Page last updated: 2024-11-13

amg-837

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Description

AMG-837: GPR40 agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID46854655
CHEMBL ID1829173
SCHEMBL ID12194429
MeSH IDM0557377

Synonyms (31)

Synonym
amg-837
CHEMBL1829173 ,
bdbm50362690
AKOS016009081
amg837
amg 837
gtpl6485
(3s)-3-[4-({3-[4-(trifluoromethyl)phenyl]phenyl}methoxy)phenyl]hex-4-ynoic acid
CS-3278
HY-13967
865231-46-5
NE6U6R66U4 ,
benzenepropanoic acid, .beta.-1-propyn-1-yl-4-((4'-(trifluoromethyl)(1,1'-biphenyl)-3-yl)methoxy)-, (.beta.s)-
unii-ne6u6r66u4
SCHEMBL12194429
(s)-3-(4-((4'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)methoxy)phenyl)hex-4-ynoic acid
AC-30223
DTXSID00676764
(3s)-3-(4-{[4'-(trifluoromethyl)[biphenyl]-3-yl]methoxy}phenyl)-4-hexynoic acid
mfcd23703041
NCGC00386948-01
AS-51920
zopnbmmvvzrsgh-nrfanrhfsa-n
Q27074441
(3s)-3-(4-{[4'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl]methoxy}phenyl)hex-4-ynoic acid
EN300-313172
(3s)-3-[4-[[3-[4-(trifluoromethyl)phenyl]phenyl]methoxy]phenyl]hex-4-ynoic acid
EX-A1792
P13904
NCGC00386948-02
Z2289809643

Research Excerpts

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
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" The improvement in glucose excursions persisted following daily dosing of AMG 837 for 21-days in Zucker fatty rats."( AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents.
Chen, JL; Chen, M; Houze, JB; Li, F; Li, XN; Lin, DC; Lin, YJ; Lopez, E; Lu, JY; Luo, J; Nguyen, K; Reagan, JD; Swaminath, G; Tang, L; Tian, H; Tonn, GR; Tran, T; Zhang, J; Zhuang, R, 2011
)
0.37
" The dose-response relationship studies suggested that the pan agonist 15 suppressed the excursion of blood glucose levels in a dose-dependent manner."( Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
Deng, F; Li, Y; Li, Z; Zhang, D; Zhang, L; Zhou, Z, 2018
)
0.48
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Free fatty acid receptor 1Homo sapiens (human)Ki0.02190.00220.05080.2188AID1308063; AID1734870
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC50 (µMol)24.15000.00402.92669.9600AID1805801
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC50 (µMol)24.15000.00022.45859.9600AID1805801
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Free fatty acid receptor 1Homo sapiens (human)EC50 (µMol)0.56830.00030.73698.8000AID1154881; AID1154882; AID1271404; AID1271405; AID1271406; AID1308064; AID1308067; AID1324909; AID1326120; AID1328827; AID1422548; AID1734871; AID1734873; AID1734879; AID620370; AID692589; AID748343
Free fatty acid receptor 1Homo sapiens (human)Kd0.00190.00190.00580.0119AID1734881
Cytochrome P450 2D6Homo sapiens (human)EC50 (µMol)0.00220.00020.82764.4400AID1326120
Free fatty acid receptor 1Mus musculus (house mouse)EC50 (µMol)0.00730.00150.01050.0190AID1734875; AID640066
Free fatty acid receptor 1Rattus norvegicus (Norway rat)EC50 (µMol)0.01310.00320.03530.0990AID1734877; AID640065
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (28)

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)
symbiont-mediated perturbation of host ubiquitin-like protein modificationReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

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)
3'-5'-RNA exonuclease activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
RNA-dependent RNA polymerase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
cysteine-type endopeptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
mRNA 5'-cap (guanine-N7-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
mRNA (nucleoside-2'-O-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
5'-3' RNA helicase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
K63-linked deubiquitinase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
K48-linked deubiquitinase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
3'-5'-RNA exonuclease activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA-dependent RNA polymerase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
cysteine-type endopeptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA 5'-cap (guanine-N7-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA (nucleoside-2'-O-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA endonuclease activity, producing 3'-phosphomonoestersReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
ISG15-specific peptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
5'-3' RNA helicase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
protein guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
plasma membraneFree fatty acid receptor 1Homo sapiens (human)
plasma membraneFree fatty acid receptor 1Homo sapiens (human)
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (128)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347167Vero cells viability qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347164384 well plate NINDS Rhodamine confirmatory qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347161Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347149Furin counterscreen qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347163384 well plate NINDS AMC confirmatory qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347152Confirmatory screen NINDS AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347156DAPI mCherry counterscreen qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347153Confirmatory 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
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347169Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347168HepG2 cells viability qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347158ZIKV-mCherry secondary qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347157Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS2020Proceedings 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.
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.
AID640069Agonist activity at GPR412012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1328817Half life in iv or po dosed rat2016Bioorganic & 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.
AID1326120Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
AID1328816Half life in iv or po dosed dog2016Bioorganic & 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.
AID1734999AUC in hyperglycemic Balb/c mouse plasma at 1 mg/kg measured upto 60 mins2016Journal 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).
AID1734869Agonist 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 ELISA2016Journal 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).
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.
AID1734884Hypoglycemic 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 IPGTT2016Journal 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).
AID1328827Agonist activity at GPR40 (unknown origin) by calcium flux assay2016Bioorganic & 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.
AID1328814Clearance in iv or po dosed monkey2016Bioorganic & 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.
AID640068Induction of insulin secretion in mouse MIN6 cells2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID640075Antidiabetic 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 test2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1328815Half life in iv or po dosed mouse2016Bioorganic & 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.
AID640169AUC in cynomolgus monkey at 0.5 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
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.
AID1734880Agonist 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 rela2016Journal 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).
AID1734881Displacement 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 m2016Journal 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).
AID640067Partial agonist activity at human GPR40 expressed in CHO cells assessed as calcium flux by aequorin assay relative to docosahexaenoic acid2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID640165Oral bioavailability in cynomolgus monkey at 0.5 mg/kg2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID640080Clearance in cynomolgus monkey at 0.5 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID640082Half life in rat at 0.5 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1734882Displacement 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 radio2016Journal 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).
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.
AID692593Agonist 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-16382012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID640167AUC in rat at 0.5 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID640171Cmax in rat at 0.5 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1328811Clearance in iv or po dosed mouse2016Bioorganic & 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.
AID640077Clearance in mouse at 0.8 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID692592Partial agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay relative to DHA2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID640071Agonist activity at PPAR-alpha by cell-based assay2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1734874Agonist 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 assa2016Journal 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).
AID1328820Oral bioavailability in rat2016Bioorganic & 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.
AID640073Agonist activity at PPAR-gamma by cell-based assay2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1154886Oral bioavailability in rat at 2 mg/kg2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Optimization of GPR40 Agonists for Type 2 Diabetes.
AID1734905Drug 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 analysis2016Journal 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).
AID1734870Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method2016Journal 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).
AID1271404Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Discovery of the imidazole-derived GPR40 agonist AM-3189.
AID1734879Agonist 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 assay2016Journal 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).
AID1154881Agonist activity at human GPR40 expressed in CHO cells by aequorin assay2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Optimization of GPR40 Agonists for Type 2 Diabetes.
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.
AID1328821Oral bioavailability in dog2016Bioorganic & 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.
AID1734875Agonist 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 assay2016Journal 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).
AID1154883Clearance in rat at 0.5 mg/kg, iv2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Optimization of GPR40 Agonists for Type 2 Diabetes.
AID1422548Agonist activity at FFA1 (unknown origin)2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
AID1734899Protein binding in plasma (unknown origin) by equilibrium dialysis method2016Journal 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).
AID640076Antidiabetic 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 test2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID748342Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay relative to AM-16382013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID1734909Protein binding in C57BL/6 mouse plasma at 3 microg/kg, iv by LC-MS/MS analysis2016Journal 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).
AID1154885Volume of distribution at steady state in rat2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Optimization of GPR40 Agonists for Type 2 Diabetes.
AID1734906Drug 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 analysis2016Journal 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).
AID640174Antidiabetic 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 test2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID620370Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry2011Journal 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.
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.
AID640083Half life in Beagle dog at 0.5 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1308065Agonist 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-7702016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer.
AID1734900Displacement 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 analysis2016Journal 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).
AID1328813Clearance in iv or po dosed dog2016Bioorganic & 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.
AID1734901Displacement 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 analysis2016Journal 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).
AID640078Clearance in rat at 0.5 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID640081Half life in mouse at 0.8 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1271430Induction of insulin release in human pancreatic islets2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Discovery of the imidazole-derived GPR40 agonist AM-3189.
AID1734883Agonist activity at GPR40 in mouse MIN6 cells assessed as induction of glucose-mediated insulin secretion incubated for 2 hrs by ELISA2016Journal 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).
AID1328818Half life in iv or po dosed monkey2016Bioorganic & 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.
AID1271406Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Discovery of the imidazole-derived GPR40 agonist AM-3189.
AID640168AUC in Beagle dog at 2 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1308067Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer.
AID640091Oral bioavailability in Beagle dog at 2 mg/kg2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1734878Agonist 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 control2016Journal 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).
AID640085Volume of distribution at steady state in mouse at 0.8 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1328819Oral bioavailability in mouse2016Bioorganic & 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.
AID640072Agonist activity at PPAR-delta by cell-based assay2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID640173Cmax in cynomolgus monkey at 0.5 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID640170Cmax in mouse at 5 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1324909Agonist activity at FFA1 receptor (unknown origin)2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Free fatty acid receptor 1 (GPR40) agonists containing spirocyclic periphery inspired by LY2881835.
AID640086Volume of distribution at steady state in rat at 0.5 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1734873Agonist 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 assa2016Journal 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).
AID1308063Displacement 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-2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer.
AID640066Agonist activity at mouse GPR402012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
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.
AID1734871Agonist 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 assay2016Journal 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).
AID1271405Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Discovery of the imidazole-derived GPR40 agonist AM-3189.
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.
AID640065Agonist activity at rat GPR402012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1734877Agonist 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 assay2016Journal 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).
AID1308064Agonist 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 assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer.
AID1328822Oral bioavailability in monkey2016Bioorganic & 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.
AID1154884Mean residence time in rat2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Optimization of GPR40 Agonists for Type 2 Diabetes.
AID1734876Agonist 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 control2016Journal 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).
AID1328812Clearance in iv or po dosed rat2016Bioorganic & 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.
AID640074Inhibition of alpha2 adrenergic receptor2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID640166AUC in mouse at 5 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1734872Agonist 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 acid2016Journal 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).
AID1734902Displacement 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 analysis2016Journal 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).
AID640090Oral bioavailability in rat at 0.5 mg/kg2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1154882Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Optimization of GPR40 Agonists for Type 2 Diabetes.
AID748325Binding affinity to human FFA1 receptor expressed in CHO cell membranes assessed as inhibition of specific binding of [3H]AMG 8372013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
AID640088Volume of distribution at steady state in cynomolgus monkey at 0.5 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID640087Volume of distribution at steady state in Beagle dog at 0.5 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID692591Partial agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay2012ACS medicinal chemistry letters, Sep-13, Volume: 3, Issue:9
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
AID640079Clearance in Beagle dog at 0.5 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 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.
AID1308068Agonist 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-7702016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer.
AID640084Half life in cynomolgus monkey at 0.5 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID640070Agonist activity at GPR432012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID640089Oral bioavailability in mouse at 5 mg/kg2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID640172Cmax in Beagle dog at 2 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
AMG 837: a potent, orally bioavailable GPR40 agonist.
AID1805801Various Assay from Article 10.1021/acs.jmedchem.1c00409: \\Perspectives on SARS-CoV-2 Main Protease Inhibitors.\\2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Perspectives on SARS-CoV-2 Main Protease Inhibitors.
AID1345809Human FFA1 receptor (Free fatty acid receptors)2012Molecular 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]

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's20 (83.33)24.3611
2020's4 (16.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.94

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 Index18.94 (24.57)
Research Supply Index3.22 (2.92)
Research Growth Index4.52 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.94)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (8.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other22 (91.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]