tak-875 profile

ID Source	ID
PubMed CID	24857286
CHEMBL ID	1829174
CHEBI ID	177451
SCHEMBL ID	204652
MeSH ID	M0556616

Synonym
HY-10480
3-benzofuranacetic acid, 6-[[2',6'-dimethyl-4'-[3-(methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]methoxy]-2,3-dihydro-, (3s)-
fasiglifam
1000413-72-8
2-[(3s)-6-[[3-[2,6-dimethyl-4-(3-methylsulonylpropoxy)phenyl]phenyl]methoxy]-2,3-dihydro-1-benzouran-3-yl]acetic acid
CHEBI:177451
tak-875 anhydrous
tak875
CHEMBL1829174 ,
fasiglifam hydrate
tak-875 ,
bdbm50386790
unii-glp1w4jxah
glp1w4jxah ,
fasiglifam [usan:inn]
((3s)-6-((3-(4-(3-methanesulfonylpropoxy)-2,6-dimethylphenyl]phenyl}methoxy)-2,3-dihydro-1-benzofuran-3-yl)acetic acid
tak 875
D10336
fasiglifam (usan/inn)
NCGC00346669-01
CS-0282
[(3s)-6-({3-[4-(3-methanesulfonylpropoxy)-2,6-dimethylphenyl]phenyl}methoxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid
(3s)-6-[[2',6'-dimethyl-4'-[3-(methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]methoxy]-2,3-dihydro-3-benzofuranacetic acid
2-[(3s)-6-({3-[4-(3-methanesulfonylpropoxy)-2,6-dimethylphenyl]phenyl}methoxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid
gtpl6484
fasiglifam [usan]
3-benzofuranacetic acid, 6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)(1,1'-biphenyl)-3-yl)methoxy)-2,3-dihydro-, (3s)-
((3s)-6-(((2',6'-dimethyl-4'-(3-(methanesulfonyl)propoxy)-(1,1'-biphenyl)-3-yl))methoxy)-2,3-dihydro-1-benzofuran-3-yl)acetic acid
fasiglifam [inn]
fasiglifam [who-dd]
BZCALJIHZVNMGJ-HSZRJFAPSA-N
SCHEMBL204652
J-501277
[(3s)-6-({2',6'-dimethyl-4'-[3-(methylsulfonyl)propoxy]biphenyl-3-yl}methoxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid
2yb ,
AKOS025289552
(s)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)-[1,1'-biphenyl]-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid
AC-25651
4PHU
EX-A203
mfcd18251445
tak-875(fasiglifam)
DB12491
Q27077287
BCP02430
AMY24164
MS-29716
2-[(3s)-6-[[3-[2,6-dimethyl-4-(3-methylsulfonylpropoxy)phenyl]phenyl]methoxy]-2,3-dihydro-1-benzofuran-3-yl]acetic acid
A25526
DTXSID601025726

Excerpt	Reference	Relevance
" Clinical adverse experiences were generally mild and transient."	( Safety, tolerability, pharmacokinetics, and pharmacodynamic properties of the GPR40 agonist TAK-875: results from a double-blind, placebo-controlled single oral dose rising study in healthy volunteers. Dote, N; Higuchi, T; Leifke, E; Naik, H; Vakilynejad, M; Viswanathan, P; Wu, J, 2012)	0.6
" The incidence and types of treatment-emergent adverse events in each fasiglifam group were similar to those in the placebo group, and hypoglycaemia was reported in 1 patient receiving fasiglifam 50 mg."	( Efficacy and safety of fasiglifam (TAK-875), a G protein-coupled receptor 40 agonist, in Japanese patients with type 2 diabetes inadequately controlled by diet and exercise: a randomized, double-blind, placebo-controlled, phase III trial. Enya, K; Kaku, K; Matsuno, R; Nakaya, R; Ohira, T, 2015)	0.69
" The overall incidence of treatment-emergent adverse events (TEAEs) was 75."	( Long-term safety and efficacy of fasiglifam (TAK-875), a G-protein-coupled receptor 40 agonist, as monotherapy and combination therapy in Japanese patients with type 2 diabetes: a 52-week open-label phase III study. Enya, K; Kaku, K; Matsuno, R; Nakaya, R; Ohira, T, 2016)	0.69
" A Liver Safety Evaluation Committee consisting of hepatologists blinded to treatment assignments evaluated hepatic adverse events (AEs) and serious AEs (SAEs) for causal relationship to study drug."	( Liver Safety of Fasiglifam (TAK-875) in Patients with Type 2 Diabetes: Review of the Global Clinical Trial Experience. Marcinak, JF; Munsaka, MS; Ohira, T; Smith, N; Watkins, PB, 2018)	0.77
" The primary outcome was the time to first occurrence of any component of the major adverse CV event composite of CV death, nonfatal myocardial infarction, nonfatal stroke, and hospitalization for unstable angina."	( Fasiglifam-Induced Liver Injury in Patients With Type 2 Diabetes: Results of a Randomized Controlled Cardiovascular Outcomes Safety Trial. Cao, C; Jasper, S; Lincoff, AM; Lopez, C; Marcinak, J; McGuire, DK; Mehta, CR; Menon, V; Nicholls, SJ; Nissen, SE; Rosenstock, J; Wolski, K, 2018)	0.48
" Liver safety had been pre-identified as a concern, and within the phase 3 trials, was measured through (1) adverse event reporting, (2) central predefined liver monitoring schedule with various thresholds for potential drug-induced liver injury, and (3) blinded adjudication of serious liver toxicity by a panel of experts in drug-induced liver injury."	( Determination of fasiglifam-induced liver toxicity: Insights from the data monitoring committee of the fasiglifam clinical trials program. DeLeve, L; Eckel, RH; Granger, CB; Gu, X; Holmes, D; Home, P; Neaton, J; Sharma, A; Shavadia, JS; Watkins, PB, 2019)	0.51
" No concerning trends were noted in adverse or serious adverse event frequency, suspected unexpected serious adverse reaction, alanine or aspartate transaminase elevations, or hepatobiliary or gastrointestinal adverse events as reported by local site investigators."	( Determination of fasiglifam-induced liver toxicity: Insights from the data monitoring committee of the fasiglifam clinical trials program. DeLeve, L; Eckel, RH; Granger, CB; Gu, X; Holmes, D; Home, P; Neaton, J; Sharma, A; Shavadia, JS; Watkins, PB, 2019)	0.51
"In spite of clear liver toxicity detected with a systematic surveillance program, liver safety signals were not identified from investigator adverse event reporting alone."	( Determination of fasiglifam-induced liver toxicity: Insights from the data monitoring committee of the fasiglifam clinical trials program. DeLeve, L; Eckel, RH; Granger, CB; Gu, X; Holmes, D; Home, P; Neaton, J; Sharma, A; Shavadia, JS; Watkins, PB, 2019)	0.51
" In contrast to TAK-875, which was metabolized through toxic glucuronidation, CPL207280 was metabolized mainly through oxidation."	( Evaluation of the hepatotoxicity of the novel GPR40 (FFAR1) agonist CPL207280 in the rat and monkey. Bazydlo-Guzenda, K; Buda, P; Dominowski, J; Drzazga, E; Gad, SC; Janiszewski, M; Kozlowska, I; Mach, M; Pieczykolan, J; Wieczorek, M; Ziolkowski, H, 2021)	0.97

Excerpt	Reference	Relevance
" TAK-875 was well tolerated in the study and has pharmacokinetic characteristics suitable for a once-daily regimen."	( Safety, tolerability, pharmacokinetics, and pharmacodynamic properties of the GPR40 agonist TAK-875: results from a double-blind, placebo-controlled single oral dose rising study in healthy volunteers. Dote, N; Higuchi, T; Leifke, E; Naik, H; Vakilynejad, M; Viswanathan, P; Wu, J, 2012)	1.51
" Study endpoints were pharmacokinetic and safety variables."	( Evaluation of the pharmacokinetics and safety of a single oral dose of fasiglifam in subjects with normal or varying degrees of impaired renal function. Marcinak, J; Mayer, M; Nudurupati, S; Peng, X, 2014)	0.4
" Blood samples were collected through 336 h post-dose for pharmacokinetic evaluation."	( Evaluation of the Pharmacokinetics and Safety of a Single Oral Dose of Fasiglifam in Subjects with Mild or Moderate Hepatic Impairment. Kogame, A; Marcinak, J; Tagawa, Y; Vakilynejad, M, 2018)	0.48
" Further evaluation of pharmacokinetic (PK) profiles and in vivo efficacy identified compound 40a with excellent PK properties and significant glucose-lowering efficacy during an oral glucose tolerance test."	( Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles. Chen, Q; Guo, B; Guo, S; Huang, J; Li, J; Xie, X; Yang, Y; Zhou, X, 2018)	0.48
" Herein, in order to further evaluate the druglikeness of TAK-875 sulfoxide analogs, the pharmacokinetic properties of compounds 2, 3, and 4 in rats were investigated and compared with that of TAK-875."	( In vivo pharmacokinetic study and oral glucose tolerance test of sulfoxide analogs of GPR40 agonist TAK-875. Dong, H; Xu, Q; Xu, W; Yan, Y; Zhang, Y; Zhao, C, 2020)	1.02

Excerpt	Reference	Relevance
" In vitro and in vivo samples were analyzed by the developed ultrahigh-performance liquid chromatography combined with Q-Exactive Orbitrap tandem mass spectrometry."	( In vitro and in vivo metabolic profiles of fasiglifam using ultrahigh-performance liquid chromatography combined with Q-Exactive Orbitrap tandem mass spectrometry. He, D; Li, J; Li, JQ; She, SY; Wang, JF; Yong, RS; Zhang, SH, 2018)	0.48

Excerpt	Reference	Relevance
" In this study, we present the first clinical data for TAK-875, a novel highly selective, orally bioavailable GPR40 agonist, in Japanese patients with type 2 diabetes insufficiently controlled by diet or exercise therapy."	( GPR40-induced insulin secretion by the novel agonist TAK-875: first clinical findings in patients with type 2 diabetes. Araki, T; Hirayama, M; Hiroi, S; Kaku, K, 2012)	0.88
" A series of novel orally bioavailable GPR40 agonists was discovered."	( Discovery of novel orally bioavailable GPR40 agonists. Dong, Q; Fei, H; Feng, J; Hu, Q; Lu, H; Sun, P; Yang, F; Yuan, J; Zhang, L; Zheng, S, 2013)	0.39
" Further optimization led to the discovery of dihydrobenzofuran derivative 9a ([(3S)-6-({2',6'-dimethyl-4'-[3-(methylsulfonyl)propoxy]biphenyl-3-yl}methoxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid hemi-hydrate, TAK-875) as a potent, selective, and orally bioavailable GPR40 agonist, with a pharmacokinetic profile enabling long-acting drug efficacy."	( Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist. Funami, M; Harada, A; Ito, M; Ito, R; Kanzaki, N; Kogame, A; Matsunaga, S; Mikami, S; Miyazaki, J; Momose, Y; Negoro, N; Odani, T; Santou, T; Sasaki, S; Suzuki, M; Suzuki, N; Takeuchi, K; Tanaka, T; Tsujihata, Y; Yasuma, T, 2010)	0.92
" All of these efforts led to the identification of compound 11 as a potent and orally bioavailable FFA1 agonist without the risk of hypoglycemia."	( Discovery of novel pyrrole-based scaffold as potent and orally bioavailable free fatty acid receptor 1 agonists for the treatment of type 2 diabetes. Cai, X; Dai, Y; Fu, M; Huang, W; Li, Z; Pan, M; Qian, H; Shi, W; Su, X, 2016)	0.43
" In this study, we hybrid FFA1 agonist AM-4668 with PPARδ agonist GW501516, leading to the identification of orally bioavailable dual agonist 32, which revealed high selectivity over other PPARs."	( Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agents. Chen, Y; Deng, L; Hu, L; Li, Z; Liu, B; Xu, Y; Zhang, L; Zhou, Z, 2019)	0.51
"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

Excerpt	Relevance	Reference
"5%) simulated individuals developed alanine aminotransferase (ALT) elevations, an incidence similar to that observed with 200 mg daily dosing in clinical trials."	( Quantitative Systems Toxicology Analysis of In Vitro Mechanistic Assays Reveals Importance of Bile Acid Accumulation and Mitochondrial Dysfunction in TAK-875-Induced Liver Injury. Dragan, YP; Herédi-Szabó, K; Howell, BA; Longo, DM; Mogyorósi, K; Mosedale, M; Siler, SQ; Walker, P; Watkins, PB; Wolenski, FS; Woodhead, JL, 2019)	0.71
" 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

Class	Description
biphenyls	Benzenoid aromatic compounds containing two phenyl or substituted-phenyl groups which are joined together by a single bond.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Fumarate hydratase	Homo sapiens (human)	Potency	37.2212	0.0030	8.7949	48.0869	AID1347053
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	11.9877	0.0123	7.9835	43.2770	AID1645841
EWS/FLI fusion protein	Homo sapiens (human)	Potency	20.9310	0.0013	10.1577	42.8575	AID1259253; AID1259255
G	Vesicular stomatitis virus	Potency	21.3174	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2D6	Homo sapiens (human)	Potency	23.9185	0.0010	8.3798	61.1304	AID1645840
polyprotein	Zika virus	Potency	37.2212	0.0030	8.7949	48.0869	AID1347053
Interferon beta	Homo sapiens (human)	Potency	21.3174	0.0033	9.1582	39.8107	AID1645842
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	21.3174	0.0123	8.9648	39.8107	AID1645842
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	21.3174	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	21.3174	0.0123	8.9648	39.8107	AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Free fatty acid receptor 1	Homo sapiens (human)	Ki	0.0183	0.0022	0.0508	0.2188	AID1308063; AID1734870
Sodium/bile acid cotransporter	Homo sapiens (human)	IC50 (µMol)	2.0000	1.0000	5.9267	9.6000	AID1600826
Canalicular multispecific organic anion transporter 1	Homo sapiens (human)	IC50 (µMol)	2.4100	2.4100	6.3433	10.0000	AID1418809
Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)	IC50 (µMol)	11.2000	0.1047	2.7195	7.0795	AID1418811
Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)	IC50 (µMol)	2.2800	0.0500	2.3797	9.7000	AID1418810
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Free fatty acid receptor 1	Homo sapiens (human)	EC50 (µMol)	0.2318	0.0003	0.7369	8.8000	AID1175641; AID1248437; AID1254056; AID1288423; AID1297630; AID1308064; AID1308067; AID1326120; AID1349597; AID1367361; AID1388773; AID1398987; AID1399212; AID1418782; AID1420968; AID1422535; AID1422548; AID1443215; AID1556955; AID1586862; AID1623598; AID1624318; AID1663987; AID1724377; AID1734871; AID1734873; AID1734879; AID1846355; AID1899745; AID620370; AID669982
Free fatty acid receptor 1	Homo sapiens (human)	Kd	0.0082	0.0019	0.0058	0.0119	AID1724380; AID1734881
Cytochrome P450 2D6	Homo sapiens (human)	EC50 (µMol)	0.0019	0.0002	0.8276	4.4400	AID1326120
Free fatty acid receptor 4	Homo sapiens (human)	EC50 (µMol)	10.0000	0.0437	2.3547	7.5858	AID1367360
Free fatty acid receptor 1	Mus musculus (house mouse)	EC50 (µMol)	0.0086	0.0015	0.0105	0.0190	AID1734875
Free fatty acid receptor 1	Rattus norvegicus (Norway rat)	EC50 (µMol)	9.0250	0.0032	0.0353	0.0990	AID1326129; AID1586864; AID1734877
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
phospholipase C-activating G protein-coupled receptor signaling pathway	Free fatty acid receptor 1	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Free fatty acid receptor 1	Homo sapiens (human)
insulin secretion	Free fatty acid receptor 1	Homo sapiens (human)
negative regulation of interleukin-1 beta production	Free fatty acid receptor 1	Homo sapiens (human)
glucose homeostasis	Free fatty acid receptor 1	Homo sapiens (human)
positive regulation of calcium ion transport	Free fatty acid receptor 1	Homo sapiens (human)
response to fatty acid	Free fatty acid receptor 1	Homo sapiens (human)
ion channel modulating, G protein-coupled receptor signaling pathway	Free fatty acid receptor 1	Homo sapiens (human)
ligand-gated ion channel signaling pathway	Free fatty acid receptor 1	Homo sapiens (human)
positive regulation of insulin secretion	Free fatty acid receptor 1	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Free fatty acid receptor 1	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell activation involved in immune response	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to virus	Interferon beta	Homo sapiens (human)
positive regulation of autophagy	Interferon beta	Homo sapiens (human)
cytokine-mediated signaling pathway	Interferon beta	Homo sapiens (human)
natural killer cell activation	Interferon beta	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT protein	Interferon beta	Homo sapiens (human)
cellular response to interferon-beta	Interferon beta	Homo sapiens (human)
B cell proliferation	Interferon beta	Homo sapiens (human)
negative regulation of viral genome replication	Interferon beta	Homo sapiens (human)
innate immune response	Interferon beta	Homo sapiens (human)
positive regulation of innate immune response	Interferon beta	Homo sapiens (human)
regulation of MHC class I biosynthetic process	Interferon beta	Homo sapiens (human)
negative regulation of T cell differentiation	Interferon beta	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Interferon beta	Homo sapiens (human)
defense response to virus	Interferon beta	Homo sapiens (human)
type I interferon-mediated signaling pathway	Interferon beta	Homo sapiens (human)
neuron cellular homeostasis	Interferon beta	Homo sapiens (human)
cellular response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
cellular response to virus	Interferon beta	Homo sapiens (human)
negative regulation of Lewy body formation	Interferon beta	Homo sapiens (human)
negative regulation of T-helper 2 cell cytokine production	Interferon beta	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell differentiation	Interferon beta	Homo sapiens (human)
natural killer cell activation involved in immune response	Interferon beta	Homo sapiens (human)
adaptive immune response	Interferon beta	Homo sapiens (human)
T cell activation involved in immune response	Interferon beta	Homo sapiens (human)
humoral immune response	Interferon beta	Homo sapiens (human)
positive regulation of T cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
adaptive immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independent	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of T cell anergy	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
defense response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
detection of bacterium	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-12 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-6 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protection from natural killer cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
innate immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of dendritic cell differentiation	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class Ib	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
coumarin metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
isoquinoline alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of cellular organofluorine metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
arachidonic acid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
sodium ion transport	Sodium/bile acid cotransporter	Homo sapiens (human)
response to organic cyclic compound	Sodium/bile acid cotransporter	Homo sapiens (human)
bile acid and bile salt transport	Sodium/bile acid cotransporter	Homo sapiens (human)
response to nutrient levels	Sodium/bile acid cotransporter	Homo sapiens (human)
bile acid signaling pathway	Sodium/bile acid cotransporter	Homo sapiens (human)
response to estrogen	Sodium/bile acid cotransporter	Homo sapiens (human)
response to ethanol	Sodium/bile acid cotransporter	Homo sapiens (human)
symbiont entry into host cell	Sodium/bile acid cotransporter	Homo sapiens (human)
transmembrane transport	Sodium/bile acid cotransporter	Homo sapiens (human)
cellular response to xenobiotic stimulus	Sodium/bile acid cotransporter	Homo sapiens (human)
regulation of bile acid secretion	Sodium/bile acid cotransporter	Homo sapiens (human)
negative regulation of cytokine production	Free fatty acid receptor 4	Homo sapiens (human)
inflammatory response	Free fatty acid receptor 4	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Free fatty acid receptor 4	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Free fatty acid receptor 4	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Free fatty acid receptor 4	Homo sapiens (human)
regulation of glucose transmembrane transport	Free fatty acid receptor 4	Homo sapiens (human)
negative regulation of interleukin-1 beta production	Free fatty acid receptor 4	Homo sapiens (human)
ghrelin secretion	Free fatty acid receptor 4	Homo sapiens (human)
negative regulation of apoptotic process	Free fatty acid receptor 4	Homo sapiens (human)
positive regulation of osteoblast differentiation	Free fatty acid receptor 4	Homo sapiens (human)
negative regulation of inflammatory response	Free fatty acid receptor 4	Homo sapiens (human)
white fat cell differentiation	Free fatty acid receptor 4	Homo sapiens (human)
brown fat cell differentiation	Free fatty acid receptor 4	Homo sapiens (human)
detection of chemical stimulus involved in sensory perception of taste	Free fatty acid receptor 4	Homo sapiens (human)
positive regulation of glucagon secretion	Free fatty acid receptor 4	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Free fatty acid receptor 4	Homo sapiens (human)
negative regulation of somatostatin secretion	Free fatty acid receptor 4	Homo sapiens (human)
positive regulation of brown fat cell differentiation	Free fatty acid receptor 4	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	Free fatty acid receptor 4	Homo sapiens (human)
cellular response to hormone stimulus	Free fatty acid receptor 4	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Free fatty acid receptor 4	Homo sapiens (human)
hormone secretion	Free fatty acid receptor 4	Homo sapiens (human)
inositol phosphate metabolic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
negative regulation of cold-induced thermogenesis	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
xenobiotic metabolic process	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
negative regulation of gene expression	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bile acid and bile salt transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bilirubin transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
heme catabolic process	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic export from cell	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transepithelial transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
leukotriene transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
monoatomic anion transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transport across blood-brain barrier	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic metabolic process	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
monoatomic ion transport	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
organic anion transport	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
bile acid and bile salt transport	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
heme catabolic process	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
sodium-independent organic anion transport	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
transmembrane transport	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
xenobiotic metabolic process	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
monoatomic ion transport	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
organic anion transport	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
bile acid and bile salt transport	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
prostaglandin transport	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
heme catabolic process	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
sodium-independent organic anion transport	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
transmembrane transport	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
thyroid hormone transport	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
G protein-coupled receptor activity	Free fatty acid receptor 1	Homo sapiens (human)
lipid binding	Free fatty acid receptor 1	Homo sapiens (human)
bioactive lipid receptor activity	Free fatty acid receptor 1	Homo sapiens (human)
cytokine activity	Interferon beta	Homo sapiens (human)
cytokine receptor binding	Interferon beta	Homo sapiens (human)
type I interferon receptor binding	Interferon beta	Homo sapiens (human)
protein binding	Interferon beta	Homo sapiens (human)
chloramphenicol O-acetyltransferase activity	Interferon beta	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
signaling receptor binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
peptide antigen binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein-folding chaperone binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2D6	Homo sapiens (human)
iron ion binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2D6	Homo 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 oxygen	Cytochrome P450 2D6	Homo sapiens (human)
heme binding	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
virus receptor activity	Sodium/bile acid cotransporter	Homo sapiens (human)
protein binding	Sodium/bile acid cotransporter	Homo sapiens (human)
bile acid:sodium symporter activity	Sodium/bile acid cotransporter	Homo sapiens (human)
G protein-coupled receptor activity	Free fatty acid receptor 4	Homo sapiens (human)
fatty acid binding	Free fatty acid receptor 4	Homo sapiens (human)
taste receptor activity	Free fatty acid receptor 4	Homo sapiens (human)
peptide binding	Free fatty acid receptor 4	Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol heptakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
protein binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
ATP binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 1-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 3-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
protein binding	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATP binding	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
organic anion transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bilirubin transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATP hydrolysis activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
serine-type endopeptidase inhibitor activity	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
bile acid transmembrane transporter activity	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activity	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
bile acid transmembrane transporter activity	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activity	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
thyroid hormone transmembrane transporter activity	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Free fatty acid receptor 1	Homo sapiens (human)
plasma membrane	Free fatty acid receptor 1	Homo sapiens (human)
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
Golgi membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
endoplasmic reticulum	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
Golgi apparatus	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
cell surface	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
ER to Golgi transport vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
secretory granule membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
phagocytic vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
early endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
recycling endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular exosome	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
lumenal side of endoplasmic reticulum membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
MHC class I protein complex	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular space	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
external side of plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
mitochondrion	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2D6	Homo sapiens (human)
cytoplasm	Cytochrome P450 2D6	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2D6	Homo sapiens (human)
plasma membrane	Sodium/bile acid cotransporter	Homo sapiens (human)
basolateral plasma membrane	Sodium/bile acid cotransporter	Homo sapiens (human)
lysosomal membrane	Free fatty acid receptor 4	Homo sapiens (human)
plasma membrane	Free fatty acid receptor 4	Homo sapiens (human)
cilium	Free fatty acid receptor 4	Homo sapiens (human)
endosome membrane	Free fatty acid receptor 4	Homo sapiens (human)
endocytic vesicle	Free fatty acid receptor 4	Homo sapiens (human)
ciliary membrane	Free fatty acid receptor 4	Homo sapiens (human)
plasma membrane	Free fatty acid receptor 4	Homo sapiens (human)
fibrillar center	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytosol	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleus	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
cell surface	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
apical plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
intercellular canaliculus	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
apical plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
plasma membrane	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
basal plasma membrane	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
basolateral plasma membrane	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
plasma membrane	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
basal plasma membrane	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
membrane	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
basolateral plasma membrane	Solute carrier organic anion transporter family member 1B1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (236)

Assay ID	Title	Year	Journal	Article
AID1624334	Antidiabetic activity in ICR mouse assessed as reduction in blood glucose AUC (0 to 120) at 10 mg/kg, po treated 30 mins prior to glucose challenge by OGTT	2019	Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6	Synthesis and biological evaluation of novel potent FFA1 agonists containing 2,3-dihydrobenzo[b][1,4]dioxine.
AID1248438	Lipophilicity, logD of the compound at pH 7.4 by shake flask method	2015	Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20	Design, synthesis and structure-activity relationship studies of novel phenoxyacetamide-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID1663989	Glucose lowering activity in normoglycemic ICR mouse assessed as reduction in AUC(0 to 120 mins) of plasma glucose at 30 mg/kg, po administered 30 mins prior to glucose challenge by OGTT	2020	Bioorganic & medicinal chemistry, 07-01, Volume: 28, Issue:13	Discovery of novel potent GPR40 agonists containing imidazo[1,2-a]pyridine core as antidiabetic agents.
AID1422546	Hypoglycemic activity in ob/ob mouse assessed as decrease in blood glucose AUC (0 to 120 mins) at 40 mg/kg, po bid administered via gavage 30 mins prior to glucose load by OGTT relative to control	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
AID1630828	Hypoglycemic effect in fasting STZ-induced type-2 diabetic C57BL/6 mouse assessed as decrease in blood glucose AUC (0 to 2 hrs) at 20 mg/kg, po administered as single dose 30 mins prior to glucose challenge measured by OGTT relative to control	2016	Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21	Discovery of novel free fatty acid receptor 1 agonists bearing triazole core via click chemistry.
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.
AID1443215	Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay	2017	Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7	Discovery of Potent and Orally Bioavailable GPR40 Full Agonists Bearing Thiophen-2-ylpropanoic Acid Scaffold.
AID1443214	Agonist activity at human GPR40 expressed in HEK293T cells transfected with 5 ug of GPR40 expression plasmid assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay	2017	Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7	Discovery of Potent and Orally Bioavailable GPR40 Full Agonists Bearing Thiophen-2-ylpropanoic Acid Scaffold.
AID1623611	Antidiabetic activity in ob/ob mouse assessed as reduction in blood glucose AUC (0 to 120 mins) at 40 mg/kg, po administered as single dose pretreated for 30 mins followed by glucose-challenge by glucometric analysis relative to control	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agents.
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).
AID1418783	Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay relative to linoleic acid	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.
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.
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).
AID1399223	Antidiabetic activity in ICR mouse assessed as blood glucose levels at 50 mg/kg, po administered 1 hr prior to glucose challenge measured at 120 mins post glucose challenge (Rvb = 53.7 +/- 9.9 mg/dl)	2018	Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18	Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings.
AID1420979	Antidiabetic activity in C57BL/6 mouse assessed as decrease in plasma glucose AUC at 3 mg/kg, po pretreated for 60 mins followed by glucose addition measured after 15 to 60 mins by OGTT relative to control	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Design, synthesis, and biological evaluations of phenylpropiolic acid derivatives as novel GPR40 agonists.
AID1624318	Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay	2019	Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6	Synthesis and biological evaluation of novel potent FFA1 agonists containing 2,3-dihydrobenzo[b][1,4]dioxine.
AID1399225	Antidiabetic activity in ICR mouse assessed as blood glucose AUC at 50 mg/kg, po administered 1 hr prior to glucose challenge measured after 120 mins post glucose challenge (Rvb = 290 +/ 23.5 mg.hr/dl)	2018	Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18	Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings.
AID1420974	Agonist activity at GPR40 in mouse MIN6 cells assessed as increase in glucose-stimulated insulin secretion at 10 uM measured after 2 hrs by ELISA relative to control	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Design, synthesis, and biological evaluations of phenylpropiolic acid derivatives as novel GPR40 agonists.
AID1418795	Cmax in Sprague-Dawley rat at 10 mg/kg, po by LC-ESI-MS analysis	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.
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.
AID1418811	Inhibition of human OATP1B3	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.
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).
AID1388773	Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay	2018	Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3	Identification of highly potent and orally available free fatty acid receptor 1 agonists bearing isoxazole scaffold.
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.
AID1630824	Agonist activity at human FFA1 receptor expressed in CHO cells assessed as intracellular calcium influx at 100 nM measured for 90 sec by Fluo-4-AM dye based FLIPR assay relative to control	2016	Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21	Discovery of novel free fatty acid receptor 1 agonists bearing triazole core via click chemistry.
AID1367361	Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay	2017	Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24	Improving metabolic stability with deuterium: The discovery of GPU-028, a potent free fatty acid receptor 4 agonists.
AID1556968	Antidiabetic activity in HFD fed/STZ-treated C57BL/6 mouse assessed as decrease in blood glucose at 20 mg/kg, po pretreated for 30 mins followed by glucose challenge and measured after up to 120 mins by OGTT	2019	European journal of medicinal chemistry, Oct-01, Volume: 179	Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.
AID1422544	Hypoglycemic activity in ob/ob mouse assessed as decrease in blood glucose AUC (0 to 120 mins) at 40 mg/kg, po bid administered via gavage for 5 days starting at 30 mins prior to glucose load by OGTT relative to control	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
AID1443212	Agonist activity at human GPR40 expressed in HEK293T cells transfected with 0.05 ug of GPR40 expression plasmid assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay	2017	Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7	Discovery of Potent and Orally Bioavailable GPR40 Full Agonists Bearing Thiophen-2-ylpropanoic Acid Scaffold.
AID1556961	AUC (0 to 24 hrs) in Sprague-Dawley rat at 10 mg/kg, po measured for 0.5 to 24 mins by LC-MS/MS analysis	2019	European journal of medicinal chemistry, Oct-01, Volume: 179	Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.
AID669982	Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA	2012	Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8	Optimization of (2,3-dihydro-1-benzofuran-3-yl)acetic acids: discovery of a non-free fatty acid-like, highly bioavailable G protein-coupled receptor 40/free fatty acid receptor 1 agonist as a glucose-dependent insulinotropic agent.
AID1556956	Lipophilicity, logD of compound in 1-octanol and PBS mixture in pH 7.4 at 100 uM incubated for 24 under shaking condition by HPLC analysis	2019	European journal of medicinal chemistry, Oct-01, Volume: 179	Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.
AID1418810	Inhibition of human OATP1BA	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.
AID1288105	Antihyperglycemic activity in overnight fasted STZ-induced type 2 dibetic C57BL/6 mouse assessed as decrease in blood glucose level at 20 mg/kg, po administered 30 mins prior to glucose challenge measured after 15 to 120 mins by OGTT method	2016	European journal of medicinal chemistry, May-04, Volume: 113	Design, synthesis and Structure-activity relationship studies of new thiazole-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID1288107	Hepatotoxicity in ICR mouse assessed as alanine aminotransferase levels in serum at 20 mg/kg qd administered through oral gavage for 30 days (Rvb = 35 +/- 4.3 IU/L)	2016	European journal of medicinal chemistry, May-04, Volume: 113	Design, synthesis and Structure-activity relationship studies of new thiazole-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID1443194	Inhibition of hepatobiliary transporter in Sprague-Dawley rat sandwich-cultured rat hepatocytes assessed as decrease in d8-TCA by measuring biliary excretion index at 1 to 25 uM incubated for 15 mins followed by d8-TCA addition measured after 15 mins by L	2017	Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7	Discovery of Potent and Orally Bioavailable GPR40 Full Agonists Bearing Thiophen-2-ylpropanoic Acid Scaffold.
AID1420970	Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs in presence of GPR40 antagonist GW-100 by calcium-5 dye based assay	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Design, synthesis, and biological evaluations of phenylpropiolic acid derivatives as novel GPR40 agonists.
AID1297630	Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay	2016	European journal of medicinal chemistry, Jun-30, Volume: 116	Synthesis and biological evaluation of GPR40/FFAR1 agonists containing 3,5-dimethylisoxazole.
AID1254056	Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay	2015	Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22	Design, synthesis and biological activity of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.
AID1388778	Cmax in fasted Sprague-Dawley rat at 3 mg/kg, po administered as single dose by LC-PDA-MS/MS analysis	2018	Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3	Identification of highly potent and orally available free fatty acid receptor 1 agonists bearing isoxazole scaffold.
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).
AID1422543	Hypoglycemic activity in ICR mouse assessed as decrease in blood glucose AUC (0 to 120 mins) at 20 mg/kg, po administered 30 mins prior to glucose load by OGTT relative to control	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
AID1288422	Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level at 100 nM measured for 90 secs by Fluo-4 AM-based FLIPR assay	2016	Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9	Discovery of novel pyrrole-based scaffold as potent and orally bioavailable free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID1349597	Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay	2017	ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12	SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists.
AID1624333	Antidiabetic activity in ICR mouse assessed as reduction in blood glucose excursion at 10 mg/kg, po treated 30 mins prior to glucose challenge and measured up to 120 mins by OGTT	2019	Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6	Synthesis and biological evaluation of novel potent FFA1 agonists containing 2,3-dihydrobenzo[b][1,4]dioxine.
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.
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).
AID1388780	Half life in fasted Sprague-Dawley rat at 3 mg/kg, po administered as single dose by LC-PDA-MS/MS analysis	2018	Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3	Identification of highly potent and orally available free fatty acid receptor 1 agonists bearing isoxazole scaffold.
AID1420981	Antidiabetic activity in patient with type-2 diabetes assessed as reduction in glycated hemoglobin level at 50 mg, po administered once daily for 24 weeks relative to control	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Design, synthesis, and biological evaluations of phenylpropiolic acid derivatives as novel GPR40 agonists.
AID1248436	Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx at 100 nM incubated for by FLIPR method	2015	Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20	Design, synthesis and structure-activity relationship studies of novel phenoxyacetamide-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID1326149	Antidiabetic activity in overnight fasted po dosed n-STZ Wistar rat assessed as reduction in blood glucose levels administered as single dose 60 mins prior to glucose challenge measured 30 to 120 mins post glucose challenge by OGTT relative to control
AID1556955	Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay	2019	European journal of medicinal chemistry, Oct-01, Volume: 179	Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.
AID1663988	Glucose lowering activity in normoglycemic ICR mouse assessed as reduction in blood glucose level at 30 mg/kg, po administered 30 mins prior to glucose challenge by OGTT	2020	Bioorganic & medicinal chemistry, 07-01, Volume: 28, Issue:13	Discovery of novel potent GPR40 agonists containing imidazo[1,2-a]pyridine core as antidiabetic agents.
AID1288101	Antidiabetic activity in overnight fasted ICR mouse assessed as decrease in blood glucose level at 20 mg/kg, po administered 30 mins prior to glucose challenge measured after 15 to 120 mins by OGTT method	2016	European journal of medicinal chemistry, May-04, Volume: 113	Design, synthesis and Structure-activity relationship studies of new thiazole-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID1254060	Antidiabetic activity in overnight fasted STZ-induced type 2 diabetic C57BL/6 mouse model assessed as decrease in blood glucose level at 20 mg/kg, po administered glucose 30 mins post compound treatment measured at 15 to 120 mins by OGTT	2015	Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22	Design, synthesis and biological activity of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.
AID1399222	Antidiabetic activity in ICR mouse assessed as blood glucose levels at 50 mg/kg, po administered 1 hr prior to glucose challenge measured at 60 mins post glucose challenge (Rvb = 175.8 +/- 25 mg/dl)	2018	Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18	Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings.
AID1815266	Half life in Wistar Han rat at 3 mg/kg, po measured after 24 hours by UPLC-MS/MS analysis	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Discovery and development of CPL207280 as new GPR40/FFA1 agonist.
AID1288427	Antihyperglycemic activity in STZ-induced type 2 diabetic C57BL/6 mouse model at 20 mg/kg, po administered as single dose 30 mins prior to glucose challenge measured up to 120 mins by OGTT	2016	Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9	Discovery of novel pyrrole-based scaffold as potent and orally bioavailable free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
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).
AID1288109	Hepatotoxicity in ICR mouse assessed as aspartate aminotransferase levels in serum at 20 mg/kg qd administered through oral gavage for 30 days (Rvb = 133.1 +/- 13.1 IU/L)	2016	European journal of medicinal chemistry, May-04, Volume: 113	Design, synthesis and Structure-activity relationship studies of new thiazole-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID1679375	Anti-glycemic activity in GPR40 knockout mouse assessed as reduction in blood glucose excursion measured for 120 mins by IPGTT	2018	Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4	Discovery of a novel potent GPR40 full agonist.
AID1815264	Tmax in Wistar Han rat at 3 mg/kg, po measured after 24 hours by UPLC-MS/MS analysis	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Discovery and development of CPL207280 as new GPR40/FFA1 agonist.
AID1399215	Inhibition of CYP2C9 in human liver microsomes at 5 uM using diclofenac sodium as substrate by LC-MS/MS analysis relative to control	2018	Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18	Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings.
AID1418797	Tmax in Sprague-Dawley rat at 10 mg/kg, po by LC-ESI-MS analysis	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.
AID1422538	Agonist activity at human GAL4 fused PPARdelta-LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
AID1724393	Cmax in Wistar Kyoto N-STZ-1.5 rat model of streptozotocin-induced diabetes at 0.1 to 1 mg/kg, po followed by glucose challenge during 2-week-dosing study	2020	Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18	Design and Identification of a GPR40 Full Agonist (
AID1815268	Oral bioavailability in Wistar Han rat at 3 mg/kg measured after 24 hours by UPLC-MS/MS analysis	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Discovery and development of CPL207280 as new GPR40/FFA1 agonist.
AID1586871	Agonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion at 10 uM after 1 hr by HTRF assay relative to (S)-3-Cyclopropyl-3-(3-(((1r,4S)-4-(2-fluoro-5-methoxyphenyl)cyclohexyl)methoxy)phenyl)propanoic acid	2019	ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1	Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination.
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).
AID669987	Lipophilicity, log D of the compound at pH 7.4 by HPLC analysis	2012	Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8	Optimization of (2,3-dihydro-1-benzofuran-3-yl)acetic acids: discovery of a non-free fatty acid-like, highly bioavailable G protein-coupled receptor 40/free fatty acid receptor 1 agonist as a glucose-dependent insulinotropic agent.
AID1724382	Binding affinity to human GPR40 expressed in CHO cells assessed as formation of protein-ternary complex by LC-MS analysis	2020	Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18	Design and Identification of a GPR40 Full Agonist (
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).
AID1326120	Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
AID1422535	Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
AID1388776	Antidiabetic activity in ICR mouse assessed as reduction in blood glucose AUC (0 to 120 mins) at 20 mg/kg, po dosed 30 minutes prior to glucose challenge by OGTT relative to control	2018	Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3	Identification of highly potent and orally available free fatty acid receptor 1 agonists bearing isoxazole scaffold.
AID1418798	Elimination half life in Sprague-Dawley rat at 10 mg/kg, po by LC-ESI-MS analysis	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.
AID1586863	Agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of Galphaq-mediated IP1 accumulation after 90 mins HTRF assay	2019	ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1	Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination.
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).
AID1679363	Induction of GLP-1 secretion in GPR40 knock-out mouse at 100 mg/kg	2018	Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4	Discovery of a novel potent GPR40 full agonist.
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.
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).
AID1248440	Hypoglycemic activity in normal ICR mouse assessed as reduction in blood glucose level at 20 mg/kg, po by OGTT method	2015	Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20	Design, synthesis and structure-activity relationship studies of novel phenoxyacetamide-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID1735000	AUC in hyperglycemic Balb/c mouse plasma at 29.4 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).
AID1418788	Antidiabetic activity in Sprague-Dawley rat assessed as reduction in blood glucose AUC (0 to 120 mins) at 10 mg/kg, po administered 60 mins prior to glucose challenge by OGTT	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.
AID1724380	Binding affinity to human GPR40 expressed in CHO cells by LC-MS analysis	2020	Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18	Design and Identification of a GPR40 Full Agonist (
AID1724376	AUC (0 to 24 hrs) in Wistar Kyoto N-STZ-1.5 rat model of streptozotocin-induced diabetes at 0.1 to 1 mg/kg, po followed by glucose challenge during 2-week-dosing study	2020	Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18	Design and Identification of a GPR40 Full Agonist (
AID1556966	Antidiabetic activity in ICR mouse assessed as glucose-stimulated change in GLP-1 secretion at 20 mg/kg, po pretreated for 0.5 hrs followed by glucose challenge and measured after 5 mins by ELISA	2019	European journal of medicinal chemistry, Oct-01, Volume: 179	Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.
AID1724378	Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay relative to gamma-linolenic acid	2020	Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18	Design and Identification of a GPR40 Full Agonist (
AID1418786	Antidiabetic activity in Sprague-Dawley rat assessed as reduction in blood glucose AUC (0 to 60 mins) at 10 mg/kg, po administered 60 mins prior to glucose challenge by OGTT	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.
AID1399216	Inhibition of CYP3A4 in human liver microsomes at 5 uM using midazolam as substrate by LC-MS/MS analysis relative to control	2018	Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18	Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings.
AID1663995	Hepatotoxicity in HFD fed/STZ-treated diabetic C57BL/6 mouse model assessed as increase in ALT level in blood at 30 mg/kg, po administered for 4 weeks	2020	Bioorganic & medicinal chemistry, 07-01, Volume: 28, Issue:13	Discovery of novel potent GPR40 agonists containing imidazo[1,2-a]pyridine core as antidiabetic agents.
AID1443209	Agonist activity at GPR40 in mouse MIN6 cells assessed as increase in 25 mM glucose-stimulated insulin secretion at 10 uM after 1 hr by ELISA	2017	Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7	Discovery of Potent and Orally Bioavailable GPR40 Full Agonists Bearing Thiophen-2-ylpropanoic Acid Scaffold.
AID1420975	Effect on 2.5 mM glucose-induced insulin secretion in mouse MIN6 cells at 10 uM measured after 2 hrs by ELISA	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Design, synthesis, and biological evaluations of phenylpropiolic acid derivatives as novel GPR40 agonists.
AID1556957	Antidiabetic activity in ICR mouse assessed as reduction in blood glucose level at 20 mg/kg, po pretreated for 30 mins followed by glucose challenge and measured up to 120 mins by OGTT	2019	European journal of medicinal chemistry, Oct-01, Volume: 179	Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.
AID1679376	Agonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion at 10 uM	2018	Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4	Discovery of a novel potent GPR40 full agonist.
AID1556960	Cmax in Sprague-Dawley rat at 10 mg/kg, po measured for 0.5 to 24 mins by LC-MS/MS analysis	2019	European journal of medicinal chemistry, Oct-01, Volume: 179	Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.
AID1899745	Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay	2022	European journal of medicinal chemistry, Feb-05, Volume: 229	Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents.
AID1623598	Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agents.
AID1370533	Agonist activity at human GPR40 expressed in CHO cells co-expressing Gqalpha assessed as IP1 accumulation	2018	Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3	Discovery of novel benzo[b]thiophene tetrazoles as non-carboxylate GPR40 agonists.
AID1443198	Antidiabetic activity in ICR mouse assessed as decrease in blood glucose AUC at 10 mg/kg, po administered 30 mins prior to glucose challenge measured 120 mins post dose by OGTT	2017	Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7	Discovery of Potent and Orally Bioavailable GPR40 Full Agonists Bearing Thiophen-2-ylpropanoic Acid Scaffold.
AID1388777	Plasma clearance in fasted Sprague-Dawley rat at 3 mg/kg, po administered as single dose measured up to 24 hrs by LC-PDA-MS/MS analysis	2018	Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3	Identification of highly potent and orally available free fatty acid receptor 1 agonists bearing isoxazole scaffold.
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.
AID1175641	Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay	2015	Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1	Synthesis and biological evaluation of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.
AID1420976	Agonist activity at GPR40 in mouse MIN6 cells assessed as increase in glucose-stimulated insulin secretion measured after 2 hrs by ELISA	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Design, synthesis, and biological evaluations of phenylpropiolic acid derivatives as novel GPR40 agonists.
AID1326151	Antidiabetic activity in po dosed db/db mouse assessed as reduction in AUC-glucose levels administered 60 mins prior to glucose challenge measured 30 to 120 mins post glucose challenge by tail clip method-based glucometric analysis
AID1254055	Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux at 100 nM by FLIPR assay relative to control	2015	Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22	Design, synthesis and biological activity of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.
AID1679374	Anti-glycemic activity in C57 mouse assessed as reduction in blood glucose excursion measured for 120 mins by IPGTT	2018	Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4	Discovery of a novel potent GPR40 full agonist.
AID1288111	Hepatotoxicity in ICR mouse assessed as total bilirubin levels in serum at 20 mg/kg qd administered through oral gavage for 30 days (Rvb = 4.1 +/- 0.4 IU/L)	2016	European journal of medicinal chemistry, May-04, Volume: 113	Design, synthesis and Structure-activity relationship studies of new thiazole-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID1399214	Inhibition of CYP2D6 in human liver microsomes at 5 uM using dextromethorphan as substrate by LC-MS/MS analysis relative to control	2018	Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18	Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings.
AID1586864	Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay	2019	ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1	Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination.
AID1297633	Antihyperglycemic effect in ICR mouse assessed as glucose AUC (0 to 120 mins) at 30 mg/kg, po administered as single dose 30 mins prior to oral glucose challenge by oral glucose tolerance test	2016	European journal of medicinal chemistry, Jun-30, Volume: 116	Synthesis and biological evaluation of GPR40/FFAR1 agonists containing 3,5-dimethylisoxazole.
AID1846355	Agonist activity at FFAR1 (unknown origin)	2021	Bioorganic & medicinal chemistry letters, 06-01, Volume: 41	FFAR1/GPR40: One target, different binding sites, many agonists, no drugs, but a continuous and unprofitable tug-of-war between ligand lipophilicity, activity, and toxicity.
AID1679370	Anti-glycemic activity in fasted Sprague-Dawley ZDF rat assessed as reduction in post-prandial hyperglycemia by measuring AUC(0 to 2 hrs) for blood glucose at 3 mg/kg administered for 1 day and measured on day 1 by OGTT	2018	Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4	Discovery of a novel potent GPR40 full agonist.
AID1443210	Agonist activity at GPR40 in mouse MIN6 cells assessed as increase in 25 mM glucose-stimulated insulin secretion at 300 nM after 1 hr by ELISA	2017	Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7	Discovery of Potent and Orally Bioavailable GPR40 Full Agonists Bearing Thiophen-2-ylpropanoic Acid Scaffold.
AID1388774	Lipophilicity, log D of the compound at 100 uM at pH 7.4 after 24 hrs by HPLC method	2018	Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3	Identification of highly potent and orally available free fatty acid receptor 1 agonists bearing isoxazole scaffold.
AID1899746	Agonist activity at human PPARalpha measured by dual luciferase reporter gene assay	2022	European journal of medicinal chemistry, Feb-05, Volume: 229	Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents.
AID1388779	AUC (0 to 24 hrs) in fasted Sprague-Dawley rat at 3 mg/kg, po administered as single dose by LC-PDA-MS/MS analysis	2018	Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3	Identification of highly potent and orally available free fatty acid receptor 1 agonists bearing isoxazole scaffold.
AID1420967	Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux at 10 uM measured for 120 secs by calcium-5 dye based assay relative to 30 uM linolenic acid	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Design, synthesis, and biological evaluations of phenylpropiolic acid derivatives as novel GPR40 agonists.
AID1175642	Hypoglycemic effect in ICR mouse assessed as improvement in glucose intolerance at 20 mg/kg, po dosed 30 mins before oral glucose challenge by oral glucose tolerance test	2015	Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1	Synthesis and biological evaluation of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.
AID1349602	Agonist activity at GPR40 in mouse MIN6 cells assessed as increase in 17 mM glucose-stimulated insulin secretion at 1 and 10 uM after 2 hrs by ELISA relative to glucose	2017	ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12	SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists.
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).
AID1724396	AUC (0 to 24 hrs) in diabetic patient at 50 mg, po	2020	Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18	Design and Identification of a GPR40 Full Agonist (
AID1556967	Antidiabetic activity in ICR mouse assessed as increase in GLP-1 secretion at 20 mg/kg, po pretreated with DPP4 inhibitor linagliptin for 1 hr followed by compound addition and measured after 4 hrs by ELISA	2019	European journal of medicinal chemistry, Oct-01, Volume: 179	Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.
AID1288421	Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level at 300 nM measured for 90 secs by Fluo-4 AM-based FLIPR assay	2016	Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9	Discovery of novel pyrrole-based scaffold as potent and orally bioavailable free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
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.
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.
AID1586862	Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay	2019	ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1	Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination.
AID1724395	Cmax in diabetic patient at 50 mg, po	2020	Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18	Design and Identification of a GPR40 Full Agonist (
AID1398987	Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay	2018	Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15	Nitric oxide donor-based FFA1 agonists: Design, synthesis and biological evaluation as potential anti-diabetic and anti-thrombotic agents.
AID1418784	Antidiabetic activity in Sprague-Dawley rat assessed as reduction in blood glucose excursion at 10 mg/kg, po administered 60 mins prior to glucose challenge by OGTT	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.
AID1623599	Transactivation of GAL4-fused human PPARdelta LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agents.
AID1254057	1-octanol-phosphate buffer partition coefficient, log D of the compound at 100 uM at pH 7.4 after 24 hrs by shake-flask method	2015	Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22	Design, synthesis and biological activity of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.
AID1815262	Cmax in Wistar Han rat at 3 mg/kg, po measured after 24 hours by UPLC-MS/MS analysis	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Discovery and development of CPL207280 as new GPR40/FFA1 agonist.
AID1398991	Antidiabetic activity in ICR mouse assessed as reduction in plasma glucose AUC (0 to 90 mins) at 20 mg/kg, po dosed 30 mins prior to glucose challenge by OGTT relative to control	2018	Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15	Nitric oxide donor-based FFA1 agonists: Design, synthesis and biological evaluation as potential anti-diabetic and anti-thrombotic agents.
AID1679367	Anti-glycemic activity in fasted Sprague-Dawley ZDF rat assessed as reduction in post-prandial hyperglycemia by measuring AUC(0 to 2 hrs) for blood glucose at 10 mg/kg administered daily for 8 days and measured on day 8 by OGTT	2018	Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4	Discovery of a novel potent GPR40 full agonist.
AID1899748	Agonist activity at human PPARdelta measured by dual luciferase reporter gene assay	2022	European journal of medicinal chemistry, Feb-05, Volume: 229	Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents.
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).
AID1399221	Antidiabetic activity in ICR mouse assessed as blood glucose levels at 50 mg/kg, po administered 1 hr prior to glucose challenge measured at 30 mins post glucose challenge (Rvb = 227.6 +/- 18.7 mg/dl)	2018	Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18	Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings.
AID1175643	Hypoglycemic effect in ICR mouse assessed as reduction in glucose AUC (0 to 120 mins) at 20 mg/kg, po dosed 30 mins before oral glucose challenge by oral glucose tolerance test	2015	Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1	Synthesis and biological evaluation of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.
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).
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).
AID1288423	Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay	2016	Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9	Discovery of novel pyrrole-based scaffold as potent and orally bioavailable free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID1399212	Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay	2018	Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18	Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings.
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).
AID1556959	Clearance in Sprague-Dawley rat at 10 mg/kg, po measured for 0.5 to 24 mins by LC-MS/MS analysis	2019	European journal of medicinal chemistry, Oct-01, Volume: 179	Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.
AID1367360	Agonist activity at human FFAR4 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by luminescence assay	2017	Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24	Improving metabolic stability with deuterium: The discovery of GPU-028, a potent free fatty acid receptor 4 agonists.
AID1663992	Antidiabetic activity in HFD fed/STZ-treated diabetic C57BL/6 mouse model assessed as reduction in AUC(0 to 120 mins) of plasma glucose at 30 mg/kg, po administered 30 mins prior to glucose challenge and measured upto 120 mins by OGTT	2020	Bioorganic & medicinal chemistry, 07-01, Volume: 28, Issue:13	Discovery of novel potent GPR40 agonists containing imidazo[1,2-a]pyridine core as antidiabetic agents.
AID1288096	Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx at 100 nM by FLIPR assay	2016	European journal of medicinal chemistry, May-04, Volume: 113	Design, synthesis and Structure-activity relationship studies of new thiazole-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID1422537	Agonist activity at human GAL4 fused PPARgamma-LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
AID1443213	Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay relative to 3-(4-((2',6'-dimethylbiphenyl-3-yl)methoxy)phenyl)propanoic acid	2017	Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7	Discovery of Potent and Orally Bioavailable GPR40 Full Agonists Bearing Thiophen-2-ylpropanoic Acid Scaffold.
AID1399213	Induction of 16.8 mM glucose-stimulated insulin secretion in ICR mouse primary pancreatic islets assessed per protein at 10 uM after 1 hr by ELISA (Rvb = 1.8 +/- 0.6 ng/ml)	2018	Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18	Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings.
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.
AID1297632	Antihyperglycemic effect in ICR mouse assessed as reduction in glucose AUC (0 to 120 mins) at 30 mg/kg, po administered as single dose 30 mins prior to oral glucose challenge by oral glucose tolerance test	2016	European journal of medicinal chemistry, Jun-30, Volume: 116	Synthesis and biological evaluation of GPR40/FFAR1 agonists containing 3,5-dimethylisoxazole.
AID1420971	Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as phosphorylation of ERK1/2 at 10 after 20 mins by Western blot analysis	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Design, synthesis, and biological evaluations of phenylpropiolic acid derivatives as novel GPR40 agonists.
AID1418782	Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.
AID1288095	Agonist activity at human FFA1 receptor expressed in CHO cells assessed as Ca2+ influx at 300 nM by FLIPR assay	2016	European journal of medicinal chemistry, May-04, Volume: 113	Design, synthesis and Structure-activity relationship studies of new thiazole-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID1297635	Antihyperglycemic effect in type 2 diabetic C57BL/6 mouse assessed as glucose AUC (0 to 120 mins) at 30 mg/kg, po administered as single dose 30 mins prior to oral glucose challenge by oral glucose tolerance test	2016	European journal of medicinal chemistry, Jun-30, Volume: 116	Synthesis and biological evaluation of GPR40/FFAR1 agonists containing 3,5-dimethylisoxazole.
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).
AID1418796	AUC (0 to t) in Sprague-Dawley rat at 10 mg/kg, po by LC-ESI-MS analysis	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.
AID1420968	Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Design, synthesis, and biological evaluations of phenylpropiolic acid derivatives as novel GPR40 agonists.
AID1679366	In vivo agonist activity at GPR40 in C57 mouse assessed as induction of GLP1 secretion at 100 mg/kg	2018	Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4	Discovery of a novel potent GPR40 full agonist.
AID1663996	Hepatotoxicity in HFD fed/STZ-treated diabetic C57BL/6 mouse model assessed as increase in AST level in blood at 30 mg/kg, po administered for 4 weeks	2020	Bioorganic & medicinal chemistry, 07-01, Volume: 28, Issue:13	Discovery of novel potent GPR40 agonists containing imidazo[1,2-a]pyridine core as antidiabetic agents.
AID1328825	Half life in human	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.
AID1679369	Anti-glycemic activity in fasted Sprague-Dawley ZDF rat assessed as reduction in post-prandial hyperglycemia by measuring AUC(0 to 2 hrs) for blood glucose at 3 mg/kg administered daily for 8 days and measured on day 8 by OGTT	2018	Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4	Discovery of a novel potent GPR40 full agonist.
AID1556958	Hepatotoxicity in sandwich-cultured Sprague-Dawley rat hepatocytes assessed as inhibition of hepatobiliary transport by measuring biliary excretion index at 25 uM incubated for 15 mins followed by d8-TCA addition and measured after 15 mins by LC-MS/MS ana	2019	European journal of medicinal chemistry, Oct-01, Volume: 179	Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.
AID1734903	Displacement of [3H]-(S)-3-(isoxazol-3-yl)-3-(4-((2-phenyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)methoxy)phenyl)propanoic acid from human recombinant full-length GPR40 expressed in human HEK293 cells assessed as dissociation constant at 1.37 to 1000 nM measu	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).
AID1556962	Half life in Sprague-Dawley rat at 10 mg/kg, po measured for 0.5 to 24 mins by LC-MS/MS analysis	2019	European journal of medicinal chemistry, Oct-01, Volume: 179	Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.
AID1444494	Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux at 1 uM measured for 90 secs by Fluo4-AM dye based FLIPR assay relative to control	2017	Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8	Design, synthesis and structure-activity relationship studies of novel free fatty acid receptor 1 agonists bearing amide linker.
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).
AID1899747	Agonist activity at human PPARgamma measured by dual luciferase reporter gene assay	2022	European journal of medicinal chemistry, Feb-05, Volume: 229	Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents.
AID1418809	Inhibition of human MRP2	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.
AID1663987	Agonist activity at GPR40 (unknown origin)	2020	Bioorganic & medicinal chemistry, 07-01, Volume: 28, Issue:13	Discovery of novel potent GPR40 agonists containing imidazo[1,2-a]pyridine core as antidiabetic agents.
AID1586866	Partial agonist activity at human GPR40 expressed in CHOK1 cells assessed as induction of GalphaS-mediated cAMP accumulation after 30 mins HTRF assay	2019	ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1	Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination.
AID1679368	Anti-glycemic activity in fasted Sprague-Dawley ZDF rat assessed as reduction in post-prandial hyperglycemia by measuring AUC(0 to 2 hrs) for blood glucose at 10 mg/kg administered for 1 day and measured on day 1 by OGTT	2018	Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4	Discovery of a novel potent GPR40 full agonist.
AID1630825	1-octanol-phosphate buffer distribution coefficient, log D of compound at 100 uM at pH 7.4 after 24 hrs by HPLC based shake flask method	2016	Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21	Discovery of novel free fatty acid receptor 1 agonists bearing triazole core via click chemistry.
AID1248435	Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx at 300 nM incubated for by FLIPR method	2015	Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20	Design, synthesis and structure-activity relationship studies of novel phenoxyacetamide-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID1896158	Antiviral activity against HBV infected human HepG2-hNTCP cells assessed as reduction of HBV DNA level preincubated for 3 hrs followed by viral infection for 16 hrs further compound washout and measured 6 days post infection by qPCR analysis	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Inhibiting Sodium Taurocholate Cotransporting Polypeptide in HBV-Related Diseases: From Biological Function to Therapeutic Potential.
AID1679372	Anti-glycemic activity in fasted Sprague-Dawley ZDF rat assessed as increase in insulin secretion by measuring insulin level in plasma at 10 mg/kg administered 30 mins prior to glucose challenge measured after 140 mins by OGTT	2018	Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4	Discovery of a novel potent GPR40 full agonist.
AID1600826	Inhibition of NTCP in human hepatocytes	2019	Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19	Design, synthesis and biological evaluation of benzamide derivatives as novel NTCP inhibitors that induce apoptosis in HepG2 cells.
AID1679378	Agonist activity at GPR40 in rat INS1 (832/13) cells assessed as induction of glucose-stimulated insulin secretion in presence of 10 mM glucose	2018	Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4	Discovery of a novel potent GPR40 full agonist.
AID1679371	Anti-glycemic activity in fasted Sprague-Dawley ZDF rat assessed as increase in insulin secretion by measuring insulin level in plasma at 3 mg/kg administered 30 mins prior to glucose challenge measured after 140 mins by OGTT	2018	Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4	Discovery of a novel potent GPR40 full 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.
AID1422536	Agonist activity at human GAL4 fused PPARalpha-LBD expressed in human HepG2 cells after 18 hrs by luciferase reporter gene assay	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
AID1699901	Antidiabetic activity in db/db mouse assessed as reduction in plasma glucose AUC at 10 mg/kg, ip administered prior to glucose challenge and measured after 1 hr by OGTT relative to control	2020	Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24	Synthesis and evaluation of 3-(4-(phenoxymethyl)phenyl)propanoic acid and N-phenylbenzenesulfonamide derivatives as FFA4 agonists.
AID1326129	Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
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).
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).
AID1444501	Antidiabetic activity in HFD/STZ-induced type2 diabetic C57BL/6 mouse assessed as decrease in blood glucose AUC at 20 mg/kg, po administered as single dose 60 mins prior to glucose challenge measured 120 mins post dose by OGTT relative to control	2017	Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8	Design, synthesis and structure-activity relationship studies of novel free fatty acid receptor 1 agonists bearing amide linker.
AID1297631	Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay relative to TAK-875	2016	European journal of medicinal chemistry, Jun-30, Volume: 116	Synthesis and biological evaluation of GPR40/FFAR1 agonists containing 3,5-dimethylisoxazole.
AID1399217	Inhibition of CYP1A2 in human liver microsomes at 5 uM using phenacetin as substrate by LC-MS/MS analysis relative to control	2018	Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18	Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings.
AID1556974	Hepatotoxicity in sandwich-cultured Sprague-Dawley rat hepatocytes assessed as decrease in accumulation of d8-TCA at 25 uM incubated for 15 mins followed by d8-TCA addition and measured after 15 mins by LC-MS/MS analysis	2019	European journal of medicinal chemistry, Oct-01, Volume: 179	Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.
AID1724377	Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay	2020	Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18	Design and Identification of a GPR40 Full Agonist (
AID1624319	Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay relative to linoleic acid	2019	Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6	Synthesis and biological evaluation of novel potent FFA1 agonists containing 2,3-dihydrobenzo[b][1,4]dioxine.
AID1288425	Decrease in plasma glucose level in ICR mouse at 20 mg/kg, po administered as single dose 30 mins prior to glucose challenge measured up to 120 mins by OGTT	2016	Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9	Discovery of novel pyrrole-based scaffold as potent and orally bioavailable free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID1175640	Agonist activity at human FFA1 expressed in CHO cells assessed as ratio of increase in intracellular Ca2+ concentration in compound treated cells at 100 nM to vehicle-treated cells by Fluo-4 AM based fluorescence assay	2015	Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1	Synthesis and biological evaluation of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.
AID1248437	Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method	2015	Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20	Design, synthesis and structure-activity relationship studies of novel phenoxyacetamide-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.
AID1418824	Toxicity in sandwich-cultured Sprague-Dawley rat hepatocytes assessed as inhibition of hepatobiliary transport by measuring biliary excretion index at 20 to 40 uM after 15 mins in presence of d8-TCA by LC-MS/MS analysis	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.
AID1420977	Agonist activity at GPR40 in mouse MIN6 cells assessed as increase in glucose-stimulated insulin secretion at 10 uM measured after 2 hrs in presence of GPR40 antagonist GW-100 by ELISA	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Design, synthesis, and biological evaluations of phenylpropiolic acid derivatives as novel GPR40 agonists.
AID1254059	Antidiabetic activity in overnight fasted ICR mouse assessed as decrease in blood glucose level at 20 mg/kg, po administered glucose 30 mins post compound treatment measured at 15 to 120 mins by OGTT	2015	Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22	Design, synthesis and biological activity of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.
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).
AID669986	Induction of apoptosis in human HepG2 cells assessed as caspase 3/7 activity at 30 uM after 1 day by CaspaseGlo assay relative to staurosporine	2012	Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8	Optimization of (2,3-dihydro-1-benzofuran-3-yl)acetic acids: discovery of a non-free fatty acid-like, highly bioavailable G protein-coupled receptor 40/free fatty acid receptor 1 agonist as a glucose-dependent insulinotropic agent.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154	Primary 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.
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1345809	Human FFA1 receptor (Free fatty acid receptors)	2010	ACS medicinal chemistry letters, Sep-09, Volume: 1, Issue:6	Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.
AID1345809	Human FFA1 receptor (Free fatty acid receptors)	2011	The Journal of pharmacology and experimental therapeutics, Oct, Volume: 339, Issue:1	TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats.
AID1345809	Human FFA1 receptor (Free fatty acid receptors)	2015	Diabetes, obesity & metabolism, Jul, Volume: 17, Issue:7	Efficacy and safety of fasiglifam (TAK-875), a G protein-coupled receptor 40 agonist, in Japanese patients with type 2 diabetes inadequately controlled by diet and exercise: a randomized, double-blind, placebo-controlled, phase III trial.
AID1345809	Human FFA1 receptor (Free fatty acid receptors)	2014	Nature, Sep-04, Volume: 513, Issue:7516	High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875.
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.
AID977611	Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB	2014	Nature, Sep-04, Volume: 513, Issue:7516	High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	95 (79.17)	24.3611
2020's	25 (20.83)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	15 (12.40%)	5.53%
Reviews	11 (9.09%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	95 (78.51%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
histamine [no description available]	2.25	1	0	aralkylamino compound; imidazoles	human metabolite; mouse metabolite; neurotransmitter
palmitic acid Palmitic Acid: A common saturated fatty acid found in fats and waxes including olive oil, palm oil, and body lipids.. hexadecanoic acid : A straight-chain, sixteen-carbon, saturated long-chain fatty acid.	2.5	2	0	long-chain fatty acid; straight-chain saturated fatty acid	algal metabolite; Daphnia magna metabolite; EC 1.1.1.189 (prostaglandin-E2 9-reductase) inhibitor; plant metabolite
azelastine azelastine: azeptin is azelastine hydrochloride; structure; eye drop formulation effective in relieving symptoms of allergic conjunctivitis; do not confuse with 5-loxin which is an extract of Boswellia. azelastine : A phthalazine compound having an oxo substituent at the 1-position, a 1-methylazepan-4-yl group at the 2-position and a 4-chlorobenzyl substituent at the 4-position.	3.51	1	0	monochlorobenzenes; phthalazines; tertiary amino compound	anti-allergic agent; anti-asthmatic drug; bronchodilator agent; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; H1-receptor antagonist; platelet aggregation inhibitor
berberine [no description available]	3.17	1	0	alkaloid antibiotic; berberine alkaloid; botanical anti-fungal agent; organic heteropentacyclic compound	antilipemic drug; antineoplastic agent; antioxidant; EC 1.1.1.141 [15-hydroxyprostaglandin dehydrogenase (NAD(+))] inhibitor; EC 1.1.1.21 (aldehyde reductase) inhibitor; EC 1.13.11.52 (indoleamine 2,3-dioxygenase) inhibitor; EC 1.21.3.3 (reticuline oxidase) inhibitor; EC 2.1.1.116 [3'-hydroxy-N-methyl-(S)-coclaurine 4'-O-methyltransferase] inhibitor; EC 2.1.1.122 [(S)-tetrahydroprotoberberine N-methyltransferase] inhibitor; EC 2.7.11.10 (IkappaB kinase) inhibitor; EC 3.1.1.4 (phospholipase A2) inhibitor; EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor; EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; geroprotector; hypoglycemic agent; metabolite; potassium channel blocker
ciglitazone ciglitazone: structure given in second source; PPAR agonist used for type II diabetes. ciglitazone : An aromatic ether that consists of 1,3-thiazolidine-2,4-dione with position 5 substituted by a 4-[(1-methylcyclohexyl)methoxy]benzyl group. A selective PPARgamma agonist.	3.51	1	0	aromatic ether; thiazolidinone	antineoplastic agent; insulin-sensitizing drug
erythrosine Fluoresceins: A family of spiro(isobenzofuran-1(3H),9'-(9H)xanthen)-3-one derivatives. These are used as dyes, as indicators for various metals, and as fluorescent labels in immunoassays.	2.13	1	0
furafylline [no description available]	2.17	1	0	oxopurine
glimepiride glimepiride: structure given in first source	10.88	4	2	sulfonamide
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.	3.39	6	0	monochlorobenzenes; 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
avapro Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.	3.78	2	0	azaspiro compound; biphenylyltetrazole	angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic
ketoprofen Ketoprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis.. ketoprofen : An oxo monocarboxylic acid that consists of propionic acid substituted by a 3-benzoylphenyl group at position 2.	2.06	1	0	benzophenones; oxo monocarboxylic acid	antipyretic; drug allergen; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; non-steroidal anti-inflammatory drug; xenobiotic
lauric acid dodecanoic acid : A straight-chain, twelve-carbon medium-chain saturated fatty acid with strong bactericidal properties; the main fatty acid in coconut oil and palm kernel oil.	2.13	1	0	medium-chain fatty acid; straight-chain saturated fatty acid	algal metabolite; antibacterial agent; plant metabolite
metformin Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1.	9.2	3	1	guanidines	environmental contaminant; geroprotector; hypoglycemic agent; xenobiotic
sulfaphenazole Sulfaphenazole: A sulfonilamide anti-infective agent.. sulfaphenazole : A sulfonamide that is sulfanilamide in which the sulfonamide nitrogen is substituted by a 1-phenyl-1H-pyrazol-5-yl group. It is a selective inhibitor of cytochrome P450 (CYP) 2C9 isozyme, and antibacterial agent.	2.17	1	0	primary amino compound; pyrazoles; substituted aniline; sulfonamide antibiotic; sulfonamide	antibacterial drug; EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor; EC 1.14.13.67 (quinine 3-monooxygenase) inhibitor; P450 inhibitor
sulfasalazine Sulfasalazine: A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see MESALAMINE) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907). sulfasalazine : An azobenzene consisting of diphenyldiazene having a carboxy substituent at the 4-position, a hydroxy substituent at the 3-position and a 2-pyridylaminosulphonyl substituent at the 4'-position.	3.78	2	0
tolbutamide Tolbutamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). tolbutamide : An N-sulfonylurea that consists of 1-butylurea having a tosyl group attached at the 3-position.	2.13	1	0	N-sulfonylurea	human metabolite; hypoglycemic agent; insulin secretagogue; potassium channel blocker
troglitazone Troglitazone: A chroman and thiazolidinedione derivative that acts as a PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS (PPAR) agonist. It was formerly used in the treatment of TYPE 2 DIABETES MELLITUS, but has been withdrawn due to hepatotoxicity.	3.51	1	0	chromanes; thiazolidinone	anticoagulant; anticonvulsant; antineoplastic agent; antioxidant; EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; hypoglycemic agent; platelet aggregation inhibitor; vasodilator agent
ici 204,219 zafirlukast: a leukotriene D4 receptor antagonist	3.78	2	0	carbamate ester; indoles; N-sulfonylcarboxamide	anti-asthmatic agent; leukotriene antagonist
3,3',5-triiodothyroacetic acid tiratricol : A monocarboxylic acid that is (4-hydroxy-3,5-diiodophenyl)acetic acid in which the phenolic hydroxy group has been replaced by a 4-hydroxy-3-iodophenoxy group. It is a thyroid hormone analogue that has been used in the treatment of thyroid hormone resistance syndrome.	3.78	2	0
biguanides Biguanides: Derivatives of biguanide (the structure formula HN(C(NH)NH2)2) that are primarily used as oral HYPOGLYCEMIC AGENTS for the treatment of DIABETES MELLITUS, TYPE 2 and PREDIABETES.. biguanides : A class of oral hypoglycemic drugs used for diabetes mellitus or prediabetes treatment. They have a structure based on the 2-carbamimidoylguanidine skeleton.	3.51	1	1	guanidines
carbon tetrachloride Carbon Tetrachloride: A solvent for oils, fats, lacquers, varnishes, rubber waxes, and resins, and a starting material in the manufacturing of organic compounds. Poisoning by inhalation, ingestion or skin absorption is possible and may be fatal. (Merck Index, 11th ed). tetrachloromethane : A chlorocarbon that is methane in which all the hydrogens have been replaced by chloro groups.	2.17	1	0	chlorocarbon; chloromethanes	hepatotoxic agent; refrigerant
taurocholic acid Taurocholic Acid: The product of conjugation of cholic acid with taurine. Its sodium salt is the chief ingredient of the bile of carnivorous animals. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as a cholagogue and cholerectic.. taurocholate : An organosulfonate oxoanion that is the conjugate base of taurocholic acid.. taurocholic acid : A bile acid taurine conjugate of cholic acid that usually occurs as the sodium salt of bile in mammals.	3.51	1	0	amino sulfonic acid; bile acid taurine conjugate	human metabolite
thiophenes Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.	2.15	1	0	mancude organic heteromonocyclic parent; monocyclic heteroarene; thiophenes; volatile organic compound	non-polar solvent
isoxazoles Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent.	2.17	1	0	isoxazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
pyrazines Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.	2.17	1	0	diazine; pyrazines	Daphnia magna metabolite
fluorescein Fluorescein: A phthalic indicator dye that appears yellow-green in normal tear film and bright green in a more alkaline medium such as the aqueous humor.. fluorescein (lactone form) : A xanthene dye that is highly fluorescent, detectable even when present in minute quantities. Used forensically to detect traces of blood, in analytical chemistry as an indicator in silver nitrate titrations and in microscopy.	2.13	1	0	2-benzofurans; gamma-lactone; organic heteropentacyclic compound; oxaspiro compound; polyphenol; xanthene dye	fluorescent dye; radioopaque medium
c.i. direct blue 1 [no description available]	3.51	1	0
squaric acid [no description available]	2.31	1	0	alicyclic ketone; carbon oxoacid	metabolite
phenyl acetate phenyl acetate: The ester formed between phenol and acetic acid. Don't confuse with phenylacetic acid derivatives listed under PHENYLACETATES.. phenyl acetate : An acetate ester obtained by the formal condensation of phenol with acetic acid.	2.21	1	0	benzenes; phenyl acetates
bezafibrate [no description available]	3.41	1	0	aromatic ether; monocarboxylic acid amide; monocarboxylic acid; monochlorobenzenes	antilipemic drug; environmental contaminant; geroprotector; xenobiotic
pirfenidone pirfenidone : A pyridone that is 2-pyridone substituted at positions 1 and 5 by phenyl and methyl groups respectively. An anti-inflammatory drug used for the treatment of idiopathic pulmonary fibrosis.	2.41	1	0	pyridone	antipyretic; non-narcotic analgesic; non-steroidal anti-inflammatory drug
thiophenoxyacetic acid thiophenoxyacetic acid: structure	3.41	1	0
epigallocatechin gallate epigallocatechin gallate: a steroid 5alpha-reductase inhibitor and antimutagen in green tea (Camellia sinensis). (-)-epigallocatechin 3-gallate : A gallate ester obtained by the formal condensation of gallic acid with the (3R)-hydroxy group of (-)-epigallocatechin.	3.51	1	0	flavans; gallate ester; polyphenol	antineoplastic agent; antioxidant; apoptosis inducer; geroprotector; Hsp90 inhibitor; neuroprotective agent; plant metabolite
betulin betulin: isolated from various white birch bark (BETULA). betulin : A pentacyclic triterpenoid that is lupane having a double bond at position 20(29) as well as 3beta-hydroxy and 28-hydroxymethyl substituents.	3.51	1	0	diol; pentacyclic triterpenoid	analgesic; anti-inflammatory agent; antineoplastic agent; antiviral agent; metabolite
rosiglitazone [no description available]	4.42	5	0	aminopyridine; thiazolidinediones	EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; insulin-sensitizing drug
bosentan anhydrous Bosentan: A sulfonamide and pyrimidine derivative that acts as a dual endothelin receptor antagonist used to manage PULMONARY HYPERTENSION and SYSTEMIC SCLEROSIS.	2.21	1	0	primary alcohol; pyrimidines; sulfonamide	antihypertensive agent; endothelin receptor antagonist
efaproxiral efaproxiral: RN & structure given in first source; allosteric effector of hemoglobin	3.41	1	0
agn 190299 AGN 190299: a metabolite of the synthetic retinoid AGN 190168; structure given in first source. tazarotenic acid : A thiochromane that is acetylene in which the hydrogens are replaced by 5-carboxypyridin-2-yl and 4,4-dimethylthiochroman-6-yl groups. It is the active form of the prodrug tazarotene.	3.41	1	0	monocarboxylic acid; pyridines; retinoid; thiochromane	keratolytic drug; teratogenic agent
ezetimibe Ezetimibe: An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.. ezetimibe : A beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer).	3.51	1	0	azetidines; beta-lactam; organofluorine compound	anticholesteremic drug; antilipemic drug; antimetabolite
benzofurans Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.	15.54	84	14
ritonavir Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.	3.51	1	0	1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas	antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic
quinidine Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy.	2.17	1	0	cinchona alkaloid	alpha-adrenergic antagonist; anti-arrhythmia drug; antimalarial; drug allergen; EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor; EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor; muscarinic antagonist; P450 inhibitor; potassium channel blocker; sodium channel blocker
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.	2.15	1	0	docosahexaenoic acid; omega-3 fatty acid	algal metabolite; antineoplastic agent; Daphnia tenebrosa metabolite; human metabolite; mouse metabolite; nutraceutical
oleic acid Oleic Acid: An unsaturated fatty acid that is the most widely distributed and abundant fatty acid in nature. It is used commercially in the preparation of oleates and lotions, and as a pharmaceutical solvent. (Stedman, 26th ed). oleic acid : An octadec-9-enoic acid in which the double bond at C-9 has Z (cis) stereochemistry.	2.11	1	0	octadec-9-enoic acid	antioxidant; Daphnia galeata metabolite; EC 3.1.1.1 (carboxylesterase) inhibitor; Escherichia coli metabolite; mouse metabolite; plant metabolite; solvent
(3R,5S)-fluvastatin (3R,5S)-fluvastatin : A (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid diastereoisomer in which the stereocentres beta- and delta- to the carboxy group have R and S configuration, respectively. The drug fluvastatin is an equimolar mixture of this compound and its enantiomer.	2.21	1	0	(6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid; statin (synthetic)
ketoconazole (2R,4S)-ketoconazole : A cis-1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine which dioxolane moiety has (2R,4S)-configuration.	2.17	1	0	cis-1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine
tenofovir tenofovir (anhydrous) : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection.	2.21	1	0	nucleoside analogue; phosphonic acids	antiviral drug; drug metabolite; HIV-1 reverse transcriptase inhibitor
curcumin Curcumin: A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes.. curcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by feruloyl groups. A natural dyestuff found in the root of Curcuma longa.	3.51	1	0	aromatic ether; beta-diketone; diarylheptanoid; enone; polyphenol	anti-inflammatory agent; antifungal agent; antineoplastic agent; biological pigment; contraceptive drug; dye; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; EC 1.1.1.21 (aldehyde reductase) inhibitor; EC 1.1.1.25 (shikimate dehydrogenase) inhibitor; EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor; EC 1.8.1.9 (thioredoxin reductase) inhibitor; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; EC 3.5.1.98 (histone deacetylase) inhibitor; flavouring agent; food colouring; geroprotector; hepatoprotective agent; immunomodulator; iron chelator; ligand; lipoxygenase inhibitor; metabolite; neuroprotective agent; nutraceutical; radical scavenger
gw 7647 GW 7647: a PPAR-alpha agonist; structure in first source. GW 7647 : A monocarboxylic acid that is 2-(phenylsulfanyl)isobutyric acid in which the phenyl group is substituted at the para- position by a 3-aza-7-cyclohexylhept-1-yl group in which the nitrogen is acylated by a (cyclohexylamino)carbonyl group.	2.66	2	0	aryl sulfide; monocarboxylic acid; ureas	PPARalpha agonist
quercetin [no description available]	3.51	1	0	7-hydroxyflavonol; pentahydroxyflavone	antibacterial agent; antineoplastic agent; antioxidant; Aurora kinase inhibitor; chelator; EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor; geroprotector; phytoestrogen; plant metabolite; protein kinase inhibitor; radical scavenger
linoleic acid Linoleic Acid: A doubly unsaturated fatty acid, occurring widely in plant glycosides. It is an essential fatty acid in mammalian nutrition and is used in the biosynthesis of prostaglandins and cell membranes. (From Stedman, 26th ed). linoleic acid : An octadecadienoic acid in which the two double bonds are at positions 9 and 12 and have Z (cis) stereochemistry.	2.59	2	0	octadecadienoic acid; omega-6 fatty acid	algal metabolite; Daphnia galeata metabolite; plant metabolite
gamma-linolenic acid gamma-Linolenic Acid: An omega-6 fatty acid produced in the body as the delta 6-desaturase metabolite of linoleic acid. It is converted to dihomo-gamma-linolenic acid, a biosynthetic precursor of monoenoic prostaglandins such as PGE1. (From Merck Index, 11th ed). gamma-linolenic acid : A C18, omega-6 acid fatty acid comprising a linolenic acid having cis- double bonds at positions 6, 9 and 12.	2.52	2	0	linolenic acid; omega-6 fatty acid	human metabolite; mouse metabolite; plant metabolite
alpha-linolenic acid linolenic acid : A two-membered subclass of octadecatrienoic acid comprising the (9Z,12Z,15Z)- and (6Z,9Z,12Z)-isomers. Linolenic acids are nutrients essential to the formation of prostaglandins and are also used in making paints and synthetic resins.. linolenate : A polyunsaturated fatty acid anion obtained by deprotonation of the carboxy group of either alpha- or gamma-linolenic acid.	2.17	1	0	linolenic acid; omega-3 fatty acid	micronutrient; mouse metabolite; nutraceutical
ergosterol-5,8-peroxide ergosterol-5,8-peroxide: also inhibits sulfatase; isolated from fungus Cercospora kikuchii; structure given in first source. ergosterol peroxide : An ergostanoid that is ergosta-6,22-dien-3-ol with a peroxy group between positions 5 and 8 (the 3beta,5alpha,8alpha,22E stereoisomer). Isolated from Ganoderma lucidum and Cordyceps sinensis, it exhibits antimycobacterial, trypanocidal and antineoplastic activities.	3.51	1	0	3beta-sterol; ergostanoid; organic peroxide; phytosterols	antimycobacterial drug; antineoplastic agent; metabolite; trypanocidal drug
neuromedin c neuromedin C: decapeptide isolated from porcine spinal cord; corresponds to the C-terminal decapeptide of gastrin-releasing peptide; bombesin-like peptide; RN given refers to all (L)-isomer	3.04	1	0
flag peptide FLAG peptide: engineered as a tag for immunoaffinity purification of genetically-engineered proteins; amino acid sequence given in first source; a polar octapeptide. FLAG peptide : An eight amino acid peptide consisting of L-aspartic acid, L-tyrosine, L-lysine, four L-aspartic acid residues, and L-lysine joined in sequence by peptide linkages. It is widely used as a fusion tag for the purification and detection of a wide variety of recombinant proteins.	2.13	1	0	peptide
gw0742 GW 610742: structure in first source	2.93	3	0	monocarboxylic acid
betulin-3-caffeate betulin-3-caffeate: has antineoplastic activity; isolated from Hibiscus syriacus; structure in first source	3.51	1	0
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.	4.82	3	2
gw9508 GW9508: structure in first source	3.66	8	0	aromatic amine
macitentan [no description available]	2.21	1	0	aromatic ether; organobromine compound; pyrimidines; ring assembly; sulfamides	antihypertensive agent; endothelin receptor antagonist; orphan drug
glucagon Glucagon: A 29-amino acid pancreatic peptide derived from proglucagon which is also the precursor of intestinal GLUCAGON-LIKE PEPTIDES. Glucagon is secreted by PANCREATIC ALPHA CELLS and plays an important role in regulation of BLOOD GLUCOSE concentration, ketone metabolism, and several other biochemical and physiological processes. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1511). glucagon : A 29-amino acid peptide hormone consisting of His, Ser, Gln, Gly, Thr, Phe, Thr, Ser, Asp, Tyr, Ser, Lys, Tyr, Leu, Asp, Ser, Arg, Arg, Ala, Gln, Asp, Phe, Val, Gln, Trp, Leu, Met, Asn and Thr residues joined in sequence.	7.48	2	0	peptide hormone
glucagon-like peptide 1 Glucagon-Like Peptide 1: A peptide of 36 or 37 amino acids that is derived from PROGLUCAGON and mainly produced by the INTESTINAL L CELLS. GLP-1(1-37 or 1-36) is further N-terminally truncated resulting in GLP-1(7-37) or GLP-1-(7-36) which can be amidated. These GLP-1 peptides are known to enhance glucose-dependent INSULIN release, suppress GLUCAGON release and gastric emptying, lower BLOOD GLUCOSE, and reduce food intake.	3.7	3	0
incretins Incretins: Peptides which stimulate INSULIN release from the PANCREATIC BETA CELLS following oral nutrient ingestion, or postprandially.	3.95	2	1
c-peptide C-Peptide: The middle segment of proinsulin that is between the N-terminal B-chain and the C-terminal A-chain. It is a pancreatic peptide of about 31 residues, depending on the species. Upon proteolytic cleavage of proinsulin, equimolar INSULIN and C-peptide are released. C-peptide immunoassay has been used to assess pancreatic beta cell function in diabetic patients with circulating insulin antibodies or exogenous insulin. Half-life of C-peptide is 30 min, almost 8 times that of insulin.	4.42	2	2
piperidines Piperidines: A family of hexahydropyridines.	2.63	2	0
amg-837 AMG-837: GPR40 agonist	5.34	9	0
tug-469 TUG-469: a GPR40 agonist with antidiabetic activity; structure in first source	2.49	2	0
tug-891 GPU-028: structure in first source	2.59	2	0
am 1638 [no description available]	3.44	6	0
insulin degludec [no description available]	2.07	1	0
concanavalin a Concanavalin A: A MANNOSE/GLUCOSE binding lectin isolated from the jack bean (Canavalia ensiformis). It is a potent mitogen used to stimulate cell proliferation in lymphocytes, primarily T-lymphocyte, cultures.	2.17	1	0

Condition	Indicated	Relationship Strength	Studies	Trials
Alloxan Diabetes [description not available]	0	3.76	9	0
Diabetes Mellitus, Adult-Onset [description not available]	0	16.81	112	10
Hyperglycemia, Postprandial Abnormally high BLOOD GLUCOSE level after a meal.	0	5.15	5	2
Insulin Sensitivity [description not available]	0	2.8	3	0
Diabetes Mellitus, Type 2 A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.	1	18.81	112	10
Hyperglycemia Abnormally high BLOOD GLUCOSE level.	0	5.15	5	2
Insulin Resistance Diminished effectiveness of INSULIN in lowering blood sugar levels: requiring the use of 200 units or more of insulin per day to prevent HYPERGLYCEMIA or KETOSIS.	0	2.8	3	0
Fasting Hypoglycemia HYPOGLYCEMIA expressed in the postabsorptive state, after prolonged FASTING, or an overnight fast.	0	5.81	5	4
Hypoglycemia A syndrome of abnormally low BLOOD GLUCOSE level. Clinical hypoglycemia has diverse etiologies. Severe hypoglycemia eventually lead to glucose deprivation of the CENTRAL NERVOUS SYSTEM resulting in HUNGER; SWEATING; PARESTHESIA; impaired mental function; SEIZURES; COMA; and even DEATH.	0	5.81	5	4
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	3.03	4	0
Obesity A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).	0	4.48	4	1
Hepatitis B Virus Infection [description not available]	0	3.84	3	0
Hepatitis B INFLAMMATION of the LIVER in humans caused by a member of the ORTHOHEPADNAVIRUS genus, HEPATITIS B VIRUS. It is primarily transmitted by parenteral exposure, such as transfusion of contaminated blood or blood products, but can also be transmitted via sexual or intimate personal contact.	0	3.84	3	0
Congenital Zika Syndrome [description not available]	0	2.25	1	0
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	0	2.25	1	0
Fatty Liver, Nonalcoholic [description not available]	0	2.72	2	0
Cirrhosis, Liver [description not available]	0	2.41	1	0
Liver Cirrhosis Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.	0	2.41	1	0
Non-alcoholic Fatty Liver Disease Fatty liver finding without excessive ALCOHOL CONSUMPTION.	0	2.72	2	0
Hepatocellular Carcinoma [description not available]	0	3.33	1	0
Cancer of Liver [description not available]	0	3.33	1	0
Carcinoma, Hepatocellular A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.	0	3.33	1	0
Liver Neoplasms Tumors or cancer of the LIVER.	0	3.33	1	0
Innate Inflammatory Response [description not available]	0	2.21	1	0
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	0	2.21	1	0
Acute Liver Injury, Drug-Induced [description not available]	0	12.73	75	3
Cirrhoses, Experimental Liver [description not available]	0	2.25	1	0
Chemical and Drug Induced Liver Injury A spectrum of clinical liver diseases ranging from mild biochemical abnormalities to ACUTE LIVER FAILURE, caused by drugs, drug metabolites, herbal and dietary supplements and chemicals from the environment.	0	12.73	75	3
Genetic Predisposition [description not available]	0	2.69	2	0
Cognitive Decline [description not available]	0	2.31	1	0
Cognitive Dysfunction Diminished or impaired mental and/or intellectual function.	0	2.31	1	0
Liver Dysfunction [description not available]	0	3.56	1	1
Liver Diseases Pathological processes of the LIVER.	0	3.56	1	1
Acute Hepatic Failure [description not available]	0	2.17	1	0
Liver Failure, Acute A form of rapid-onset LIVER FAILURE, also known as fulminant hepatic failure, caused by severe liver injury or massive loss of HEPATOCYTES. It is characterized by sudden development of liver dysfunction and JAUNDICE. Acute liver failure may progress to exhibit cerebral dysfunction even HEPATIC COMA depending on the etiology that includes hepatic ISCHEMIA, drug toxicity, malignant infiltration, and viral hepatitis such as post-transfusion HEPATITIS B and HEPATITIS C.	0	2.17	1	0
Diabetes Mellitus A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE.	1	4.58	2	0
Diabetic Angiopathies VASCULAR DISEASES that are associated with DIABETES MELLITUS.	0	4.48	1	1
Cardiovascular Diseases Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.	0	4.48	1	1
Disease Exacerbation [description not available]	0	2.08	1	0
B16 Melanoma [description not available]	0	2.1	1	0
Kidney Diseases Pathological processes of the KIDNEY or its component tissues.	0	3.48	1	1
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	0	2.13	1	0
Anxiety Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.	0	2.13	1	0
Diseases, Metabolic [description not available]	0	3.06	1	0
Metabolic Diseases Generic term for diseases caused by an abnormal metabolic process. It can be congenital due to inherited enzyme abnormality (METABOLISM, INBORN ERRORS) or acquired due to disease of an endocrine organ or failure of a metabolically important organ such as the liver. (Stedman, 26th ed)	0	3.06	1	0
Weight Reduction [description not available]	0	2.07	1	0
Weight Loss Decrease in existing BODY WEIGHT.	0	2.07	1	0

tak-875

Cross-References

Synonyms (50)

Research Excerpts

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Drug Classes (1)

Protein Targets (19)

Potency Measurements

Inhibition Measurements

Activation Measurements

Biological Processes (116)

Molecular Functions (48)

Ceullar Components (34)

Bioassays (236)

Research

Studies (120)

Market Indicators

Research Demand Index: 31.12

Study Types

tak-875

Cross-References

Synonyms (50)

Research Excerpts

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Drug Classes (1)

Protein Targets (19)

Potency Measurements

Inhibition Measurements

Activation Measurements

Biological Processes (116)

Molecular Functions (48)

Ceullar Components (34)

Bioassays (236)

Research

Studies (120)

Market Indicators

Research Demand Index: 31.12

Study Types

Related Drugs (72)

Related Conditions (47)