of autotaxin in healthy human plasma assessed as reduction in LPA level after 3 hrs by mass spectrometric analysis2016ACS medicinal chemistry letters, Sep-08, Volume: 7, Issue:9
ISSN: 1948-5875		Novel Autotaxin Inhibitors for the Treatment of Osteoarthritis Pain: Lead Optimization via Structure-Based Drug Design.
AID1488986Inhibition of recombinant human ATX beta expressed in HEK293 cells using LPC as substrate measured after 30 mins by LC-MS/MS analysis2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
ISSN: 1464-3405		Design, synthesis, docking and biological evaluation of 4-phenyl-thiazole derivatives as autotaxin (ATX) inhibitors.
AID1908948Inhibition of rat ATX lysoPLD activity using LPC as substrate assessed as reduction in choline release measured after 60 mins by HVA fluorescence based analysis2022Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
ISSN: 1520-4804		Structure-Based Design of a Novel Class of Autotaxin Inhibitors Based on Endogenous Allosteric Modulators.
AID1488987Inhibition of recombinant human ATX beta expressed in HEK293 cells using FS-3 as substrate pretreated for 15 mins followed by substrate addition measured after 30 mins2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
ISSN: 1464-3405		Design, synthesis, docking and biological evaluation of 4-phenyl-thiazole derivatives as autotaxin (ATX) inhibitors.
AID1312309Plasma concentration in Lewis rat air pouch model of inflammation at 3 mg/kg, po administered through gavage 1 hr before carrageenan injection measured after 3 hrs by LC-MS/MS analysis relative to control2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
ISSN: 1520-4804		Development of Autotaxin Inhibitors: An Overview of the Patent and Primary Literature.
AID1497192Inhibition of ATX (unknown origin) assessed as decrease in choline release2018Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13
ISSN: 1464-3405		Development of autotaxin inhibitors: A series of zinc binding triazoles.
AID1497193Permeability assessed as drug absorption at 50 ug/ml after 5 hrs by PAMPA2018Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13
ISSN: 1464-3405		Development of autotaxin inhibitors: A series of zinc binding triazoles.
AID1633000Inhibition of recombinant full length human C-terminal His-tagged autotaxin expressed in human 293E cells assessed as choline release using lysophosphatidylcholine as substrate after 1 hr by Amplex red fluorescence assay2016ACS medicinal chemistry letters, Sep-08, Volume: 7, Issue:9
ISSN: 1948-5875		Novel Autotaxin Inhibitors for the Treatment of Osteoarthritis Pain: Lead Optimization via Structure-Based Drug Design.
AID1632555Inhibition of recombinant ATX (unknown origin) expressed in HEK293 cells using FS-3 as substrate after 15 mins2016Bioorganic & medicinal chemistry, 10-01, Volume: 24, Issue:19
ISSN: 1464-3391		Discovery and synthetic optimization of a novel scaffold for hydrophobic tunnel-targeted autotaxin inhibition.
AID1480297In vivo inhibition of ATX in Lewis rat assessed as decrease in plasma LPA levels at 30 mg/kg administered via oral gavage measured over 4 hrs LC-MS/MS method relative to control2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
ISSN: 1520-4804		Hydroxamic Acids Constitute a Novel Class of Autotaxin Inhibitors that Exhibit in Vivo Efficacy in a Pulmonary Fibrosis Model.
AID1633008Inhibition of autotaxin in healthy human whole blood assessed as reduction in LPA level after 2 hrs by LC-MS/MS analysis2016ACS medicinal chemistry letters, Sep-08, Volume: 7, Issue:9
ISSN: 1948-5875		Novel Autotaxin Inhibitors for the Treatment of Osteoarthritis Pain: Lead Optimization via Structure-Based Drug Design.
AID1480294Inhibition of recombinant mouse ATX expressed in HEK293 cells using FS3 as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
ISSN: 1520-4804		Hydroxamic Acids Constitute a Novel Class of Autotaxin Inhibitors that Exhibit in Vivo Efficacy in a Pulmonary Fibrosis Model.
AID1908646Cytotoxicity against human NCI-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jun-05, Volume: 236ISSN: 1768-3254Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors.
AID1325587Inhibition of human recombinant ATX using Rac-1-Palmitoyl-glycero-3-phosphocholine as substrate incubated for 2 hrs using ADHP fluorogenic peroxidase substrate by horseradish peroxidase/choline oxidase-coupled assay2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
ISSN: 1464-3405		Discovery of potent inhibitors of the lysophospholipase autotaxin.
AID1739783Inhibition of human C-terminal His6-tagged ATX beta expressed in Sf9 insect cells using FS-3 as substrate preincubated for 45 mins followed by substrate addition and measured at 1 min interval for 30 mins by fluorescence assay2020European journal of medicinal chemistry, Sep-01, Volume: 201ISSN: 1768-3254Structure guided design of potent indole-based ATX inhibitors bearing hydrazone moiety with tumor suppression effects.
AID1739787Antiproliferative activity against human NCI-H2228 cells measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Sep-01, Volume: 201ISSN: 1768-3254Structure guided design of potent indole-based ATX inhibitors bearing hydrazone moiety with tumor suppression effects.
AID1325588Inhibition of ATX in human plasma assessed as decrease in hydrolysis of lysophosphatidylcholine by measuring choline release after 24 hrs by horseradish peroxidase/choline oxidase-coupled assay2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
ISSN: 1464-3405		Discovery of potent inhibitors of the lysophospholipase autotaxin.
AID1908649Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jun-05, Volume: 236ISSN: 1768-3254Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors.
AID1908644Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jun-05, Volume: 236ISSN: 1768-3254Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors.
AID1349341Inhibition of human ERG expressed in HEK293 cells by patch clamp assay2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
ISSN: 1948-5875		Discovery of BI-2545: A Novel Autotaxin Inhibitor That Significantly Reduces LPA Levels in Vivo.
AID1312304Effective half life in Lewis rat at 1 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
ISSN: 1520-4804		Development of Autotaxin Inhibitors: An Overview of the Patent and Primary Literature.
AID1349340Inhibition of ATX in rat whole blood using LPA 17:0 as substrate after 1 hr by LC-MS/MS analysis2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
ISSN: 1948-5875		Discovery of BI-2545: A Novel Autotaxin Inhibitor That Significantly Reduces LPA Levels in Vivo.
AID1497189Oral bioavailability in Lewis rat at 1 to 100 mg/kg dosed via gavage after 1.25 to 24 hrs2018Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13
ISSN: 1464-3405		Development of autotaxin inhibitors: A series of zinc binding triazoles.
AID1908643Cytotoxicity against human MCF-7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jun-05, Volume: 236ISSN: 1768-3254Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors.
AID1312310Plasma concentration in Lewis rat air pouch model of inflammation at 100 mg/kg, po administered through gavage 1 hr before carrageenan injection measured after 3 hrs by LC-MS/MS analysis relative to control2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
ISSN: 1520-4804		Development of Autotaxin Inhibitors: An Overview of the Patent and Primary Literature.
AID1739785Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Sep-01, Volume: 201ISSN: 1768-3254Structure guided design of potent indole-based ATX inhibitors bearing hydrazone moiety with tumor suppression effects.
AID1656153Inhibition of human ATX pre-incubated for 45 mins before fluorogenic substrate-3 addition and measured every minute for 30 mins by fluorescence based assay2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
ISSN: 1520-4804		Discovery of Novel Indole-Based Allosteric Highly Potent ATX Inhibitors with Great
AID1908648Cytotoxicity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jun-05, Volume: 236ISSN: 1768-3254Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors.
AID1739784Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Sep-01, Volume: 201ISSN: 1768-3254Structure guided design of potent indole-based ATX inhibitors bearing hydrazone moiety with tumor suppression effects.
AID1438632Inhibition of human ATX expressed in HEK293 cells using FS-3 as substrate after 15 mins2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
ISSN: 1520-4804		Rational Design of Autotaxin Inhibitors by Structural Evolution of Endogenous Modulators.
AID1739786Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Sep-01, Volume: 201ISSN: 1768-3254Structure guided design of potent indole-based ATX inhibitors bearing hydrazone moiety with tumor suppression effects.
AID1312308Invivo inhibition of ATX in Lewis rat air pouch model of inflammation assessed as inhibition of carrageenan-induced LPA production in pouch fluid at 100 mg/kg, po administered through gavage 1 hr before carrageenan injection measured after 3 hrs by LC-MS/2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
ISSN: 1520-4804		Development of Autotaxin Inhibitors: An Overview of the Patent and Primary Literature.
AID1908647Cytotoxicity against human H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Jun-05, Volume: 236ISSN: 1768-3254Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors.
AID1240355Antitumor activity against human MeWo cells xenografted in athymic nude mouse at 30 mg/kg, ip administered every other day of 21 days post tumor cell injection2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
ISSN: 1464-3391		Vinyl sulfone analogs of lysophosphatidylcholine irreversibly inhibit autotaxin and prevent angiogenesis in melanoma.
AID1497191Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells after 45 mins by scintillation counting method2018Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13
ISSN: 1464-3405		Development of autotaxin inhibitors: A series of zinc binding triazoles.
AID1480296Inhibition of ATX in human whole blood assessed as decrease in LPA levels after 2 hrs by LC-MS/MS method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
ISSN: 1520-4804		Hydroxamic Acids Constitute a Novel Class of Autotaxin Inhibitors that Exhibit in Vivo Efficacy in a Pulmonary Fibrosis Model.
AID1438631In vivo inhibition of ATX in mouse assessed as decrease in eight abundant LPA species level at 10 mg/kg, ip measured after 8 hrs by HPLC electrospray ionization tandem mass spectrometry relative to control2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
ISSN: 1520-4804		Rational Design of Autotaxin Inhibitors by Structural Evolution of Endogenous Modulators.
AID1480295Inhibition of recombinant mouse ATX expressed in HEK293 cells using LPC 17:0 as substrate after 30 mins by LC-MS/MS method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
ISSN: 1520-4804		Hydroxamic Acids Constitute a Novel Class of Autotaxin Inhibitors that Exhibit in Vivo Efficacy in a Pulmonary Fibrosis Model.
AID1908642Negative allosteric modulation activity against human ATX using FS-3 as substrate preincubated for 45 mins followed by substrate addition and measured every 30 mins by multi-mode microplate reader2022European journal of medicinal chemistry, Jun-05, Volume: 236ISSN: 1768-3254Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors.
AID1312306Oral bioavailability in Lewis rat at 1 to 100 mg/kg administered through gavage measured up to 24 hrs by LC-MS/MS analysis2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
ISSN: 1520-4804		Development of Autotaxin Inhibitors: An Overview of the Patent and Primary Literature.
AID1433834Inhibition of human ATX expressed in HEK293 cells using FS-3 as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
ISSN: 1520-4804		Structure-Activity Relationships of Small Molecule Autotaxin Inhibitors with a Discrete Binding Mode.
AID1240356Antitumor activity against human MeWo cells xenografted in athymic nude mouse assessed as reduction of ATX level in serum at 30 mg/kg, ip administered every other day of 21 days post tumor cell injection2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
ISSN: 1464-3391		Vinyl sulfone analogs of lysophosphatidylcholine irreversibly inhibit autotaxin and prevent angiogenesis in melanoma.
AID1312307Invivo inhibition of ATX in Lewis rat air pouch model of inflammation assessed as inhibition of carrageenan-induced LPA production in plasma at 100 mg/kg, po administered through gavage 1 hr before carrageenan injection measured after 3 hrs by LC-MS/MS an2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
ISSN: 1520-4804		Development of Autotaxin Inhibitors: An Overview of the Patent and Primary Literature.
AID1312303Inhibition of recombinant human ATX expressed in HEK293 cells using FS3 as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
ISSN: 1520-4804		Development of Autotaxin Inhibitors: An Overview of the Patent and Primary Literature.
AID1349372Inhibition of human full length ATX expressed in HEK cells using FS-3 as substrate incubated for 15 mins followed by substrate addition measured after 30 mins2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
ISSN: 1948-5875		Discovery of BI-2545: A Novel Autotaxin Inhibitor That Significantly Reduces LPA Levels in Vivo.
AID1656151Inhibition of human ATX by fluorogenic substrate-3 assay2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
ISSN: 1520-4804		Discovery of Novel Indole-Based Allosteric Highly Potent ATX Inhibitors with Great
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
ISSN: 1091-6490		Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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
ISSN: 1091-6490		Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346280Human autotaxin (LPA synthesis)2010The Journal of pharmacology and experimental therapeutics, Jul, Volume: 334, Issue:1
ISSN: 1521-0103		A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation.

Research

Studies (24)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's14 (58.33)24.3611
2020's10 (41.67)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (4.17%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other23 (95.83%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
4-methoxyphenylboronic acid
1
202220222.0high000001
ursodoxicoltaurine
1
bile acid taurine conjugateanti-inflammatory agent;
apoptosis inhibitor;
bone density conservation agent;
cardioprotective agent;
human metabolite;
neuroprotective agent		201720177.0high000010
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Adjuvant Arthritis0
1
2010201014.0low000100
Allodynia0
1
2010201014.0low000100
Alveolitis, Fibrosing0
2
201820205.0medium000020
Angiogenesis, Pathologic0
1
201520159.0low000010
Benign Neoplasms0
3
201620224.0medium000012
Congenital Zika Syndrome0
1
202020204.0low000010
Disease Models, Animal0
2
202020204.0medium000020
Malignant Melanoma0
1
201520159.0low000010
Melanoma0
1
201520159.0low000010
Neoplasms0
3
201620224.0medium000012
Pulmonary Fibrosis0
2
201820205.0medium000020
Zika Virus Infection0
1
202020204.0low000010

Bioavailability (2)

ArticleYear
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, , Volume: 96, Issue:5		2019
A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation.
The Journal of pharmacology and experimental therapeutics, , Volume: 334, Issue:1		2010

Dosage (1)

ArticleYear
A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation.
The Journal of pharmacology and experimental therapeutics, , Volume: 334, Issue:1		2010