Compounds > am 1638
Page last updated: 2024-11-13

am 1638

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 CID57706778
CHEMBL ID2152070
SCHEMBL ID2495289
MeSH IDM0581311

Synonyms (14)

Synonym
am-1638
bdbm50392861
chembl2152070 ,
SCHEMBL2495289
AKOS025290929
1142214-62-7
(s)-3-cyclopropyl-3-(3-((2-(5,5-dimethylcyclopent-1-en-1-yl)-2'-fluoro-5'-methoxy-[1,1'-biphenyl]-4-yl)methoxy)phenyl)propanoic acid
CS-0007046
HY-13467
tris(2,2
MS-29554
(3s)-3-cyclopropyl-3-[3-[[3-(5,5-dimethylcyclopenten-1-yl)-4-(2-fluoro-5-methoxyphenyl)phenyl]methoxy]phenyl]propanoic acid
(betas)-beta-cyclopropyl-3-[[2-(5,5-dimethyl-1-cyclopenten-1-yl)-2'-fluoro-5'-methoxy[1,1'-biphenyl]-4-yl]methoxy]benzenepropanoic acid
DTXSID001102788

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" This led to the discovery of new GPR40 full agonists with significantly improved pharmacokinetic propeties."( Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists.
Brown, SP; Connors, R; Dransfield, PJ; Du, X; Guo, Q; Houze, JB; Jiao, X; Kohn, T; Li, AR; Li, F; Lin, DC; Liu, JJ; Luo, J; Medina, JC; Su, Y; Swaminath, G; Tran, T; Vimolratana, M; Wang, Y; Wang, Z; Wong, S; Yu, M; Zhang, J; Zhu, L; Zhuang, R, 2014)		0.4

Bioavailability

ExcerptReferenceRelevance
" A potent, orally bioavailable small molecule GPR40 agonist is hypothesized to be an effective antidiabetic posing little or no risk of hypoglycemia."( Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
Brown, SP; Dransfield, PJ; Guo, Q; Houze, JB; Jiao, X; Li, F; Lin, DC; Liu, J; Luo, J; Medina, JC; Pattaropong, V; Sun, Y; Swaminath, G; Vimolratana, M; Wong, S; Zhang, J; Zhu, L; Zhuang, R, 2012)		0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Free fatty acid receptor 1Homo sapiens (human)EC50 (µMol)0.20930.00030.73698.8000AID1137750; AID1137756; AID1337107; AID1337109; AID1385252; AID1590184; AID1590251; AID1679417; AID1724377; AID1750089; AID692589; AID692590; AID748343
Free fatty acid receptor 1Homo sapiens (human)Kd0.00500.00190.00580.0119AID1724380
Free fatty acid receptor 1Rattus norvegicus (Norway rat)EC50 (µMol)0.01140.00320.03530.0990AID1679416
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Free fatty acid receptor 1Homo sapiens (human)fEC500.00010.00010.00010.0001AID1590184
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (11)

Processvia Protein(s)Taxonomy
phospholipase C-activating G protein-coupled receptor signaling pathwayFree fatty acid receptor 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationFree fatty acid receptor 1Homo sapiens (human)
insulin secretionFree fatty acid receptor 1Homo sapiens (human)
negative regulation of interleukin-1 beta productionFree fatty acid receptor 1Homo sapiens (human)
glucose homeostasisFree fatty acid receptor 1Homo sapiens (human)
positive regulation of calcium ion transportFree fatty acid receptor 1Homo sapiens (human)
response to fatty acidFree fatty acid receptor 1Homo sapiens (human)
ion channel modulating, G protein-coupled receptor signaling pathwayFree fatty acid receptor 1Homo sapiens (human)
ligand-gated ion channel signaling pathwayFree fatty acid receptor 1Homo sapiens (human)
positive regulation of insulin secretionFree fatty acid receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayFree fatty acid receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityFree fatty acid receptor 1Homo sapiens (human)
lipid bindingFree fatty acid receptor 1Homo sapiens (human)
bioactive lipid receptor activityFree fatty acid receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneFree fatty acid receptor 1Homo sapiens (human)
plasma membraneFree fatty acid receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (119)

Assay IDTitleYearJournalArticle
AID748329Half life in cynomolgus monkey at 0.5 mg/kg, iv2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID748328Oral bioavailability in Sprague-Dawley rat at 2 mg/kg2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID692637Clearance in rat at 2 mg/kg, po and 0.5 mg/kg, iv2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID1590192Inhibition of human sodium dependent noradrenaline transporter at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID692633Tmax in cynomolgus monkey at 2 mg/kg, po and 0.5 mg/kg, iv2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID1337110Positive 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 control2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Design and Synthesis of Novel, Selective GPR40 AgoPAMs.
AID748336Inhibition of human dopamine D1 receptor at 10 uM relative to control2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID692595Tmax in mouse at 5 mg/kg, po and 1 mg/kg, iv2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID1590191Inhibition of human sodium dependent dopamine transporter at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1586863Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination.
AID748335Inhibition of rat kappa opioid receptor at 10 uM relative to control2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID1590208Inhibition of human muscarinic M3 receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID692627Antidiabetic activity in DIO BDF mouse model assessed as increase in insulin AUC at 60 mg/kg, po administered 1 hr prior glucose-challenge challenge measured after 1 hr by ELISA2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID1385272Oral bioavailability in cynomolgus monkey at 10 mg/kg2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
AID1590209Inhibition of human kappa type opioid receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1137765Antidiabetic activity in high fat fed C57/Bl6 mouse streptozotocin-induced type 2 diabetic model assessed as reduction of blood glucose level at 60 mg/kg, po up to 120 mins by oral glucose tolerance test2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists.
AID692640Tmax in rat at 2 mg/kg, po and 0.5 mg/kg, iv2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID1385257Clearance in rat at 2 mg/kg, po2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
AID1590181Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1137762Oral bioavailability in rat at 2 mg/kg2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists.
AID1137750Agonist activity at GPR40 (unknown origin) expressed in mouse A9 cells assessed as inositol phosphate accumulation using [myo-3H]inositol after 1 hr by scintillation counting in presence of 0.3% human serum albumin2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists.
AID1137761Half life in rat at 0.5 mg/kg, iv2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists.
AID1590193Inhibition of human recombinant cyclooxygenase COX1 expressed in baculovirus infected Sf9 cells at 10 uM using arachidonic acid as substrate preincubated for 15 mins followed by substrate addition and measured after 3 mins by ampliflu red reagent-based sp2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1590187Displacement of [3H]LTD4 from human full-length recombinant cysteinyl leukotriene type-2 receptor expressed in HEK293 cells at 10 uM measured after 60 mins by scintillation counting method relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1679378Agonist activity at GPR40 in rat INS1 (832/13) cells assessed as induction of glucose-stimulated insulin secretion in presence of 10 mM glucose2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Discovery of a novel potent GPR40 full agonist.
AID1385262Fraction unbound in cynomolgus monkey plasma at 0.5 mg/kg, iv2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
AID1590196Inhibition of human full-length recombinant caspase 8 expressed in Escherichia coli at 10 uM using Ac-IETD-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by spectrofluorimetric analysis relative to cont2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1590199Inhibition of human recombinant full-length ERK1 expressed in Escherichia coli at 10 uM using myelin basic protein as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins in the presence of [gamma32P]ATP by scintill2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID748317Antidiabetic activity in high-fat diet fed streptozotocin-induced C57BL/6J mouse at 60 mg/kg, po by oral glucose tolerance test2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID1590207Inhibition of human histamine H2 receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID692630Oral bioavailability in cynomolgus monkey at 2 mg/kg2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID748333Clearance in cynomolgus monkey at 0.5 mg/kg, iv2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID1590237Inhibition of human 5-HT2B receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1679416Agonist activity at rat GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Discovery of a novel potent GPR40 full agonist.
AID1590221Glucose lowering effect in GPR40 knockout mouse assessed as increase in GLP-1 level2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1590198Inhibition of human neutrophil cathepsin G at 10 uM using Suc-Ala-Ala-Pro-Phe-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by spectrofluorimetric analysis relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1590195Inhibition of human full-length recombinant MAOA expressed in insect cells at 10 mM using kynuramine as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by spectrofluorimetric analysis relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID748326Positive cooperativite binding to human FFA1 receptor expressed in CHO cell membranes assessed as enhancement of specific binding of [3H]AMG 837 by reciprocal competition assay2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID748332Volume of distribution at steady state in Sprague-Dawley rat at 0.5 mg/kg, iv2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID1385260Oral bioavailability in rat at 2 mg/kg2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
AID1590178Inhibition of rat P2Y receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1724378Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay relative to gamma-linolenic acid2020Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
Design and Identification of a GPR40 Full Agonist (
AID1137760Clearance in rat at 0.5 mg/kg, iv2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists.
AID692639Cmax in rat at 2 mg/kg, po2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID1586865Full agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of GalphaS-mediated cAMP accumulation after 30 mins HTRF assay2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination.
AID748338Inhibition of human CCK2 receptor at 10 uM relative to control2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID748331Volume of distribution at steady state in cynomolgus monkey at 0.5 mg/kg, iv2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID692628Antidiabetic 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 ELISA2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID1590205Inhibition of rat GABAA receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1385253Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay relative to AM-16382018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
AID1385268Volume of distribution at steady state in cynomolgus monkey at 10 mg/kg, po2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
AID692589Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID692635Oral bioavailability in rat at 2 mg/kg2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID1385252Agonist activity at GPR40 (unknown origin) expressed in CHO cells incubated for 2 hrs measured over 20 secs in presence of human serum albumin by aequorin based luminescence assay2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
AID1724380Binding affinity to human GPR40 expressed in CHO cells by LC-MS analysis2020Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
Design and Identification of a GPR40 Full Agonist (
AID1370533Agonist activity at human GPR40 expressed in CHO cells co-expressing Gqalpha assessed as IP1 accumulation2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Discovery of novel benzo[b]thiophene tetrazoles as non-carboxylate GPR40 agonists.
AID1590210Inhibition of human mu type opioid receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1385266Clearance in cynomolgus monkey at 10 mg/kg, po2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
AID692629Antidiabetic 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 OGTT2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID692641Half life in mouse at 1 mg/kg, iv2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID692594Cmax in mouse at 5 mg/kg, po2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID1590235Inhibition of human 5HT1A receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID748341Inhibition of human adenosine A1 receptor at 10 uM relative to control2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID1590184Positive allosteric modulation of recombinant human GPR40 expressed in HEK293 cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins in presence of 100% human serum by microbeta counting method2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID692588Clearance in mouse at 5 mg/kg, po and 1 mg/kg, iv2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID692626Antidiabetic 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 )2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID692631Half life in cynomolgus monkey at 0.5 mg/kg, iv2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID1385254Fraction unbound in rat plasma at 0.5 mg/kg, iv or 2 mg/kg, po2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
AID1590236Inhibition of human 5-HT2A receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1590180Inhibition of human full-length recombinant MARK3 expressed in insect cells at 10 uM using CHKtide as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins in presence of [gamma32P]ATP by scintillation counting analy2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID692632Clearance in cynomolgus monkey at 2 mg/kg, po and 0.5 mg/kg, iv2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID1385258Volume of distribution at steady state in rat at 2 mg/kg, po2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
AID1590203Inhibition of human dopamine D1 receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID748343Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID748339Inhibition of human norepinephrine transporter at 10 uM relative to control2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID1337118Displacement 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 method2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Design and Synthesis of Novel, Selective GPR40 AgoPAMs.
AID1590246Hypoglycemic 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 control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1590201Inhibition of human adrenergic alpha2C receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1590206Inhibition of human histamine H1 receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1385264AUC in cynomolgus monkey at 10 mg/kg, po2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
AID1370534Agonist activity at human GPR40 expressed in CHO cells assessed as cAMP production2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Discovery of novel benzo[b]thiophene tetrazoles as non-carboxylate GPR40 agonists.
AID1590186Inhibition of human recombinant full length acetylcholine esterase expressed in HEK293 cells at 10 uM using acetylcholine as substrate preincubated for 15 mins followed by substrate addition measured after 20 mins by spectrophotometric analysis2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1590238Inhibition of human 5-HT2C receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1590202Displacement of [3H]Kallidin(des-Arg10,Leu9) from human recombinant bradykinin B1 receptor expressed in CHOK1 cells at 10 uM after 60 mins by scintillation counting assay relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1679376Agonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion at 10 uM2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Discovery of a novel potent GPR40 full agonist.
AID1750089Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hrs by Bright-Glo based serum response element (SRE) luciferase reporter assay
AID1590183Positive allosteric modulation of recombinant human GPR40 expressed in CHO cells assessed as increase in [3H]-myo-inositol phosphate accumulation measured after 60 mins by microbeta counting method2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID748327Oral bioavailability in cynomolgus monkey at 2 mg/kg2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID1679417Agonist activity at human GPR40 transfected in HEK293 cells assessed as increase in intracellular calcium level incubated for 1 hr by Fluo-8 dye based fluorescence analysis2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Discovery of a novel potent GPR40 full agonist.
AID692636Half life in rat at 0.5 mg/kg, iv2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID1590197Inhibition of human full-length recombinant caspase 9 expressed in Escherichia coli at 10 uM using Ac-LEHD-AFC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by spectrofluorimetric analysis relative to cont2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID692634Cmax in cynomolgus monkey at 2 mg/kg, po2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID1590259Solubility of the compound in FASSIF2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1590204Inhibition of human dopamine D2s receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1385270Half life in cynomolgus monkey at 0.5 mg/kg, iv2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
AID748337Inhibition of human histamine H4 receptor at 10 uM relative to control2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID1590251Positive 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 method2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID692590Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID1337130Stimulation of GLP-1 secretion in po dosed GPR40 knockout C57BL/6 mouse measured after 24 hrs2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Design and Synthesis of Novel, Selective GPR40 AgoPAMs.
AID1337108Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay relative to DMSO control2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Design and Synthesis of Novel, Selective GPR40 AgoPAMs.
AID1590211Inhibition of human prostanoid EP1 receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1590182Positive 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 control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1724377Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay2020Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
Design and Identification of a GPR40 Full Agonist (
AID1590194Inhibition of human recombinant cyclooxygenase COX2 expressed in baculovirus infected Sf9 cells at 10 uM using arachidonic acid as substrate preincubated for 15 mins followed by substrate addition and measured after 3 mins by ampliflu red reagent-based sp2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1385259Half life in rat at 0.5 mg/kg, iv2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
AID1385256AUC in rat at 2 mg/kg, po2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.
AID1590200Inhibition of human adrenergic alpha2A receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID748340Inhibition of human TRH1 receptor at 10 uM relative to control2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID1590190Inhibition of human SERT at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID748330Half life in Sprague-Dawley rat at 0.5 mg/kg, iv2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID1590212Inhibition of human prostanoid EP3 receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID692638Oral bioavailability in mouse at 5 mg/kg2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID748334Clearance in Sprague-Dawley rat at 0.5 mg/kg, iv2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID1137756Agonist activity at GPR40 (unknown origin) expressed in CHO cells assessed as luminescence for 20 seconds interval by aequorin assay in presence of 0.01% human serum albumin2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists.
AID1590260Inhibition of human histamine H4 receptor at 10 uM relative to control2019Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
AID1337131Stimulation of GLP-1 secretion in po dosed wild-type C57BL/6 mouse measured after 24 hrs2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Design and Synthesis of Novel, Selective GPR40 AgoPAMs.
AID1337109Positive 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 assay2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Design and Synthesis of Novel, Selective GPR40 AgoPAMs.
AID1337107Positive allosteric modulation of human GPR40 expressed in HEK293 cells assessed as IP1 accumulation measured after 60 mins by HTRF assay2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Design and Synthesis of Novel, Selective GPR40 AgoPAMs.
AID1337119Displacement 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 countin2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Design and Synthesis of Novel, Selective GPR40 AgoPAMs.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's9 (81.82)24.3611
2020's2 (18.18)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.65

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 Index19.65 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.65)

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%
Other11 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
glyburide
Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide. glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group.		2.1710monochlorobenzenes;
N-sulfonylurea		anti-arrhythmia drug;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor;
hypoglycemic agent
docosahexaenoate
efalex: a mixture of fish oil and primrose oil; used as a high-docosahexaenoic acid fatty acid supplement. docosahexaenoic acid : Any C22 polyunsaturated fatty acid containing six double bonds.. docosahexaenoate : A polyunsaturated fatty acid anion that is the conjugate base of docosahexaenoic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3.. all-cis-docosa-4,7,10,13,16,19-hexaenoic acid : A docosahexaenoic acid having six cis-double bonds at positions 4, 7, 10, 13, 16 and 19.		2.0710docosahexaenoic acid;
omega-3 fatty acid		algal metabolite;
antineoplastic agent;
Daphnia tenebrosa metabolite;
human metabolite;
mouse metabolite;
nutraceutical
sitagliptin
sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity.		2.1710triazolopyrazine;
trifluorobenzene		EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
environmental contaminant;
hypoglycemic agent;
serine proteinase inhibitor;
xenobiotic
sitagliptin phosphate
Sitagliptin Phosphate: A pyrazine-derived DIPEPTIDYL-PEPTIDASE IV INHIBITOR and HYPOGLYCEMIC AGENT that increases the levels of the INCRETIN hormones GLUCAGON-LIKE PEPTIDE-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). It is used in the treatment of TYPE 2 DIABETES.		2.2510
exenatide
[no description available]		2.0810
tak-875
[no description available]		3.4460biphenyls
amg-837
AMG-837: GPR40 agonist		3.0340
ConditionIndicatedRelationship StrengthStudiesTrials
Alloxan Diabetes
[description not available]		02.2510