Assay ID | Title | Year | Journal | Article |
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. |
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. |
AID1347167 | Vero cells viability 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. |
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. |
AID1347164 | 384 well plate NINDS Rhodamine confirmatory 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. |
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. |
AID1347149 | Furin counterscreen 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. |
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. |
AID1347163 | 384 well plate NINDS AMC confirmatory 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. |
AID1347152 | Confirmatory screen NINDS AMC 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. |
AID1347156 | DAPI mCherry counterscreen 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. |
AID1347153 | Confirmatory screen GU AMC 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. |
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. |
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. |
AID1347168 | HepG2 cells viability 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. |
AID1347158 | ZIKV-mCherry secondary 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. |
AID1347411 | qHTS 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) Libary | 2020 | ACS 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. |
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. |
AID1337119 | Displacement of [3H](2S,3R)-3-((R)-2-(2'-fluoro-5'-methoxybiphenyl-4-yl)chroman-7-yl)-2-methylbutanoic acid from human GPR40 expressed in CHO-K1 cell membranes incubated for 30 mins on orbital shaker measured after 16 hrs by TopCount scintillation countin | 2017 | ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
| Design and Synthesis of Novel, Selective GPR40 AgoPAMs. |
AID640069 | Agonist activity at GPR41 | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1328817 | Half life in iv or po dosed rat | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
| GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space. |
AID1326120 | Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay | | | |
AID1328816 | Half life in iv or po dosed dog | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
| GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space. |
AID1734999 | AUC in hyperglycemic Balb/c mouse plasma at 1 mg/kg measured upto 60 mins | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1734869 | Agonist activity at GPR40 in Sprague-Dawley rat pancreatic islets assessed as induction of glucose-mediated insulin secretion measured after 90 mins in EBSS buffer by ELISA | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1337118 | Displacement of [3H]L358 from human GPR40 expressed in CHO-K1 cell membranes incubated for 30 mins on orbital shaker measured after 16 hrs by TopCount scintillation counting method | 2017 | ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
| Design and Synthesis of Novel, Selective GPR40 AgoPAMs. |
AID1590246 | Hypoglycemic activity in Sprague-Dawley rat assessed as reduction in blood glucose AUC at 0.3 mg/kg, po pretreated for 1 hr followed by glucose challenge by OGTT relative to control | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs. |
AID1734884 | Hypoglycemic activity in Balb/c mouse assessed as effective dose causing reduction in blood glucose level administered orally 60 mins prior to glucose challenge measured for 60 mins by IPGTT | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1328827 | Agonist activity at GPR40 (unknown origin) by calcium flux assay | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
| GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space. |
AID1328814 | Clearance in iv or po dosed monkey | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
| GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space. |
AID640068 | Induction of insulin secretion in mouse MIN6 cells | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID640075 | Antidiabetic activity in wild type mouse assessed as reduction in plasma glucose excursion at 10 mg/kg, po pretreated 60 mins before glucose challenge measured for 2 hrs by oral glucose tolerance test | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1328815 | Half life in iv or po dosed mouse | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
| GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space. |
AID640169 | AUC in cynomolgus monkey at 0.5 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID692589 | Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum | 2012 | ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
| Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist. |
AID1734880 | Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay rela | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1734881 | Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant m | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID640067 | Partial agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by aequorin assay relative to docosahexaenoic acid | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID640165 | Oral bioavailability in cynomolgus monkey at 0.5 mg/kg | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID640080 | Clearance in cynomolgus monkey at 0.5 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID640082 | Half life in rat at 0.5 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1734882 | Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as residence time by radio | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1590182 | Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in absence of human serum by microbeta counting method relative to control | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs. |
AID692593 | Agonist activity at GPR40 expressed in CHO cells assessed as intrinsic efficacy after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum relative to AM-1638 | 2012 | ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
| Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist. |
AID640167 | AUC in rat at 0.5 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID640171 | Cmax in rat at 0.5 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1328811 | Clearance in iv or po dosed mouse | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
| GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space. |
AID640077 | Clearance in mouse at 0.8 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID692592 | Partial agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay relative to DHA | 2012 | ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
| Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist. |
AID640071 | Agonist activity at PPAR-alpha by cell-based assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1734874 | Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assa | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1328820 | Oral bioavailability in rat | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
| GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space. |
AID640073 | Agonist activity at PPAR-gamma by cell-based assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1154886 | Oral bioavailability in rat at 2 mg/kg | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Optimization of GPR40 Agonists for Type 2 Diabetes. |
AID1734905 | Drug distribution in C57BL/6 mouse spleen at 3 microg/kg, iv administered as single dose observed at 20 to 40 mins by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1734870 | Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1271404 | Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis | 2016 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
| Discovery of the imidazole-derived GPR40 agonist AM-3189. |
AID1734879 | Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1154881 | Agonist activity at human GPR40 expressed in CHO cells by aequorin assay | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Optimization of GPR40 Agonists for Type 2 Diabetes. |
AID692628 | Antidiabetic activity in DIO BDF mouse model assessed as increase in plasma insulin level at 60 mg/kg, po administered 1 hr prior glucose-challenge challenge measured after 1 hr by ELISA | 2012 | ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
| Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist. |
AID1328821 | Oral bioavailability in dog | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
| GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space. |
AID1734875 | Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1154883 | Clearance in rat at 0.5 mg/kg, iv | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Optimization of GPR40 Agonists for Type 2 Diabetes. |
AID1422548 | Agonist activity at FFA1 (unknown origin) | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ. |
AID1734899 | Protein binding in plasma (unknown origin) by equilibrium dialysis method | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID640076 | Antidiabetic activity in GPR40 knockout mouse assessed as reduction in plasma glucose excursion at 10 mg/kg, po pretreated 60 mins before glucose challenge measured for 2 hrs by oral glucose tolerance test | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID748342 | Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay relative to AM-1638 | 2013 | ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
| Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles. |
AID1734909 | Protein binding in C57BL/6 mouse plasma at 3 microg/kg, iv by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1154885 | Volume of distribution at steady state in rat | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Optimization of GPR40 Agonists for Type 2 Diabetes. |
AID1734906 | Drug distribution in C57BL/6 mouse colon at 3 microg/kg, iv administered as single dose observed at 20 to 40 mins by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID640174 | Antidiabetic activity in wild type mouse assessed as reduction of total glucose AUC at 10 mg/kg, po pretreated 60 mins before glucose challenge measured for 2 hrs by oral glucose tolerance test | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID620370 | Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
| Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties. |
AID748343 | Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay | 2013 | ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
| Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles. |
AID640083 | Half life in Beagle dog at 0.5 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1308065 | Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay relative to TUG-770 | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer. |
AID1734900 | Displacement of [3H]-MuCi from PPARalpha (unknown origin) expressed in baculovirus infected Sf9 insect cells upto 30 uM measured after 10 hrs by microbeta scintillation counting analysis | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1328813 | Clearance in iv or po dosed dog | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
| GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space. |
AID1734901 | Displacement of [3H]-MuCi from PPARdelta (unknown origin) expressed in baculovirus infected Sf9 insect cells upto 30 uM measured after 10 hrs by microbeta scintillation counting analysis | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID640078 | Clearance in rat at 0.5 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID640081 | Half life in mouse at 0.8 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1271430 | Induction of insulin release in human pancreatic islets | 2016 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
| Discovery of the imidazole-derived GPR40 agonist AM-3189. |
AID1734883 | Agonist activity at GPR40 in mouse MIN6 cells assessed as induction of glucose-mediated insulin secretion incubated for 2 hrs by ELISA | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1328818 | Half life in iv or po dosed monkey | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
| GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space. |
AID1271406 | Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum | 2016 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
| Discovery of the imidazole-derived GPR40 agonist AM-3189. |
AID640168 | AUC in Beagle dog at 2 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1308067 | Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer. |
AID640091 | Oral bioavailability in Beagle dog at 2 mg/kg | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1734878 | Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay relative to control | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID640085 | Volume of distribution at steady state in mouse at 0.8 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1328819 | Oral bioavailability in mouse | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
| GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space. |
AID640072 | Agonist activity at PPAR-delta by cell-based assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID640173 | Cmax in cynomolgus monkey at 0.5 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID640170 | Cmax in mouse at 5 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1324909 | Agonist activity at FFA1 receptor (unknown origin) | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
| Free fatty acid receptor 1 (GPR40) agonists containing spirocyclic periphery inspired by LY2881835. |
AID640086 | Volume of distribution at steady state in rat at 0.5 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1734873 | Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assa | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1308063 | Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX- | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer. |
AID640066 | Agonist activity at mouse GPR40 | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID692629 | Antidiabetic activity in DIO BDF mouse model assessed as improvement in glucose-challenge AUC(0 to 60 mins) at 60 mg/kg, po administered 1 hr prior glucose-challenge challenge measured after 1 hr by OGTT | 2012 | ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
| Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist. |
AID1734871 | Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1271405 | Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin | 2016 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
| Discovery of the imidazole-derived GPR40 agonist AM-3189. |
AID1337110 | Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay relative to DMSO control | 2017 | ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
| Design and Synthesis of Novel, Selective GPR40 AgoPAMs. |
AID640065 | Agonist activity at rat GPR40 | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1734877 | Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1308064 | Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer. |
AID1328822 | Oral bioavailability in monkey | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
| GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space. |
AID1154884 | Mean residence time in rat | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Optimization of GPR40 Agonists for Type 2 Diabetes. |
AID1734876 | Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay relative to control | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1328812 | Clearance in iv or po dosed rat | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
| GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space. |
AID640074 | Inhibition of alpha2 adrenergic receptor | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID640166 | AUC in mouse at 5 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1734872 | Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay relative to 100 uM linoleic acid | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID1734902 | Displacement of [3H]-MuCi from PPARgamma (unknown origin) expressed in baculovirus infected Sf9 insect cells upto 30 uM measured after 10 hrs by microbeta scintillation counting analysis | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). |
AID640090 | Oral bioavailability in rat at 0.5 mg/kg | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1154882 | Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Optimization of GPR40 Agonists for Type 2 Diabetes. |
AID748325 | Binding affinity to human FFA1 receptor expressed in CHO cell membranes assessed as inhibition of specific binding of [3H]AMG 837 | 2013 | ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
| Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles. |
AID640088 | Volume of distribution at steady state in cynomolgus monkey at 0.5 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID640087 | Volume of distribution at steady state in Beagle dog at 0.5 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID692591 | Partial agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay | 2012 | ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
| Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist. |
AID640079 | Clearance in Beagle dog at 0.5 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID692626 | Antidiabetic activity in DIO BDF mouse model assessed as reduction in blood glucose-challenge excursion at 60 mg/kg, po administered 1 hr prior glucose-challenge challenge measured after 1 hr by OGTT ( Rvb = 462 mg/dl ) | 2012 | ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
| Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist. |
AID1308068 | Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay relative to TUG-770 | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer. |
AID640084 | Half life in cynomolgus monkey at 0.5 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID640070 | Agonist activity at GPR43 | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID640089 | Oral bioavailability in mouse at 5 mg/kg | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID640172 | Cmax in Beagle dog at 2 mg/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
| AMG 837: a potent, orally bioavailable GPR40 agonist. |
AID1805801 | Various Assay from Article 10.1021/acs.jmedchem.1c00409: \\Perspectives on SARS-CoV-2 Main Protease Inhibitors.\\ | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
| Perspectives on SARS-CoV-2 Main Protease Inhibitors. |
AID1345809 | Human FFA1 receptor (Free fatty acid receptors) | 2012 | Molecular pharmacology, Nov, Volume: 82, Issue:5
| Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |