Compounds > t0901317
Page last updated: 2024-11-08

t0901317

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Description

T0901317: an LXRalpha and LXRbeta agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID447912
CHEMBL ID62136
SCHEMBL ID457231
MeSH IDM0384448

Synonyms (70)

Synonym
HMS3268P10
BRD-K23383398-001-01-6
gtpl2755
t0901317
t 0901317
293754-55-9
n-(2,2,2-trifluoroethyl)-n-{4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl}benzenesulfonamide
t0901317, >=98%
NCGC00159555-01
to-901317
NCGC00159555-02
t-0901317
n-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-n-(2,2,2-trifluoroethyl)benzenesulfonamide
n-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl)-n-(2,2,2-trifluoroethyl)benzenesulfonamide
[3h]t0901317
bdbm19993
chembl62136 ,
n-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-n-(2,2,2-trifluoroethyl)benzenesulfonamide
sr-05000000453
SR-05000000453-1
ml125
t-1317
t-901317
DB07080
MLS002554297
smr001456586
NCGC00159555-03
BCP0726000164
1PQC
2O9I
4NB6
S7076
AKOS017345034
SCHEMBL457231
n-(2,2,2-trifluoroethyl)-n-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]benzenesulfonamide
to901317
benzenesulfonamide, n-(2,2,2-trifluoroethyl)-n-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-
AC-32646
n-(2,2,2-trifluoroethyl)-n-(4-(2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl)phenyl)benzenesulfonamide
A07663A39I ,
benzenesulfonamide, n-(2,2,2-trifluoroethyl)-n-(4-(2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl)phenyl)-
HMS3649G14
to 901317
t 1317
unii-a07663a39i
DTXSID6040618
J1.503.100J ,
HY-10626
EX-A1278
HMS3652B22
SR-05000000453-2
CS-5951
J-017492
NCGC00159555-06
sgiwfelwjpnfdh-uhfffaoysa-n
SW203816-2
benzenesulfonamide,n-(2,2,2-trifluoroethyl)-n-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-
BCP03658
HMS3677I08
Q27088909
SR-05000000453-5
HMS3413I08
SB19595
HMS3886B11
CCG-269558
A876482
C74506
n-(2,2,2-trifluoroethyl)-n-[4-[2,2,2-trifluoro-1-hydroxy-1(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide
n-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-n-(2,2, 2-trifluoroethyl)benzenesulfonamide
benzenesulfonamide,?n-(2,2,2-trifluoroethyl)-n-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-

Research Excerpts

Overview

T0901317 is a potent non-steroidal synthetic liver X receptor (LXR) agonist.

ExcerptReferenceRelevance
"T0901317 is a potent non-steroidal synthetic liver X receptor (LXR) agonist. "( The liver X receptor agonist T0901317 acts as androgen receptor antagonist in human prostate cancer cells.
Chen, RY; Chuu, CP; Hiipakka, RA; Kokontis, JM; Liao, S; Warner, KV; Xiang, J, 2007)		2.07

Treatment

Treatment in cigarette smoke-exposed mice failed to increase the ability of alveolar macrophages to export cholesterol and markedly exacerbated IL-1α release. T0901317 treatment significantly attenuated STZ and HFD-induced memory deficits, biochemical and histopathological alterations as well as HFD induced rise in cholesterol content.

ExcerptReferenceRelevance
"T0901317 treatment increased ABCA1 and ABCG1 levels; reversed macrophage-derived foam-cell formation in THP-1 macrophages and reduced atherosclerotic lesions in ApoE"( Homocysteine accelerates atherosclerosis via inhibiting LXRα-mediated ABCA1/ABCG1-dependent cholesterol efflux from macrophages.
Bian, Y; Cong, G; Jia, S; Jin, P; Ma, X; Sha, Y; Wang, K; Yan, R; Yuan, Z; Zhou, J, 2018)		1.2
"T0901317 treatment in cigarette smoke-exposed mice failed to increase the ability of alveolar macrophages to export cholesterol and markedly exacerbated IL-1α release."( Pharmacological activation of liver X receptor during cigarette smoke exposure adversely affects alveolar macrophages and pulmonary surfactant homeostasis.
Aubin, S; Beaulieu, MJ; Jubinville, É; Laplante, M; Maranda-Robitaille, M; Milad, N; Morissette, MC; Paré, MÈ; Pineault, M; Routhier, J; Talbot, M, 2019)		1.24
"T0901317 treatment significantly attenuated STZ and HFD-induced memory deficits, biochemical and histopathological alterations as well as HFD induced rise in cholesterol content."( Liver X receptor agonist T0901317 reduces neuropathological changes and improves memory in mouse models of experimental dementia.
Singh, N; Sodhi, RK, 2014)		1.43
"T0901317 treatment induced significant insulin resistance in C57BL/6 mice."( Regulation of insulin resistance and adiponectin signaling in adipose tissue by liver X receptor activation highlights a cross-talk with PPARγ.
Li, H; Lu, W; Pan, Q; Wu, F; Yin, X; Yu, D; Zhang, S; Zheng, F, 2014)		1.12
"T0901317 treatment suppressed PSA expression while GW3965 treatment enhanced PSA expression."( Divergent effect of liver X receptor agonists on prostate-specific antigen expression is dependent on androgen receptor in prostate carcinoma cells.
Chang, PL; Chen, WT; Chung, LC; Feng, TH; Juang, HH; Lee, TY; Tsui, KH, 2015)		1.14
"T0901317 pretreatment also reduced HIV-induced dyslipidemia in infected mice."( Stimulation of Liver X Receptor Has Potent Anti-HIV Effects in a Humanized Mouse Model of HIV Infection.
Bukrinsky, M; Dubrovsky, L; Fitzgerald, ML; Karandish, S; Pushkarsky, T; Raj, DS; Ramezani, A; Sviridov, D, 2015)		1.14
"T0901317 treatment evidently abolished the high level of TGF-β1 and inhibited NF-κB DNA-binding activity in lung."( The effect of a liver-X-receptor ligand on bleomycin induced pulmonary fibrosis in mice.
Chen, Q; Gu, W; Shi, Y; Yan, H, 2016)		1.16
"T0901317 treatment decreased atherosclerosis with a much more pronounced response and dose dependence in the innominate artery than in the aortic sinus."( Differential anti-atherosclerotic effects in the innominate artery and aortic sinus by the liver X receptor agonist T0901317.
Getz, GS; Hiipakka, RA; Liao, S; Peng, D; Reardon, CA, 2009)		1.28
"T0901317 treatment reduced the aortic atherosclerotic lesion area by 64.2% in the prevention group and 58.3% in the treatment group."( Liver X receptor agonist T0901317 reduces atherosclerotic lesions in apoE-/- mice by up-regulating NPC1 expression.
Cao, D; Dai, X; Hao, X; Hu, Y; Li, X; Long, Z; Ou, X; Tang, C; Tang, Y, 2008)		1.37
"Upon T0901317 treatment, hyperinsulinemia failed to reduce VLDL particle size or suppress VLDL-TG production rate, but the contribution of DNL to VLDL-TG was increased."( Reduced insulin-mediated inhibition of VLDL secretion upon pharmacological activation of the liver X receptor in mice.
Grefhorst, A; Parks, EJ, 2009)		0.81
"T0901317 treatment increased absolute de novo synthesis and chain elongation of hepatic oleic acid in dams and fetuses."( Fetal liver X receptor activation acutely induces lipogenesis but does not affect plasma lipid response to a high-fat diet in adult mice.
Baller, JF; Huijkman, NC; Kuipers, F; Plösch, T; van Dijk, TH; van Meer, H; van Straten, EM; Verkade, HJ, 2009)		1.07
"The T0901317-treated animals showed significant improvement in the plasma level of lactate, whereas base deficit and bicarbonate levels both trended toward improvement."( Liver X receptor α activation with the synthetic ligand T0901317 reduces lung injury and inflammation after hemorrhage and resuscitation via inhibition of the nuclear factor κB pathway.
Denenberg, A; Hake, PW; Lentsch, A; O'Connor, M; Piraino, G; Solan, PD; Zingarelli, B, 2011)		1.1
"T0901317 treatment decreased the percentage of the cell population in S-phase and caused G(1) cell cycle arrest."( Antiproliferative effect of LXR agonists T0901317 and 22(R)-hydroxycholesterol on multiple human cancer cell lines.
Chuu, CP; Lin, HP, 2010)		1.35
"T0901317 treatment also inhibited premature differentiation of Bergmann glia during cerebellum development, which is related to the decreased levels of TGF-β1 and Smad4 in the cerebellum."( Liver X receptor agonist treatment promotes the migration of granule neurons during cerebellar development.
Fan, X; Xing, Y; Ying, D, 2010)		1.08
"T0901317 pretreatment efficiently reduced the production of TNF-α, IL-1β, and IL-6, while elevated the level of IL-10 in BALF of rats with ALI."( Synthetic LXR agonist T0901317 attenuates lipopolysaccharide-induced acute lung injury in rats.
Dai, C; Liu, M; Luo, M; Tang, C; Wang, D; Wang, J; Wang, Y; Xiao, J; Yan, P; Zhang, X, 2011)		1.41
"T0901317 treatment induced fecal neutral sterol secretion by ~300% in wild-type but not in Lxrα deficient mice."( Pharmacological LXR activation reduces presence of SR-B1 in liver membranes contributing to LXR-mediated induction of HDL-cholesterol.
Boesjes, M; Brufau, G; Grefhorst, A; Groen, AK; Kuipers, F; Oosterveer, MH, 2012)		1.1
"T0901317-treated mice presented increased [³H]cholesterol in plasma and HDL 48 h after the label injection."( Resveratrol administration or SIRT1 overexpression does not increase LXR signaling and macrophage-to-feces reverse cholesterol transport in vivo.
Andres-Lacueva, C; Blanco-Vaca, F; Escolà-Gil, JC; Julve, J; Lee-Rueckert, M; Llaverias, G; Silvennoinen, R; Urpi-Sarda, M, 2013)		1.11
"T0901317 treatment induced reversible aggregation of lipids in the liver."( The liver X receptor agonist T0901317 protects mice from high fat diet-induced obesity and insulin resistance.
Gao, M; Liu, D, 2013)		1.4
"T0901317 treatment of 11-week-old APP23 mice for 6 days showed a significant increase in ABCA1 expression and a decrease in the ratio of soluble APP (sAPP)beta- to sAPPalpha-cleavage products."( The liver X receptor ligand T0901317 decreases amyloid beta production in vitro and in a mouse model of Alzheimer's disease.
Glorioso, JC; Huang, S; Koldamova, RP; Lazo, JS; Lefterov, IM; Roth, MG; Staufenbiel, M; Walter, M; Wolfe, D, 2005)		1.34
"In T0901317-treated mice, SSAO gene expression was significantly decreased in the aorta, liver, small intestine, and brain."( Synthetic liver X receptor agonist T0901317 inhibits semicarbazide-sensitive amine oxidase gene expression and activity in apolipoprotein E knockout mice.
Cao, D; Dai, X; Hao, X; Hu, Y; Li, X; Ou, X; Tang, C; Tang, Y, 2008)		1.14
"T0901317 treatment reduced aortic atherosclerotic lesion area by 64.2% in prevention group (P < 0.001) and 58.3% in treatment group (P < 0.001) and resulted in a reduction in macrophage content."( The effect of T0901317 on ATP-binding cassette transporter A1 and Niemann-Pick type C1 in apoE-/- mice.
Cao, DL; Dai, XY; Hao, XR; Hu, YW; Li, XX; Ou, X; Tang, CK; Tang, YL, 2008)		1.43
"Treatment with T0901317 inhibited the tube formation and migration of HUVECs and reduced the"( Activation of liver X receptor suppresses angiogenesis
Chang, CH; Chen, TH; Cheng, HC; Chung, CJ; Chuu, CP; Huang, SH; Lai, CJ; Lin, CY; Wang, HD, 2017)		0.79
"Treatment with T0901317 on hepatocytes increased intracellular fat accumulation and this increase was suppressed by resveratrol; the suppressive effect of resveratrol was greatly repressed by Compound C which is an inhibitor of AMPK."( Resveratrol suppresses T0901317-induced hepatic fat accumulation in mice.
Gao, M; Liu, D, 2013)		1.04
"Treatment with T0901317 improved glucose tolerance of diabetic mice, which was associated with repressed expression of key genes involved in hepatic gluconeogenesis such as Pepck and G6p."( Cold Exposure Improves the Anti-diabetic Effect of T0901317 in Streptozotocin-Induced Diabetic Mice.
Gao, M; Liu, D; Ma, Y; Zhang, C, 2015)		1.01
"Pre-treatment with T0901317 before LPS stimulation can suppress the expressions of IRF3 and GRIP1 to inhibit the inflammation and hence Kupffer cell activation."( [Liver X receptor alpha inhibits LPS-induced inflammation by down-regulating IFR3 and GRIP1 in mouse Kupffer cells].
Gong, JP; Huang, QY; Ou, ZB; Sun, K; Tu, B; Wei, SD, 2009)		0.68
"Treatment with T0901317, 1 and 6 h after the SCI, significantly decreased (i) the degree of spinal cord inflammation and tissue injury (histological score); (ii) neutrophil infiltration (myeloperoxidase activity); (iii) inducible nitric oxide synthase expression; (iv) nitrotyrosine, lipid peroxidation, and poly-ADP-ribose formation; (v) pro-inflammatory cytokines expression; (vi) nuclear factor-kappa B activation; and (vii) apoptosis (terminal deoxynucleotidyltransferase-mediated UTP end labeling staining, FAS ligand, Bax, and Bcl-2 expression)."( Liver X receptor agonist treatment regulates inflammatory response after spinal cord trauma.
Bramanti, P; Crisafulli, C; Cuzzocrea, S; Di Paola, R; Galuppo, M; Genovese, T; Mazzon, E; Paterniti, I, 2010)		0.7
"Treatment with T0901317 significantly improved the cardiac and stroke volume indices as well as the heart rate of rats during the resuscitation period as compared with vehicle-treated rats."( Liver X receptor α activation with the synthetic ligand T0901317 reduces lung injury and inflammation after hemorrhage and resuscitation via inhibition of the nuclear factor κB pathway.
Denenberg, A; Hake, PW; Lentsch, A; O'Connor, M; Piraino, G; Solan, PD; Zingarelli, B, 2011)		0.96
"Treatment with T0901317 also increased liver ABCA1, G1, and G5 gene expression and reduced intestinal cholesterol absorption which were changes that were associated with a 2.8-fold increase in macrophage-derived [³H]cholesterol in feces."( Resveratrol administration or SIRT1 overexpression does not increase LXR signaling and macrophage-to-feces reverse cholesterol transport in vivo.
Andres-Lacueva, C; Blanco-Vaca, F; Escolà-Gil, JC; Julve, J; Lee-Rueckert, M; Llaverias, G; Silvennoinen, R; Urpi-Sarda, M, 2013)		0.73

Compound-Compound Interactions

ExcerptReferenceRelevance
"In vitro approaches for predicting drug-drug interactions (DDIs) caused by alterations in transporter protein regulation are not well established."( Hepatic Transporter Alterations by Nuclear Receptor Agonist T0901317 in Sandwich-Cultured Human Hepatocytes: Proteomic Analysis and PBPK Modeling to Evaluate Drug-Drug Interaction Risk.
Brouwer, KLR; Guo, C; Ito, K; Malinen, MM; Sjöstedt, N, 2020)		0.8

Bioavailability

ExcerptReferenceRelevance
" Quinoline 16 showed good oral bioavailability and in vivo efficacy in a LDLr knockout mouse model for lesions."( Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.
Azam, F; Basso, M; Bonn, T; Chen, L; Clerin, V; Collini, M; Enroth, C; Farnegardh, M; Feingold, I; Goos-Nilsson, A; Halpern, A; Hu, B; Huselton, C; Keith, J; Liu, QY; Miller, C; Nambi, P; Quinet, E; Resmini, C; Savio, D; Singhaus, R; Unwalla, R; Wilhelmsson, A; Wrobel, J, 2006)		0.33
" We conclude that LXR agonism improves TNF-α-impaired endothelial function via its anti-apoptotic, anti-inflammatory, and anti-oxidative properties and its capacity to restore TNF-α-impaired NO bioavailability independent of its cholesterol-modulating effects."( LXR agonism improves TNF-α-induced endothelial dysfunction in the absence of its cholesterol-modulating effects.
Lorenz, M; Miteva, K; Schultheiss, HP; Spillmann, F; Stangl, V; Tschöpe, C; Van Linthout, S, 2014)		0.4
" We sought to determine if the effects of LXR activation can be ameliorated through modification of cholesterol bioavailability or inhibition of LXR-driven cholesterol efflux in trophoblasts."( Impairment of trophoblast survival and differentiation by LXR ligands is prevented by cholesterol but not ABCA1 silencing.
Harmon, CM; Larkin, JC; McGonigal, S, 2018)		0.48
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51

Dosage Studied

ExcerptRelevanceReference
" After oral dosing at 10 mg/kg to C57BL/6 mice, 12 increased expression of the reverse cholesterol transporter ABCA1 in the small intestine and peripheral macrophages and increased the plasma concentrations of HDL cholesterol by 30%."( Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines.
Beaudet, EJ; Binz, JG; Collins, JL; Fivush, AM; Galardi, CM; Kliewer, SA; Lewis, MC; Moore, LB; Morgan, DG; Parks, DJ; Plunket, KD; Tippin, TK; Watson, MA; Whitney, KD; Willson, TM; Wilson, JG, 2002)		0.31
" The appearance of these HDL particles upon oral dosing of T0901317 in C57/BL6 mice was closely correlated with the increased plasma PLTP activity and liver PLTP mRNA levels."( Phospholipid transfer protein is regulated by liver X receptors in vivo.
Bensch, WR; Beyer, TP; Cao, G; Eacho, PI; Gao, H; Jiang, XC; Kauffman, RF; Liang, Y; Ryan, TP; Schmidt, RJ; Yang, XP; Zhang, Y, 2002)		0.56
" These findings were replicated by subchronic dosing studies in non-human primates, where cerebrospinal fluid levels of apoE and amyloid-β peptides were increased concomitantly with an improved peripheral lipid profile relative to that of nonselective compounds."( Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease.
Ballard, J; Bennett, DJ; Bilodeau, MT; Brnardic, E; Chen, Z; Cooke, AJ; Cosden, M; DiMuzio, J; Fradera, X; Holahan, M; Kim, Y; Klein, DJ; Li, J; Li, Y; Lu, J; Maxwell, J; Meissner, R; Michener, MS; Nanda, KK; Parthasarathy, G; Rada, V; Renger, J; Rudd, MT; Stachel, SJ; Suon, S; Szczerba, P; Uebele, VN; Uslaner, JM; Wessner, K; Wu, Z; Wuelfing, P; Yuan, Y; Zerbinatti, C, 2016)		0.43
" Dose-response curves demonstrated that plasma concentrations observed in clinical trials are sufficient for LXR activation and thus could account for LXR-mediated side-effects such as hypercholesterolemia and hyperlipidemia."( DrugBank screening revealed alitretinoin and bexarotene as liver X receptor modulators.
Achenbach, J; Heitel, P; Merk, D; Moser, D; Proschak, E, 2017)		0.46
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (53)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
glp-1 receptor, partialHomo sapiens (human)Potency11.22020.01846.806014.1254AID624417
pregnane X receptorRattus norvegicus (Norway rat)Potency1.12200.025127.9203501.1870AID651751
TDP1 proteinHomo sapiens (human)Potency26.88940.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency0.63100.180013.557439.8107AID1468
AR proteinHomo sapiens (human)Potency44.66840.000221.22318,912.5098AID588516
Smad3Homo sapiens (human)Potency28.93420.00527.809829.0929AID588855
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency0.18870.011212.4002100.0000AID1030
PINK1Homo sapiens (human)Potency26.17872.818418.895944.6684AID624263
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency39.81070.000214.376460.0339AID588533
retinoid X nuclear receptor alphaHomo sapiens (human)Potency12.58930.000817.505159.3239AID588546
farnesoid X nuclear receptorHomo sapiens (human)Potency23.22330.375827.485161.6524AID588526; AID588527
pregnane X nuclear receptorHomo sapiens (human)Potency0.02000.005428.02631,258.9301AID720659
estrogen nuclear receptor alphaHomo sapiens (human)Potency44.66840.000229.305416,493.5996AID588513
67.9K proteinVaccinia virusPotency14.17330.00018.4406100.0000AID720579; AID720580
ParkinHomo sapiens (human)Potency26.17870.819914.830644.6684AID624263
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency44.66840.001024.504861.6448AID588534
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency35.48130.001019.414170.9645AID588536
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency42.80000.023723.228263.5986AID588541; AID588543
IDH1Homo sapiens (human)Potency23.10930.005210.865235.4813AID686970
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency0.04470.010039.53711,122.0200AID588547
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency112.20203.548119.542744.6684AID743266
nuclear factor NF-kappa-B p105 subunit isoform 1Homo sapiens (human)Potency50.11874.466824.832944.6684AID651749
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency56.82760.000627.21521,122.0200AID651741; AID720636
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency79.43280.050127.073689.1251AID588590
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency1.99530.00798.23321,122.0200AID2551
DNA polymerase kappa isoform 1Homo sapiens (human)Potency35.48130.031622.3146100.0000AID588579
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency8.91256.309660.2008112.2020AID720709
Alpha-synucleinHomo sapiens (human)Potency35.48130.56239.398525.1189AID652106
TAR DNA-binding protein 43Homo sapiens (human)Potency22.38721.778316.208135.4813AID652104
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency44.66843.981146.7448112.2020AID720708
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Oxysterols receptor LXR-betaHomo sapiens (human)IC50 (µMol)0.10000.10000.10000.1000AID977608
Chain A, Oxysterols receptor LXR-betaHomo sapiens (human)IC50 (µMol)0.10000.10000.10000.1000AID977608
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)IC50 (µMol)0.03860.00240.31511.7700AID1775046; AID1798107; AID293510
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.02600.00010.739610.0000AID1172001
Retinoic acid receptor RXR-alphaHomo sapiens (human)Ki0.12680.00040.56927.6320AID1172000; AID1172001; AID1243261; AID1243262
Nuclear receptor ROR-alphaHomo sapiens (human)IC50 (µMol)8.12240.19951.59982.6000AID1139695; AID1168690; AID1177720; AID1398740; AID1595545
Nuclear receptor ROR-alphaHomo sapiens (human)Ki0.13200.13200.15200.1720AID1177722
Alpha-glucosidase MAL32Saccharomyces cerevisiae S288CIC50 (µMol)100.00004.80007.10009.9000AID1798364
Presenilin-1Homo sapiens (human)IC50 (µMol)22.25000.00010.23785.6800AID309256; AID309258
Presenilin-2Homo sapiens (human)IC50 (µMol)22.25000.00010.24355.6800AID309256; AID309258
Nuclear receptor ROR-gammaHomo sapiens (human)IC50 (µMol)1.61130.06001.93579.4100AID1059103; AID1127096; AID1127097; AID1127100; AID1139697; AID1168683; AID1168688; AID1177719; AID1177729; AID1287457; AID1295291; AID1398744; AID1595542; AID1821363; AID1821366
Nuclear receptor ROR-gammaHomo sapiens (human)Ki0.05100.05100.08900.1110AID1177721
Oxysterols receptor LXR-betaHomo sapiens (human)IC50 (µMol)6.32070.00790.92859.9000AID1249975; AID1797933; AID1798364; AID1798629; AID1799289; AID271505; AID273407; AID313446; AID345471; AID391700; AID424748; AID451979; AID452860; AID452959; AID454632; AID454925; AID472479; AID474683; AID478580; AID653687; AID703029
Oxysterols receptor LXR-betaHomo sapiens (human)Ki0.06910.00220.07300.3520AID1172001; AID1243262; AID1316521; AID1562690; AID1691874
Oxysterols receptor LXR-alphaHomo sapiens (human)IC50 (µMol)6.54020.00901.06049.9000AID1249975; AID1595550; AID1797932; AID1798364; AID1798629; AID1799289; AID271504; AID273406; AID313447; AID345472; AID391699; AID424749; AID451978; AID452861; AID452960; AID454631; AID454924; AID472480; AID478581; AID653688; AID703029
Oxysterols receptor LXR-alphaHomo sapiens (human)Ki0.09500.02400.11630.2300AID1172000; AID1243261; AID1316520
Gamma-secretase subunit APH-1BHomo sapiens (human)IC50 (µMol)22.25000.00010.24355.6800AID309256; AID309258
NicastrinHomo sapiens (human)IC50 (µMol)22.25000.00010.24355.6800AID309256; AID309258
Nuclear receptor ROR-betaHomo sapiens (human)IC50 (µMol)7.50590.12595.062910.0000AID1168686; AID1168691
Gamma-secretase subunit APH-1AHomo sapiens (human)IC50 (µMol)22.25000.00010.24355.6800AID309256; AID309258
Bile acid receptorHomo sapiens (human)IC50 (µMol)5.30000.01834.560310.0000AID1595551
Gamma-secretase subunit PEN-2Homo sapiens (human)IC50 (µMol)22.25000.00010.24425.6800AID309256; AID309258
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC50 (µMol)0.06840.00203.519610.0000AID1059091; AID1177755; AID1287454; AID1368956; AID1398739; AID1543103; AID1605742; AID293511
Plasma kallikreinHomo sapiens (human)EC50 (µMol)0.04000.04000.20350.3670AID299788
Cytochrome P450 3A4Homo sapiens (human)EC50 (µMol)0.02000.00010.23283.2000AID1301876
Retinoic acid receptor RXR-alphaHomo sapiens (human)EC50 (µMol)0.00010.00010.34279.1000AID1691869; AID1691870
Nuclear receptor ROR-alphaHomo sapiens (human)EC50 (µMol)5.00005.00005.00005.0000AID1059098; AID1177751
Presenilin-1Homo sapiens (human)EC50 (µMol)3.60000.00010.68575.7000AID309260
Presenilin-2Homo sapiens (human)EC50 (µMol)3.60000.00011.06175.7000AID309260
Nuclear receptor ROR-gammaHomo sapiens (human)EC50 (µMol)0.27280.02000.70359.0000AID1059100; AID1059102; AID1177731; AID1177749; AID1368955
Oxysterols receptor LXR-betaHomo sapiens (human)EC50 (µMol)0.12340.00010.40077.3000AID1059093; AID1139700; AID1168706; AID1172003; AID1172005; AID1177754; AID1192873; AID1233302; AID1243265; AID1249980; AID1287452; AID1301876; AID1306543; AID1368963; AID1373988; AID1480571; AID1576220; AID1614979; AID1686020; AID1691870; AID1797957; AID1798792; AID1892224; AID240219; AID271507; AID273408; AID293512; AID299787; AID299789; AID307303; AID307304; AID313450; AID313460; AID345473; AID418425; AID418427; AID424751; AID451981; AID452863; AID452962; AID454635; AID472468; AID472470; AID472476; AID472478; AID474686; AID478582; AID569815; AID703193; AID715944; AID758939
Oxysterols receptor LXR-betaHomo sapiens (human)Kd0.10300.10300.10300.1030AID758944
Oxysterols receptor LXR-alphaHomo sapiens (human)EC50 (µMol)0.20130.00010.63026.7100AID101836; AID101837; AID1059095; AID1139698; AID1172002; AID1172005; AID1177753; AID1192871; AID1233300; AID1243263; AID1249978; AID1287451; AID1301877; AID1306539; AID1368961; AID1373986; AID1480570; AID1576218; AID1594667; AID1614978; AID1691869; AID1797956; AID1797958; AID1798792; AID1892223; AID240223; AID262339; AID271506; AID299788; AID307302; AID313452; AID313460; AID345475; AID418426; AID418705; AID424922; AID451981; AID452963; AID454634; AID474685; AID569814; AID703198; AID715945; AID758940
Oxysterols receptor LXR-alphaHomo sapiens (human)Kd0.09240.09243.12566.9700AID758943
Oxysterols receptor LXR-betaMus musculus (house mouse)EC50 (µMol)0.02700.02700.02700.0270AID452866
Oxysterols receptor LXR-betaRattus norvegicus (Norway rat)EC50 (µMol)0.03000.03000.07700.1240AID1542682
Gamma-secretase subunit APH-1BHomo sapiens (human)EC50 (µMol)3.60000.00011.06175.7000AID309260
NicastrinHomo sapiens (human)EC50 (µMol)3.60000.00010.79995.7000AID309260
Nuclear receptor ROR-betaHomo sapiens (human)EC50 (µMol)6.00006.00006.00006.0000AID1059099; AID1177750
Gamma-secretase subunit APH-1AHomo sapiens (human)EC50 (µMol)3.60000.00010.79995.7000AID309260
Bile acid receptorHomo sapiens (human)EC50 (µMol)1.90000.00401.419110.0000AID1059097; AID1177752; AID1287453
Gamma-secretase subunit PEN-2Homo sapiens (human)EC50 (µMol)3.60000.00010.79995.7000AID309260
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
interferon gamma precursorHomo sapiens (human)AC5016.60000.128015.173038.6100AID1259418; AID1259420
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (352)

Processvia Protein(s)Taxonomy
negative regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic metabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
signal transductionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
steroid metabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of gene expressionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic catabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic transportNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group I member 2Homo sapiens (human)
cell differentiationNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group I member 2Homo sapiens (human)
angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
adaptive immune responseRap guanine nucleotide exchange factor 3Homo sapiens (human)
signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 3Homo sapiens (human)
associative learningRap guanine nucleotide exchange factor 3Homo sapiens (human)
Rap protein signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of actin cytoskeleton organizationRap guanine nucleotide exchange factor 3Homo sapiens (human)
negative regulation of syncytium formation by plasma membrane fusionRap guanine nucleotide exchange factor 3Homo sapiens (human)
intracellular signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of GTPase activityRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of protein export from nucleusRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of stress fiber assemblyRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of syncytium formation by plasma membrane fusionRap guanine nucleotide exchange factor 3Homo sapiens (human)
establishment of endothelial barrierRap guanine nucleotide exchange factor 3Homo sapiens (human)
cellular response to cAMPRap guanine nucleotide exchange factor 3Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 3Homo sapiens (human)
Factor XII activationPlasma kallikreinHomo sapiens (human)
proteolysisPlasma kallikreinHomo sapiens (human)
blood coagulationPlasma kallikreinHomo sapiens (human)
zymogen activationPlasma kallikreinHomo sapiens (human)
plasminogen activationPlasma kallikreinHomo sapiens (human)
fibrinolysisPlasma kallikreinHomo sapiens (human)
positive regulation of fibrinolysisPlasma kallikreinHomo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
positive regulation of cholesterol effluxRetinoic acid receptor RXR-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIRetinoic acid receptor RXR-alphaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIRetinoic acid receptor RXR-alphaHomo sapiens (human)
positive regulation of thyroid hormone mediated signaling pathwayRetinoic acid receptor RXR-alphaHomo sapiens (human)
hormone-mediated signaling pathwayRetinoic acid receptor RXR-alphaHomo sapiens (human)
positive regulation of bone mineralizationRetinoic acid receptor RXR-alphaHomo sapiens (human)
positive regulation of transporter activityRetinoic acid receptor RXR-alphaHomo sapiens (human)
response to retinoic acidRetinoic acid receptor RXR-alphaHomo sapiens (human)
peroxisome proliferator activated receptor signaling pathwayRetinoic acid receptor RXR-alphaHomo sapiens (human)
mRNA transcription by RNA polymerase IIRetinoic acid receptor RXR-alphaHomo sapiens (human)
steroid hormone mediated signaling pathwayRetinoic acid receptor RXR-alphaHomo sapiens (human)
positive regulation of DNA-templated transcriptionRetinoic acid receptor RXR-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIRetinoic acid receptor RXR-alphaHomo sapiens (human)
retinoic acid receptor signaling pathwayRetinoic acid receptor RXR-alphaHomo sapiens (human)
positive regulation of vitamin D receptor signaling pathwayRetinoic acid receptor RXR-alphaHomo sapiens (human)
cell differentiationRetinoic acid receptor RXR-alphaHomo sapiens (human)
anatomical structure developmentRetinoic acid receptor RXR-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear receptor ROR-alphaHomo sapiens (human)
angiogenesisNuclear receptor ROR-alphaHomo sapiens (human)
regulation of DNA-templated transcriptionNuclear receptor ROR-alphaHomo sapiens (human)
xenobiotic metabolic processNuclear receptor ROR-alphaHomo sapiens (human)
nitric oxide biosynthetic processNuclear receptor ROR-alphaHomo sapiens (human)
regulation of smoothened signaling pathwayNuclear receptor ROR-alphaHomo sapiens (human)
positive regulation of vascular endothelial growth factor productionNuclear receptor ROR-alphaHomo sapiens (human)
regulation of glucose metabolic processNuclear receptor ROR-alphaHomo sapiens (human)
regulation of steroid metabolic processNuclear receptor ROR-alphaHomo sapiens (human)
cerebellar Purkinje cell differentiationNuclear receptor ROR-alphaHomo sapiens (human)
cerebellar granule cell precursor proliferationNuclear receptor ROR-alphaHomo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor ROR-alphaHomo sapiens (human)
circadian regulation of gene expressionNuclear receptor ROR-alphaHomo sapiens (human)
cellular response to sterolNuclear receptor ROR-alphaHomo sapiens (human)
cholesterol homeostasisNuclear receptor ROR-alphaHomo sapiens (human)
muscle cell differentiationNuclear receptor ROR-alphaHomo sapiens (human)
positive regulation of circadian rhythmNuclear receptor ROR-alphaHomo sapiens (human)
regulation of macrophage activationNuclear receptor ROR-alphaHomo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionNuclear receptor ROR-alphaHomo sapiens (human)
negative regulation of fat cell differentiationNuclear receptor ROR-alphaHomo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor ROR-alphaHomo sapiens (human)
cGMP metabolic processNuclear receptor ROR-alphaHomo sapiens (human)
negative regulation of inflammatory responseNuclear receptor ROR-alphaHomo sapiens (human)
triglyceride homeostasisNuclear receptor ROR-alphaHomo sapiens (human)
cellular response to interleukin-1Nuclear receptor ROR-alphaHomo sapiens (human)
cellular response to tumor necrosis factorNuclear receptor ROR-alphaHomo sapiens (human)
cellular response to hypoxiaNuclear receptor ROR-alphaHomo sapiens (human)
T-helper 17 cell differentiationNuclear receptor ROR-alphaHomo sapiens (human)
regulation of transcription by RNA polymerase IINuclear receptor ROR-alphaHomo sapiens (human)
calcium ion homeostasisAlpha-synucleinHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIAlpha-synucleinHomo sapiens (human)
microglial cell activationAlpha-synucleinHomo sapiens (human)
positive regulation of receptor recyclingAlpha-synucleinHomo sapiens (human)
positive regulation of neurotransmitter secretionAlpha-synucleinHomo sapiens (human)
negative regulation of protein kinase activityAlpha-synucleinHomo sapiens (human)
fatty acid metabolic processAlpha-synucleinHomo sapiens (human)
neutral lipid metabolic processAlpha-synucleinHomo sapiens (human)
phospholipid metabolic processAlpha-synucleinHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
mitochondrial membrane organizationAlpha-synucleinHomo sapiens (human)
adult locomotory behaviorAlpha-synucleinHomo sapiens (human)
response to xenobiotic stimulusAlpha-synucleinHomo sapiens (human)
response to iron(II) ionAlpha-synucleinHomo sapiens (human)
regulation of phospholipase activityAlpha-synucleinHomo sapiens (human)
negative regulation of platelet-derived growth factor receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
regulation of glutamate secretionAlpha-synucleinHomo sapiens (human)
regulation of dopamine secretionAlpha-synucleinHomo sapiens (human)
synaptic vesicle exocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle primingAlpha-synucleinHomo sapiens (human)
regulation of transmembrane transporter activityAlpha-synucleinHomo sapiens (human)
negative regulation of microtubule polymerizationAlpha-synucleinHomo sapiens (human)
receptor internalizationAlpha-synucleinHomo sapiens (human)
protein destabilizationAlpha-synucleinHomo sapiens (human)
response to magnesium ionAlpha-synucleinHomo sapiens (human)
negative regulation of transporter activityAlpha-synucleinHomo sapiens (human)
response to lipopolysaccharideAlpha-synucleinHomo sapiens (human)
negative regulation of monooxygenase activityAlpha-synucleinHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationAlpha-synucleinHomo sapiens (human)
response to type II interferonAlpha-synucleinHomo sapiens (human)
cellular response to oxidative stressAlpha-synucleinHomo sapiens (human)
SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
positive regulation of SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
regulation of locomotionAlpha-synucleinHomo sapiens (human)
dopamine biosynthetic processAlpha-synucleinHomo sapiens (human)
mitochondrial ATP synthesis coupled electron transportAlpha-synucleinHomo sapiens (human)
regulation of macrophage activationAlpha-synucleinHomo sapiens (human)
positive regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of neuron apoptotic processAlpha-synucleinHomo sapiens (human)
positive regulation of endocytosisAlpha-synucleinHomo sapiens (human)
negative regulation of exocytosisAlpha-synucleinHomo sapiens (human)
positive regulation of exocytosisAlpha-synucleinHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityAlpha-synucleinHomo sapiens (human)
synaptic vesicle endocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle transportAlpha-synucleinHomo sapiens (human)
positive regulation of inflammatory responseAlpha-synucleinHomo sapiens (human)
regulation of acyl-CoA biosynthetic processAlpha-synucleinHomo sapiens (human)
protein tetramerizationAlpha-synucleinHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolAlpha-synucleinHomo sapiens (human)
neuron apoptotic processAlpha-synucleinHomo sapiens (human)
dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of serotonin uptakeAlpha-synucleinHomo sapiens (human)
regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
negative regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
excitatory postsynaptic potentialAlpha-synucleinHomo sapiens (human)
long-term synaptic potentiationAlpha-synucleinHomo sapiens (human)
positive regulation of inositol phosphate biosynthetic processAlpha-synucleinHomo sapiens (human)
negative regulation of thrombin-activated receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
response to interleukin-1Alpha-synucleinHomo sapiens (human)
cellular response to copper ionAlpha-synucleinHomo sapiens (human)
cellular response to epinephrine stimulusAlpha-synucleinHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityAlpha-synucleinHomo sapiens (human)
supramolecular fiber organizationAlpha-synucleinHomo sapiens (human)
negative regulation of mitochondrial electron transport, NADH to ubiquinoneAlpha-synucleinHomo sapiens (human)
positive regulation of glutathione peroxidase activityAlpha-synucleinHomo sapiens (human)
positive regulation of hydrogen peroxide catabolic processAlpha-synucleinHomo sapiens (human)
regulation of synaptic vesicle recyclingAlpha-synucleinHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processAlpha-synucleinHomo sapiens (human)
positive regulation of protein localization to cell peripheryAlpha-synucleinHomo sapiens (human)
negative regulation of chaperone-mediated autophagyAlpha-synucleinHomo sapiens (human)
regulation of presynapse assemblyAlpha-synucleinHomo sapiens (human)
amyloid fibril formationAlpha-synucleinHomo sapiens (human)
synapse organizationAlpha-synucleinHomo sapiens (human)
chemical synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of low-density lipoprotein receptor activityPresenilin-1Homo sapiens (human)
endoplasmic reticulum calcium ion homeostasisPresenilin-1Homo sapiens (human)
cell-cell adhesionPresenilin-1Homo sapiens (human)
autophagosome assemblyPresenilin-1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIPresenilin-1Homo sapiens (human)
blood vessel developmentPresenilin-1Homo sapiens (human)
cell fate specificationPresenilin-1Homo sapiens (human)
somitogenesisPresenilin-1Homo sapiens (human)
neuron migrationPresenilin-1Homo sapiens (human)
positive regulation of receptor recyclingPresenilin-1Homo sapiens (human)
negative regulation of protein phosphorylationPresenilin-1Homo sapiens (human)
positive regulation of protein phosphorylationPresenilin-1Homo sapiens (human)
heart loopingPresenilin-1Homo sapiens (human)
positive regulation of L-glutamate import across plasma membranePresenilin-1Homo sapiens (human)
hematopoietic progenitor cell differentiationPresenilin-1Homo sapiens (human)
astrocyte activation involved in immune responsePresenilin-1Homo sapiens (human)
T cell activation involved in immune responsePresenilin-1Homo sapiens (human)
neural retina developmentPresenilin-1Homo sapiens (human)
protein glycosylationPresenilin-1Homo sapiens (human)
membrane protein ectodomain proteolysisPresenilin-1Homo sapiens (human)
mitochondrial transportPresenilin-1Homo sapiens (human)
DNA damage responsePresenilin-1Homo sapiens (human)
response to oxidative stressPresenilin-1Homo sapiens (human)
Notch receptor processingPresenilin-1Homo sapiens (human)
learning or memoryPresenilin-1Homo sapiens (human)
memoryPresenilin-1Homo sapiens (human)
post-embryonic developmentPresenilin-1Homo sapiens (human)
regulation of gene expressionPresenilin-1Homo sapiens (human)
positive regulation of gene expressionPresenilin-1Homo sapiens (human)
negative regulation of gene expressionPresenilin-1Homo sapiens (human)
regulation of neuron projection developmentPresenilin-1Homo sapiens (human)
protein transportPresenilin-1Homo sapiens (human)
choline transportPresenilin-1Homo sapiens (human)
synaptic vesicle targetingPresenilin-1Homo sapiens (human)
protein processingPresenilin-1Homo sapiens (human)
cerebellum developmentPresenilin-1Homo sapiens (human)
cerebral cortex cell migrationPresenilin-1Homo sapiens (human)
Cajal-Retzius cell differentiationPresenilin-1Homo sapiens (human)
dorsal/ventral neural tube patterningPresenilin-1Homo sapiens (human)
embryonic limb morphogenesisPresenilin-1Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processPresenilin-1Homo sapiens (human)
endoplasmic reticulum calcium ion homeostasisPresenilin-1Homo sapiens (human)
positive regulation of tumor necrosis factor productionPresenilin-1Homo sapiens (human)
amyloid-beta formationPresenilin-1Homo sapiens (human)
intracellular signal transductionPresenilin-1Homo sapiens (human)
locomotionPresenilin-1Homo sapiens (human)
positive regulation of protein import into nucleusPresenilin-1Homo sapiens (human)
regulation of phosphorylationPresenilin-1Homo sapiens (human)
amyloid precursor protein metabolic processPresenilin-1Homo sapiens (human)
amyloid precursor protein catabolic processPresenilin-1Homo sapiens (human)
myeloid dendritic cell differentiationPresenilin-1Homo sapiens (human)
positive regulation of apoptotic processPresenilin-1Homo sapiens (human)
negative regulation of apoptotic processPresenilin-1Homo sapiens (human)
negative regulation of neuron apoptotic processPresenilin-1Homo sapiens (human)
skin morphogenesisPresenilin-1Homo sapiens (human)
positive regulation of glycolytic processPresenilin-1Homo sapiens (human)
positive regulation of DNA-templated transcriptionPresenilin-1Homo sapiens (human)
astrocyte activationPresenilin-1Homo sapiens (human)
regulation of synaptic plasticityPresenilin-1Homo sapiens (human)
thymus developmentPresenilin-1Homo sapiens (human)
neuron developmentPresenilin-1Homo sapiens (human)
skeletal system morphogenesisPresenilin-1Homo sapiens (human)
brain morphogenesisPresenilin-1Homo sapiens (human)
epithelial cell proliferationPresenilin-1Homo sapiens (human)
negative regulation of axonogenesisPresenilin-1Homo sapiens (human)
synapse organizationPresenilin-1Homo sapiens (human)
positive regulation of coagulationPresenilin-1Homo sapiens (human)
T cell receptor signaling pathwayPresenilin-1Homo sapiens (human)
sequestering of calcium ionPresenilin-1Homo sapiens (human)
neuron apoptotic processPresenilin-1Homo sapiens (human)
smooth endoplasmic reticulum calcium ion homeostasisPresenilin-1Homo sapiens (human)
regulation of synaptic transmission, glutamatergicPresenilin-1Homo sapiens (human)
regulation of resting membrane potentialPresenilin-1Homo sapiens (human)
regulation of canonical Wnt signaling pathwayPresenilin-1Homo sapiens (human)
positive regulation of dendritic spine developmentPresenilin-1Homo sapiens (human)
neuron cellular homeostasisPresenilin-1Homo sapiens (human)
calcium ion transmembrane transportPresenilin-1Homo sapiens (human)
apoptotic signaling pathwayPresenilin-1Homo sapiens (human)
regulation of synaptic vesicle cyclePresenilin-1Homo sapiens (human)
L-glutamate import across plasma membranePresenilin-1Homo sapiens (human)
regulation of postsynapse organizationPresenilin-1Homo sapiens (human)
protein catabolic process at postsynapsePresenilin-1Homo sapiens (human)
cellular response to amyloid-betaPresenilin-1Homo sapiens (human)
negative regulation of core promoter bindingPresenilin-1Homo sapiens (human)
positive regulation of amyloid fibril formationPresenilin-1Homo sapiens (human)
neuron projection maintenancePresenilin-1Homo sapiens (human)
negative regulation of ubiquitin-dependent protein catabolic processPresenilin-1Homo sapiens (human)
negative regulation of apoptotic signaling pathwayPresenilin-1Homo sapiens (human)
calcium ion homeostasisPresenilin-1Homo sapiens (human)
Notch signaling pathwayPresenilin-1Homo sapiens (human)
response to hypoxiaPresenilin-2Homo sapiens (human)
membrane protein ectodomain proteolysisPresenilin-2Homo sapiens (human)
Notch receptor processingPresenilin-2Homo sapiens (human)
protein processingPresenilin-2Homo sapiens (human)
amyloid-beta formationPresenilin-2Homo sapiens (human)
intracellular signal transductionPresenilin-2Homo sapiens (human)
amyloid precursor protein catabolic processPresenilin-2Homo sapiens (human)
regulation of calcium import into the mitochondrionPresenilin-2Homo sapiens (human)
mitochondrion-endoplasmic reticulum membrane tetheringPresenilin-2Homo sapiens (human)
calcium ion homeostasisPresenilin-2Homo sapiens (human)
Notch signaling pathwayPresenilin-2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
xenobiotic metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of glucose metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of steroid metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor ROR-gammaHomo sapiens (human)
circadian regulation of gene expressionNuclear receptor ROR-gammaHomo sapiens (human)
cellular response to sterolNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of circadian rhythmNuclear receptor ROR-gammaHomo sapiens (human)
regulation of fat cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor ROR-gammaHomo sapiens (human)
adipose tissue developmentNuclear receptor ROR-gammaHomo sapiens (human)
T-helper 17 cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
hormone-mediated signaling pathwayOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of macrophage derived foam cell differentiationOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of triglyceride biosynthetic processOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of cholesterol effluxOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of lipid storageOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of cholesterol storageOxysterols receptor LXR-betaHomo sapiens (human)
intracellular receptor signaling pathwayOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of lipid transportOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of cholesterol transportOxysterols receptor LXR-betaHomo sapiens (human)
phosphatidylcholine acyl-chain remodelingOxysterols receptor LXR-betaHomo sapiens (human)
cholesterol homeostasisOxysterols receptor LXR-betaHomo sapiens (human)
mRNA transcription by RNA polymerase IIOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of fatty acid biosynthetic processOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of proteolysisOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of DNA-templated transcriptionOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of DNA-templated transcriptionOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of pinocytosisOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of lipoprotein lipase activityOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of protein metabolic processOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of type II interferon-mediated signaling pathwayOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of high-density lipoprotein particle assemblyOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of pancreatic juice secretionOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of secretion of lysosomal enzymesOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of cold-induced thermogenesisOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of miRNA transcriptionOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of response to endoplasmic reticulum stressOxysterols receptor LXR-betaHomo sapiens (human)
cell differentiationOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIOxysterols receptor LXR-alphaHomo sapiens (human)
hormone-mediated signaling pathwayOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of macrophage derived foam cell differentiationOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of triglyceride biosynthetic processOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of cholesterol effluxOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of cholesterol storageOxysterols receptor LXR-alphaHomo sapiens (human)
intracellular receptor signaling pathwayOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of lipid transportOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of cholesterol transportOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of transporter activityOxysterols receptor LXR-alphaHomo sapiens (human)
response to progesteroneOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of toll-like receptor 4 signaling pathwayOxysterols receptor LXR-alphaHomo sapiens (human)
phosphatidylcholine acyl-chain remodelingOxysterols receptor LXR-alphaHomo sapiens (human)
cholesterol homeostasisOxysterols receptor LXR-alphaHomo sapiens (human)
regulation of circadian rhythmOxysterols receptor LXR-alphaHomo sapiens (human)
mRNA transcription by RNA polymerase IIOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of macrophage activationOxysterols receptor LXR-alphaHomo sapiens (human)
apoptotic cell clearanceOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of fatty acid biosynthetic processOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of proteolysisOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of DNA-templated transcriptionOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of lipid biosynthetic processOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of pinocytosisOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of inflammatory responseOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of lipoprotein lipase activityOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of protein metabolic processOxysterols receptor LXR-alphaHomo sapiens (human)
lipid homeostasisOxysterols receptor LXR-alphaHomo sapiens (human)
sterol homeostasisOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of type II interferon-mediated signaling pathwayOxysterols receptor LXR-alphaHomo sapiens (human)
triglyceride homeostasisOxysterols receptor LXR-alphaHomo sapiens (human)
cellular response to lipopolysaccharideOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of pancreatic juice secretionOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of secretion of lysosomal enzymesOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of cold-induced thermogenesisOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of response to endoplasmic reticulum stressOxysterols receptor LXR-alphaHomo sapiens (human)
cell differentiationOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
protein processingGamma-secretase subunit APH-1BHomo sapiens (human)
Notch receptor processingGamma-secretase subunit APH-1BHomo sapiens (human)
positive regulation of endopeptidase activityGamma-secretase subunit APH-1BHomo sapiens (human)
protein processingGamma-secretase subunit APH-1BHomo sapiens (human)
membrane protein intracellular domain proteolysisGamma-secretase subunit APH-1BHomo sapiens (human)
amyloid-beta formationGamma-secretase subunit APH-1BHomo sapiens (human)
amyloid precursor protein catabolic processGamma-secretase subunit APH-1BHomo sapiens (human)
Notch signaling pathwayGamma-secretase subunit APH-1BHomo sapiens (human)
adaptive immune responseRap guanine nucleotide exchange factor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
calcium-ion regulated exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
positive regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of synaptic vesicle cycleRap guanine nucleotide exchange factor 4Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
myeloid cell homeostasisNicastrinHomo sapiens (human)
proteolysisNicastrinHomo sapiens (human)
membrane protein ectodomain proteolysisNicastrinHomo sapiens (human)
dopamine receptor signaling pathwayNicastrinHomo sapiens (human)
glutamate receptor signaling pathwayNicastrinHomo sapiens (human)
Notch signaling pathwayNicastrinHomo sapiens (human)
Notch receptor processingNicastrinHomo sapiens (human)
learning or memoryNicastrinHomo sapiens (human)
positive regulation of endopeptidase activityNicastrinHomo sapiens (human)
protein processingNicastrinHomo sapiens (human)
cerebellum developmentNicastrinHomo sapiens (human)
central nervous system myelinationNicastrinHomo sapiens (human)
adult behaviorNicastrinHomo sapiens (human)
membrane protein intracellular domain proteolysisNicastrinHomo sapiens (human)
amyloid-beta formationNicastrinHomo sapiens (human)
T cell proliferationNicastrinHomo sapiens (human)
amyloid precursor protein metabolic processNicastrinHomo sapiens (human)
amyloid precursor protein biosynthetic processNicastrinHomo sapiens (human)
positive regulation of amyloid precursor protein biosynthetic processNicastrinHomo sapiens (human)
amyloid precursor protein catabolic processNicastrinHomo sapiens (human)
epithelial cell proliferationNicastrinHomo sapiens (human)
neuron apoptotic processNicastrinHomo sapiens (human)
cellular response to calcium ionNicastrinHomo sapiens (human)
regulation of long-term synaptic potentiationNicastrinHomo sapiens (human)
short-term synaptic potentiationNicastrinHomo sapiens (human)
regulation of DNA-templated transcriptionNuclear receptor ROR-betaHomo sapiens (human)
G protein-coupled receptor signaling pathwayNuclear receptor ROR-betaHomo sapiens (human)
visual perceptionNuclear receptor ROR-betaHomo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor ROR-betaHomo sapiens (human)
amacrine cell differentiationNuclear receptor ROR-betaHomo sapiens (human)
eye photoreceptor cell developmentNuclear receptor ROR-betaHomo sapiens (human)
regulation of circadian rhythmNuclear receptor ROR-betaHomo sapiens (human)
negative regulation of osteoblast differentiationNuclear receptor ROR-betaHomo sapiens (human)
negative regulation of DNA-templated transcriptionNuclear receptor ROR-betaHomo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor ROR-betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear receptor ROR-betaHomo sapiens (human)
retinal rod cell developmentNuclear receptor ROR-betaHomo sapiens (human)
retinal cone cell developmentNuclear receptor ROR-betaHomo sapiens (human)
rhythmic processNuclear receptor ROR-betaHomo sapiens (human)
retina development in camera-type eyeNuclear receptor ROR-betaHomo sapiens (human)
cellular response to retinoic acidNuclear receptor ROR-betaHomo sapiens (human)
regulation of transcription by RNA polymerase IINuclear receptor ROR-betaHomo sapiens (human)
metanephros developmentGamma-secretase subunit APH-1AHomo sapiens (human)
membrane protein ectodomain proteolysisGamma-secretase subunit APH-1AHomo sapiens (human)
Notch receptor processingGamma-secretase subunit APH-1AHomo sapiens (human)
positive regulation of endopeptidase activityGamma-secretase subunit APH-1AHomo sapiens (human)
protein processingGamma-secretase subunit APH-1AHomo sapiens (human)
membrane protein intracellular domain proteolysisGamma-secretase subunit APH-1AHomo sapiens (human)
amyloid-beta formationGamma-secretase subunit APH-1AHomo sapiens (human)
amyloid precursor protein metabolic processGamma-secretase subunit APH-1AHomo sapiens (human)
amyloid precursor protein catabolic processGamma-secretase subunit APH-1AHomo sapiens (human)
Notch signaling pathwayGamma-secretase subunit APH-1AHomo sapiens (human)
negative regulation of very-low-density lipoprotein particle remodelingBile acid receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionBile acid receptorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIBile acid receptorHomo sapiens (human)
nitrogen catabolite activation of transcription from RNA polymerase II promoterBile acid receptorHomo sapiens (human)
intracellular glucose homeostasisBile acid receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIBile acid receptorHomo sapiens (human)
transcription by RNA polymerase IIBile acid receptorHomo sapiens (human)
inflammatory responseBile acid receptorHomo sapiens (human)
cell-cell junction assemblyBile acid receptorHomo sapiens (human)
Notch signaling pathwayBile acid receptorHomo sapiens (human)
bile acid metabolic processBile acid receptorHomo sapiens (human)
negative regulation of tumor necrosis factor-mediated signaling pathwayBile acid receptorHomo sapiens (human)
regulation of low-density lipoprotein particle clearanceBile acid receptorHomo sapiens (human)
intracellular receptor signaling pathwayBile acid receptorHomo sapiens (human)
negative regulation of type II interferon productionBile acid receptorHomo sapiens (human)
negative regulation of interleukin-1 productionBile acid receptorHomo sapiens (human)
negative regulation of interleukin-2 productionBile acid receptorHomo sapiens (human)
negative regulation of interleukin-6 productionBile acid receptorHomo sapiens (human)
negative regulation of tumor necrosis factor productionBile acid receptorHomo sapiens (human)
positive regulation of interleukin-17 productionBile acid receptorHomo sapiens (human)
toll-like receptor 9 signaling pathwayBile acid receptorHomo sapiens (human)
regulation of urea metabolic processBile acid receptorHomo sapiens (human)
intracellular triglyceride homeostasisBile acid receptorHomo sapiens (human)
positive regulation of insulin secretion involved in cellular response to glucose stimulusBile acid receptorHomo sapiens (human)
bile acid signaling pathwayBile acid receptorHomo sapiens (human)
intracellular bile acid receptor signaling pathwayBile acid receptorHomo sapiens (human)
cholesterol homeostasisBile acid receptorHomo sapiens (human)
defense response to bacteriumBile acid receptorHomo sapiens (human)
negative regulation of apoptotic processBile acid receptorHomo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionBile acid receptorHomo sapiens (human)
innate immune responseBile acid receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIBile acid receptorHomo sapiens (human)
positive regulation of insulin receptor signaling pathwayBile acid receptorHomo sapiens (human)
fatty acid homeostasisBile acid receptorHomo sapiens (human)
regulation of insulin secretion involved in cellular response to glucose stimulusBile acid receptorHomo sapiens (human)
regulation of bile acid biosynthetic processBile acid receptorHomo sapiens (human)
cellular response to lipopolysaccharideBile acid receptorHomo sapiens (human)
cellular response to fatty acidBile acid receptorHomo sapiens (human)
cellular response to organonitrogen compoundBile acid receptorHomo sapiens (human)
negative regulation of monocyte chemotactic protein-1 productionBile acid receptorHomo sapiens (human)
regulation of cholesterol metabolic processBile acid receptorHomo sapiens (human)
cellular response to bile acidBile acid receptorHomo sapiens (human)
positive regulation of adipose tissue developmentBile acid receptorHomo sapiens (human)
positive regulation of phosphatidic acid biosynthetic processBile acid receptorHomo sapiens (human)
positive regulation of glutamate metabolic processBile acid receptorHomo sapiens (human)
positive regulation of ammonia assimilation cycleBile acid receptorHomo sapiens (human)
cell differentiationBile acid receptorHomo sapiens (human)
negative regulation of inflammatory responseBile acid receptorHomo sapiens (human)
membrane protein ectodomain proteolysisGamma-secretase subunit PEN-2Homo sapiens (human)
Notch signaling pathwayGamma-secretase subunit PEN-2Homo sapiens (human)
Notch receptor processingGamma-secretase subunit PEN-2Homo sapiens (human)
positive regulation of endopeptidase activityGamma-secretase subunit PEN-2Homo sapiens (human)
protein processingGamma-secretase subunit PEN-2Homo sapiens (human)
membrane protein intracellular domain proteolysisGamma-secretase subunit PEN-2Homo sapiens (human)
amyloid-beta formationGamma-secretase subunit PEN-2Homo sapiens (human)
amyloid precursor protein metabolic processGamma-secretase subunit PEN-2Homo sapiens (human)
amyloid precursor protein catabolic processGamma-secretase subunit PEN-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (101)

Processvia Protein(s)Taxonomy
RNA polymerase II transcription regulatory region sequence-specific DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear receptor activityNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
protein bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
zinc ion bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear receptor bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 3Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
protein domain specific bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
serine-type endopeptidase activityPlasma kallikreinHomo sapiens (human)
protein bindingPlasma kallikreinHomo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D response element bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
transcription cis-regulatory region bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificRetinoic acid receptor RXR-alphaHomo sapiens (human)
transcription coregulator bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
retinoic acid bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
double-stranded DNA bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
DNA-binding transcription factor activityRetinoic acid receptor RXR-alphaHomo sapiens (human)
nuclear steroid receptor activityRetinoic acid receptor RXR-alphaHomo sapiens (human)
nuclear receptor activityRetinoic acid receptor RXR-alphaHomo sapiens (human)
protein bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
zinc ion bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
enzyme bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
peptide bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
identical protein bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
nuclear vitamin D receptor bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
sequence-specific DNA bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
retinoic acid-responsive element bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
DNA binding domain bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
LBD domain bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
sequence-specific double-stranded DNA bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingNuclear receptor ROR-alphaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor ROR-alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor ROR-alphaHomo sapiens (human)
transcription coregulator bindingNuclear receptor ROR-alphaHomo sapiens (human)
transcription corepressor bindingNuclear receptor ROR-alphaHomo sapiens (human)
transcription coactivator bindingNuclear receptor ROR-alphaHomo sapiens (human)
DNA bindingNuclear receptor ROR-alphaHomo sapiens (human)
DNA-binding transcription factor activityNuclear receptor ROR-alphaHomo sapiens (human)
protein bindingNuclear receptor ROR-alphaHomo sapiens (human)
beta-catenin bindingNuclear receptor ROR-alphaHomo sapiens (human)
oxysterol bindingNuclear receptor ROR-alphaHomo sapiens (human)
zinc ion bindingNuclear receptor ROR-alphaHomo sapiens (human)
sequence-specific DNA bindingNuclear receptor ROR-alphaHomo sapiens (human)
ligand-activated transcription factor activityNuclear receptor ROR-alphaHomo sapiens (human)
nuclear receptor activityNuclear receptor ROR-alphaHomo sapiens (human)
fatty acid bindingAlpha-synucleinHomo sapiens (human)
phospholipase D inhibitor activityAlpha-synucleinHomo sapiens (human)
SNARE bindingAlpha-synucleinHomo sapiens (human)
magnesium ion bindingAlpha-synucleinHomo sapiens (human)
transcription cis-regulatory region bindingAlpha-synucleinHomo sapiens (human)
actin bindingAlpha-synucleinHomo sapiens (human)
protein kinase inhibitor activityAlpha-synucleinHomo sapiens (human)
copper ion bindingAlpha-synucleinHomo sapiens (human)
calcium ion bindingAlpha-synucleinHomo sapiens (human)
protein bindingAlpha-synucleinHomo sapiens (human)
phospholipid bindingAlpha-synucleinHomo sapiens (human)
ferrous iron bindingAlpha-synucleinHomo sapiens (human)
zinc ion bindingAlpha-synucleinHomo sapiens (human)
lipid bindingAlpha-synucleinHomo sapiens (human)
oxidoreductase activityAlpha-synucleinHomo sapiens (human)
kinesin bindingAlpha-synucleinHomo sapiens (human)
Hsp70 protein bindingAlpha-synucleinHomo sapiens (human)
histone bindingAlpha-synucleinHomo sapiens (human)
identical protein bindingAlpha-synucleinHomo sapiens (human)
alpha-tubulin bindingAlpha-synucleinHomo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
tau protein bindingAlpha-synucleinHomo sapiens (human)
phosphoprotein bindingAlpha-synucleinHomo sapiens (human)
molecular adaptor activityAlpha-synucleinHomo sapiens (human)
dynein complex bindingAlpha-synucleinHomo sapiens (human)
cuprous ion bindingAlpha-synucleinHomo sapiens (human)
endopeptidase activityPresenilin-1Homo sapiens (human)
aspartic-type endopeptidase activityPresenilin-1Homo sapiens (human)
calcium channel activityPresenilin-1Homo sapiens (human)
protein bindingPresenilin-1Homo sapiens (human)
beta-catenin bindingPresenilin-1Homo sapiens (human)
PDZ domain bindingPresenilin-1Homo sapiens (human)
aspartic endopeptidase activity, intramembrane cleavingPresenilin-1Homo sapiens (human)
cadherin bindingPresenilin-1Homo sapiens (human)
ATPase bindingPresenilin-1Homo sapiens (human)
growth factor receptor bindingPresenilin-1Homo sapiens (human)
protein bindingPresenilin-2Homo sapiens (human)
aspartic endopeptidase activity, intramembrane cleavingPresenilin-2Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
protein bindingNuclear receptor ROR-gammaHomo sapiens (human)
oxysterol bindingNuclear receptor ROR-gammaHomo sapiens (human)
zinc ion bindingNuclear receptor ROR-gammaHomo sapiens (human)
ligand-activated transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
nuclear receptor activityNuclear receptor ROR-gammaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingOxysterols receptor LXR-betaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificOxysterols receptor LXR-betaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificOxysterols receptor LXR-betaHomo sapiens (human)
DNA bindingOxysterols receptor LXR-betaHomo sapiens (human)
protein bindingOxysterols receptor LXR-betaHomo sapiens (human)
zinc ion bindingOxysterols receptor LXR-betaHomo sapiens (human)
chromatin DNA bindingOxysterols receptor LXR-betaHomo sapiens (human)
apolipoprotein A-I receptor bindingOxysterols receptor LXR-betaHomo sapiens (human)
nuclear retinoid X receptor bindingOxysterols receptor LXR-betaHomo sapiens (human)
ATPase bindingOxysterols receptor LXR-betaHomo sapiens (human)
nuclear receptor activityOxysterols receptor LXR-betaHomo sapiens (human)
transcription cis-regulatory region bindingOxysterols receptor LXR-alphaHomo sapiens (human)
transcription cis-regulatory region bindingOxysterols receptor LXR-alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificOxysterols receptor LXR-alphaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificOxysterols receptor LXR-alphaHomo sapiens (human)
DNA bindingOxysterols receptor LXR-alphaHomo sapiens (human)
nuclear receptor activityOxysterols receptor LXR-alphaHomo sapiens (human)
protein bindingOxysterols receptor LXR-alphaHomo sapiens (human)
zinc ion bindingOxysterols receptor LXR-alphaHomo sapiens (human)
cholesterol bindingOxysterols receptor LXR-alphaHomo sapiens (human)
chromatin DNA bindingOxysterols receptor LXR-alphaHomo sapiens (human)
sterol response element bindingOxysterols receptor LXR-alphaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingOxysterols receptor LXR-alphaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
protein bindingGamma-secretase subunit APH-1BHomo sapiens (human)
protein-macromolecule adaptor activityGamma-secretase subunit APH-1BHomo sapiens (human)
endopeptidase activator activityGamma-secretase subunit APH-1BHomo sapiens (human)
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein-macromolecule adaptor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
small GTPase bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein bindingNicastrinHomo sapiens (human)
protein-macromolecule adaptor activityNicastrinHomo sapiens (human)
aspartic endopeptidase activity, intramembrane cleavingNicastrinHomo sapiens (human)
ATPase bindingNicastrinHomo sapiens (human)
growth factor receptor bindingNicastrinHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor ROR-betaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificNuclear receptor ROR-betaHomo sapiens (human)
DNA-binding transcription factor activityNuclear receptor ROR-betaHomo sapiens (human)
protein bindingNuclear receptor ROR-betaHomo sapiens (human)
zinc ion bindingNuclear receptor ROR-betaHomo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor ROR-betaHomo sapiens (human)
nuclear receptor activityNuclear receptor ROR-betaHomo sapiens (human)
melatonin receptor activityNuclear receptor ROR-betaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor ROR-betaHomo sapiens (human)
protein bindingGamma-secretase subunit APH-1AHomo sapiens (human)
enzyme bindingGamma-secretase subunit APH-1AHomo sapiens (human)
protein-macromolecule adaptor activityGamma-secretase subunit APH-1AHomo sapiens (human)
endopeptidase activator activityGamma-secretase subunit APH-1AHomo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingBile acid receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingBile acid receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificBile acid receptorHomo sapiens (human)
transcription coregulator bindingBile acid receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificBile acid receptorHomo sapiens (human)
DNA-binding transcription factor activityBile acid receptorHomo sapiens (human)
nuclear receptor activityBile acid receptorHomo sapiens (human)
protein bindingBile acid receptorHomo sapiens (human)
zinc ion bindingBile acid receptorHomo sapiens (human)
nuclear receptor bindingBile acid receptorHomo sapiens (human)
bile acid bindingBile acid receptorHomo sapiens (human)
bile acid receptor activityBile acid receptorHomo sapiens (human)
sequence-specific DNA bindingBile acid receptorHomo sapiens (human)
nuclear retinoid X receptor bindingBile acid receptorHomo sapiens (human)
chenodeoxycholic acid bindingBile acid receptorHomo sapiens (human)
protein bindingGamma-secretase subunit PEN-2Homo sapiens (human)
enzyme bindingGamma-secretase subunit PEN-2Homo sapiens (human)
endopeptidase activator activityGamma-secretase subunit PEN-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (79)

Processvia Protein(s)Taxonomy
nucleoplasmNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
transcription regulator complexNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear bodyNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
intermediate filament cytoskeletonNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
chromatinNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nucleusNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
cortical actin cytoskeletonRap guanine nucleotide exchange factor 3Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
microvillusRap guanine nucleotide exchange factor 3Homo sapiens (human)
endomembrane systemRap guanine nucleotide exchange factor 3Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
lamellipodiumRap guanine nucleotide exchange factor 3Homo sapiens (human)
filopodiumRap guanine nucleotide exchange factor 3Homo sapiens (human)
extracellular exosomeRap guanine nucleotide exchange factor 3Homo sapiens (human)
extracellular regionPlasma kallikreinHomo sapiens (human)
extracellular spacePlasma kallikreinHomo sapiens (human)
plasma membranePlasma kallikreinHomo sapiens (human)
extracellular exosomePlasma kallikreinHomo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
nucleusRetinoic acid receptor RXR-alphaHomo sapiens (human)
nucleoplasmRetinoic acid receptor RXR-alphaHomo sapiens (human)
transcription regulator complexRetinoic acid receptor RXR-alphaHomo sapiens (human)
mitochondrionRetinoic acid receptor RXR-alphaHomo sapiens (human)
cytosolRetinoic acid receptor RXR-alphaHomo sapiens (human)
RNA polymerase II transcription regulator complexRetinoic acid receptor RXR-alphaHomo sapiens (human)
chromatinRetinoic acid receptor RXR-alphaHomo sapiens (human)
receptor complexRetinoic acid receptor RXR-alphaHomo sapiens (human)
nucleusNuclear receptor ROR-alphaHomo sapiens (human)
nucleoplasmNuclear receptor ROR-alphaHomo sapiens (human)
nucleolusNuclear receptor ROR-alphaHomo sapiens (human)
chromatinNuclear receptor ROR-alphaHomo sapiens (human)
nucleusNuclear receptor ROR-alphaHomo sapiens (human)
platelet alpha granule membraneAlpha-synucleinHomo sapiens (human)
extracellular regionAlpha-synucleinHomo sapiens (human)
extracellular spaceAlpha-synucleinHomo sapiens (human)
nucleusAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
mitochondrionAlpha-synucleinHomo sapiens (human)
lysosomeAlpha-synucleinHomo sapiens (human)
cytosolAlpha-synucleinHomo sapiens (human)
plasma membraneAlpha-synucleinHomo sapiens (human)
cell cortexAlpha-synucleinHomo sapiens (human)
actin cytoskeletonAlpha-synucleinHomo sapiens (human)
membraneAlpha-synucleinHomo sapiens (human)
inclusion bodyAlpha-synucleinHomo sapiens (human)
axonAlpha-synucleinHomo sapiens (human)
growth coneAlpha-synucleinHomo sapiens (human)
synaptic vesicle membraneAlpha-synucleinHomo sapiens (human)
perinuclear region of cytoplasmAlpha-synucleinHomo sapiens (human)
postsynapseAlpha-synucleinHomo sapiens (human)
supramolecular fiberAlpha-synucleinHomo sapiens (human)
protein-containing complexAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
axon terminusAlpha-synucleinHomo sapiens (human)
neuronal cell bodyAlpha-synucleinHomo sapiens (human)
smooth endoplasmic reticulumPresenilin-1Homo sapiens (human)
dendritePresenilin-1Homo sapiens (human)
Golgi membranePresenilin-1Homo sapiens (human)
kinetochorePresenilin-1Homo sapiens (human)
nucleusPresenilin-1Homo sapiens (human)
nuclear outer membranePresenilin-1Homo sapiens (human)
nucleoplasmPresenilin-1Homo sapiens (human)
mitochondrionPresenilin-1Homo sapiens (human)
mitochondrial inner membranePresenilin-1Homo sapiens (human)
endoplasmic reticulumPresenilin-1Homo sapiens (human)
endoplasmic reticulum membranePresenilin-1Homo sapiens (human)
smooth endoplasmic reticulumPresenilin-1Homo sapiens (human)
rough endoplasmic reticulumPresenilin-1Homo sapiens (human)
Golgi apparatusPresenilin-1Homo sapiens (human)
centrosomePresenilin-1Homo sapiens (human)
plasma membranePresenilin-1Homo sapiens (human)
cell cortexPresenilin-1Homo sapiens (human)
synaptic vesiclePresenilin-1Homo sapiens (human)
cell surfacePresenilin-1Homo sapiens (human)
membranePresenilin-1Homo sapiens (human)
aggresomePresenilin-1Homo sapiens (human)
cell junctionPresenilin-1Homo sapiens (human)
growth conePresenilin-1Homo sapiens (human)
neuromuscular junctionPresenilin-1Homo sapiens (human)
early endosome membranePresenilin-1Homo sapiens (human)
nuclear membranePresenilin-1Homo sapiens (human)
ciliary rootletPresenilin-1Homo sapiens (human)
azurophil granule membranePresenilin-1Homo sapiens (human)
sarcolemmaPresenilin-1Homo sapiens (human)
presynaptic membranePresenilin-1Homo sapiens (human)
neuron projectionPresenilin-1Homo sapiens (human)
neuronal cell bodyPresenilin-1Homo sapiens (human)
dendritic shaftPresenilin-1Homo sapiens (human)
membrane raftPresenilin-1Homo sapiens (human)
postsynapsePresenilin-1Homo sapiens (human)
glutamatergic synapsePresenilin-1Homo sapiens (human)
protein-containing complexPresenilin-1Homo sapiens (human)
gamma-secretase complexPresenilin-1Homo sapiens (human)
Golgi membranePresenilin-2Homo sapiens (human)
kinetochorePresenilin-2Homo sapiens (human)
nuclear inner membranePresenilin-2Homo sapiens (human)
early endosomePresenilin-2Homo sapiens (human)
endoplasmic reticulumPresenilin-2Homo sapiens (human)
endoplasmic reticulum membranePresenilin-2Homo sapiens (human)
Golgi apparatusPresenilin-2Homo sapiens (human)
centrosomePresenilin-2Homo sapiens (human)
plasma membranePresenilin-2Homo sapiens (human)
synaptic vesiclePresenilin-2Homo sapiens (human)
membranePresenilin-2Homo sapiens (human)
presynaptic membranePresenilin-2Homo sapiens (human)
protein-containing complexPresenilin-2Homo sapiens (human)
gamma-secretase complexPresenilin-2Homo sapiens (human)
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
nucleoplasmNuclear receptor ROR-gammaHomo sapiens (human)
nuclear bodyNuclear receptor ROR-gammaHomo sapiens (human)
chromatinNuclear receptor ROR-gammaHomo sapiens (human)
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
nucleusOxysterols receptor LXR-betaHomo sapiens (human)
nucleoplasmOxysterols receptor LXR-betaHomo sapiens (human)
cytoplasmOxysterols receptor LXR-betaHomo sapiens (human)
cytosolOxysterols receptor LXR-betaHomo sapiens (human)
RNA polymerase II transcription regulator complexOxysterols receptor LXR-betaHomo sapiens (human)
chromatinOxysterols receptor LXR-betaHomo sapiens (human)
nucleusOxysterols receptor LXR-betaHomo sapiens (human)
nucleusOxysterols receptor LXR-alphaHomo sapiens (human)
nucleoplasmOxysterols receptor LXR-alphaHomo sapiens (human)
cytoplasmOxysterols receptor LXR-alphaHomo sapiens (human)
cytosolOxysterols receptor LXR-alphaHomo sapiens (human)
RNA polymerase II transcription regulator complexOxysterols receptor LXR-alphaHomo sapiens (human)
chromatinOxysterols receptor LXR-alphaHomo sapiens (human)
receptor complexOxysterols receptor LXR-alphaHomo sapiens (human)
nucleusOxysterols receptor LXR-alphaHomo sapiens (human)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
Golgi membraneGamma-secretase subunit APH-1BHomo sapiens (human)
endoplasmic reticulum membraneGamma-secretase subunit APH-1BHomo sapiens (human)
plasma membraneGamma-secretase subunit APH-1BHomo sapiens (human)
endosome membraneGamma-secretase subunit APH-1BHomo sapiens (human)
membraneGamma-secretase subunit APH-1BHomo sapiens (human)
transport vesicleGamma-secretase subunit APH-1BHomo sapiens (human)
gamma-secretase complexGamma-secretase subunit APH-1BHomo sapiens (human)
endoplasmic reticulumGamma-secretase subunit APH-1BHomo sapiens (human)
cytosolRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
Golgi membraneNicastrinHomo sapiens (human)
lysosomal membraneNicastrinHomo sapiens (human)
early endosomeNicastrinHomo sapiens (human)
endoplasmic reticulumNicastrinHomo sapiens (human)
endoplasmic reticulum membraneNicastrinHomo sapiens (human)
Golgi apparatusNicastrinHomo sapiens (human)
plasma membraneNicastrinHomo sapiens (human)
focal adhesionNicastrinHomo sapiens (human)
synaptic vesicleNicastrinHomo sapiens (human)
endosome membraneNicastrinHomo sapiens (human)
membraneNicastrinHomo sapiens (human)
azurophil granule membraneNicastrinHomo sapiens (human)
sarcolemmaNicastrinHomo sapiens (human)
melanosomeNicastrinHomo sapiens (human)
presynaptic membraneNicastrinHomo sapiens (human)
extracellular exosomeNicastrinHomo sapiens (human)
gamma-secretase complexNicastrinHomo sapiens (human)
plasma membraneNicastrinHomo sapiens (human)
nucleusNuclear receptor ROR-betaHomo sapiens (human)
nucleoplasmNuclear receptor ROR-betaHomo sapiens (human)
chromatinNuclear receptor ROR-betaHomo sapiens (human)
nucleusNuclear receptor ROR-betaHomo sapiens (human)
Golgi membraneGamma-secretase subunit APH-1AHomo sapiens (human)
early endosomeGamma-secretase subunit APH-1AHomo sapiens (human)
endoplasmic reticulumGamma-secretase subunit APH-1AHomo sapiens (human)
endoplasmic reticulum membraneGamma-secretase subunit APH-1AHomo sapiens (human)
Golgi apparatusGamma-secretase subunit APH-1AHomo sapiens (human)
plasma membraneGamma-secretase subunit APH-1AHomo sapiens (human)
synaptic vesicleGamma-secretase subunit APH-1AHomo sapiens (human)
endosome membraneGamma-secretase subunit APH-1AHomo sapiens (human)
membraneGamma-secretase subunit APH-1AHomo sapiens (human)
Golgi cisterna membraneGamma-secretase subunit APH-1AHomo sapiens (human)
presynaptic membraneGamma-secretase subunit APH-1AHomo sapiens (human)
gamma-secretase complexGamma-secretase subunit APH-1AHomo sapiens (human)
endoplasmic reticulumGamma-secretase subunit APH-1AHomo sapiens (human)
nucleoplasmBile acid receptorHomo sapiens (human)
chromatinBile acid receptorHomo sapiens (human)
euchromatinBile acid receptorHomo sapiens (human)
receptor complexBile acid receptorHomo sapiens (human)
RNA polymerase II transcription regulator complexBile acid receptorHomo sapiens (human)
nucleusBile acid receptorHomo sapiens (human)
Golgi membraneGamma-secretase subunit PEN-2Homo sapiens (human)
endoplasmic reticulumGamma-secretase subunit PEN-2Homo sapiens (human)
endoplasmic reticulum membraneGamma-secretase subunit PEN-2Homo sapiens (human)
Golgi apparatusGamma-secretase subunit PEN-2Homo sapiens (human)
plasma membraneGamma-secretase subunit PEN-2Homo sapiens (human)
endosome membraneGamma-secretase subunit PEN-2Homo sapiens (human)
membraneGamma-secretase subunit PEN-2Homo sapiens (human)
Golgi cisterna membraneGamma-secretase subunit PEN-2Homo sapiens (human)
presynaptic membraneGamma-secretase subunit PEN-2Homo sapiens (human)
gamma-secretase complexGamma-secretase subunit PEN-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (557)

Assay IDTitleYearJournalArticle
AID758940Agonist activity at human LXRalpha-LBD assessed as recruitment of co-activator peptide after 2 hrs by TR-FRET assay2013Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
Cyanidin, a natural flavonoid, is an agonistic ligand for liver X receptor alpha and beta and reduces cellular lipid accumulation in macrophages and hepatocytes.
AID1821365Inhibition of human recombinant DHODH expressed in Escherichia coli BL21 (DE3) using dihydroorotate as substrate and CoQ6 as co-substrate incubated for 10 mins by DCIP based multimode microplate reader analysis
AID391700Displacement of [N-methyl-3H]GW0438 from human biotinylated LXRbeta ligand binding domain2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.
AID345474Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay relative to TO9013172008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
AID1139696Inverse agonist activity at human ROR-beta expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (RORγ)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand.
AID1691869Agonist activity at human RXRalpha/LXRalpha expressed in HEK293 cells measured after 20 hrs by dual luciferase reporter gene assay2020European journal of medicinal chemistry, May-15, Volume: 194Discovery of new LXRβ agonists as glioblastoma inhibitors.
AID309258Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as reduction of Amyloid beta-40 formation LPECL assay2007Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19
Conversion of the LXR-agonist TO-901317--from inverse to normal modulation of gamma-secretase by addition of a carboxylic acid and a lipophilic anchor.
AID293511Antagonist activity at human PXR by transient transfection assay2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.
AID472517Agonist activity at human LXRbeta assessed as induction of PCAF cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID478583Agonist activity at human recombinant LXRbeta ligand binding domain in HuH7 cells by Gal4 transactivation assay relative to T09013172010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.
AID1301869Increase in amyloid beta42 in CSF of rhesus monkey at 10 mg/kg, po administered for 2 weeks2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease.
AID1059101Inverse agonist activity at N-terminal 6xHis-tagged human RORc ligand binding domain (241 to 486) expressed in bacterial expression system assessed as inhibition of SRC1 co-activator peptide recruitment after 3 hrs by TR-FRET analysis relative to apo-RORc2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID313455Effect on ABCA1 gene expression in human THP1 cells relative to TO9013172008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
AID1192888Effect on Plasma triglyceride level in high-fat-and-cholesterol diet fed Male Bio F1B hamster at 3 mg/kg, po relative to control2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists.
AID1480571Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
DrugBank screening revealed alitretinoin and bexarotene as liver X receptor modulators.
AID758933Agonist activity at LXR in human HepG2 cells assessed as upregulation of ABCA1 expression at 10 uM after 24 hrs by RT-qPCR analysis relative to control2013Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
Cyanidin, a natural flavonoid, is an agonistic ligand for liver X receptor alpha and beta and reduces cellular lipid accumulation in macrophages and hepatocytes.
AID1168691Inverse agonist activity at RORbeta (unknown origin) by M1H assay2014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.
AID1301855Increase in amyloid beta40 in CSF of rhesus monkey at 10 mg/kg, po administered for 2 weeks2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease.
AID472476Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID703193Transactivational agonist activity at human LXRbeta transfected in HEK293 cells expressing CMX-Gal4N assessed as luciferase activity after 16 hrs by reporter gene assay2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID1233341Increase in ABCG5 gene expression in Bio F1B hamster intestine at 10 mg/kg, po2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists.
AID1172003Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase reporter gene assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ.
AID454634Agonist activity at human Gal4-LBD fused LXRalpha LBD expressed in Huh7 cells by transient transactivation assay2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
AID1172024Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase reporter gene assay relative to 1-(2,4-difluorobenzyl)-2-oxo-6-(4-phenoxyphenyl)-4-(trifluoromethyl)-1,2-dihydropyridine-3-carbonitrile2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ.
AID472506Agonist activity at human LXRalpha assessed as induction of NRP1-3 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID331154Induction of APOE gene expression in human THP1 cells at 10 uM by array plate mRNA assay2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators.
AID768573Induction of intracellular triglyceride accumulation in human HepG2 cells at 1 uM after 4 days relative to vehicle-treated control2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Synthesis and identification of new flavonoids targeting liver X receptor β involved pathway as potential facilitators of Aβ clearance with reduced lipid accumulation.
AID1458220Agonist activity at LXR in human U937 cells assessed as upregulation of ABCA1 mRNA levels at 10 uM after 6 hrs by qPCR analysis2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID1139698Agonist activity at human LXR-alpha expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (RORγ)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand.
AID1566009Increase in hepatic triglyceride level in high fat diet-induced C57BL/6 mouse model of hypercholesterolemia at 20 mg/kg, po administered for 12 weeks2019European journal of medicinal chemistry, Nov-15, Volume: 182Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis.
AID1892226Toxicity in human HEK293 cells assessed as reduction in cell viability at 10 uM2022Bioorganic & medicinal chemistry, 07-15, Volume: 66Design, synthesis and structure-activity relationship of 4-(1,1,1,3,3,3-hexafluoro-2-hydroxyisoprop-2-yl)phenylsilane derivatives as liver X receptor agonists.
AID1304680Agonist activity at LXR in human THP1 cells assessed as upregulation of ABCA1 gene expression at 1 uM after 24 hrs by RT-PCR analysis relative to control2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist.
AID715911Agonist activity at LXR-alpha in human THP1 cells assessed as reduced cellular cholesterol concentration at 1 uM2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells.
AID472511Agonist activity at human LXRbeta assessed as induction of SRC2-3 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID1233302Agonist activity at LXRbeta (unknown origin)2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists.
AID478581Displacement of [3H]T0901317 from LXRalpha ligand binding domain2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.
AID1306541Agonist activity at GAL4 fused LXRalpha (unknown origin) transfected in CHOK1 cells at 10 uM after 24 hrs by luciferase reporter gene assay in presence of T09013172016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency and β-selectivity of liver X receptor agonist.
AID1059096Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay relative to apo-receptor2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID1249983Antagonist activity at human LXR-beta transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay in presence of 0.1 uM N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-(2,2,2-trifluoroethyl)benzenesulfonamide2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators.
AID331156Induction of FASN gene expression in human THP1 cells at 10 uM by array plate mRNA assay2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators.
AID1614979Agonist activity LXRbeta (unknown origin)2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation.
AID478582Agonist activity at human recombinant LXRbeta ligand binding domain in HuH7 cells by Gal4 transactivation assay2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.
AID1301867Increase in amyloid beta42 in CSF of rhesus monkey at 5 mg/kg, po administered for 2 weeks2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease.
AID1398740Inhibition of human RORalpha1 expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Development of novel silanol-based human pregnane X receptor (PXR) agonists with improved receptor selectivity.
AID418427Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides.
AID424924Induction of ABCA1 mRNA expression in mouse J774A1 cells after 18 hrs by RT-PCR2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRbeta.
AID1192884Effect on HDL-C level in high-fat-and-cholesterol diet fed Male Bio F1B hamster plasma at 10 mg/kg, po relative to control2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists.
AID758931Agonist activity at LXR in human HepG2 cells assessed as upregulation of ABCG5 expression at 10 uM after 24 hrs by RT-qPCR analysis relative to control2013Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
Cyanidin, a natural flavonoid, is an agonistic ligand for liver X receptor alpha and beta and reduces cellular lipid accumulation in macrophages and hepatocytes.
AID418425Agonist activity at LXRbeta ligand binding domain by FRET based SRC1 recruitment assay2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides.
AID1614978Agonist activity LXRalpha (unknown origin)2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation.
AID452860Displacement of [3H]T0901317 from human recombinant LXRbeta ligand binding domain2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
4-(3-aryloxyaryl)quinoline alcohols are liver X receptor agonists.
AID262338Half life in dog at 5 mg/kg, po2006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Discovery and optimization of a novel series of liver X receptor-alpha agonists.
AID1127096Antagonist activity at Gal4-fused RORgamma (unknown origin) expressed in 293T cells after 24 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, May-06, Volume: 78Discovery of 2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide derivatives as new RORγ inhibitors using virtual screening, synthesis and biological evaluation.
AID313454Effect on ABCA1 gene expression in human THP1 cells2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
AID1243271Increase in ABCA1 mRNA expression in C57Bl/6 mouse blood at 1 mg/kg, po dosed daily for 7 days2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Discovery and structure-guided optimization of tert-butyl 6-(phenoxymethyl)-3-(trifluoromethyl)benzoates as liver X receptor agonists.
AID1775047Displacement of BODIPY FL vindoline from GST-tagged human PXR LBD at 10 uM incubated for 60 mins by TR-FRET assay relative to control
AID758939Agonist activity at human LXRbeta-LBD assessed as recruitment of co-activator peptide after 2 hrs by TR-FRET assay2013Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
Cyanidin, a natural flavonoid, is an agonistic ligand for liver X receptor alpha and beta and reduces cellular lipid accumulation in macrophages and hepatocytes.
AID1192894Effect on area of lipid accumulation in high-fat-and-cholesterol diet fed Male Bio F1B hamster aortic arch at 10 mg/kg, po relative to control2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists.
AID1576220Agonist activity at LXR beta (unknown origin) by Alpha Screen assay2019MedChemComm, Aug-01, Volume: 10, Issue:8
Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool.
AID472512Agonist activity at human LXRbeta assessed as induction of SRC3-2 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID313453Agonist activity at human LXRalpha expressed in Huh7 cells by Gal4 transactivation assay relative to TO9013172008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
AID391701Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production after 6 hrs by ELISA2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.
AID1301876Agonist activity at LXRbeta (unknown origin) expressed in human H4 cells co-expressing ABCA1 promoter measured after 48 hrs by cell-based transactivation assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease.
AID472480Binding affinity to human recombinant LXRalpha ligand binding domain2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID1233301Agonist activity at LXRalpha (unknown origin) relative to control2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists.
AID345476Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay relative to TO9013172008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
AID1059094Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay relative to apo-receptor2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID1066846Modulation of LXR in human HepG2 cells assessed as increase of ABCA1 mRNA expression at 1 uM after 4 days by qPCR analysis2014European journal of medicinal chemistry, Mar-03, Volume: 74Development of new LXR modulators that regulate LXR target genes and reduce lipogenesis in human cell models.
AID703036Binding affinity to human GST-tagged LXRalpha expressed in Escherichia coli BL21(DE3) assessed as inhibition of 2-(4-(4-methoxyphenethyl)phenyl)-5- (dimethylamino)isoindoline-1,3-dione binding after 1 hr by fluorescence polarization assay2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID1562690Binding affinity to recombinant human LXRbeta-LBD expressed in Escherichia coli BL21 (DE3) assessed as inhibitory constant incubated for 30 mins by fluorescence polarization binding assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Identify liver X receptor β modulator building blocks by developing a fluorescence polarization-based competition assay.
AID1368956Transactivation of PXR in human HepG2 cells by receptor transactivation assay2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
AID452861Displacement of [3H]T0901317 from human recombinant LXRalpha ligand binding domain2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
4-(3-aryloxyaryl)quinoline alcohols are liver X receptor agonists.
AID1177751Agonist activity at RoRa (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).
AID653687Displacement of [3H]N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-methylbenzenesulfonamide from LXRbeta by scintillation proximity assay2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of a new binding mode for a series of liver X receptor agonists.
AID307303Agonist activity at LXRbeta LBD by HTRF cofactor peptide recruitment assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists.
AID1316539Induction of ABCA1 mRNA expression in C57BL mouse brain at 30 mg/kg, po measured after 4 hrs relative to control2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
AID1066847Modulation of LXR in human HepG2 cells assessed as increase of SCD1 mRNA expression at 1 uM after 4 days by qPCR analysis2014European journal of medicinal chemistry, Mar-03, Volume: 74Development of new LXR modulators that regulate LXR target genes and reduce lipogenesis in human cell models.
AID703046Inhibition of LPS-induced IL-6 production in LXRalpha,LXRbeta-deficient C57BL/6J mouse peritoneal macrophages at 3 uM incubated for 6 hrs prior to LPS-challenge measured after 18 hrs by ELISA2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID1059092Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay relative to apo-receptor2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID345494Effect on SREBP1c gene expression in human HepG2 cells2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
AID1168683Inverse agonist activity at human recombinant N-terminally 6xHis-tagged RORgamma ligand binding domain (unknown origin) expressed in Escherichia coli incubated for 1 hr by FRET assay2014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.
AID472501Agonist activity at human LXRalpha assessed as induction of PGC-1a cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID1458223Agonist activity at LXR in human HepG2 cells assessed as upregulation of SCD1 mRNA levels at 10 uM after 6 hrs by qPCR analysis2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID331157Induction of SCD1 gene expression in human THP1 cells at 10 uM by array plate mRNA assay2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators.
AID1177722Binding affinity to RORa (unknown origin) by radioligand binding assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).
AID1821368Metabolic stability in mouse liver microsomes assessed as half life at 1 mM preincubated for 10 mins in presence of NADPH followed by compound addition and measured upto 60 mins by HPLC-MS/MS analysis
AID1168687Inverse agonist activity at recombinant N-terminally GST-tagged RORbeta ligand binding domain (unknown origin) expressed in Escherichia coli incubated for 1 hr by FRET assay relative to control2014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.
AID331161Induction of ACTB gene expression in human THP1 cells at 10 uM by array plate mRNA assay2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators.
AID472470Agonist activity at human LXRbeta in HEK293 cells assessed as Gal4 transactivation2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID1316533Plasma concentration in wild type C57BL mouse at 30 mg/kg, po measured after 4 hrs2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
AID1594667Transactivation of recombinant GAL4-fused human LXRalpha LBD (163 to 447 residues) expressed in human L02 cells measured after 24 hrs by luciferase reporter gene assay2019Journal of natural products, 06-28, Volume: 82, Issue:6
Diketopiperazine-Type Alkaloids from a Deep-Sea-Derived Aspergillus puniceus Fungus and Their Effects on Liver X Receptor α.
AID452866Agonist activity at LXRbeta in mouse J774 cells assessed as upregulation of ABCA1 mRNA expression2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
4-(3-aryloxyaryl)quinoline alcohols are liver X receptor agonists.
AID758944Binding affinity to human LXRbeta-LBD by surface plasmon resonance2013Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
Cyanidin, a natural flavonoid, is an agonistic ligand for liver X receptor alpha and beta and reduces cellular lipid accumulation in macrophages and hepatocytes.
AID1233353Hypolipidemic effect in Bio F1B hamster fed with high fat and cholesterol diet assessed as LDL-cholesterol level at 10 mg/kg, po relative to control2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists.
AID1398738Octanol/water partition co-efficient, log P of the compound by HPLC method2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Development of novel silanol-based human pregnane X receptor (PXR) agonists with improved receptor selectivity.
AID1301909Increase in apoE level in CSF of rhesus monkey at 10 mg/kg, po administered for 2 weeks by apoE ELISA relative to control2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease.
AID472507Agonist activity at human LXRalpha assessed as induction of NRP1-6 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID299788Agonist activity at human LXRalpha receptor after 1 hr by HTRF cofactor recruitment assay2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.
AID309260Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as increase in Amyloid beta-42 formation LPECL assay2007Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19
Conversion of the LXR-agonist TO-901317--from inverse to normal modulation of gamma-secretase by addition of a carboxylic acid and a lipophilic anchor.
AID1243265Agonist activity at human LXRbeta expressed in African green monkey kidney CV1 cells co-expressing pTAL-LXRE including LXR response element incubated for 20 hrs by luciferase reporter gene assay2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Discovery and structure-guided optimization of tert-butyl 6-(phenoxymethyl)-3-(trifluoromethyl)benzoates as liver X receptor agonists.
AID1458218Agonist activity at LXR in human U937 cells assessed as upregulation of SREBP1c mRNA levels at 10 uM after 6 hrs by qPCR analysis2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID1249978Agonist activity at human LXR-alpha transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators.
AID424922Agonist activity at human LXRalpha ligand binding domain (205-448) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRbeta.
AID1233344Increase in ABCG8 gene expression in Bio F1B hamster intestine at 10 mg/kg, po2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists.
AID1192872Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells assessed as maximal efficacy at 10 uM after 24 hrs by luciferase reporter gene assay relative to T0901317 luminescence intensity2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists.
AID1316563Effect on amyloid beta (1 to 42) level in Sprague-Dawley rat CSF at 30 mg/kg, po qd administered for 5 days2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
AID454929Induction of ABCA1 mRNA upregulation in human THP1 cells relative to T09013172010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists.
AID1059090Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay relative to apo-receptor2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID1458217Agonist activity at LXR in human U937 cells assessed as upregulation of SCD1 mRNA levels at 10 uM after 6 hrs by qPCR analysis relative to control2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID1059089Selectivity ratio of EC50 for GAL4-fused human RORb expressed in HEK293T cells to EC50 for GAL4-fused human RORc expressed in HEK293T cells2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID454647Half life in rat liver microsomes2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
AID474691Inhibition of GW-3965-induced ABCA1 expression in human THP1 cells2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Discovery of tertiary sulfonamides as potent liver X receptor antagonists.
AID1243280Agonist activity at His-LXRalpha/FLAG-RXRalpha (unknown origin) assessed as recruitment of ASC2 peptide (1481 to 1510 residues) pre-incubated for 60 mins before ASC2 peptide addition followed by one night of incubation by FRET assay2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Discovery and structure-guided optimization of tert-butyl 6-(phenoxymethyl)-3-(trifluoromethyl)benzoates as liver X receptor agonists.
AID1605742Agonist activity at His-tagged PXR-LBD/SRC-1p (unknown origin) expressed in Escherichia coli BL21(DE3) by coactivator recruitment based Alpha-screen assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1374012Agonist activity at LXRalpha ligand-binding domain (unknown origin) at 3 uM incubated for 1.5 hrs using fluorescein-labeled coactivator peptide by TR-FRET competitive binding assay2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Structural development of tetrachlorophthalimides as liver X receptor β (LXRβ)-selective agonists with improved aqueous solubility.
AID1168685Inverse agonist activity at recombinant N-terminally 6xHis-tagged RORgamma ligand binding domain (unknown origin) expressed in Escherichia coli incubated for 1 hr by FRET assay relative to control2014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.
AID1744023Agonist activity at RXR-alpha in mouse RAW264.7 cells assessed as inhibition of LPS-induced NF-kappaB transcription by measuring NF-kappaB level at 0.01 to 10 uM incubated for 24 hrs by SEAP dependent NF-kappaB reporter assay2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Discovery of a "Gatekeeper" Antagonist that Blocks Entry Pathway to Retinoid X Receptors (RXRs) without Allosteric Ligand Inhibition in Permissive RXR Heterodimers.
AID1316557Effect on amyloid beta (1 to 40) level in Sprague-Dawley rat cerebrum at 30 mg/kg qd administered via oral gavage for 5 days2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
AID1316545Plasma concentration in Sprague-Dawley rat at 30 mg/kg qd administered via oral gavage for 5 days measured 4 hrs post last dose2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
AID758945Agonist activity at LXRalpha (unknown origin) expressed in CHOK1 cells assessed as induction of transactivation activity at 2 uM after 24 hrs by luciferase reporter gene assay relative to control2013Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
Cyanidin, a natural flavonoid, is an agonistic ligand for liver X receptor alpha and beta and reduces cellular lipid accumulation in macrophages and hepatocytes.
AID240223Effective concentration for Steroid receptor coactivator-1 (SRC1) recruitment to human LXRalpha (Liver X receptor)2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.
AID1177755Agonist activity at PXR (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).
AID1892225Selectivity index, ratio of EC50 for agonist activity at human LXRalpha to EC50 for agonist activity at LXRbeta2022Bioorganic & medicinal chemistry, 07-15, Volume: 66Design, synthesis and structure-activity relationship of 4-(1,1,1,3,3,3-hexafluoro-2-hydroxyisoprop-2-yl)phenylsilane derivatives as liver X receptor agonists.
AID345493Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL relative to TO9013172008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
AID1328923Effect on plasma triglyceride level in cynomolgus monkey at 10 mg/kg, po qd administered via gavage for 14 days measured after 24 hrs of last-dose relative to base line2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Discovery of Highly Potent Liver X Receptor β Agonists.
AID1177749Agonist activity at RoRc (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).
AID472516Agonist activity at human LXRbeta assessed as induction of CPB/p300-2 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID1542682Transactivation of rat LXRbeta expressed in HEK293FT cells measured after 14 to 18 hrs by dual-luciferase reporter gene assay2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Structural requirements of cholenamide derivatives as the LXR ligands.
AID418716Upregulation of ABCA1 mRNA level in mouse brain homogenates at 10 umol/kg, po daily once after 3 days relative to control2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides.
AID1059088Selectivity ratio of EC50 for GAL4-fused human RORa expressed in HEK293T cells to EC50 for GAL4-fused human RORc expressed in HEK293T cells2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID1458219Agonist activity at LXR in human U937 cells assessed as upregulation of FASN mRNA levels at 10 uM after 6 hrs by qPCR analysis2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID299789Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.
AID345497Effect on triglyceride accumulation in human HepG2 cells relative to TO9013172008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
AID758924Agonist activity at LXR in human THP1 cells assessed as reduction in cellular triglyceride at 10 uM after 24 hrs2013Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
Cyanidin, a natural flavonoid, is an agonistic ligand for liver X receptor alpha and beta and reduces cellular lipid accumulation in macrophages and hepatocytes.
AID414317Increase in liver triglyceride level in C57BL/6J mouse at 10 mg/kg/day, ip dosed for 5 days measured 2 hrs after last dose2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Discovery of tetrahydro-cyclopenta[b]indole as selective LXRs modulator.
AID391703Lipogenic activity against human HuH7 cells assessed as triglyceride accumulation at 10 uM after 4 days relative to N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-(2,2,2-trifluoroethyl)benzenesulfonamide2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.
AID345471Displacement of [3H]TO901317 from human recombinant LXRbeta expressed in Escherichia coli by flashplate method2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
AID1595546Inverse agonist activity at Gal4-fused RORbeta LBD (unknown origin) expressed in 293T cells measured after 24 hrs by dual-luciferase reporter gene assay2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
AID452963Agonist activity at human LXRalpha ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.
AID1066853Modulation of LXR in human myotubes assessed as increase of ABCA1 mRNA expression at 1 uM after 4 days by qPCR analysis2014European journal of medicinal chemistry, Mar-03, Volume: 74Development of new LXR modulators that regulate LXR target genes and reduce lipogenesis in human cell models.
AID307309Ratio of induction of cholesterol efflux in THP1 cells at 10 uM to control after 18 hrs2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists.
AID1066848Modulation of LXR in human HepG2 cells assessed as increase of FAS mRNA expression at 1 uM after 4 days by qPCR analysis2014European journal of medicinal chemistry, Mar-03, Volume: 74Development of new LXR modulators that regulate LXR target genes and reduce lipogenesis in human cell models.
AID313456Effect on ABCA1 gene expression in mouse J774 cells2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
AID1192909Effect on HDL-C level in high-fat-and-cholesterol diet fed Male Bio F1B hamster plasma at 3 to 10 mg/kg, po relative to control2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists.
AID1301877Agonist activity at LXRalpha (unknown origin) expressed in human HepG2 cells co-expressing ABCA1 promoter measured after 48 hrs by cell-based transactivation assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease.
AID1542683Transactivation of rat LXRbeta expressed in HEK293FT cells measured after 14 to 18 hrs by dual-luciferase reporter gene assay relative to T09013172019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Structural requirements of cholenamide derivatives as the LXR ligands.
AID391704Metabolic stability in human HuH7 cells at 1 uM after 24 hrs2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.
AID1249975Transrepression activity of LXR in human THP1 cells assessed as inhibition of LPS-induced IL-6 level after 18 hrs by ELISA2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators.
AID454648Half life in human liver microsomes2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
AID715906Upregulation of FAS gene expression in human HepG2 cells at 1 uM by qPCR analysis2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells.
AID299793Induction of cholesterol efflux in THP1 cells2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.
AID1480570Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
DrugBank screening revealed alitretinoin and bexarotene as liver X receptor modulators.
AID1595545Inverse agonist activity at Gal4-fused RORalpha LBD (unknown origin) expressed in 293T cells measured after 24 hrs by dual-luciferase reporter gene assay2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
AID452960Displacement of [3H]TO901317 from human recombinant LXRalpha expressed in Escherichia coli by flashplate method2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.
AID703196Transrepressional activity at LXR in human TPA-activated THP1 cells assessed as inhibition of LPS-induced IL6 production at 10 uM incubated for 6 hrs prior to LPS-challenge measured after 18 hrs by ELISA2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID758923Agonist activity at LXR in human HepG2 cells assessed as increase in cellular triglyceride at 10 uM after 24 hrs relative to control2013Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
Cyanidin, a natural flavonoid, is an agonistic ligand for liver X receptor alpha and beta and reduces cellular lipid accumulation in macrophages and hepatocytes.
AID451982Agonist activity at human recombinant LXR-LBD by Gal4beta transactivation assay relative to T09013172010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists.
AID1059086Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA relative to control2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID1821367Metabolic stability in mouse liver microsomes assessed as intrinsic clearance at 1 mM preincubated for 10 mins in presence of NADPH followed by compound addition and measured upto 60 mins by HPLC-MS/MS analysis
AID1306543Agonist activity at GAL4 fused LXRbeta-LBD (unknown origin) transfected in CHOK1 cells after 24 hrs by luciferase reporter gene assay2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency and β-selectivity of liver X receptor agonist.
AID424749Displacement of [3H]T0901317 from human recombinant N-terminal biotinylated tagged LXRalpha ligand binding domain (197-447) expressed in Escherichia coli2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRbeta.
AID1233303Agonist activity at LXRbeta (unknown origin) relative to control2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists.
AID331152Induction of ABCA1 gene expression in human THP1 cells at 10 uM by array plate mRNA assay2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators.
AID1316536Drug uptake in wild type C57BL mouse brain at 30 mg/kg, po measured after 4 hrs2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
AID454927Induction of ABCA1 mRNA upregulation in human THP1 cells2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists.
AID1139704Antagonist activity at human LXR-alpha expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (RORγ)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand.
AID472514Agonist activity at human LXRbeta assessed as induction of PGC-1a cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID478591Increase in triglyceride level in human HepG2 cells relative to T09013172010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.
AID703040Inhibition of LPS-induced IL-1beta mRNA expression in LXRalpha-deficient C57BL/6J mouse peritoneal macrophages at 3 uM incubated for 6 hrs prior to LPS-challenge measured after 18 hrs by RT-PCR analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID703186Transactivational agonist activity at human LXRalpha transfected in HEK293 cells coexpressing CMX-Gal4N-SRC1 assessed as SRC1 recruitment at 0.03 to 10 uM after 16 hrs by mammalian two-hybrid assay2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID715908Induction of lipid accumulation in human HepG2 cells assessed as increase in cellular triglyceride level at 1 uM by Oil Red O staining relative to control2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells.
AID472500Agonist activity at human LXRalpha assessed as induction of TRAP220-1 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID313446Binding affinity at human LXRbeta2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
AID1821363Inhibition of human GAL4-fused RORgammat LBD transfected in HEK293T cell measured after 24 hrs by by dual-glo luciferase assay
AID299791Induction of ABCA1 gene expression in THP1 cells at 10 uM relative to control2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.
AID1691875Antiproliferative activity against human U87 cells overexpressing EGFR variant III measured after 7 days by CCK8 assay2020European journal of medicinal chemistry, May-15, Volume: 194Discovery of new LXRβ agonists as glioblastoma inhibitors.
AID1368962Agonist activity at GAL4-tagged human LXRalpha assessed as receptor activation expressed in African green monkey CV1 cells by luciferase reporter gene assay relative to untreated control2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
AID1233356Effect in lipid profiles in Bio F1B hamster fed with high fat and cholesterol diet assessed as triglyceride level at 10 mg/kg, po relative to control2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists.
AID331162Induction of B2M gene expression in human THP1 cells at 10 uM by array plate mRNA assay2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators.
AID391720Effect on LXRbeta ligand binding domain transfected in monkey CV1 cells assessed as recruitment of steroid receptor coactivator 1 at 5 uM after 24 hrs by mammalian two-hybrid assay2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.
AID414314Increase in plasma triglyceride level in C57BL/6J mouse at 10 mg/kg/day, ip dosed for 5 days measured 2 hrs after last dose2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Discovery of tetrahydro-cyclopenta[b]indole as selective LXRs modulator.
AID1059103Displacement of [3H2]-25-hydroxycholesterol from N-terminal 6xHis-tagged human RORc ligand binding domain (241 to 486) expressed in bacterial expression system after 3 hrs by scintillation counting analysis2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID472520Agonist activity at human LXRbeta assessed as induction of NRP1-6 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID1327579Activation of PXR/LXR in human LS180 cells assessed as induction of P-gp by measuring decrease in intracellular accumulation of Rhodamine-123 at 0.3 uM preincubated for 48 hrs followed by 40 mins incubation with HANKS buffer and subsequent addition of Rho2016European journal of medicinal chemistry, Oct-21, Volume: 122Functional induction of P-glycoprotein efflux pump by phenyl benzenesulfonamides: Synthesis and biological evaluation of T0901317 analogs.
AID703185Transactivational agonist activity at human LXRalpha transfected in HEK293 cells coexpressing CMX-Gal4N-DRIP205 assessed as DRIP205 recruitment at 0.03 to 10 uM after 16 hrs by mammalian two-hybrid assay2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID1233335Increase in ABCA1 gene expression in Bio F1B hamster intestine at 10 mg/kg, po2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists.
AID1249991Increase in ABCA1 gene expression in human THP1 cells at 5 uM by RT-PCR analysis2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators.
AID101843Relative efficacy compared to 24(S),25-epoxy cholesterol in Liver X receptor-alpha ligand-sensing assay2002Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines.
AID1192878Effect on total cholesterol level in high-fat-and-cholesterol diet fed Male Bio F1B hamster plasma at 3 mg/kg, po relative to control2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists.
AID1287450Octanol-water partition coefficient, log P of the compound by HPLC method2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.
AID1287451Agonist activity at human LXRalpha transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.
AID391721Effect on LXRbeta ligand binding domain transfected in monkey CV1 cells assessed as displacement of nuclear co-repressor at 5 uM after 24 hrs by mammalian two-hybrid assay2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.
AID472485Binding affinity to PPARalpha2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID1249981Antagonist activity at human LXR-alpha transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay in presence of 0.3 uM N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-(2,2,2-trifluoroethyl)benzenesulfonamide2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators.
AID715909Induction of lipid accumulation in human HepG2 cells assessed as cellular triglyceride concentration at 1 uM2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells.
AID1575237Full agonist activity at LXR in human HepG2 cells assessed as increase in FASN mRNA level at 10 uM after 24 hrs by qPCR analysis relative to control2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Development of novel liver X receptor modulators based on a 1,2,4-triazole scaffold.
AID474683Displacement of [N-methyl-3H]T1317 from human biotinylated LXRbeta LBD after 3 hrs by LEAD seeker binding assay2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Discovery of tertiary sulfonamides as potent liver X receptor antagonists.
AID1775048Agonist activity at human PXR expressed in HepG2 cells co-expressing luciferase gene under control of CYP3A4 promoter incubated for 24 hrs by luciferase reporter assay
AID1287454Agonist activity at human PXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.
AID1287457Inverse agonist activity at human RORgamma transfected in HEK293 cells after 24 hrs by beta galactosidase luciferase reporter gene assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.
AID345490Effect on ABCA1 gene expression in human differentiated THP1 cells2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
AID299790Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay relative to GW-39652007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.
AID345473Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
AID653688Displacement of [3H]N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-methylbenzenesulfonamide from LXRalpa by scintillation proximity assay2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of a new binding mode for a series of liver X receptor agonists.
AID454639Induction of ABCA1 mRNA upregulation in human THP1 cells2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
AID1575238Full agonist activity at LXR in human HepG2 cells assessed as increase in SREBP-1c mRNA level at 10 uM after 24 hrs by qPCR analysis relative to control2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Development of novel liver X receptor modulators based on a 1,2,4-triazole scaffold.
AID703052Transactivational activity at LXR in C57BL/6J mouse peritoneal macrophages assessed as increase in abca1 mRNA expression at 1 uM by RT-PCR analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID1233350Hypolipidemic effect in Bio F1B hamster fed with high fat and cholesterol diet assessed as HDL-cholesterol level at 10 mg/kg, po relative to control2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists.
AID454930Increase in cellular triglyceride level in human HepG2 cells relative to T09013172010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists.
AID1691870Agonist activity at human RXRalpha/LXRbeta expressed in HEK293 cells measured after 20 hrs by dual luciferase reporter gene assay2020European journal of medicinal chemistry, May-15, Volume: 194Discovery of new LXRβ agonists as glioblastoma inhibitors.
AID1177731Inverse agonist activity at human RoRc-LBD fusion protein with GST expressed in BL-21 (BL3) cells assessed as SRC1 coactivator peptide recruitment2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).
AID1059098Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID424926Induction of SREBP-1C mRNA expression in human HuH7 cells after 18 hrs by RT-PCR2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRbeta.
AID1691871Agonist activity at human RXRalpha/LXRalpha expressed in HEK293 cells measured after 20 hrs by dual luciferase reporter gene assay relative to GW39652020European journal of medicinal chemistry, May-15, Volume: 194Discovery of new LXRβ agonists as glioblastoma inhibitors.
AID454928Increase in cellular triglyceride level in human HepG2 cells2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists.
AID472513Agonist activity at human LXRbeta assessed as induction of TRAP220-1 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID454641Induction of ABCA1 mRNA upregulation in human THP1 cells relative to T09013172010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
AID1066837Modulation of LXR in human HepG2 cells assessed as increase of lipogenesis using [1-14C]acetate at 1 uM after 4 days by scintillation counting2014European journal of medicinal chemistry, Mar-03, Volume: 74Development of new LXR modulators that regulate LXR target genes and reduce lipogenesis in human cell models.
AID1373986Agonist activity at human LXRalpha expressed in HEK293 cells co-expressing CMX-beta-galactosidase incubated for 16 hrs by luciferase reporter gene assay2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Structural development of tetrachlorophthalimides as liver X receptor β (LXRβ)-selective agonists with improved aqueous solubility.
AID262337Half life in mice at 5 mg/kg, po2006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Discovery and optimization of a novel series of liver X receptor-alpha agonists.
AID1595551Agonist activity at Gal4-fused FXR LBD (unknown origin) expressed in 293T cells measured after 24 hrs by dual-luciferase reporter gene assay2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
AID1328935In vivo agonist activity at LXR-beta in cynomolgus monkey assessed as induction of ABCG1 gene at 10 mg/kg/day, po qd administered via gavage for 14 days2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Discovery of Highly Potent Liver X Receptor β Agonists.
AID1543103Agonist activity at PXR (unknown origin) by AlphaScreen assay2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Exploiting Chemical Toolboxes for the Expedited Generation of Tetracyclic Quinolines as a Novel Class of PXR Agonists.
AID1304688Agonist activity at LXR in human HepG2 cells assessed as upregulation of SREBP1C gene expression at 1 uM after 24 hrs by RT-PCR analysis relative to control2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist.
AID239785Relative efficacy for Steroid receptor coactivator-1 (SRC1) recruitment to human LXRalpha compared to GW-39652005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.
AID1287455Inverse agonist activity at human RORalpha transfected in HEK293 cells after 24 hrs by beta galactosidase luciferase reporter gene assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.
AID1243261Binding affinity to His-LXRalpha/FLAG-RXRalpha (unknown origin) by FITC-labeled T0901317 based fluorescence polarization assay2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Discovery and structure-guided optimization of tert-butyl 6-(phenoxymethyl)-3-(trifluoromethyl)benzoates as liver X receptor agonists.
AID1775050Inverse agonist activity at human PXR expressed in HepG2 cells co-expressing luciferase gene under control of CYP3A4 promoter incubated for 24 hrs by luciferase reporter assay
AID1177729Binding affinity to RORgamma (unknown origin)2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).
AID1686020Agonist activity at human LXR-beta2016Journal of medicinal chemistry, Oct-13, Volume: 59, Issue:19
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.
AID452973Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.
AID454635Agonist activity at human Gal4-LBD fused LXRbeta LBD expressed in Huh7 cells by transient transactivation assay2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
AID1301901Toxicity in Tg2576 mouse assessed as increase in liver triglyceride level at 10 mg/kg, sc dosed for 3 weeks2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease.
AID299787Agonist activity at human LXRbeta receptor after 1 hr by HTRF cofactor recruitment assay2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.
AID414323Drug level in C57BL/6J mouse liver at 10 mg/kg/day, ip dosed for 5 days2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Discovery of tetrahydro-cyclopenta[b]indole as selective LXRs modulator.
AID1192874Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells assessed as maximal efficacy at 10 uM after 24 hrs by luciferase reporter gene assay relative to T0901317 luminescence intensity2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists.
AID452966Effect on ABCA1 gene expression in human differentiated THP1 cells2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.
AID1327580Activation of PXR/LXR in human LS180 cells assessed as induction of P-gp at 5 uM measured after 24 hrs by Western blot analysis2016European journal of medicinal chemistry, Oct-21, Volume: 122Functional induction of P-glycoprotein efflux pump by phenyl benzenesulfonamides: Synthesis and biological evaluation of T0901317 analogs.
AID478585Half life in human liver microsome2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.
AID424931Agonist activity at human PPARgamma ligand binding domain (206-477) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRbeta.
AID1316549Drug uptake in Sprague-Dawley rat brain at 30 mg/kg qd administered via oral gavage for 5 days measured 4 hrs post last dose2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
AID1328920Agonist activity at LXR-beta in cynomolgus monkey whole blood assessed as ABCA1 gene induction by measuring ABCA1 mRNA level after 4 hrs by SYBR-Green dye-based Q-PCR analysis relative to control2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Discovery of Highly Potent Liver X Receptor β Agonists.
AID451985Half life in rat liver microsomes after 30 mins2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists.
AID1306571Upregulation of SREBP-1c expression in LDL receptor knock-out mouse liver at 10 mg/kg, po relative to control2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency and β-selectivity of liver X receptor agonist.
AID1692276Inhibition of collagen-induced platelet aggregation in human platelet suspension preincubated for 10 mins followed by collagen stimulation by light transmission-based assay2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Progress toward a Glycoprotein VI Modulator for the Treatment of Thrombosis.
AID1243263Agonist activity at human LXRalpha expressed in African green monkey kidney CV1 cells co-expressing pTAL-LXRE including LXR response element incubated for 20 hrs by luciferase reporter gene assay2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Discovery and structure-guided optimization of tert-butyl 6-(phenoxymethyl)-3-(trifluoromethyl)benzoates as liver X receptor agonists.
AID1466797Chaperone activity at FLAG/GFP-tagged NPC1 I1061T mutant (unknown origin) expressed in HEK293 cells assessed as increase in localization of protein mutant in late endosomes at 30 uM after 24 hrs by Hoechst 33342 staining based fluorescence microscopic ana2017Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12
Phenanthridin-6-one derivatives as the first class of non-steroidal pharmacological chaperones for Niemann-Pick disease type C1 protein.
AID345472Displacement of [3H]TO901317 from human recombinant LXRalpha expressed in Escherichia coli by flashplate method2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
AID1172002Transactivation of LXRalpha (unknown origin) expressed in CV1 cells by luciferase reporter gene assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ.
AID1192873Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists.
AID418717Upregulation of ABCG1 mRNA level in mouse brain homogenates at 10 umol/kg, po daily once after 3 days relative to control2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides.
AID478589Upregulation of SREB1c mRNA level in human HuH7 cells relative to T09013172010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.
AID269847Agonist activity at FXR in HepG2 cells by luciferase activity relative to DMSO at 10 uM2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Identification of a lead pharmacophore for the development of potent nuclear receptor modulators as anticancer and X syndrome disease therapeutic agents.
AID307302Agonist activity at LXRalpha LBD by HTRF cofactor peptide recruitment assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists.
AID452962Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.
AID1691874Displacement of hyodeoxycholicacid-based fluorescent tracer from recombinant human LXRbeta LBD (215 to 461 residues) expressed in Escherichia coli BL21 (DE3) preincubated for 10 mins under shaking condition and measured after 30 mins by fluorescence polar2020European journal of medicinal chemistry, May-15, Volume: 194Discovery of new LXRβ agonists as glioblastoma inhibitors.
AID240219Effective concentration for Steroid receptor coactivator-1 (SRC1) recruitment to human LXRbeta (Liver X receptor)2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.
AID1172001Binding affinity to LXRbeta-RXRalpha heterodimer (unknown origin) expressed in insect cells by scintillation proximity assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ.
AID454631Displacement of [3H]T0901317 from human recombinant LXRalpha LBD2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
AID1595542Inverse agonist activity at Gal4-fused RORgamma LBD (unknown origin) expressed in 293T cells measured after 24 hrs by dual-luciferase reporter gene assay2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
AID271507Transactivation of LXRbeta by luciferase reporter gene assay2006Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
Synthesis and evaluation of anilinohexafluoroisopropanols as activators/modulators of LXRalpha and beta.
AID472505Agonist activity at human LXRalpha assessed as induction of NRIP1-1 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID424930Agonist activity at human PPARalpha ligand binding domain (189-468) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRbeta.
AID1177752Agonist activity at FXR (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).
AID715910Agonist activity at LXR in human THP1 cells assessed as increase in ApoE mRNA level at 1 uM after 48 hrs by qPCR analysis relative to control2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells.
AID1243281Agonist activity at His-LXRbeta/FLAG-RXRalpha (unknown origin) assessed as recruitment of PGC1alpha peptide (130 to 154 residues) pre-incubated for 60 mins before PGC1alpha addition followed by one night of incubation by FRET assay2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Discovery and structure-guided optimization of tert-butyl 6-(phenoxymethyl)-3-(trifluoromethyl)benzoates as liver X receptor agonists.
AID297211Induction on FAS gene expression in human primary hepatocytes at 1 uM2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta.
AID451981Agonist activity at human recombinant LXR-LBD by Gal4beta transactivation assay2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists.
AID414320Plasma concentration in C57BL/6J mouse at 10 mg/kg/day, ip dosed for 5 days2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Discovery of tetrahydro-cyclopenta[b]indole as selective LXRs modulator.
AID1059084Cytotoxicity against human PBMC assessed as effect on cell physiology after 48 hrs by CellTiter-Glo assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID262334AUC in Sprague-Dawley rat at 5 mg/kg, po2006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Discovery and optimization of a novel series of liver X receptor-alpha agonists.
AID715912Agonist activity at LXR-alpha in human THP1 cells assessed as increase cholesterol efflux to HDL at 1 uM by FACs analysis2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells.
AID313459Effect on SREBP1c gene expression in human HepG2 cells relative to TO9013172008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
AID452970Agonist activity at human PPARdelta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.
AID1168689Inverse agonist activity at RORgammaT (unknown origin) by M1H assay relative to control2014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.
AID454632Displacement of [3H]T0901317 from human recombinant LXRbeta LBD2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
AID1192889Effect on Plasma triglyceride level in high-fat-and-cholesterol diet fed Male Bio F1B hamster at 10 mg/kg, po relative to control2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists.
AID391699Displacement of [N-methyl-3H]GW0438 from human biotinylated LXRalpha ligand binding domain2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.
AID307304Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists.
AID478587Upregulation of ABCA1 mRNA level in mouse J774 cells relative to T09013172010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.
AID1059095Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID240246Effective concentration in human ATP binding cassette transporter A1 (ABCA1) transcriptional activation assay2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.
AID1060429Induction of lipogenesis in human myotubes at 1 uM after 4 days by scintillation counting analysis in presence of [1-14C]acetate2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Synthesis and initial biological evaluation of new mimics of the LXR-modulator 22(S)-hydroxycholesterol.
AID313452Agonist activity at human LXRalpha expressed in Huh7 cells by Gal4 transactivation assay2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
AID1566010Toxicity in high fat diet-induced C57BL/6 mouse model of hypercholesterolemia assessed as reduction in liver weight at 20 mg/kg, po administered for 12 weeks by H and E staining-based assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis.
AID313461Effect on LXR-mediated intracellular triglyceride level in human HepG2 cells after 4 to 5 days2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
AID101836Ligand-dependent recruitment of steroid receptor co-activator 1 (SRC1) to Liver X receptor-alpha2002Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines.
AID451984Induction of ABCA1 mRNA expression in mouse J774A1 cells relative to T09013172010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists.
AID1177754Agonist activity at LXRbeta (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).
AID391702Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production by ELISA relative to N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-(2,2,2-trifluoroethyl)benzenesulfonamide2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.
AID1127097Antagonist activity at full-length RORgamma (unknown origin) expressed in 293T cells after 24 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, May-06, Volume: 78Discovery of 2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide derivatives as new RORγ inhibitors using virtual screening, synthesis and biological evaluation.
AID293512Antagonist activity at human LXRbeta by transient transfection assay2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.
AID1821366Inhibition of human APC-labeled RORgammat LBD (262 to 518 residues) transfected in Escherichia coli BL21 (DE3) assessed as biotinylated SRC recruitment incubated for 1 hr by dual FRET assay
AID1168686Inverse agonist activity at recombinant N-terminally GST-tagged RORbeta ligand binding domain (unknown origin) expressed in Escherichia coli incubated for 1 hr by FRET assay2014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.
AID1168706Agonist activity at human LXRbeta expressed in HEK293 cells by luciferase reporter gene assay2014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.
AID273407Displacement of [3H]T-0901317 from human LXR beta receptor2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.
AID1566006Induction of hepatic steatosis in C57BL/6 mouse assessed as accumulation of serum triglyceride level at 50 mg/kg/day, ig administered for 7 days2019European journal of medicinal chemistry, Nov-15, Volume: 182Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis.
AID331159Induction of IL6 gene expression in human THP1 cells at 10 uM by array plate mRNA assay2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators.
AID452959Displacement of [3H]TO901317 from human recombinant LXRbeta expressed in Escherichia coli by flashplate method2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.
AID1059085Inhibition of IFNgamma production in human PBMC after 48 hrs by Sandwich ELISA2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID452969Agonist activity at human PPARgamma ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.
AID1368957Transactivation of PXR in human HepG2 cells by receptor transactivation assay relative to untreated control2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
AID1594668Transactivation of recombinant GAL4-fused human LXRalpha LBD (163 to 447 residues) expressed in human L02 cells measured after 24 hrs by luciferase reporter gene assay relative to control2019Journal of natural products, 06-28, Volume: 82, Issue:6
Diketopiperazine-Type Alkaloids from a Deep-Sea-Derived Aspergillus puniceus Fungus and Their Effects on Liver X Receptor α.
AID1306553Antiatherosclerosis activity in LDL receptor knock out mouse model assessed as decrease in area of lipid accumulation at 10 mg/kg, po by HPLC analysis relative to control2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency and β-selectivity of liver X receptor agonist.
AID1595550Agonist activity at Gal4-fused LXRalpha LBD (unknown origin) expressed in 293T cells measured after 24 hrs by dual-luciferase reporter gene assay2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
AID454926Selectivity ratio of IC50 for human recombinant LXRalpha LBD to IC50 for human recombinant LXRbeta LBD2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists.
AID1066855Modulation of LXR in human myotubes assessed as increase of FAS mRNA expression at 1 uM after 4 days by qPCR analysis2014European journal of medicinal chemistry, Mar-03, Volume: 74Development of new LXR modulators that regulate LXR target genes and reduce lipogenesis in human cell models.
AID313462Agonist activity at human recombinant PPARgamma2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
AID1192883Effect on HDL-C level in high-fat-and-cholesterol diet fed Male Bio F1B hamster plasma at 3 mg/kg, po relative to control2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists.
AID474686Agonist activity at LXRbeta ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Discovery of tertiary sulfonamides as potent liver X receptor antagonists.
AID703180Transactivational antagonist activity at human LXRalpha transfected in HEK293 cells coexpressing CMX-Gal4N-NCoR assessed as NCoR recruitment at 0.03 to 10 uM after 16 hrs by reporter gene assay2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID331160Induction of Cox2 gene expression in human THP1 cells at 10 uM by array plate mRNA assay2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators.
AID1139705Antagonist activity at human LXR-beta expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (RORγ)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand.
AID472504Agonist activity at human LXRalpha assessed as induction of PCAF cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID313450Agonist activity at human LXRbeta expressed in Huh7 cells by Gal4 transactivation assay2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
AID454925Displacement of [3H]T0901317 from human recombinant LXRbeta LBD2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists.
AID345492Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
AID1328919Agonist activity at LXR-beta in cynomolgus monkey whole blood assessed as ABCA1 gene induction by measuring ABCA1 mRNA level after 4 hrs by SYBR-Green dye-based Q-PCR analysis2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Discovery of Highly Potent Liver X Receptor β Agonists.
AID1192871Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists.
AID262336AUC in dog at 5 mg/kg, po2006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Discovery and optimization of a novel series of liver X receptor-alpha agonists.
AID101837Effective concentration in LXR alpha-Gal4 receptor gene assay2002Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines.
AID1306556Antiatherosclerosis activity in LDL receptor knock out mouse model assessed as increase in TG levels at 10 mg/kg, po by HPLC analysis relative to control2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency and β-selectivity of liver X receptor agonist.
AID703049Transactivational activity at LXR in human HuH7 cells assessed as increase in fas mRNA expression at 0.1 uM after 24 hrs by RT-PCR analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID1177720Inhibition of RORa (unknown origin) assessed as inhibition of coactivator recruitment by GAL4-nuclear receptor LBD assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).
AID1059102Inverse agonist activity at N-terminal 6xHis-tagged human RORc ligand binding domain (241 to 486) expressed in bacterial expression system assessed as inhibition of SRC1 co-activator peptide recruitment after 3 hrs by TR-FRET analysis2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID452863Agonist activity at human recombinant LXRbeta expressed in CHO cells assessed as effect on secreted alkaline phosphatase by LAFbeta assay2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
4-(3-aryloxyaryl)quinoline alcohols are liver X receptor agonists.
AID1172005Transactivation of LXR (unknown origin) expressed in human HeLa cells by ABCA1 LXREx3 reporter assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ.
AID313448Selectivity for human LXRbeta over human LXRalpha2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
AID1139695Inverse agonist activity at human ROR-alpha1 expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (RORγ)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand.
AID1192893Effect on area of lipid accumulation in high-fat-and-cholesterol diet fed Male Bio F1B hamster aortic arch at 3 mg/kg, po relative to control2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists.
AID424751Agonist activity at human LXRbeta ligand binding domain (219-462) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRbeta.
AID1316521Displacement of radiolabeled T0901317 from LXRbeta LBD (unknown origin)2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
AID345495Effect on SREBP1c gene expression in human HepG2 cells relative to TO9013172008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
AID703188Transactivational antagonist activity at human LXRbeta transfected in HEK293 cells expressing CMX-Gal4N assessed as inhibition of T1317-induced luciferase activity after 16 hrs by reporter gene assay2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID313458Effect on SREBP1c gene expression in human HepG2 cells2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
AID1327582Therapeutic index, ratio of effective concentration for cytotoxicity in human LS180 cells to effective concentration for activation of PXR/LXR in human LS180 cells assessed as induction of P-gp2016European journal of medicinal chemistry, Oct-21, Volume: 122Functional induction of P-glycoprotein efflux pump by phenyl benzenesulfonamides: Synthesis and biological evaluation of T0901317 analogs.
AID313457Effect on ABCA1 gene expression in mouse J774 cells relative to TO9013172008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
AID101842Relative efficacy compared to 24(S),25-epoxy cholesterol in LXR alpha-Gal4 receptor gene assay2002Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines.
AID1168690Inverse agonist activity at RORalpha (unknown origin) by M1H assay2014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.
AID451983Induction of ABCA1 mRNA expression in mouse J774A1 cells2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists.
AID715905Upregulation of SCD1 gene expression in human HepG2 cells at 1 uM by qPCR analysis2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells.
AID345496Effect on triglyceride accumulation in human HepG2 cells2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
AID1691872Agonist activity at human RXRalpha/LXRbeta expressed in HEK293 cells measured after 20 hrs by dual luciferase reporter gene assay relative to GW39652020European journal of medicinal chemistry, May-15, Volume: 194Discovery of new LXRβ agonists as glioblastoma inhibitors.
AID1301866Increase in amyloid beta40 in CSF of rhesus monkey at 5 mg/kg, po administered for 2 weeks2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease.
AID1287453Agonist activity at human FXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.
AID1059091Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID241121Inhibition of human GSK3-beta; NT=Not tested2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.
AID1060434Agonist activity at LXR in human myotubes assessed as upregulation of SCD1 expression at 1 uM after 4 days by qPCR analysis2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Synthesis and initial biological evaluation of new mimics of the LXR-modulator 22(S)-hydroxycholesterol.
AID703194Transactivational agonist activity at human LXRalpha transfected in HEK293 cells expressing CMX-Gal4N assessed as luciferase activity after 16 hrs by reporter gene assay relative to N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-methylbenzami2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID1192908Effect on Plasma triglyceride level in high-fat-and-cholesterol diet fed Male Bio F1B hamster at 3 to 10 mg/kg, po relative to control2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists.
AID1177753Agonist activity at LXRalpha (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).
AID1306559Antiatherosclerosis activity in LDL receptor knock out mouse model assessed as decrease in LDL-C levels at 10 mg/kg, po by HPLC analysis relative to control2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency and β-selectivity of liver X receptor agonist.
AID331155Induction of SREBP1c gene expression in human THP1 cells at 10 uM by array plate mRNA assay2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators.
AID703191Transactivational agonist activity at human LXRbeta transfected in HEK293 cells expressing CMX-Gal4N assessed as luciferase activity after 16 hrs by reporter gene assay relative to N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-methylbenzamid2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID1233338Increase in ABCA1 gene expression in Bio F1B hamster peripheral blood at 10 mg/kg, po2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists.
AID1512050Agonist activity at full-length human RXR/LXR expressed in HEK293T cells at 1 uM after 14 to 16 hrs by dual-glo luciferase reporter gene assay relative to untreated control2019ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9
A Novel Biphenyl-based Chemotype of Retinoid X Receptor Ligands Enables Subtype and Heterodimer Preferences.
AID703029Transrepressional activity at LXR in human TPA-activated THP1 cells assessed as inhibition of LPS-induced IL6 production incubated for 6 hrs prior to LPS-challenge measured after 18 hrs by ELISA2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID1295291Inverse agonist activity at recombinant human GST-tagged ROR-gamma receptor ligand binding domain assessed as inhibition of receptor and co-activator TRAP220 interaction by FRET assay2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Discovery of biaryls as RORγ inverse agonists by using structure-based design.
AID703179Transactivational antagonist activity at human LXRalpha transfected in HEK293 cells coexpressing CMX-Gal4N-SMRT assessed as SMRT recruitment at 0.03 to 10 uM after 16 hrs by reporter gene assay2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID331150Induction of NR1H2 gene expression in human THP1 cells at 10 uM by array plate mRNA assay2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators.
AID758932Agonist activity at LXR in human HepG2 cells assessed as upregulation of SREBP1C expression at 10 uM after 24 hrs by RT-qPCR analysis relative to control2013Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
Cyanidin, a natural flavonoid, is an agonistic ligand for liver X receptor alpha and beta and reduces cellular lipid accumulation in macrophages and hepatocytes.
AID472484Tmax in C57 mouse at 10 mg/kg, po2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID1398744Inhibition of human RORgamma1 expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Development of novel silanol-based human pregnane X receptor (PXR) agonists with improved receptor selectivity.
AID1127098Antagonist activity at Gal4-fused RORgamma (unknown origin) expressed in 293T cells at 10 uM after 24 hrs by luciferase reporter gene assay relative to control2014European journal of medicinal chemistry, May-06, Volume: 78Discovery of 2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide derivatives as new RORγ inhibitors using virtual screening, synthesis and biological evaluation.
AID299792Induction of SREBP1c gene expression in HepG2 cells at 10 uM relative to control2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.
AID1458213Agonist activity at LXR in human HepG2 cells assessed as upregulation of FASN mRNA levels at 10 uM after 6 hrs by qPCR analysis2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID474689Agonist activity at LXRalpha ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay relative to T13172010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Discovery of tertiary sulfonamides as potent liver X receptor antagonists.
AID1892223Agonist activity against human LXRalpha expressed in human HEK293T cells co-expressing CMX-GAL4N-hLXRalpha incubated for 24 hrs by reporter gene assay2022Bioorganic & medicinal chemistry, 07-15, Volume: 66Design, synthesis and structure-activity relationship of 4-(1,1,1,3,3,3-hexafluoro-2-hydroxyisoprop-2-yl)phenylsilane derivatives as liver X receptor agonists.
AID472496Agonist activity at human LXRalpha assessed as induction of SRC1-3 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID569814Agonist activity at LXRalpha by TR-FRET assay2011Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3
Identification of diaryl ether-based ligands for estrogen-related receptor α as potential antidiabetic agents.
AID472612Agonist activity at human LXRalpha assessed as induction of p300-1 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID307308Ratio of induction of lipogenesis in HepG2 cells at 10 uM to control after 24 hrs2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists.
AID1368963Agonist activity at GAL4-tagged human LXRbeta assessed as receptor activation expressed in African green monkey CV1 cells by luciferase reporter gene assay2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
AID451978Displacement of [3H]T0901317 from human recombinant LXRalpha-LBD2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists.
AID474690Agonist activity at LXRbeta ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay relative to T13172010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Discovery of tertiary sulfonamides as potent liver X receptor antagonists.
AID1576218Agonist activity at LXR alpha (unknown origin) by Alpha Screen assay2019MedChemComm, Aug-01, Volume: 10, Issue:8
Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool.
AID472478Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID478586Upregulation of ABCA1 mRNA level in mouse J774 cells2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.
AID472510Agonist activity at human LXRbeta assessed as induction of SRC2-1 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID1368961Agonist activity at GAL4-tagged human LXRalpha assessed as receptor activation expressed in African green monkey CV1 cells by luciferase reporter gene assay2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
AID768571Induction of cytoplasmic lipid accumulation in human HepG2 cells at 1 uM after 4 days by oil red O staining-based light microscopic analysis2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Synthesis and identification of new flavonoids targeting liver X receptor β involved pathway as potential facilitators of Aβ clearance with reduced lipid accumulation.
AID454642Increase in cellular triglyceride level in human HepG2 cells relative to T09013172010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
AID715949Transactivation of human LXR-alpha transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells.
AID1306539Agonist activity at GAL4 fused LXRalpha (unknown origin) transfected in CHOK1 cells after 24 hrs by luciferase reporter gene assay2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency and β-selectivity of liver X receptor agonist.
AID1595549Inverse agonist activity at Gal4-fused RORalpha LBD (unknown origin) expressed in 293T cells measured after 24 hrs by dual-luciferase reporter gene assay relative to control2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
AID472515Agonist activity at human LXRbeta assessed as induction of PGC1b-2 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID1368964Agonist activity at GAL4-tagged human LXRbeta assessed as receptor activation expressed in African green monkey CV1 cells by luciferase reporter gene assay relative to untreated control2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
AID1316520Displacement of radiolabeled T0901317 from LXRalpha LBD (unknown origin)2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
AID1127100Antagonist activity at human His6-tagged RORgamma ligand binding domain (262 to 507 aa) assessed as inhibition of SRC1-4 co-activator peptide recruitment by luminescence-based AlphaScreen assay2014European journal of medicinal chemistry, May-06, Volume: 78Discovery of 2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide derivatives as new RORγ inhibitors using virtual screening, synthesis and biological evaluation.
AID331163Induction of TBP gene expression in human THP1 cells at 10 uM using by array plate mRNA assay2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators.
AID1306562Antiatherosclerosis activity in LDL receptor knock out mouse model assessed as decrease in HDL-C levels at 10 mg/kg, po by HPLC analysis relative to control2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency and β-selectivity of liver X receptor agonist.
AID273406Displacement of [3H]T-0901317 from human LXR alpha receptor2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.
AID703056Transrepressional activity at LXR in C57BL/6J mouse peritoneal macrophages assessed as inhibition of LPS-induced IL-6 mRNA expression at 3 uM incubated for 6 hr prior to LPS-challenge measured after 18 hrs by RT-PCR analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID307307Induction of cholesterol efflux in THP1 cells after 18 hrs2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists.
AID1059087Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID1306568Upregulation of ABCA1 mRNA expression in LDL receptor knock-out mouse blood at 10 mg/kg, po relative to control2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency and β-selectivity of liver X receptor agonist.
AID1172006Transactivation of LXR (unknown origin) expressed in human HeLa cells by ABCA1 LXREx3 reporter assay relative to 1-(2,4-difluorobenzyl)-2-oxo-6-(4-phenoxyphenyl)-4-(trifluoromethyl)-1,2-dihydropyridine-3-carbonitrile2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ.
AID472472Induction of [3H]cholesterol efflux in human HepG2 cells loaded with ac-LDL assessed as lipid accumulation2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID331153Induction of ABCG1 gene expression in human THP1 cells at 10 uM by array plate mRNA assay2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators.
AID1066840Modulation of LXR in human myotubes assessed as increase of lipogenesis using [1-14C]acetate at 1 uM after 4 days by scintillation counting2014European journal of medicinal chemistry, Mar-03, Volume: 74Development of new LXR modulators that regulate LXR target genes and reduce lipogenesis in human cell models.
AID1066854Modulation of LXR in human myotubes assessed as increase of SCD1 mRNA expression at 1 uM after 4 days by qPCR analysis2014European journal of medicinal chemistry, Mar-03, Volume: 74Development of new LXR modulators that regulate LXR target genes and reduce lipogenesis in human cell models.
AID1373988Agonist activity at human LXRbeta expressed in HEK293 cells co-expressing CMX-beta-galactosidase incubated for 16 hrs by luciferase reporter gene assay2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Structural development of tetrachlorophthalimides as liver X receptor β (LXRβ)-selective agonists with improved aqueous solubility.
AID1605741Agonist activity at His-tagged PXR-LBD/SRC-1p (unknown origin) expressed in Escherichia coli BL21(DE3) at 10 uM by coactivator recruitment based Alpha-screen assay2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
AID1327577Cytotoxicity against human LS180 cells assessed as effect on cell viability measured after 24 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Functional induction of P-glycoprotein efflux pump by phenyl benzenesulfonamides: Synthesis and biological evaluation of T0901317 analogs.
AID758941Agonist activity at LXRbeta (unknown origin) expressed in CHOK1 cells assessed as induction of transactivation activity at 2 uM after 24 hrs by luciferase reporter gene assay relative to control2013Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
Cyanidin, a natural flavonoid, is an agonistic ligand for liver X receptor alpha and beta and reduces cellular lipid accumulation in macrophages and hepatocytes.
AID478590Increase in triglyceride level in human HepG2 cells2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.
AID1243262Binding affinity to His-LXRbeta/FLAG-RXRalpha (unknown origin) by FITC-labeled T0901317 based fluorescence polarization assay2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Discovery and structure-guided optimization of tert-butyl 6-(phenoxymethyl)-3-(trifluoromethyl)benzoates as liver X receptor agonists.
AID1316559Effect on amyloid beta (1 to 40) level in Sprague-Dawley rat CSF at 30 mg/kg qd administered via oral gavage for 5 days2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
AID418705Agonist activity at human LXRalpha expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides.
AID1398739Agonist activity at VP16-fused human PXR expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Development of novel silanol-based human pregnane X receptor (PXR) agonists with improved receptor selectivity.
AID271505Binding affinity to LXRbeta by radioligand displacement assay2006Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
Synthesis and evaluation of anilinohexafluoroisopropanols as activators/modulators of LXRalpha and beta.
AID703198Transactivational agonist activity at human LXRalpha transfected in HEK293 cells expressing CMX-Gal4N assessed as luciferase activity after 16 hrs by reporter gene assay2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID1301900Toxicity in Tg2576 transgenic mouse assessed as increase in plasma triglyceride level at 10 mg/kg, sc dosed for 3 weeks2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease.
AID472518Agonist activity at human LXRbeta assessed as induction of NRIP1-1 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID1059099Inverse agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID454646Half life in mouse liver microsomes2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
AID1327575Cytotoxicity against human LS180 cells assessed as effect on cell viability at 50 uM measured after 24 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Oct-21, Volume: 122Functional induction of P-glycoprotein efflux pump by phenyl benzenesulfonamides: Synthesis and biological evaluation of T0901317 analogs.
AID328049Agonist activity at LXR2008Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development.
AID1177719Inhibition of RORc (unknown origin) assessed as inhibition of coactivator recruitment by GAL4-nuclear receptor LBD assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).
AID451986Half life in human liver microsomes after 30 mins2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists.
AID472503Agonist activity at human LXRalpha assessed as induction of CPB/p300-2 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID307305Ratio of induction of ABCA1 gene expression in THP1 cells at 10 uM to control2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists.
AID1327578Cytotoxicity against human SH-SY5Y cells assessed as effect on cell viability measured after 24 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Functional induction of P-glycoprotein efflux pump by phenyl benzenesulfonamides: Synthesis and biological evaluation of T0901317 analogs.
AID1287452Agonist activity at human LXRbeta transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.
AID451979Displacement of [3H]T0901317 from human recombinant LXRbeta-LBD2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists.
AID472519Agonist activity at human LXRbeta assessed as induction of NRP1-3 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID703050Transactivational activity at LXR in human HuH7 cells assessed as increase in srebp1c mRNA expression at 0.1 uM after 24 hrs by RT-PCR analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID1854609Inhibition of IL-17A production in PMA/ionomycin-stimulated mouse EL4 cells at 20 uM measured by ELISA relative to control2022Bioorganic & medicinal chemistry, 10-01, Volume: 71Design, synthesis and in vitro biological evaluation of marine phidianidine derivatives as potential anti-inflammatory agents.
AID472613Agonist activity at human LXRbeta assessed as induction of p300-1 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID271504Binding affinity to LXRalpha by radioligand displacement assay2006Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
Synthesis and evaluation of anilinohexafluoroisopropanols as activators/modulators of LXRalpha and beta.
AID452971Effect on triglyceride accumulation in human HepG2 cells2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.
AID1059100Inverse agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID262339Activity against LXR alpha transiently transfected in HEK293 cells2006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Discovery and optimization of a novel series of liver X receptor-alpha agonists.
AID307306Ratio of induction of SREBP1c gene expression in THP1 cells at 10 uM to control2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists.
AID331158Induction of HDS11B1 gene expression in human THP1 cells at 10 uM using Array plate mRNA assay2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators.
AID1327583Therapeutic index, ratio of effective concentration for cytotoxicity in human SH-SY5Y cells to effective concentration for activation of PXR/LXR in human LS180 cells assessed as induction of P-gp2016European journal of medicinal chemistry, Oct-21, Volume: 122Functional induction of P-glycoprotein efflux pump by phenyl benzenesulfonamides: Synthesis and biological evaluation of T0901317 analogs.
AID1177721Binding affinity to RORc (unknown origin) by radioligand binding assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).
AID452968Agonist activity at human PPARalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.
AID1233359Hypolipidemic effect in Bio F1B hamster fed with high fat and cholesterol diet assessed as lipid-accumulation area in aortic arch at 10 mg/kg, po relative to control2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists.
AID474685Agonist activity at LXRalpha ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Discovery of tertiary sulfonamides as potent liver X receptor antagonists.
AID414311Increase in HDL-cholesterol level in C57BL/6J mouse at 10 mg/kg/day, ip dosed for 5 days measured 2 hrs after last dose2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Discovery of tetrahydro-cyclopenta[b]indole as selective LXRs modulator.
AID454640Increase in cellular triglyceride level in human HepG2 cells2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
AID1127099Antagonist activity at full-length RORgamma (unknown origin) expressed in 293T cells at 10 uM after 24 hrs by luciferase reporter gene assay relative to control2014European journal of medicinal chemistry, May-06, Volume: 78Discovery of 2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide derivatives as new RORγ inhibitors using virtual screening, synthesis and biological evaluation.
AID1316561Effect on amyloid beta (1 to 42) level in Sprague-Dawley rat cerebrum at 30 mg/kg, po qd administered for 5 days2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
AID472509Agonist activity at human LXRbeta assessed as induction of SRC1-3 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID715948Transactivation of human LXR-beta transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells.
AID1168688Inverse agonist activity at RORgammaT (unknown origin) by M1H assay2014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.
AID1306544Agonist activity at GAL4 fused LXRbeta-LBD (unknown origin) transfected in CHOK1 cells at 10 uM after 24 hrs by luciferase reporter gene assay in presence of T09013172016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency and β-selectivity of liver X receptor agonist.
AID472479Binding affinity to human recombinant LXRbeta ligand binding domain2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID1172004Transactivation of LXRalpha (unknown origin) expressed in CV1 cells by luciferase reporter gene assay relative to 1-(2,4-difluorobenzyl)-2-oxo-6-(4-phenoxyphenyl)-4-(trifluoromethyl)-1,2-dihydropyridine-3-carbonitrile2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ.
AID328046Inhibition of Saccharomyces sp. alpha-glucosidase2008Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development.
AID1192879Effect on total cholesterol level in high-fat-and-cholesterol diet fed Male Bio F1B hamster plasma at 10 mg/kg, po relative to control2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists.
AID345491Effect on ABCA1 gene expression in human differentiated THP1 cells relative to TO9013172008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
AID293510Displacement of [N-methyl-3H]GW0438X from human PXR2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.
AID472498Agonist activity at human LXRalpha assessed as induction of SRC2-3 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID1458214Agonist activity at LXR in human HepG2 cells assessed as upregulation of SREBP1c mRNA levels at 10 uM after 6 hrs by qPCR analysis2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID472468Agonist activity at human LXRalpha in HEK293 cells assessed as Gal4 transactivation2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID715944Agonist activity at human LXR-beta assessed as increase in recruitment of Trap 220/D22 coactivator peptide by TR-FRET assay2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells.
AID1287456Inverse agonist activity at human RORbeta transfected in HEK293 cells after 24 hrs by beta galactosidase luciferase reporter gene assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.
AID1306565Antiatherosclerosis activity in LDL receptor knock out mouse model assessed as decrease in TC levels at 10 mg/kg, po by HPLC analysis relative to control2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency and β-selectivity of liver X receptor agonist.
AID758943Binding affinity to human LXRalpha-LBD by surface plasmon resonance2013Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
Cyanidin, a natural flavonoid, is an agonistic ligand for liver X receptor alpha and beta and reduces cellular lipid accumulation in macrophages and hepatocytes.
AID454924Displacement of [3H]T0901317 from human recombinant LXRalpha LBD2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists.
AID1566014Induction of hepatic steatosis in C57BL/6 mouse assessed as accumulation of hepatic triglyceride level at 50 mg/kg/day, ig administered for 7 days2019European journal of medicinal chemistry, Nov-15, Volume: 182Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis.
AID703028Transrepressional activity at LXR in human TPA-activated THP1 cells assessed as inhibition of LPS-induced IL6 production incubated for 6 hrs prior to LPS-challenge measured after 18 hrs by ELISA relative to 2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID1691873Selectivity index, ratio of EC50 for agonist activity at human RXRalpha/LXRalpha expressed in HEK293 cells to EC50 for agonist activity at human RXRalpha/LXRbeta expressed in HEK293 cells2020European journal of medicinal chemistry, May-15, Volume: 194Discovery of new LXRβ agonists as glioblastoma inhibitors.
AID472502Agonist activity at human LXRalpha assessed as induction of PGC1b-2 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID1172000Binding affinity to LXRalpha-RXRalpha heterodimer (unknown origin) expressed in insect cells by scintillation proximity assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ.
AID1243282Agonist activity at His-LXRbeta/FLAG-RXRalpha (unknown origin) assessed as recruitment of ASC2 peptide (1481 to 1510 residues) pre-incubated for 60 mins before ASC2 peptide addition followed by one night of incubation by FRET assay2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Discovery and structure-guided optimization of tert-butyl 6-(phenoxymethyl)-3-(trifluoromethyl)benzoates as liver X receptor agonists.
AID715904Upregulation of SREBP-1 gene expression in human HepG2 cells at 1 uM by immunoblot analysis2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells.
AID472508Agonist activity at human LXRbeta assessed as induction of SRC1-1 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID703044Induction of LPS-induced IL-6 production in LXRalpha,LXRbeta-deficient C57BL/6J mouse peritoneal macrophages at 3 uM incubated for 6 hrs prior to LPS-induction measured after 18 hrs by ELISA2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID1301857Increase in hepatic fat content in rhesus monkey at 10 mg/kg, po qd for 2 weeks by magnetic resonance spectroscopic imaging method relative to vehicle control2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease.
AID715945Agonist activity at human LXR-alpha assessed as increase in recruitment of Trap 220/Drip2 coactivator peptide by TR-FRET assay2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells.
AID1192907Effect on LDL-C level in high-fat-and-cholesterol diet fed Male Bio F1B hamster plasma at 3 to 10 mg/kg, po relative to control2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists.
AID478584Half life in rat liver microsome2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.
AID1327573Activation of PXR/LXR in human LS180 cells assessed as induction of P-gp measured as intracellular accumulation of Rhodamine-123 at 5 uM preincubated for 48 hrs followed by 40 mins incubation with HANKS buffer and subsequent addition of Rhodamine-123 meas2016European journal of medicinal chemistry, Oct-21, Volume: 122Functional induction of P-glycoprotein efflux pump by phenyl benzenesulfonamides: Synthesis and biological evaluation of T0901317 analogs.
AID478580Displacement of [3H]T0901317 from LXRbeta ligand binding domain2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.
AID703055Transrepressional activity at LXR in C57BL/6J mouse peritoneal macrophages assessed as inhibition of LPS-induced IL-1beta mRNA expression at 3 uM incubated for 6 hr prior to LPS-challenge measured after 18 hrs by RT-PCR analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID472497Agonist activity at human LXRalpha assessed as induction of SRC2-1 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID1316553Induction of ABCA1 mRNA expression in Sprague-Dawley rat brain at 30 mg/kg qd administered via oral gavage for 5 days measured 4 hrs post last dose relative to control2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
AID472499Agonist activity at human LXRalpha assessed as induction of SRC3-2 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID1177750Agonist activity at RoRb (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).
AID452974Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL relative to TO9013172010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.
AID715907Upregulation of SREBP-1 gene expression in human HepG2 cells at 1 uM by qPCR analysis2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells.
AID1249992Increase in SREBP-1c gene expression in human THP1 cells at 5 uM by RT-PCR analysis2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators.
AID424932Agonist activity at human PPARdelta ligand binding domain (165-441) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRbeta.
AID1892224Agonist activity against human LXRbeta expressed in human HEK293T cells co-expressing CMX-GAL4N-hLXRbeta incubated for 24 hrs by reporter gene assay2022Bioorganic & medicinal chemistry, 07-15, Volume: 66Design, synthesis and structure-activity relationship of 4-(1,1,1,3,3,3-hexafluoro-2-hydroxyisoprop-2-yl)phenylsilane derivatives as liver X receptor agonists.
AID271506Transactivation of LXRalpha by luciferase reporter gene assay2006Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
Synthesis and evaluation of anilinohexafluoroisopropanols as activators/modulators of LXRalpha and beta.
AID313460Effect on LXR-mediated intracellular triglyceride level in human HepG2 cells after 4 to 5 days2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
AID1327576Cytotoxicity against human SH-SY5Y cells assessed as effect on cell viability at 50 uM measured after 24 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Oct-21, Volume: 122Functional induction of P-glycoprotein efflux pump by phenyl benzenesulfonamides: Synthesis and biological evaluation of T0901317 analogs.
AID345475Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
AID313447Binding affinity at human LXRalpha2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
AID703190Transactivational antagonist activity at human LXRalpha transfected in HEK293 cells expressing CMX-Gal4N assessed as inhibition of T1317-induced luciferase activity after 16 hrs by reporter gene assay2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID239783Relative efficacy in human ATP binding cassette transporter A1 (ABCA1) transcriptional activation assay compared to GW-39652005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.
AID1059093Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID262335AUC in mice at 5 mg/kg, po2006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Discovery and optimization of a novel series of liver X receptor-alpha agonists.
AID569815Agonist activity at LXRbeta by TR-FRET assay2011Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3
Identification of diaryl ether-based ligands for estrogen-related receptor α as potential antidiabetic agents.
AID1139700Agonist activity at human LXR-beta expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (RORγ)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand.
AID472495Agonist activity at human LXRalpha assessed as induction of SRC1-1 cofactor recruitment2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID418426Agonist activity at LXRalpha ligand binding domain by FRET based SRC1 recruitment assay2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides.
AID1458221Agonist activity at LXR in human U937 cells assessed as downregulation of LPS-induced CCL2 mRNA expression at 10 uM after 6 hrs by qPCR analysis2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID1233300Agonist activity at LXRalpha (unknown origin)2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists.
AID313451Agonist activity at human LXRbeta expressed in Huh7 cells by Gal4 transactivation assay relative to TO9013172008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
AID1249980Agonist activity at human LXR-beta transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators.
AID1368955Inverse agonist activity at Gal4-tagged human RORgammat ligand binding domain expressed in human Jurkat cells by native IL17 promoter driven luciferase reporter gene assay2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
AID1775052Antagonist activity at human PXR expressed in HepG2 cells co-expressing luciferase gene under control of CYP3A4 promoter incubated for 24 hrs in presence of 5 uM rifampicin by luciferase reporter assay
AID472474Induction of ABCA1 expression in human THP1 cells2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
AID703042Inhibition of LPS-induced IL-6 mRNA expression in LXRalpha-deficient C57BL/6J mouse peritoneal macrophages at 3 uM incubated for 6 hrs prior to LPS-challenge measured after 18 hrs by RT-PCR analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
AID424748Displacement of [3H]T0901317 from human recombinant N-terminal biotinylated tagged LXRbeta ligand binding domain (154-461) expressed in Escherichia coli2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRbeta.
AID452961Selectivity ratio, IC50 for human LXRalpha to IC50 for human LXRbeta2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.
AID1328921Plasma concentration in cynomolgus monkey at 10 mg/kg, po qd administered via gavage for 14 days measured after 5 hrs of last-dose by LC/MS/MS analysis2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Discovery of Highly Potent Liver X Receptor β Agonists.
AID1775046Displacement of BODIPY FL vindoline from GST-tagged human PXR LBD incubated for 60 mins by TR-FRET assay
AID1698085Agonist activity at GST-tagged human LXR assessed as induction of biotinylated coactivator SRC-1 peptide recruitment measured after 2 hrs by streptavidin-conjugated AlphaScreen assay2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis.
AID1233347Hypolipidemic effect in Bio F1B hamster fed with high fat and cholesterol diet assessed as total cholesterol level at 10 mg/kg, po relative to control2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists.
AID299795Induction of Lipogenesis in HepG2 cells at 10 uM relative to control2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.
AID424750Selectivity ratio of IC50 for human recombinant N-terminal biotinylated tagged LXRalpha ligand binding domain (197-447) to IC50 for human recombinant N-terminal biotinylated tagged LXRbeta ligand binding domain (154-461)2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRbeta.
AID1243279Agonist activity at His-LXRalpha/FLAG-RXRalpha (unknown origin) assessed as recruitment of PGC1alpha peptide (130 to 154 residues) pre-incubated for 60 mins before PGC1alpha addition followed by one night of incubation by FRET assay2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Discovery and structure-guided optimization of tert-butyl 6-(phenoxymethyl)-3-(trifluoromethyl)benzoates as liver X receptor agonists.
AID1059097Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID1139697Inverse agonist activity at human ROR-gamma1 expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (RORγ)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand.
AID478588Upregulation of SREB1c mRNA level in human HuH7 cells2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.
AID331151Induction of LXRalpha gene expression in human THP1 cells at 10 uM by array plate mRNA assay2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators.
AID273408Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.
AID299794Induction of cholesterol efflux in THP1 cells at 10 uM relative to control2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.
AID309256Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as reduction of Amyloid beta-38 formation by LPECL assay2007Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19
Conversion of the LXR-agonist TO-901317--from inverse to normal modulation of gamma-secretase by addition of a carboxylic acid and a lipophilic anchor.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1798629LXR Binding Assay and hLXR Reporter Assay from Article 10.1021/jm800799q: \\Indazole-Based Liver X Receptor (LXR) Modulators with Maintained Atherosclerotic Lesion Reduction Activity but Diminished Stimulation of Hepatic Triglyceride Synthesis\\2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
AID1798364alpha-Glucosidase Inhibition Assay from Article 10.1016/j.bmc.2008.02.078: \\Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development.\\2008Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development.
AID1797956Cell-Free Ligand Sensing Assay (LiSA)-LXRalpha-SRC1 Assay from Article 10.1021/jm050532w: \\Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.\\2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.
AID1797933LXR Binding Assay and hLXR beta Reporter Assay from Article 10.1021/jm0609566: \\Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.\\2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.
AID1798792HTRF Cofactor Peptide Recruitment Assay from Article 10.1016/j.bmcl.2007.06.017: \\2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.\\2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.
AID1798107Competition Ligand Binding Assay and Transient Transfection Assay from Article 10.1016/j.bmc.2006.12.026: \\Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.\\2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.
AID1797958Cell-Free Ligand Sensing Assay (LiSA)-LXRalpha-SRC1 Assay from Article 10.1021/jm0255116: \\Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines.\\2002Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines.
AID1799289LXRbeta Binding Assay (IC50) and LAFbeta Functional Assay (EC50) from Article 10.1016/j.bmc.2009.10.001: \\4-(3-aryloxyaryl)quinoline alcohols are liver X receptor agonists.\\2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
4-(3-aryloxyaryl)quinoline alcohols are liver X receptor agonists.
AID1797932LXR Binding Assay from Article 10.1021/jm0609566: \\Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.\\2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.
AID1797957Cell-Free Ligand Sensing Assay (LiSA)-LXRbeta-SRC1 Assay from Article 10.1021/jm050532w: \\Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.\\2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of a new binding mode for a series of liver X receptor agonists.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
AID1346993Human Liver X receptor-beta (1H. Liver X receptor-like receptors)2000Genes & development, Nov-15, Volume: 14, Issue:22
Role of LXRs in control of lipogenesis.
AID1346755Human Liver X receptor-alpha (1H. Liver X receptor-like receptors)2000Genes & development, Nov-15, Volume: 14, Issue:22
Role of LXRs in control of lipogenesis.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (563)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's187 (33.21)29.6817
2010's337 (59.86)24.3611
2020's39 (6.93)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.92

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index28.92 (24.57)
Research Supply Index6.35 (2.92)
Research Growth Index6.91 (4.65)
Search Engine Demand Index36.71 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.92)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (0.53%)5.53%
Reviews7 (1.23%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other557 (98.24%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
protocatechuic acid
protocatechuic acid: RN given refers to parent cpd; structure. 3,4-dihydroxybenzoic acid : A dihydroxybenzoic acid in which the hydroxy groups are located at positions 3 and 4.		2.0810catechols;
dihydroxybenzoic acid		antineoplastic agent;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.14.11.2 (procollagen-proline dioxygenase) inhibitor;
human xenobiotic metabolite;
plant metabolite
gamma-aminobutyric acid
gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4.		2.2510amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid		human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule
lactic acid
Lactic Acid: A normal intermediate in the fermentation (oxidation, metabolism) of sugar. The concentrated form is used internally to prevent gastrointestinal fermentation. (From Stedman, 26th ed). 2-hydroxypropanoic acid : A 2-hydroxy monocarboxylic acid that is propanoic acid in which one of the alpha-hydrogens is replaced by a hydroxy group.		2.06102-hydroxy monocarboxylic acidalgal metabolite;
Daphnia magna metabolite
glycerol
Moon: The natural satellite of the planet Earth. It includes the lunar cycles or phases, the lunar month, lunar landscapes, geography, and soil.		2.0110alditol;
triol		algal metabolite;
detergent;
Escherichia coli metabolite;
geroprotector;
human metabolite;
mouse metabolite;
osmolyte;
Saccharomyces cerevisiae metabolite;
solvent
hydrogen carbonate
Bicarbonates: Inorganic salts that contain the -HCO3 radical. They are an important factor in determining the pH of the blood and the concentration of bicarbonate ions is regulated by the kidney. Levels in the blood are an index of the alkali reserve or buffering capacity.. hydrogencarbonate : The carbon oxoanion resulting from the removal of a proton from carbonic acid.		2.0610carbon oxoanioncofactor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
hydrogen
Hydrogen: The first chemical element in the periodic table with atomic symbol H, and atomic number 1. Protium (atomic weight 1) is by far the most common hydrogen isotope. Hydrogen also exists as the stable isotope DEUTERIUM (atomic weight 2) and the radioactive isotope TRITIUM (atomic weight 3). Hydrogen forms into a diatomic molecule at room temperature and appears as a highly flammable colorless and odorless gas.. dihydrogen : An elemental molecule consisting of two hydrogens joined by a single bond.		7.4110elemental hydrogen;
elemental molecule;
gas molecular entity		antioxidant;
electron donor;
food packaging gas;
fuel;
human metabolite
methanol
Methanol: A colorless, flammable liquid used in the manufacture of FORMALDEHYDE and ACETIC ACID, in chemical synthesis, antifreeze, and as a solvent. Ingestion of methanol is toxic and may cause blindness.. primary alcohol : A primary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has either three hydrogen atoms attached to it or only one other carbon atom and two hydrogen atoms attached to it.. methanol : The primary alcohol that is the simplest aliphatic alcohol, comprising a methyl and an alcohol group.		2.1110alkyl alcohol;
one-carbon compound;
primary alcohol;
volatile organic compound		amphiprotic solvent;
Escherichia coli metabolite;
fuel;
human metabolite;
mouse metabolite;
Mycoplasma genitalium metabolite
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.		2.7830long-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
pyruvic acid
Pyruvic Acid: An intermediate compound in the metabolism of carbohydrates, proteins, and fats. In thiamine deficiency, its oxidation is retarded and it accumulates in the tissues, especially in nervous structures. (From Stedman, 26th ed). pyruvic acid : A 2-oxo monocarboxylic acid that is the 2-keto derivative of propionic acid. It is a metabolite obtained during glycolysis.		2.05102-oxo monocarboxylic acidcofactor;
fundamental metabolite
am 580
Am 580: a selctive retinoic acid receptor (alpha) agonist; structure given in first source. 4-{[(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)carbonyl]amino}benzoic acid : An amidobenzoic acid obtained by formal condensation of the carboxy group of (5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)benzoic acid with the anilino group of 4-aminobenzoic acid. A selective RARalpha agonist.		2.4720amidobenzoic acid;
tetralins		antineoplastic agent;
retinoic acid receptor alpha/beta agonist
acetovanillone
apocynin : An aromatic ketone that is 1-phenylethanone substituted by a hydroxy group at position 4 and a methoxy group at position 3.		2.0510acetophenones;
aromatic ketone;
methyl ketone		antirheumatic drug;
EC 1.6.3.1. [NAD(P)H oxidase (H2O2-forming)] inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
peripheral nervous system drug;
plant metabolite
candesartan
candesartan: a nonpeptide angiotensin II receptor antagonist. candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension.		2.2510benzimidazolecarboxylic acid;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		2.0710aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
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.		2.0310aromatic ether;
thiazolidinone		antineoplastic agent;
insulin-sensitizing drug
cilostazol
[no description available]		2.110lactam;
tetrazoles		anticoagulant;
bronchodilator agent;
EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor;
fibrin modulating drug;
neuroprotective agent;
platelet aggregation inhibitor;
vasodilator agent
clofibrate
angiokapsul: contains clofibrate & insoitolnicotinate		2.0310aromatic ether;
ethyl ester;
monochlorobenzenes		anticholesteremic drug;
antilipemic drug;
geroprotector;
PPARalpha agonist
clofibric acid
Clofibric Acid: An antilipemic agent that is the biologically active metabolite of CLOFIBRATE.. clofibric acid : A monocarboxylic acid that is isobutyric acid substituted at position 2 by a p-chlorophenoxy group. It is a metabolite of the drug clofibrate.		2.0410aromatic ether;
monocarboxylic acid;
monochlorobenzenes		anticholesteremic drug;
antilipemic drug;
antineoplastic agent;
herbicide;
marine xenobiotic metabolite;
PPARalpha agonist
diazoxide
Diazoxide: A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.. diazoxide : A benzothiadiazine that is the S,S-dioxide of 2H-1,2,4-benzothiadiazine which is substituted at position 3 by a methyl group and at position 7 by chlorine. A peripheral vasodilator, it increases the concentration of glucose in the plasma and inhibits the secretion of insulin by the beta- cells of the pancreas. It is used orally in the management of intractable hypoglycaemia and intravenously in the management of hypertensive emergencies.		2.0810benzothiadiazine;
organochlorine compound;
sulfone		antihypertensive agent;
beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
diuretic;
K-ATP channel agonist;
sodium channel blocker;
sympathomimetic agent;
vasodilator agent
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.		2.0710
fenofibrate
Pharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINE		3.77100aromatic ether;
chlorobenzophenone;
isopropyl ester;
monochlorobenzenes		antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic
flutamide
Flutamide: An antiandrogen with about the same potency as cyproterone in rodent and canine species.		2.0310(trifluoromethyl)benzenes;
monocarboxylic acid amide		androgen antagonist;
antineoplastic agent
glyburide
Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide. glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group.		2.0810monochlorobenzenes;
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.		2.2510azaspiro compound;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
lg 100268
LG 100268: a retinoid X receptor (RXR) selective compound; structure given in first source		2.9640
losartan
Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position		2.2510biphenylyltetrazole;
imidazoles		angiotensin receptor antagonist;
anti-arrhythmia drug;
antihypertensive agent;
endothelin receptor antagonist
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first source		2.0810chromones;
morpholines;
organochlorine compound		autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector
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.		2.0610guanidinesenvironmental contaminant;
geroprotector;
hypoglycemic agent;
xenobiotic
methapyrilene
Methapyrilene: Histamine H1 antagonist with sedative action used as a hypnotic and in allergies.. methapyrilene : A member of the class of ethylenediamine derivatives that is ethylenediamine in which one of the nitrogens is substituted by two methyl groups, and the other nitrogen is substituted by a 2-pyridyl group and a (2-thienyl)methyl group.		2.1510ethylenediamine derivativeanti-allergic agent;
carcinogenic agent;
H1-receptor antagonist;
sedative
4-chlorophenol
4-chlorophenol: used as a root canal irrigant. 4-chlorophenol : A monochlorophenol substituted at the pare position by a chlorine atom.		2.2110monochlorophenol
pioglitazone
Pioglitazone: A thiazolidinedione and PPAR GAMMA agonist that is used in the treatment of TYPE 2 DIABETES MELLITUS.. pioglitazone : A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity.		2.4820aromatic ether;
pyridines;
thiazolidinediones		antidepressant;
cardioprotective agent;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
geroprotector;
hypoglycemic agent;
insulin-sensitizing drug;
PPARgamma agonist;
xenobiotic
ag 1879
3-(4-chlorophenyl)-1-(1,1-dimethylethyl)-1H-pyrazolo(3,4-d)pyrimidin-4-amine: Fyn kinase inhibitor		2.0810aromatic amine;
monochlorobenzenes;
pyrazolopyrimidine		beta-adrenergic antagonist;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector
probucol
Probucol: A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993).. probucol : A dithioketal that is propane-2,2-dithiol in which the hydrogens attached to both sulfur atoms are replaced by 3,5-di-tert-butyl-4-hydroxyphenyl groups. An anticholesteremic drug with antioxidant and anti-inflammatory properties, it is used to treat high levels of cholesterol in blood.		2.7830dithioketal;
polyphenol		anti-inflammatory drug;
anticholesteremic drug;
antilipemic drug;
antioxidant;
cardiovascular drug
sulforaphane
sulforaphane: from Cardaria draba L.. sulforaphane : An isothiocyanate having a 4-(methylsulfinyl)butyl group attached to the nitrogen.		2.0610isothiocyanate;
sulfoxide		antineoplastic agent;
antioxidant;
EC 3.5.1.98 (histone deacetylase) inhibitor;
plant metabolite
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.		2.0710chromanes;
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
pirinixic acid
pirinixic acid: structure		3.2960aryl sulfide;
organochlorine compound;
pyrimidines
corticosterone
[no description available]		2.051011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone		human metabolite;
mouse metabolite
prednisolone
Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone.		2.131011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
drug metabolite;
environmental contaminant;
immunosuppressive agent;
xenobiotic
aldosterone
[no description available]		2.542011beta-hydroxy steroid;
18-oxo steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid hormone;
mineralocorticoid;
primary alpha-hydroxy ketone;
steroid aldehyde		human metabolite;
mouse metabolite
dehydroepiandrosterone
Dehydroepiandrosterone: A major C19 steroid produced by the ADRENAL CORTEX. It is also produced in small quantities in the TESTIS and the OVARY. Dehydroepiandrosterone (DHEA) can be converted to TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE. Most of DHEA is sulfated (DEHYDROEPIANDROSTERONE SULFATE) before secretion.. dehydroepiandrosterone : An androstanoid that is androst-5-ene substituted by a beta-hydroxy group at position 3 and an oxo group at position 17. It is a naturally occurring steroid hormone produced by the adrenal glands.		2.071017-oxo steroid;
3beta-hydroxy-Delta(5)-steroid;
androstanoid		androgen;
human metabolite;
mouse metabolite
triiodothyronine
Triiodothyronine: A T3 thyroid hormone normally synthesized and secreted by the thyroid gland in much smaller quantities than thyroxine (T4). Most T3 is derived from peripheral monodeiodination of T4 at the 5' position of the outer ring of the iodothyronine nucleus. The hormone finally delivered and used by the tissues is mainly T3.. 3,3',5-triiodo-L-thyronine : An iodothyronine compound having iodo substituents at the 3-, 3'- and 5-positions. Although some is produced in the thyroid, most of the 3,3',5-triiodo-L-thyronine in the body is generated by mono-deiodination of L-thyroxine in the peripheral tissues. Its metabolic activity is about 3 to 5 times that of L-thyroxine. The sodium salt is used in the treatment of hypothyroidism.		2.1102-halophenol;
amino acid zwitterion;
iodophenol;
iodothyronine		human metabolite;
mouse metabolite;
thyroid hormone
alanine
Alanine: A non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases IMMUNITY, and provides energy for muscle tissue, BRAIN, and the CENTRAL NERVOUS SYSTEM.. alanine : An alpha-amino acid that consists of propionic acid bearing an amino substituent at position 2.		2.1310alanine zwitterion;
alanine;
L-alpha-amino acid;
proteinogenic amino acid;
pyruvate family amino acid		EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor;
fundamental metabolite
lysine
Lysine: An essential amino acid. It is often added to animal feed.. lysine : A diamino acid that is caproic (hexanoic) acid bearing two amino substituents at positions 2 and 6.. L-lysine : An L-alpha-amino acid; the L-isomer of lysine.		2.0310aspartate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
lysine;
organic molecular entity;
proteinogenic amino acid		algal metabolite;
anticonvulsant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
testosterone propionate
Testosterone Propionate: An ester of TESTOSTERONE with a propionate substitution at the 17-beta position.. androgen : A sex hormone that stimulates or controls the development and maintenance of masculine characteristics in vertebrates by binding to androgen receptors.		2.0310steroid ester
tyrosine
Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.. tyrosine : An alpha-amino acid that is phenylalanine bearing a hydroxy substituent at position 4 on the phenyl ring.		2.0510amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
tyrosine		EC 1.3.1.43 (arogenate dehydrogenase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical
cycloheximide
Cycloheximide: Antibiotic substance isolated from streptomycin-producing strains of Streptomyces griseus. It acts by inhibiting elongation during protein synthesis.. cycloheximide : A dicarboximide that is 4-(2-hydroxyethyl)piperidine-2,6-dione in which one of the hydrogens attached to the carbon bearing the hydroxy group is replaced by a 3,5-dimethyl-2-oxocyclohexyl group. It is an antibiotic produced by the bacterium Streptomyces griseus.		2.1510antibiotic fungicide;
cyclic ketone;
dicarboximide;
piperidine antibiotic;
piperidones;
secondary alcohol		anticoronaviral agent;
bacterial metabolite;
ferroptosis inhibitor;
neuroprotective agent;
protein synthesis inhibitor
histidine
Histidine: An essential amino acid that is required for the production of HISTAMINE.. L-histidine : The L-enantiomer of the amino acid histidine.. histidine : An alpha-amino acid that is propanoic acid bearing an amino substituent at position 2 and a 1H-imidazol-4-yl group at position 3.		2.0110amino acid zwitterion;
histidine;
L-alpha-amino acid;
polar amino acid zwitterion;
proteinogenic amino acid		algal metabolite;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
tryptophan
Tryptophan: An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals.. tryptophan : An alpha-amino acid that is alanine bearing an indol-3-yl substituent at position 3.		2.4620erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
tryptophan zwitterion;
tryptophan		antidepressant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
tert-butylhydroperoxide
tert-Butylhydroperoxide: A direct-acting oxidative stress-inducing agent used to examine the effects of oxidant stress on Ca(2+)-dependent signal transduction in vascular endothelial cells. It is also used as a catalyst in polymerization reactions and to introduce peroxy groups into organic molecules.. tert-butyl hydroperoxide : An alkyl hydroperoxide in which the alkyl group is tert-butyl. It is widely used in a variety of oxidation processes.		2.1710alkyl hydroperoxideantibacterial agent;
oxidising agent
bisphenol a
4,4'-isopropylidene diphenol: stimulates proliferative responses and cytokine productions of murine spleen cells and thymus cells in vitro. bisphenol : By usage, the methylenediphenols, HOC6H4CH2C6H4OH, commonly p,p-methylenediphenol, and their substitution products (generally derived from condensation of two equivalent amounts of a phenol with an aldehyde or ketone). The term also includes analogues in the the methylene (or substituted methylene) group has been replaced by a heteroatom.. bisphenol A : A bisphenol that is 4,4'-methanediyldiphenol in which the methylene hydrogens are replaced by two methyl groups.		2.0810bisphenolendocrine disruptor;
environmental contaminant;
xenobiotic;
xenoestrogen
diphenyl
diphenyl: RN given refers to unlabeled cpd; structure		2.610aromatic fungicide;
benzenes;
biphenyls		antifungal agrochemical;
antimicrobial food preservative
butylparaben
[no description available]		2.2110organic molecular entity
3-chlorophenol
3-chlorophenol : A monochlorophenol carrying the chloro substituent at position 3.		2.2110monochlorophenol
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		2.0810pyrrole;
secondary amine
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		2.2510mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
catechin
Catechin: An antioxidant flavonoid, occurring especially in woody plants as both (+)-catechin and (-)-epicatechin (cis) forms.. catechin : Members of the class of hydroxyflavan that have a flavan-3-ol skeleton and its substituted derivatives.. rac-catechin : A racemate comprising equimolar amounts of (+)- and (-)-catechin. (+)-catechin : The (+)-enantiomer of catechin and a polyphenolic antioxidant plant metabolite.		2.1110catechinantioxidant;
plant metabolite
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		2.110azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
indazoles
Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.		3.6120indazole
thiazoles
[no description available]		3.17501,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
aminoimidazole carboxamide
Aminoimidazole Carboxamide: An imidazole derivative which is a metabolite of the antineoplastic agents BIC and DIC. By itself, or as the ribonucleotide, it is used as a condensation agent in the preparation of nucleosides and nucleotides. Compounded with orotic acid, it is used to treat liver diseases.. 5-aminoimidazole-4-carboxamide : An aminoimidazole in which the amino group is at C-5 with a carboxamido group at C-4.		2.4920aminoimidazole;
monocarboxylic acid amide		mouse metabolite
cyproterone acetate
[no description available]		2.031020-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
chlorinated steroid;
steroid ester		androgen antagonist;
geroprotector;
progestin
lithocholic acid
Lithocholic Acid: A bile acid formed from chenodeoxycholate by bacterial action, usually conjugated with glycine or taurine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as cholagogue and choleretic.. lithocholic acid : A monohydroxy-5beta-cholanic acid with a alpha-hydroxy substituent at position 3. It is a bile acid obtained from chenodeoxycholic acid by bacterial action.. lithocholate : A bile acid anion that is the conjugate base of lithocholic acid.		2.1310bile acid;
C24-steroid;
monohydroxy-5beta-cholanic acid		geroprotector;
human metabolite;
mouse metabolite
fluorobenzenes
Fluorobenzenes: Derivatives of BENZENE that contain FLUORINE.. monofluorobenzene : The simplest member of the class of monofluorobenzenes that is benzene carrying a single fluoro substituent.. fluorobenzenes : Any fluoroarene that is a benzene or a substituted benzene carrying at least one fluoro group.		2.0610monofluorobenzenesNMR chemical shift reference compound
chenodeoxycholic acid
Chenodeoxycholic Acid: A bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine. It is used as cholagogue, a choleretic laxative, and to prevent or dissolve gallstones.. chenodeoxycholic acid : A dihydroxy-5beta-cholanic acid that is (5beta)-cholan-24-oic acid substituted by hydroxy groups at positions 3 and 7 respectively.. chenodeoxycholate : Conjugate base of chenodeoxycholic acid; major species at pH 7.3.		8.4770bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite
oleanolic acid
[no description available]		2.1710hydroxy monocarboxylic acid;
pentacyclic triterpenoid		plant metabolite
podophyllotoxin
Podophyllum: A genus of poisonous American herbs, family BERBERIDACEAE. The roots yield PODOPHYLLOTOXIN and other pharmacologically important agents. The plant was formerly used as a cholagogue and cathartic. It is different from the European mandrake, MANDRAGORA.		2.1710furonaphthodioxole;
lignan;
organic heterotetracyclic compound		antimitotic;
antineoplastic agent;
keratolytic drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
dihydrotestosterone
Dihydrotestosterone: A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.. 17beta-hydroxyandrostan-3-one : A 17beta-hydroxy steroid that is testosterone in which the 4-5 double bond has been reduced to a single bond with unspecified configuration at position 5.. 17beta-hydroxy-5alpha-androstan-3-one : A 17beta-hydroxy steroid that is testosterone in which the 4,5 double bond has been reduced to a single bond with alpha-configuration at position 5.		2.462017beta-hydroxy steroid;
17beta-hydroxyandrostan-3-one;
3-oxo-5alpha-steroid		androgen;
Daphnia magna metabolite;
human metabolite;
mouse metabolite
malondialdehyde
Malondialdehyde: The dialdehyde of malonic acid.. malonaldehyde : A dialdehyde that is propane substituted by two oxo groups at the terminal carbon atoms respectively. A biomarker of oxidative damage to lipids caused by smoking, it exists in vivo mainly in the enol form.		2.0810dialdehydebiomarker
methylnitrosourea
Methylnitrosourea: A nitrosourea compound with alkylating, carcinogenic, and mutagenic properties.. N-methyl-N-nitrosourea : A member of the class of N-nitrosoureas that is urea in which one of the nitrogens is substituted by methyl and nitroso groups.		2.0410N-nitrosoureasalkylating agent;
carcinogenic agent;
mutagen;
teratogenic agent
4-phenoxyphenol
[no description available]		2.2110phenoxyphenol
hexafluoroisopropanol
1,1,1,3,3,3-hexafluoropropan-2-ol : An organofluorine compound formed by substitution of all the methyl protons in propan-2-ol by fluorine. It is a metabolite of inhalation anesthetic sevoflurane.		2.0810organofluorine compound;
secondary alcohol		drug metabolite
phenazocine
Phenazocine: An opioid analgesic with actions and uses similar to MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1095)		2.0410
d-alpha tocopherol
Vitamin E: A generic descriptor for all TOCOPHEROLS and TOCOTRIENOLS that exhibit ALPHA-TOCOPHEROL activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of ISOPRENOIDS.. tocopherol : A collective name for a group of closely related lipids that contain a chroman-6-ol nucleus substituted at position 2 by a methyl group and by a saturated hydrocarbon chain consisting of three isoprenoid units. They are designated as alpha-, beta-, gamma-, and delta-tocopherol depending on the number and position of additional methyl substituents on the aromatic ring. Tocopherols occur in vegetable oils and vegetable oil products, almost exclusively with R,R,R configuration. Tocotrienols differ from tocopherols only in having three double bonds in the hydrocarbon chain.. vitamin E : Any member of a group of fat-soluble chromanols that exhibit biological activity against vitamin E deficiency. The vitamers in this class consists of a chroman-6-ol core which is substituted at position 2 by a methyl group and (also at position 2) either a saturated or a triply-unsaturated hydrocarbon chain consisting of three isoprenoid units. The major function of vitamin E is to act as a natural antioxidant by scavenging free radicals and molecular oxygen.. (R,R,R)-alpha-tocopherol : An alpha-tocopherol that has R,R,R configuration. The naturally occurring stereoisomer of alpha-tocopherol, it is found particularly in sunflower and olive oils.		3.7330alpha-tocopherolalgal metabolite;
antiatherogenic agent;
anticoagulant;
antioxidant;
antiviral agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
immunomodulator;
micronutrient;
nutraceutical;
plant metabolite
tocopherols
[no description available]		2.0810
pregnenolone carbonitrile
Pregnenolone Carbonitrile: A catatoxic steroid and microsomal enzyme inducer having significant effects on the induction of cytochrome P450. It has also demonstrated the potential for protective capability against acetaminophen-induced liver damage.		2.0410aliphatic nitrile
paraquat
Paraquat: A poisonous dipyridilium compound used as contact herbicide. Contact with concentrated solutions causes irritation of the skin, cracking and shedding of the nails, and delayed healing of cuts and wounds.. paraquat : An organic cation that consists of 4,4'-bipyridine bearing two N-methyl substituents loctated at the 1- and 1'-positions.		2.1510organic cationgeroprotector;
herbicide
pristane
pristane: structure. pristane : A norterpene that is an acyclic saturated hydrocarbon derived from phytane by loss of its C-16 terminal methyl group.		2.1710long-chain alkane;
norterpene		biomarker;
immunological adjuvant
uridine diphosphate glucuronic acid
Uridine Diphosphate Glucuronic Acid: A nucleoside diphosphate sugar which serves as a source of glucuronic acid for polysaccharide biosynthesis. It may also be epimerized to UDP iduronic acid, which donates iduronic acid to polysaccharides. In animals, UDP glucuronic acid is used for formation of many glucosiduronides with various aglycones.. UDP-alpha-D-glucuronic acid : A UDP-sugar having alpha-D-glucuronic acid as the sugar component.		2.2510UDP-D-glucuronic acidEscherichia coli metabolite;
human metabolite;
mouse metabolite
bis(4-oxyphenyl)sulfide
4,4'-thiodiphenol: structure in first source		2.2110phenols
cyclic cmp
Cyclic CMP: A cyclic nucleotide formed from CYTIDINE TRIPHOSPHATE by the action of cytidylate cyclase. It is a potential cyclic nucleotide intracellular mediator of signal transductions.. 3',5'-cyclic CMP : A 3',5'-cyclic pyrimidine nucleotide having cytosine as the nucleobase.		2.05103',5'-cyclic pyrimidine nucleotidehuman metabolite
gold
Gold: A yellow metallic element with the atomic symbol Au, atomic number 79, and atomic weight 197. It is used in jewelry, goldplating of other metals, as currency, and in dental restoration. Many of its clinical applications, such as ANTIRHEUMATIC AGENTS, are in the form of its salts.		2.2110copper group element atom;
elemental gold
ozone
Ozone: The unstable triatomic form of oxygen, O3. It is a powerful oxidant that is produced for various chemical and industrial uses. Its production is also catalyzed in the ATMOSPHERE by ULTRAVIOLET RAY irradiation of oxygen or other ozone precursors such as VOLATILE ORGANIC COMPOUNDS and NITROGEN OXIDES. About 90% of the ozone in the atmosphere exists in the stratosphere (STRATOSPHERIC OZONE).. ozone : An elemental molecule with formula O3. An explosive, pale blue gas (b.p. -112degreeC) that has a characteristic, pungent odour, it is continuously produced in the upper atmosphere by the action of solar ultraviolet radiation on atmospheric oxygen. It is an antimicrobial agent used in the production of bottled water, as well as in the treatment of meat, poultry and other foodstuffs.		2.1310elemental molecule;
gas molecular entity;
reactive oxygen species;
triatomic oxygen		antiseptic drug;
disinfectant;
electrophilic reagent;
greenhouse gas;
mutagen;
oxidising agent;
tracer
tetradecanoylphorbol acetate
Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.. phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.. phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types.		210acetate ester;
diester;
phorbol ester;
tertiary alpha-hydroxy ketone;
tetradecanoate ester		antineoplastic agent;
apoptosis inducer;
carcinogenic agent;
mitogen;
plant metabolite;
protein kinase C agonist;
reactive oxygen species generator
1-deoxynojirimycin
1-deoxy-nojirimycin: structure in first source. duvoglustat : An optically active form of 2-(hydroxymethyl)piperidine-3,4,5-triol having 2R,3R,4R,5S-configuration.		2.04102-(hydroxymethyl)piperidine-3,4,5-triol;
piperidine alkaloid		anti-HIV agent;
anti-obesity agent;
bacterial metabolite;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
hepatoprotective agent;
hypoglycemic agent;
plant metabolite
4-ethylphenol
4-ethylphenol: RN given refers to parent cpd. 4-ethylphenol : A member of the class of phenols carrying an ethyl substituent at position 4.		2.2110phenolsfungal xenobiotic metabolite
ursodeoxycholic acid
Ursodeoxycholic Acid: An epimer of chenodeoxycholic acid. It is a mammalian bile acid found first in the bear and is apparently either a precursor or a product of chenodeoxycholate. Its administration changes the composition of bile and may dissolve gallstones. It is used as a cholagogue and choleretic.. ursodeoxycholic acid : A bile acid found in the bile of bears (Ursidae) as a conjugate with taurine. Used therapeutically, it prevents the synthesis and absorption of cholesterol and can lead to the dissolution of gallstones.. ursodeoxycholate : A bile acid anion that is the conjugate base of ursodeoxycholic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3.		2.5220bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite
pregnanolone
Pregnanolone: A pregnane found in the urine of pregnant women and sows. It has anesthetic, hypnotic, and sedative properties.. 3alpha-hydroxy-5beta-pregnan-20-one : The 3alpha-stereoisomer of 3-hydroxy-5beta-pregnan-20-one.		2.03103-hydroxy-5beta-pregnan-20-one;
3alpha-hydroxy steroid		human metabolite;
intravenous anaesthetic;
sedative
glutamic acid
Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.		2.0810glutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
azoxymethane
Azoxymethane: A potent carcinogen and neurotoxic compound. It is particularly effective in inducing colon carcinomas.		2.0410
bezafibrate
[no description available]		2.0510aromatic ether;
monocarboxylic acid amide;
monocarboxylic acid;
monochlorobenzenes		antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic
colforsin
Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.		2.0710acetate ester;
cyclic ketone;
labdane diterpenoid;
organic heterotricyclic compound;
tertiary alpha-hydroxy ketone;
triol		adenylate cyclase agonist;
anti-HIV agent;
antihypertensive agent;
plant metabolite;
platelet aggregation inhibitor;
protein kinase A agonist
lovastatin
Lovastatin: A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.. lovastatin : A fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom).		210delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
polyketide;
statin (naturally occurring)		anticholesteremic drug;
antineoplastic agent;
Aspergillus metabolite;
prodrug
simvastatin
Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug.		3.1750delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
statin (semi-synthetic)		EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
ferroptosis inducer;
geroprotector;
prodrug
pravastatin
Pravastatin: An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).. pravastatin : A carboxylic ester resulting from the formal condensation of (S)-2-methylbutyric acid with the hydroxy group adjacent to the ring junction of (3R,5R)-7-[(1S,2S,6S,8S,8aR)-6,8-dihydroxy-2-methyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid. Derived from microbial transformation of mevastatin, pravastatin is a reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA). The sodium salt is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin.		2.04103-hydroxy carboxylic acid;
carbobicyclic compound;
carboxylic ester;
hydroxy monocarboxylic acid;
secondary alcohol;
statin (semi-synthetic)		anticholesteremic drug;
environmental contaminant;
metabolite;
xenobiotic
atorvastatin
[no description available]		2.0810aromatic amide;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
pyrroles;
statin (synthetic)		environmental contaminant;
xenobiotic
valsartan
Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity.		2.2510biphenylyltetrazole;
monocarboxylic acid amide;
monocarboxylic acid		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
darglitazone
[no description available]		2.0110
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol
[no description available]		2.110stilbenoid
mevastatin
mevastatin: antifungal metabolite from Penicillium brevicopactum; potent inhibitory activity to sterol synthesis; structure. mevastatin : A carboxylic ester that is pravastatin that is lacking the allylic hydroxy group. A hydroxymethylglutaryl-CoA reductase inhibitor (statin) isolated from Penicillium citrinum and from Penicillium brevicompactum, its clinical use as a lipid-regulating drug ceased following reports of toxicity in animals.		2102-pyranones;
carboxylic ester;
hexahydronaphthalenes;
polyketide;
statin (naturally occurring)		antifungal agent;
apoptosis inducer;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
fungal metabolite;
Penicillium metabolite
fenofibric acid
fenofibric acid: RN given refers to parent cpd without isomeric designation; structure. fenofibric acid : A monocarboxylic acid that is 2-methylpropanoic acid substituted by a 4-(4-chlorobenzoyl)phenoxy group at position 2. It is a metabolite of the drug fenofibrate.		2.4620aromatic ketone;
chlorobenzophenone;
monocarboxylic acid		drug metabolite;
marine xenobiotic metabolite
ursolic acid
[no description available]		2.110hydroxy monocarboxylic acid;
pentacyclic triterpenoid		geroprotector;
plant metabolite
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.		2.1110flavans;
gallate ester;
polyphenol		antineoplastic agent;
antioxidant;
apoptosis inducer;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent;
plant metabolite
cholesteryl sulfate
cholesteryl sulfate: component of human seminal plasma & spermatozoa; RN given refers to (3beta)-isomer. cholesterol sulfate : A steroid sulfate that is cholesterol substituted by a sulfoxy group at position 3.		2.1510steroid sulfatehuman metabolite
25-hydroxycholesterol
[no description available]		3.7710025-hydroxy steroid;
oxysterol		human metabolite
aica ribonucleotide
AICA ribonucleotide: purine precursor that has antineoplastic activity. AICA ribonucleotide : A 1-(phosphoribosyl)imidazolecarboxamide that is acadesine in which the hydroxy group at the 5' position has been converted to its monophosphate derivative.		2.49201-(phosphoribosyl)imidazolecarboxamide;
aminoimidazole		cardiovascular drug;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
telmisartan
Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension.		2.2510benzimidazoles;
biphenyls;
carboxybiphenyl		angiotensin receptor antagonist;
antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
environmental contaminant;
xenobiotic
4-phenylbenzoic acid
4-phenylbenzoic acid: RN given refers to 4-carboxylic cpd		2.2110
2-ethoxybenzoic acid
[no description available]		2.2110
2,4,6-trihydroxybenzaldehyde
2,4,6-trihydroxybenzaldehyde: structure in first source		2.0810carboxylic ester
biphenyl-2-carboxylic acid
biphenyl-2-carboxylic acid: structure in first source		2.2510
honokiol
[no description available]		2.2510biphenyls
coumarin 153
coumarin 153: structure in first source		2.11107-aminocoumarinsfluorochrome
oxazolidin-2-one
Oxazolidinones: Derivatives of oxazolidin-2-one. They represent an important class of synthetic antibiotic agents.. oxazolidin-2-one : An oxazolidinone that is 1,3-oxazolidine with an oxo substituent at position 2.. oxazolidinone : An oxazolidine containing one or more oxo groups.		2.110carbamate ester;
oxazolidinone		metabolite
rosiglitazone
[no description available]		3.97120aminopyridine;
thiazolidinediones		EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
insulin-sensitizing drug
bexarotene
[no description available]		3.460benzoic acids;
naphthalenes;
retinoid		antineoplastic agent
7-ketocholesterol
7-ketocholesterol: inhibits uptake of cholesterol in rabbit aorta. 7-ketocholesterol : A cholestanoid that consists of cholesterol bearing an oxo substituent at position 7.		2.45203beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
7-oxo steroid;
cholestanoid		neuroprotective agent
homocysteine
Homocysteine: A thiol-containing amino acid formed by a demethylation of METHIONINE.. homocysteine : A sulfur-containing amino acid consisting of a glycine core with a 2-mercaptoethyl side-chain.. L-homocysteine : A homocysteine that has L configuration.		2.7630amino acid zwitterion;
homocysteine;
serine family amino acid		fundamental metabolite;
mouse metabolite
gamma-tocopherol
gamma-Tocopherol: A natural tocopherol with less antioxidant activity than ALPHA-TOCOPHEROL. It exhibits antioxidant activity by virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus. As in BETA-TOCOPHEROL, it also has three methyl groups on the 6-chromanol nucleus but at different sites.. gamma-tocopherol : A tocopherol in which the chroman-6-ol core is substituted by methyl groups at positions 7 and 8. It is found particularly in maize (corn) oil and soya bean (soybean) oils.		3.1710tocopherol;
vitamin E		algal metabolite;
food antioxidant;
plant metabolite
glucuronic acid
Glucuronic Acid: A sugar acid formed by the oxidation of the C-6 carbon of GLUCOSE. In addition to being a key intermediate metabolite of the uronic acid pathway, glucuronic acid also plays a role in the detoxification of certain drugs and toxins by conjugating with them to form GLUCURONIDES.. D-glucuronic acid : The D-enantiomer of glucuronic acid.. D-glucopyranuronic acid : A D-glucuronic acid in cyclic pyranose form.		2.0610D-glucuronic acidalgal metabolite
diosgenin
[no description available]		2.46203beta-sterol;
hexacyclic triterpenoid;
sapogenin;
spiroketal		antineoplastic agent;
antiviral agent;
apoptosis inducer;
metabolite
22-hydroxycholesterol
[no description available]		9.18160cholanoid
schizandrin b
schizandrin B: a phytogenic antineoplastic agent with anti-inflammatory activity; isolated from Schisandra plant		2.1510
liquiritigenin
liquiritigenin: structure given in first source; isolated from Pterocarpus marsupium. 4',7-dihydroxyflavanone : A dihydroxyflavanone in which the two hydroxy substituents are located at positions 4' and 7.. liquiritigenin : A dihydroxyflavanone compound having the two hydroxy substituents at the 4'- and 7-positions. Isolated from the root of Glycyrrhizae uralensis, it is a selective agonist for oestrogen receptor beta.		2.06104',7-dihydroxyflavanonehormone agonist;
plant metabolite
(20s)-20-hydroxycholesterol
20-hydroxycholesterol: RN given refers to (20S)-isomer. 20-hydroxycholesterol : An oxysterol that is cholesterol substituted by a hydroxy group at position 20.		21020-hydroxy steroid;
3beta-hydroxy-Delta(5)-steroid;
oxysterol		human metabolite;
mouse metabolite
gefitinib
[no description available]		7.8430aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
epidermal growth factor receptor antagonist
27-hydroxycholesterol
(25R)-cholest-5-ene-3beta,26-diol : A 26-hydroxycholesterol in which the 25-position has R-configuration.		3.447026-hydroxycholesterolapoptosis inducer;
human metabolite;
mouse metabolite;
neuroprotective agent
dibutyryl cyclic-3',5'-cytidine monophosphate
[no description available]		2.0510
cyanidin
cyanidin: RN given refers to parent cpd; structure. cyanidin cation : An anthocyanidin cation that is flavylium substituted at positions 3, 3', 4', 5 and 7 by hydroxy groups.		2.08105-hydroxyanthocyanidinantioxidant;
metabolite;
neuroprotective agent
triiodothyronine
L-homocysteine thiolactone : A thiolactone arising from formal condensation of the mercapto (sulfanyl) and carboxylic acid groups of L-homocysteine.		2.0510tetrahydrothiophenes;
thiolactone		human metabolite
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).		2.3110azetidines;
beta-lactam;
organofluorine compound		anticholesteremic drug;
antilipemic drug;
antimetabolite
mn(iii) 5,10,15,20-tetrakis(n-methylpyridinium-2-yl)porphyrin
[no description available]		2.0310
olmesartan
olmesartan: an active metabolite of CS 866		2.2510biphenylyltetrazoleangiotensin receptor antagonist;
antihypertensive agent
resiquimod
S 28463: structure given in first source		2.1310imidazoquinoline
(22r)-22-hydroxycholesterol
(22R)-22-hydroxycholesterol : An oxysterol that is the 22R-hydroxy derivative of cholesterol.		3.014022-hydroxy steroid;
3beta-hydroxy-Delta(5)-steroid;
oxysterol
22s-hydroxycholesterol
(22S)-22-hydroxycholesterol : An oxysterol that is the 22S-hydroxy derivative of cholesterol.		2.52022-hydroxy steroid;
3beta-hydroxy-Delta(5)-steroid;
oxysterol
angiotensin ii
Giapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock. Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).		2.7430amino acid zwitterion;
angiotensin II		human metabolite
campesterol
campesterol: RN refers to (3beta,24R)-isomer; structure		2.02103beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
C28-steroid;
phytosterols		mouse metabolite
cholic acid
Cholic Acid: A major primary bile acid produced in the liver and usually conjugated with glycine or taurine. It facilitates fat absorption and cholesterol excretion.. cholic acid : A bile acid that is 5beta-cholan-24-oic acid bearing three alpha-hydroxy substituents at position 3, 7 and 12.		2.131012alpha-hydroxy steroid;
3alpha-hydroxy steroid;
7alpha-hydroxy steroid;
bile acid;
C24-steroid;
trihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite
3-nitrotyrosine
3-nitrotyrosine: RN given refers to parent cpd without isomeric designation. 3-nitrotyrosine : A nitrotyrosine comprising tyrosine having a nitro group at the 3-position on the phenyl ring.		2.05102-nitrophenols;
C-nitro compound;
nitrotyrosine;
non-proteinogenic alpha-amino acid
2-chloro-1,4-dimethoxybenzene
[no description available]		2.2110dimethoxybenzene
anthricin
anthricin: antitumor constituent from Anthriscus sylvestris (L.) Hoffm; structure in first source. deoxypodophyllotoxin : A member of the class of furonaphthodioxoles that is (5R,5aR,8aR)-5,8,8a,9-tetrahydro-2H-furo[3',4':6,7]naphtho[2,3-d][1,3]dioxol-6(5aH)-one substituted at position 5 by a 3,4,5-trimethoxyphenyl group.		2.1710furonaphthodioxole;
gamma-lactone;
lignan;
methoxybenzenes		antineoplastic agent;
apoptosis inducer;
plant metabolite
calcein am
calcein AM: a non-fluorescent compound cleaved to a fluorescent compound by non-specific intracellular esterases. calcein am : An organic heteropentacyclic compound that is calcein in which all four carboxy group hydrogens have been substituted by (acetyloxy)methoxy groups and the hyrodgens of the two hydroxy groups have been substituted by acetyl groups. It is a a non-fluorescent probe cleaved to a fluorescent probe by non-specific intracellular esterases.		2.07102-benzofurans;
acetate ester;
gamma-lactone;
organic heteropentacyclic compound;
oxaspiro compound;
xanthene dye		fluorochrome
leupeptins
Leupeptins: A group of acylated oligopeptides produced by Actinomycetes that function as protease inhibitors. They have been known to inhibit to varying degrees trypsin, plasmin, KALLIKREINS, papain and the cathepsins.		2.0310
glycogen
glycogen : A polydisperse, highly branched glucan composed of chains of D-glucopyranose residues in alpha(1->4) glycosidic linkage, joined together by alpha(1->6) glycosidic linkages. A small number of alpha(1->3) glycosidic linkages and some cumulative alpha(1->6) links also may occur. The branches in glycogen typically contain 8 to 12 glucose residues.		2.0210
mevalonic acid
Mevalonic Acid: A dihydroxy monocarboxylic acid and precursor in the biosynthetic pathway known as the mevalonate pathway, which produces terpenes and steroids that are vital for diverse cellular functions.. mevalonic acid : A racemate composed of equimolar amounts of (R)- and (S)-mevalonic acid.. (R)-mevalonic acid : The (R)-enantiomer of mevalonic acid.		2103,5-dihydroxy-3-methylpentanoic acid
desmosterol
Desmosterol: An intermediate in the synthesis of cholesterol.. desmosterol : A cholestanoid that is cholesta-5,24-diene substituted by a beta-hydroxy group at position 3. It is an intermediate metabolite obtained during the synthesis of cholesterol.		2.42203beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
C27-steroid;
cholestanoid		human metabolite;
mouse metabolite
indican
[no description available]		2.1110beta-D-glucoside;
exopolysaccharide;
indolyl carbohydrate
lignans
Lignans: A class of dibenzylbutane derivatives which occurs in higher plants and in fluids (bile, serum, urine, etc.) in man and other animals. These compounds, which have a potential anti-cancer role, can be synthesized in vitro by human fecal flora. (From Singleton & Sainsbury, Dictionary of Microbiology and Molecular Biology, 2d ed)		2.4920
betadex
beta-Cyclodextrins: Cyclic GLUCANS consisting of seven (7) glucopyranose units linked by 1,4-glycosidic bonds.		2.0310cyclodextrin
ergosterol
[no description available]		2.46203beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
ergostanoid;
phytosterols		fungal metabolite;
Saccharomyces cerevisiae metabolite
tretinoin
Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry.		5.04120retinoic acid;
vitamin A		anti-inflammatory agent;
antineoplastic agent;
antioxidant;
AP-1 antagonist;
human metabolite;
keratolytic drug;
retinoic acid receptor agonist;
retinoid X receptor agonist;
signalling molecule
arachidonic acid
icosa-5,8,11,14-tetraenoic acid : Any icosatetraenoic acid with the double bonds at positions 5, 8, 11 and 14.. arachidonate : A long-chain fatty acid anion resulting from the removal of a proton from the carboxy group of arachidonic acid.		2.4420icosa-5,8,11,14-tetraenoic acid;
long-chain fatty acid;
omega-6 fatty acid		Daphnia galeata metabolite;
EC 3.1.1.1 (carboxylesterase) inhibitor;
human metabolite;
mouse metabolite
resveratrol
trans-resveratrol : A resveratrol in which the double bond has E configuration.		7.7830resveratrolantioxidant;
phytoalexin;
plant metabolite;
quorum sensing inhibitor;
radical scavenger
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.		2.7430octadec-9-enoic acidantioxidant;
Daphnia galeata metabolite;
EC 3.1.1.1 (carboxylesterase) inhibitor;
Escherichia coli metabolite;
mouse metabolite;
plant metabolite;
solvent
eicosapentaenoic acid
icosapentaenoic acid : Any straight-chain, C20 polyunsaturated fatty acid having five C=C double bonds.. all-cis-5,8,11,14,17-icosapentaenoic acid : An icosapentaenoic acid having five cis-double bonds at positions 5, 8, 11, 14 and 17.		2.4520icosapentaenoic acid;
omega-3 fatty acid		anticholesteremic drug;
antidepressant;
antineoplastic agent;
Daphnia galeata metabolite;
fungal metabolite;
micronutrient;
mouse metabolite;
nutraceutical
sr 12813
SR 12813: structure given in first source. SR12813 : An organic phosphonate that is the tetraethyl ester of [2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethene-1,1-diyl]bis(phosphonic acid).		2.8130organic phosphonate;
phenols		pregnane X receptor agonist
lycopene
[no description available]		7.5320acyclic caroteneantioxidant;
plant metabolite
geranylgeranyl pyrophosphate
geranylgeranyl pyrophosphate: RN given refers to (E,E,E)-isomer. geranylgeranyl diphosphate : A polyprenol diphosphate having geranylgeranyl as the polyprenyl component.. 2-trans,6-trans,10-trans-geranylgeranyl diphosphate : The all-trans-isomer of geranylgeranyl diphosphate.		2.0510geranylgeranyl diphosphatemouse metabolite
obeticholic acid
obeticholic acid: A farnesoid X receptor agonist and anticholestatic agent that is used in the treatment of chronic liver diseases; structure in first source.. obeticholic acid : A dihydroxy-5beta-cholanic acid that is chenodeoxycholic acid carrying an additional ethyl substituent at the 6alpha-position. A semi-synthetic bile acid which acts as a farnesoid X receptor agonist and is used for treatment of primary biliary cholangitis.		2.9303alpha-hydroxy steroid;
7alpha-hydroxy steroid;
dihydroxy-5beta-cholanic acid		farnesoid X receptor agonist;
hepatoprotective agent
gw 3965
GW 3965: a liver X receptor ligand		7.57690diarylmethane
prostaglandin d2
Prostaglandin D2: The principal cyclooxygenase metabolite of arachidonic acid. It is released upon activation of mast cells and is also synthesized by alveolar macrophages. Among its many biological actions, the most important are its bronchoconstrictor, platelet-activating-factor-inhibitory, and cytotoxic effects.. prostaglandin D2 : A member of the class of prostaglandins D that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9 and 15 and an oxo group at position 11 (the 5Z,9alpha,13E,15S- stereoisomer).		2.0310prostaglandins Dhuman metabolite;
mouse metabolite
alitretinoin
Alitretinoin: A retinoid that is used for the treatment of chronic hand ECZEMA unresponsive to topical CORTICOSTEROIDS. It is also used to treat cutaneous lesions associated with AIDS-related KAPOSI SARCOMA.		4.87100retinoic acidantineoplastic agent;
keratolytic drug;
metabolite;
retinoid X receptor agonist
gamma-sitosterol
clionasterol : A member of the class of phytosterols that is poriferast-5-ene carrying a beta-hydroxy substituent at position 3.		2.42203beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
phytosterols		marine metabolite;
plant metabolite
benzyloxycarbonylleucyl-leucyl-leucine aldehyde
benzyloxycarbonylleucyl-leucyl-leucine aldehyde: proteasome inhibitor. N-benzyloxycarbonyl-L-leucyl-L-leucyl-L-leucinal : A tripeptide that is L-leucyl-L-leucyl-L-leucine in which the C-terminal carboxy group has been reduced to the corresponding aldehyde and the N-terminal amino group is protected as its benzyloxycarbonyl derivative.		2.0310amino aldehyde;
carbamate ester;
tripeptide		proteasome inhibitor
stilbenes
Stilbenes: Organic compounds that contain 1,2-diphenylethylene as a functional group.. trans-stilbene : The trans-isomer of stilbene.		3.250stilbene
sesquiterpenes
[no description available]		2.3110
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.		2.1710aromatic 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
1-ethyl-2-oxo-N-(2-pyridinylmethyl)-6-benzo[cd]indolesulfonamide
[no description available]		2.110naphthalenes;
sulfonic acid derivative
1-ethyl-N-[3-(4-morpholinyl)propyl]-2-oxo-6-benzo[cd]indolesulfonamide
[no description available]		2.110naphthalenes;
sulfonic acid derivative
fatostatin
fatostatin: inhibits activation of SREBP; structure in first source		2.5420thiazoles
D-fructopyranose
[no description available]		2.6120cyclic hemiketal;
D-fructose;
fructopyranose		sweetening agent
digoxin
Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666). digoxin : A cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small.		3.1910cardenolide glycoside;
steroid saponin		anti-arrhythmia drug;
cardiotonic drug;
EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor;
epitope
tamoxifen
[no description available]		2.1310stilbenoid;
tertiary amino compound		angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator
u 0126
U 0126: protein kinase kinase inhibitor; structure in first source		2.1110aryl sulfide;
dinitrile;
enamine;
substituted aniline		antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
osteogenesis regulator;
vasoconstrictor agent
2-fluoro-2-deoxyglucose-6-phosphate
2-fluoro-2-deoxyglucose-6-phosphate: metabolite of 2-fluoro-2-deoxyglucose; RN given refers to D-Glu cpd; RN for parent cpd not avail 10/90		2.0710
cytellin
cytellin: a phytosterol preparation of mainly B-sitosterol, that was marketed by Eli Lilly to lower cholesterol 1957 to 1982		2.4220
24,25-epoxycholesterol
24,25-epoxycholesterol: Rn given refers to (3alpha,5beta)-isomer; structure given in first source. 24(S),25-epoxycholesterol : A 3beta-hydroxy-Delta(5)-steroid that is desmosterol in which the double bond at position 24-25 has been oxidised to the corresponding epoxide (the 24S diastereoisomer). It is an oxysterol agonist of the liver X receptor.		3.911203beta-hydroxy-Delta(5)-steroid;
cholestanoid;
epoxy steroid		liver X receptor agonist
ovalbumin
Ovalbumin: An albumin obtained from the white of eggs. It is a member of the serpin superfamily.		2.7430
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.		3.3460aryl sulfide;
monocarboxylic acid;
ureas		PPARalpha agonist
ex 527
6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide: structure in first source. 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide : A member of the class of carbazoles that is 2,3,4,9-tetrahydro-1H-carbazole which is substituted at position 1 by an aminocarbohyl group and at position 6 by a chlorine.		2.2110carbazoles;
monocarboxylic acid amide;
organochlorine compound
bilirubin
[no description available]		2.6920biladienes;
dicarboxylic acid		antioxidant;
human metabolite;
mouse metabolite
dinoprostone
prostaglandin E2 : Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostaglandins.		2.110prostaglandins Ehuman metabolite;
mouse metabolite;
oxytocic
dinoprost
Dinoprost: A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions.. prostaglandin F2alpha : A prostaglandins Falpha that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15. It is a naturally occurring prostaglandin used to induce labor.		2.0810monocarboxylic acid;
prostaglandins Falpha		human metabolite;
mouse metabolite
calcitriol
dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes		2.4720D3 vitamins;
hydroxycalciol;
triol		antineoplastic agent;
antipsoriatic;
bone density conservation agent;
calcium channel agonist;
calcium channel modulator;
hormone;
human metabolite;
immunomodulator;
metabolite;
mouse metabolite;
nutraceutical
stigmasterol
stigmasta-5,22-dien-3-ol: isolated from freeze-dried powder of Blackberries (Rubus ursinus L.) which showed an activity on inhibition of chemocarcinogen. stigmasterol : A 3beta-sterol that consists of 3beta-hydroxystigmastane having double bonds at the 5,6- and 22,23-positions.		2.59203beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
phytosterols;
stigmastane sterol		plant metabolite
cholecalciferol
Cholecalciferol: Derivative of 7-dehydroxycholesterol formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. It differs from ERGOCALCIFEROL in having a single bond between C22 and C23 and lacking a methyl group at C24.. calciol : A hydroxy seco-steroid that is (5Z,7E)-9,10-secocholesta-5,7,10(19)-triene in which the pro-S hydrogen at position 3 has been replaced by a hydroxy group. It is the inactive form of vitamin D3, being hydroxylated in the liver to calcidiol (25-hydroxyvitamin D3), which is then further hydroxylated in the kidney to give calcitriol (1,25-dihydroxyvitamin D3), the active hormone.		2.4920D3 vitamins;
hydroxy seco-steroid;
seco-cholestane;
secondary alcohol;
steroid hormone		geroprotector;
human metabolite
zeaxanthin
Zeaxanthins: Carotenoids found in fruits and vegetables. Zeaxanthin accumulates in the MACULA LUTEA.		2.110carotenolantioxidant;
bacterial metabolite;
cofactor
genistein
[no description available]		2.46207-hydroxyisoflavonesantineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor
pulmicort
Budesonide: A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.. budesonide : A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis.		2.572011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
cyclic acetal;
glucocorticoid;
primary alpha-hydroxy ketone		anti-inflammatory drug;
bronchodilator agent;
drug allergen
lutein
Lutein: A xanthophyll found in the major LIGHT-HARVESTING PROTEIN COMPLEXES of plants. Dietary lutein accumulates in the MACULA LUTEA.. xanthophyll : A subclass of carotenoids consisting of the oxygenated carotenes.		2.110carotenolfood colouring;
plant metabolite
trans-2,3',4,5'-tetrahydroxystilbene
trans-2,3',4,5'-tetrahydroxystilbene: hydroxystilbene oxyresveratrol		2.1710stilbenoid
pterostilbene
[no description available]		2.1310diether;
methoxybenzenes;
stilbenol		anti-inflammatory agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
hypoglycemic agent;
neuroprotective agent;
neurotransmitter;
plant metabolite;
radical scavenger
rottlerin
rottlerin: an angiogenesis inhibitor; an inhibitor of protein kinase Cdelta (PKCdelta) and calmodulin kinase III; RN refers to (E)-isomer; do not confuse this chalcone with an anthraquinone that is also called rottlerin (RN 481-72-1);. rottlerin : A chromenol that is 2,2-dimethyl-2H-chromene substituted by hydroxy groups at positions 5 and 7, a 3-acetyl-2,4,6-trihydroxy-5-methylbenzyl group at position 6 and a (1E)-3-oxo-1-phenylprop-1-en-3-yl group at position 8. A potassium channel opener, it is isolated from Mallotus philippensis.		2.0710aromatic ketone;
benzenetriol;
chromenol;
enone;
methyl ketone		anti-allergic agent;
antihypertensive agent;
antineoplastic agent;
apoptosis inducer;
K-ATP channel agonist;
metabolite
cerulenin
Cerulenin: An epoxydodecadienamide isolated from several species, including ACREMONIUM, Acrocylindrum, and Helicoceras. It inhibits the biosynthesis of several lipids by interfering with enzyme function.. cerulenin : An epoxydodecadienamide isolated from several species, including Acremonium, Acrocylindrum and Helicoceras. It inhibits the biosynthesis of several lipids by interfering with enzyme function.		2.0410epoxide;
monocarboxylic acid amide		antifungal agent;
antiinfective agent;
antilipemic drug;
antimetabolite;
antimicrobial agent;
fatty acid synthesis inhibitor
tocotrienol, delta
delta-tocotrienol : A tocotrienol that is chroman-6-ol substituted by methyl groups at positions 2 and 8 and a farnesyl chain at position 2.		3.1710tocotrienol;
vitamin E		anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
bone density conservation agent;
NF-kappaB inhibitor;
plant metabolite;
radiation protective agent;
Saccharomyces cerevisiae metabolite
pitavastatin
pitavastatin : A dihydroxy monocarboxylic acid that is (6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]hept-6-enoic acid in which the two hydroxy groups are located at positions 3 and 5 (the 3R,5S-stereoisomer). Used as its calcium salt for treatment of hypercholesterolemia (elevated levels of cholesterol in the blood) on patients unable to sufficiently lower their cholesterol levels by diet and exercise.		3.5111cyclopropanes;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
quinolines;
statin (synthetic)		antioxidant
purmorphamine
purmorphamine: structure in first source. purmorphamine : A member of the class of purines that is purine substituted at C-2 by a 1-naphthyloxy group, at C-4 by a 4-morpholinophenylamino group, and at N-9 by a cyclohexyl group.		2.0510aromatic ether;
morpholines;
purines;
secondary amino compound		osteogenesis regulator;
SMO receptor agonist
4-(2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl)benzoic acid
4-(2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl)benzoic acid: RN refers to (E)-isomer; structure given in first source. arotinoid acid : A retinoid that consists of benzoic acid substituted at position 4 by a 2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)prop-1-en-1-yl group. It is a synthetic retinoid that acts as a selective agonist for the retinoic acid receptors (RAR).		3.620benzoic acids;
naphthalenes;
retinoid		antineoplastic agent;
retinoic acid receptor agonist;
teratogenic agent
cinanserin
Cinanserin: A serotonin antagonist with limited antihistaminic, anticholinergic, and immunosuppressive activity.. cinanserin : An aryl sulfide that is (2E)-3-phenyl-N-(2-sulfanylphenyl)prop-2-enamide in which the hydrogen of the thiol group is substituted by a 3-(dimethylamino)propyl group. It is a 5-hydroxytryptamine receptor antagonist and an inhibitor of SARS-CoV replication.		2.2510aryl sulfide;
cinnamamides;
secondary carboxamide;
tertiary amino compound		anticoronaviral agent;
antiviral agent;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor
4,4'-diisothiocyanostilbene-2,2'-disulfonic acid
4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid: An inhibitor of anion conductance including band 3-mediated anion transport.		2.0710
(3S,5S,6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid
Fluvastatin: An indole-heptanoic acid derivative that inhibits HMG COA REDUCTASE and is used to treat HYPERCHOLESTEROLEMIA. In contrast to other statins, it does not appear to interact with other drugs that inhibit CYP3A4.. (3S,5S,6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid : A (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid diastereoisomer in which both chiral centres have S configuration.. fluvastatin : A racemate comprising equimolar amounts of (3R,5S)- and (3S,5R)-fluvastatin. An HMG-CoA reductase inhibitor, it is used (often as the corresponding sodium salt) to reduce triglycerides and LDL-cholesterol, and increase HDL-chloesterol, in the treatment of hyperlipidaemia.		2.0510(6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid
dizocilpine maleate
Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.. dizocilpine maleate : A maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid.		2.0810maleate salt;
tetracyclic antidepressant		anaesthetic;
anticonvulsant;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist
pregna-4,17-diene-3,16-dione
pregna-4,17-diene-3,16-dione: steroid from guggulu extract; RN & N1 from C1 Form index; RN given refers to cpd without isomeric designation; structure in first source; antagonist of farnesoid X receptor		2.52203-hydroxy steroidandrogen
gw 1929
GW 1929: activates peroxisome proliferator-activated receptor-gamma; structure in first source		2.5720benzophenones
androst-16-en-3-one
androst-16-en-3-one: boar taint steroid; RN given refers to (5alpha)-isomer. 5alpha-androst-16-en-3-one : An androstanoid that is 5alpha-androst-16-ene substituted by an oxo group at position 3. It is a steroid pheromone found in high concentrations in the saliva of male pigs,.		2.04103-oxo steroid;
androstanoid		mammalian metabolite;
pheromone
dalcetrapib
dalcetrapib: inhibits cholesteryl ester transfer protein (CETP)		2.110anilide
xct790
XCT790: structure in first source		2.0610cinnamamides
6-(4-chlorophenyl)imidazo(2,1-b)(1,3)thiazole-5-carbaldehyde o-(3,4-dichlorobenzyl)oxime
6-(4-chlorophenyl)imidazo(2,1-b)(1,3)thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl)oxime: a constitutive androstane receptor agonist; structure in first source		3.0340
exp-3179
[no description available]		2.2510
gw 501516
GW 501516: a selective PPARdelta agonist; structure in first source. GW 501516 : An aromatic ether that is phenoxyacetic acid in which the phenyl group is substituted at position 2 by a methyl group and at position 4 by a (1,3-thiazol-5-ylmethyl)sulfanediyl group, and in which the 1,3-thiazolyl group is substituted at positions 2 and 4 by p-trifluoromethylphenyl and methyl groups, respectively.		2.1101,3-thiazoles;
aromatic ether;
aryl sulfide;
monocarboxylic acid;
organofluorine compound		carcinogenic agent;
PPARbeta/delta agonist
efatutazone
efatutazone: a high-affinity PPARgamma agonist with antineoplastic activity		7.1710
bms201038
BMS201038: an anticholesteremic agent and microsomal triglycide transfer protein inhibitor. lomitapide : A member of the class of benzamides obtained by formal condensation of the carboxy group of 4'-(trifluoromethyl)biphenyl-2-carboxylic acid with the primary amino group of 9-[4-(4-aminopiperidin-1-yl)butyl]-N-(2,2,2-trifluoroethyl)-9H-fluorene-9-carboxamide. Used (as its mesylate salt) as a complement to a low-fat diet and other lipid-lowering treatments in patients with homozygous familial hypercholesterolemia.		2.0810(trifluoromethyl)benzenes;
benzamides;
fluorenes;
piperidines		anticholesteremic drug;
MTP inhibitor
mocetinostat
mocetinostat: undergoing phase II clinical trials for treatment of cancer. mocetinostat : A benzamide obtained by formal condensation of the carboxy group of 4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzoic acid with one of the amino groups of benzene-1,2-diamine. It is an orally active and isotype-selective HDAC inhibitor which exhibits antitumour activity (IC50 = 0.15, 0.29, 1.66 and 0.59 muM for HDAC1, HDAC2, HDAC3 and HDAC11).		3.1750aminopyrimidine;
benzamides;
pyridines;
secondary amino compound;
secondary carboxamide;
substituted aniline		antineoplastic agent;
apoptosis inducer;
autophagy inducer;
cardioprotective agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
hepatotoxic agent
gw 4064
[no description available]		2.8630stilbenoid
gw0742
GW 610742: structure in first source		3.0240monocarboxylic acid
3,4,5,6-tetrahydroxyxanthone
[no description available]		2.0410
cynandione a
cynandione A: isolated from Cynanchum wilfordii; structure in first source		2.2510
riccardin c
riccardin C: isolated from liverworts; functions as a liver X receptor (LXR)alpha agonist and an LXRbeta antagonist; structure in first source		2.0410
alpha-synuclein
alpha-Synuclein: A synuclein that is a major component of LEWY BODIES and plays a role in SYNUCLEINOPATHIES, neurodegeneration and neuroprotection.		2.0410
trans-delta-tocotrienoloic acid
tocotrienoloic acid: from leaves of Tovomitopsis psychotriifolia; structure given in first source		3.1710tocotrienol
glaucocalyxin a
glaucocalyxin A: chemical constituent of Rabdosia japonica var. glaucocalyx		2.2510
anacetrapib
[no description available]		2.110
24-hydroxycholesterol
24-hydroxycholesterol : An oxysterol that is cholesterol which is substituted by a hydroxy group at position 24.		2.462024-hydroxy steroid;
3beta-hydroxy-Delta(5)-steroid;
oxysterol
phytosterols
Phytosterols: A class of organic compounds known as sterols or STEROIDS derived from plants.. phytosterols : Sterols similar to cholesterol which occur in plants and vary only in carbon side chains and/or presence or absence of a double bond.		2.9740
nad
NAD(1-) : An anionic form of nicotinamide adenine dinucleotide arising from deprotonation of the two OH groups of the diphosphate moiety.		2.0810organophosphate oxoanioncofactor;
human metabolite;
hydrogen acceptor;
Saccharomyces cerevisiae metabolite
mdv 3100
[no description available]		2.2110(trifluoromethyl)benzenes;
benzamides;
imidazolidinone;
monofluorobenzenes;
nitrile;
thiocarbonyl compound		androgen antagonist;
antineoplastic agent
oligonucleotides
[no description available]		2.0810
endothelin-1
Endothelin-1: A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)		7.4720
way 252623
2-(2-chloro-4-fluorobenzyl)-3-(4-fluorophenyl)-7-(trifluoromethyl)-2H-indazole: a partial LXR agonist		4.780
jsh 23
4-methyl-N1-(3-phenylpropyl)benzene-1,2-diamine: structure in first source. JSH-23 : A diamine that is 1,2-phenylenediamine carrying a methyl substituent at position 4 and a 3-phenylpropyl substituent at position N1.		2.1310diamine;
substituted aniline		NF-kappaB inhibitor
sr 1078
SR 1078: a RORalpha and RORgamma agonist; structure in first source		2.0810
aramchol
[no description available]		2.0310
15-deoxyprostaglandin j2
15-deoxyprostaglandin J2: 15d-PGJ2 abbreviation is also used for 15-deoxy-delta(12,14)PGJ2		2.0310
s-adenosylmethionine
(R)-S-adenosyl-L-methionine : An S-adenosyl-L-methionine that has R-configuration.. S-adenosyl-L-methionine zwitterion : A zwitterionic tautomer of S-adenosyl-L-methionine arising from shift of the proton from the carboxy group to the amino group.. (R)-S-adenosyl-L-methionine zwitterion : An S-adenosyl-L-methionine zwitterion that has R-configuration; major species at pH 7.3.. (S)-S-adenosyl-L-methionine zwitterion : An S-adenosyl-L-methionine zwitterion that has S-configuration; major species at pH 7.3.. S-adenosyl-L-methionine : A sulfonium compound that is the S-adenosyl derivative of L-methionine. It is an intermediate in the metabolic pathway of methionine.		2.2510organic cation;
sulfonium compound		coenzyme;
cofactor;
human metabolite;
micronutrient;
Mycoplasma genitalium metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
cholenic acid dimethylamide
cholenic acid dimethylamide: binds LXRalpha receptor; structure in first source		2.2110
pci 32765
ibrutinib: a Btk protein inhibitor. ibrutinib : A member of the class of acrylamides that is (3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine in which the piperidine nitrogen is replaced by an acryloyl group. A selective and covalent inhibitor of the enzyme Bruton's tyrosine kinase, it is used for treatment of B-cell malignancies.		2.2510acrylamides;
aromatic amine;
aromatic ether;
N-acylpiperidine;
pyrazolopyrimidine;
tertiary carboxamide		antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
cardiovascular agents
Cardiovascular Agents: Agents that affect the rate or intensity of cardiac contraction, blood vessel diameter, or blood volume.		2.4620
incb-018424
[no description available]		2.2110nitrile;
pyrazoles;
pyrrolopyrimidine		antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
sr1001
SR1001: a selective RORalpha and RORgamma inverse agonist; structure in first source		3.8830sulfonamide
interleukin-8
Interleukin-8: A member of the CXC chemokine family that plays a role in the regulation of the acute inflammatory response. It is secreted by variety of cell types and induces CHEMOTAXIS of NEUTROPHILS and other inflammatory cells.		2.4820
int-777
[no description available]		2.5820
exenatide
Exenatide: A synthetic form of exendin-4, a 39-amino acid peptide isolated from the venom of the Gila monster lizard (Heloderma suspectum). Exenatide increases CYCLIC AMP levels in pancreatic acinar cells and acts as a GLUCAGON-LIKE PEPTIDE-1 RECEPTOR (GLP-1) agonist and incretin mimetic, enhancing insulin secretion in response to increased glucose levels; it also suppresses inappropriate glucagon secretion and slows gastric emptying. It is used an anti-diabetic and anti-obesity agent.		2.0810
sr2211
[no description available]		3.9130
ascorbic acid
Ascorbic Acid: A six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant.. L-ascorbic acid : The L-enantiomer of ascorbic acid and conjugate acid of L-ascorbate.. L-ascorbate : The L-enantiomer of ascorbate and conjugate base of L-ascorbic acid, arising from selective deprotonation of the 3-hydroxy group. Required for a range of essential metabolic reactions in all animals and plants.. vitamin C : Any member of a group of vitamers that belong to the chemical structural class called butenolides that exhibit biological activity against vitamin C deficiency in animals. The vitamers include L-ascorbic acid and its salt, ionized and oxidized forms.		2.0710ascorbic acid;
vitamin C		coenzyme;
cofactor;
flour treatment agent;
food antioxidant;
food colour retention agent;
geroprotector;
plant metabolite;
skin lightening agent
lfm a13
LFM-A13 : An enamide obtained by formal condensation of the carboxy group of (2Z)-2-cyano-3-hydroxybut-2-enoic acid with the amino group of 2,5-dibromoaniline. It is a dual-function inhibitor of Bruton's tyrosine kinase (BTK) and Polo-like kinases (PLK) that exhibits anticancer properties.		2.2510aromatic amide;
dibromobenzene;
enamide;
enol;
nitrile;
secondary carboxamide		antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 2.7.11.21 (polo kinase) inhibitor;
geroprotector;
platelet aggregation inhibitor
okadaic acid
Okadaic Acid: A specific inhibitor of phosphoserine/threonine protein phosphatase 1 and 2a. It is also a potent tumor promoter. It is produced by DINOFLAGELLATES and causes diarrhetic SHELLFISH POISONING.. okadaic acid : A polycyclic ether that is produced by several species of dinoflagellates, and is known to accumulate in both marine sponges and shellfish. A polyketide, polyether derivative of a C38 fatty acid, it is one of the primary causes of diarrhetic shellfish poisoning (DSP). It is a potent inhibitor of specific protein phosphatases and is known to have a variety of negative effects on cells.		2.0310ketal
gkt137831
setanaxib: NOX4/NOX1 inhibitor; a pyrazolopyridine dione derivative		2.2510
acp-196
acalabrutinib: inhibits Bruton’s tyrosine kinase; has antineoplastic activity. acalabrutinib : A member of the class of imidazopyrazines that is imidazo[1,5-a]pyrazine substituted by 4-(pyridin-2-ylcarbamoyl)phenyl, (2S)-1-(but-2-ynoyl)pyrrolidin-2-yl, and amino groups at positions 1, 3 and 8, respectively. It is an irreversible second-generation Bruton's tyrosine kinase (BTK) inhibitor that is approved by the FDA for the treatment of adult patients with mantle cell lymphoma (MCL) who have received at least one prior therapy.		2.2510aromatic amine;
benzamides;
imidazopyrazine;
pyridines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary carboxamide;
ynone		antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
sr9238
SR9238: liver-selective LXR inverse agonist that suppresses hepatic steatosis; structure in first source		2.6320
cyclin d1
Cyclin D1: Protein encoded by the bcl-1 gene which plays a critical role in regulating the cell cycle. Overexpression of cyclin D1 is the result of bcl-1 rearrangement, a t(11;14) translocation, and is implicated in various neoplasms.		2.7930
caseins
Caseins: A mixture of related phosphoproteins occurring in milk and cheese. The group is characterized as one of the most nutritive milk proteins, containing all of the common amino acids and rich in the essential ones.		2.0410
sgc707
[no description available]		2.1710
thromboplastin
Thromboplastin: Constituent composed of protein and phospholipid that is widely distributed in many tissues. It serves as a cofactor with factor VIIa to activate factor X in the extrinsic pathway of blood coagulation.		3.1310
amyloid beta-peptides
amyloid beta-protein (1-40): although acutely neurotoxic in both rat & monkey cerebral cortex, neuronal degeneration in primates resembles more closely to that found in Alzheimer's disease; amino acid sequence has been determined		2.5220
neopterin
[no description available]		2.0810
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		3.0240cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
leptin
Leptin: A 16-kDa peptide hormone secreted from WHITE ADIPOCYTES. Leptin serves as a feedback signal from fat cells to the CENTRAL NERVOUS SYSTEM in regulation of food intake, energy balance, and fat storage.		7.7630
ConditionIndicatedRelationship StrengthStudiesTrials
Hypertriglyceridemia
A condition of elevated levels of TRIGLYCERIDES in the blood.		03.75100
Cardiometabolic Syndrome
A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components not only include metabolic dysfunctions of METABOLIC SYNDROME but also HYPERTENSION, and ABDOMINAL OBESITY.		03.3520
Benign Neoplasms
[description not available]		02.8130
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		02.8130
Metabolic Syndrome
A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components of metabolic syndrome include ABDOMINAL OBESITY; atherogenic DYSLIPIDEMIA; HYPERTENSION; HYPERGLYCEMIA; INSULIN RESISTANCE; a proinflammatory state; and a prothrombotic (THROMBOSIS) state.		03.3520
Atherogenesis
[description not available]		06.59450
Atherosclerosis
A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.		011.59450
Arteriosclerosis
Thickening and loss of elasticity of the walls of ARTERIES of all sizes. There are many forms classified by the types of lesions and arteries involved, such as ATHEROSCLEROSIS with fatty lesions in the ARTERIAL INTIMA of medium and large muscular arteries.		04.3270
Innate Inflammatory Response
[description not available]		07.88251
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.		07.88251
Insulin Sensitivity
[description not available]		03.6890
Diabetes Mellitus
A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE.		02.7230
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.		08.6890
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).		08.5580
Amyloid Deposits
[description not available]		02.0810
Acute Confusional Senile Dementia
[description not available]		04.3160
Alzheimer Disease
A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)		04.3160
Androgen-Independent Prostatic Cancer
[description not available]		02.2110
Prostatic Neoplasms, Castration-Resistant
Tumors or cancer of the PROSTATE which can grow in the presence of low or residual amount of androgen hormones such as TESTOSTERONE.		02.2110
Astrocytoma, Grade IV
[description not available]		02.2510
Experimental Neoplasms
[description not available]		02.5520
Glioblastoma
A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.		02.2510
Blood Clot
[description not available]		02.5220
Thrombosis
Formation and development of a thrombus or blood clot in the blood vessel.		02.5220
Acute Liver Injury, Drug-Induced
[description not available]		03.0640
Fatty Liver, Nonalcoholic
[description not available]		03.87100
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.		03.0640
Non-alcoholic Fatty Liver Disease
Fatty liver finding without excessive ALCOHOL CONSUMPTION.		03.87100
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		05.07390
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.		02.2510
Anoxia-Ischemia, Brain
[description not available]		03.5240
Anoxemia
[description not available]		03.3750
Acute Brain Injuries
[description not available]		03.5460
Hypoxia
Sub-optimal OXYGEN levels in the ambient air of living organisms.		03.3750
Brain Injuries
Acute and chronic (see also BRAIN INJURIES, CHRONIC) injuries to the brain, including the cerebral hemispheres, CEREBELLUM, and BRAIN STEM. Clinical manifestations depend on the nature of injury. Diffuse trauma to the brain is frequently associated with DIFFUSE AXONAL INJURY or COMA, POST-TRAUMATIC. Localized injuries may be associated with NEUROBEHAVIORAL MANIFESTATIONS; HEMIPARESIS, or other focal neurologic deficits.		03.5460
Ischemia
A hypoperfusion of the BLOOD through an organ or tissue caused by a PATHOLOGIC CONSTRICTION or obstruction of its BLOOD VESSELS, or an absence of BLOOD CIRCULATION.		03.450
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		04.37180
Hypoxia-Ischemia, Brain
A disorder characterized by a reduction of oxygen in the blood combined with reduced blood flow (ISCHEMIA) to the brain from a localized obstruction of a cerebral artery or from systemic hypoperfusion. Prolonged hypoxia-ischemia is associated with ISCHEMIC ATTACK, TRANSIENT; BRAIN INFARCTION; BRAIN EDEMA; COMA; and other conditions.		03.5240
Diabetes Mellitus, Gestational
[description not available]		02.610
Diabetes, Gestational
Diabetes mellitus induced by PREGNANCY but resolved at the end of pregnancy. It does not include previously diagnosed diabetics who become pregnant (PREGNANCY IN DIABETICS). Gestational diabetes usually develops in late pregnancy when insulin antagonistic hormones peaks leading to INSULIN RESISTANCE; GLUCOSE INTOLERANCE; and HYPERGLYCEMIA.		02.610
Eczema, Atopic
[description not available]		02.2510
Dermatitis, Atopic
A chronic inflammatory genetically determined disease of the skin marked by increased ability to form reagin (IgE), with increased susceptibility to allergic rhinitis and asthma, and hereditary disposition to a lowered threshold for pruritus. It is manifested by lichenification, excoriation, and crusting, mainly on the flexural surfaces of the elbow and knee. In infants it is known as infantile eczema.		02.2510
Alloxan Diabetes
[description not available]		03.250
Autoimmune Diabetes
[description not available]		02.5720
Diabetes Mellitus, Adult-Onset
[description not available]		05.16101
Asymmetric Diabetic Proximal Motor Neuropathy
[description not available]		02.2510
Diabetes Mellitus, Type 1
A subtype of DIABETES MELLITUS that is characterized by INSULIN deficiency. It is manifested by the sudden onset of severe HYPERGLYCEMIA, rapid progression to DIABETIC KETOACIDOSIS, and DEATH unless treated with insulin. The disease may occur at any age, but is most common in childhood or adolescence.		02.5720
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.		05.16101
Diabetic Neuropathies
Peripheral, autonomic, and cranial nerve disorders that are associated with DIABETES MELLITUS. These conditions usually result from diabetic microvascular injury involving small blood vessels that supply nerves (VASA NERVORUM). Relatively common conditions which may be associated with diabetic neuropathy include third nerve palsy (see OCULOMOTOR NERVE DISEASES); MONONEUROPATHY; mononeuropathy multiplex; diabetic amyotrophy; a painful POLYNEUROPATHY; autonomic neuropathy; and thoracoabdominal neuropathy. (From Adams et al., Principles of Neurology, 6th ed, p1325)		02.2510
Carcinogenesis
The origin, production or development of cancer through genotypic and phenotypic changes which upset the normal balance between cell proliferation and cell death. Carcinogenesis generally requires a constellation of steps, which may occur quickly or over a period of many years.		02.2510
Cancer of Liver
[description not available]		03.78100
Liver Neoplasms
Tumors or cancer of the LIVER.		03.78100
Hepatitis B Virus Infection
[description not available]		02.520
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.		02.520
Bilirubinemia
[description not available]		02.3110
Crigler Najjar Syndrome
[description not available]		02.3110
Breast Cancer
[description not available]		02.8330
Breast Neoplasms
Tumors or cancer of the human BREAST.		02.8330
Hemorrhage, Subarachnoid
[description not available]		02.3110
Subarachnoid Hemorrhage
Bleeding into the intracranial or spinal SUBARACHNOID SPACE, most resulting from INTRACRANIAL ANEURYSM rupture. It can occur after traumatic injuries (SUBARACHNOID HEMORRHAGE, TRAUMATIC). Clinical features include HEADACHE; NAUSEA; VOMITING, nuchal rigidity, variable neurological deficits and reduced mental status.		07.3110
Age-Related Macular Degeneration
[description not available]		02.1510
Macular Degeneration
Degenerative changes in the RETINA usually of older adults which results in a loss of vision in the center of the visual field (the MACULA LUTEA) because of damage to the retina. It occurs in dry and wet forms.		02.1510
Idiopathic Parkinson Disease
[description not available]		02.1510
MPTP Neurotoxicity Syndrome
[description not available]		02.1510
Parkinson Disease
A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)		02.1510
Astrocytosis
[description not available]		02.1510
Retinal Degeneration
A retrogressive pathological change in the retina, focal or generalized, caused by genetic defects, inflammation, trauma, vascular disease, or aging. Degeneration affecting predominantly the macula lutea of the retina is MACULAR DEGENERATION. (Newell, Ophthalmology: Principles and Concepts, 7th ed, p304)		02.1510
Lung Injury, Acute
[description not available]		02.7730
Acute Lung Injury
A condition of lung damage that is characterized by bilateral pulmonary infiltrates (PULMONARY EDEMA) rich in NEUTROPHILS, and in the absence of clinical HEART FAILURE. This can represent a spectrum of pulmonary lesions, endothelial and epithelial, due to numerous factors (physical, chemical, or biological).		07.7730
Liver Steatosis
[description not available]		04.61240
Fatty Liver
Lipid infiltration of the hepatic parenchymal cells resulting in a yellow-colored liver. The abnormal lipid accumulation is usually in the form of TRIGLYCERIDES, either as a single large droplet or multiple small droplets. Fatty liver is caused by an imbalance in the metabolism of FATTY ACIDS.		04.61240
Carcinoma, Non-Small Cell Lung
[description not available]		02.5820
Cancer of Lung
[description not available]		02.8330
Invasiveness, Neoplasm
[description not available]		02.5820
Carcinoma, Non-Small-Cell Lung
A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.		02.5820
Lung Neoplasms
Tumors or cancer of the LUNG.		02.8330
Hypertrophy, Right Ventricular
Enlargement of the RIGHT VENTRICLE of the heart. This increase in ventricular mass is often attributed to PULMONARY HYPERTENSION and is a contributor to cardiovascular morbidity and mortality.		02.1510
Pulmonary Hypertension
[description not available]		02.1510
Hypertension, Pulmonary
Increased VASCULAR RESISTANCE in the PULMONARY CIRCULATION, usually secondary to HEART DISEASES or LUNG DISEASES.		02.1510
Atheroma
[description not available]		03.8100
HIV Coinfection
[description not available]		05.4951
HIV
Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.		04.8421
HIV Infections
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).		05.4951
Blood Poisoning
[description not available]		02.5320
Cardiac Rupture, Traumatic
[description not available]		02.1510
Sepsis
Systemic inflammatory response syndrome with a proven or suspected infectious etiology. When sepsis is associated with organ dysfunction distant from the site of infection, it is called severe sepsis. When sepsis is accompanied by HYPOTENSION despite adequate fluid infusion, it is called SEPTIC SHOCK.		02.5320
Hepatocellular Carcinoma
[description not available]		03.4570
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.		03.4570
Chronic Kidney Diseases
[description not available]		02.5420
Renal Insufficiency, Chronic
Conditions in which the KIDNEYS perform below the normal level for more than three months. Chronic kidney insufficiency is classified by five stages according to the decline in GLOMERULAR FILTRATION RATE and the degree of kidney damage (as measured by the level of PROTEINURIA). The most severe form is the end-stage renal disease (CHRONIC KIDNEY FAILURE). (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002)		02.5420
Bleeding
[description not available]		02.1710
Libman-Sacks Disease
[description not available]		02.5920
Hemorrhage
Bleeding or escape of blood from a vessel.		02.1710
Lupus Erythematosus, Systemic
A chronic, relapsing, inflammatory, and often febrile multisystemic disorder of connective tissue, characterized principally by involvement of the skin, joints, kidneys, and serosal membranes. It is of unknown etiology, but is thought to represent a failure of the regulatory mechanisms of the autoimmune system. The disease is marked by a wide range of system dysfunctions, an elevated erythrocyte sedimentation rate, and the formation of LE cells in the blood or bone marrow.		02.5920
Lung Adenocarcinoma
[description not available]		07.1710
Adenocarcinoma of Lung
A carcinoma originating in the lung and the most common lung cancer type in never-smokers. Malignant cells exhibit distinct features such as glandular epithelial, or tubular morphology. Mutations in KRAS, EGFR, BRAF, and ERBB2 genes are associated with this cancer.		02.1710
Cancer of Colon
[description not available]		02.8130
Colonic Neoplasms
Tumors or cancer of the COLON.		02.8130
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		02.7630
Cancer of Stomach
[description not available]		02.2110
Stomach Neoplasms
Tumors or cancer of the STOMACH.		02.2110
Aging
The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.		02.5220
Disease Exacerbation
[description not available]		02.9840
Glomerulonephritis, Lupus
[description not available]		02.2110
Lupus Nephritis
Glomerulonephritis associated with autoimmune disease SYSTEMIC LUPUS ERYTHEMATOSUS. Lupus nephritis is histologically classified into 6 classes: class I - normal glomeruli, class II - pure mesangial alterations, class III - focal segmental glomerulonephritis, class IV - diffuse glomerulonephritis, class V - diffuse membranous glomerulonephritis, and class VI - advanced sclerosing glomerulonephritis (The World Health Organization classification 1982).		02.2110
Surgical Incision
[description not available]		02.2110
Hyperlipemia
[description not available]		03.1750
Hyperlipidemias
Conditions with excess LIPIDS in the blood.		03.1750
Alveolar Bone Atrophy
[description not available]		02.0810
Acute Myelogenous Leukemia
[description not available]		02.110
Leukemia, Myeloid, Acute
Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.		02.110
Diabetic Glomerulosclerosis
[description not available]		02.4820
Diabetic Nephropathies
KIDNEY injuries associated with diabetes mellitus and affecting KIDNEY GLOMERULUS; ARTERIOLES; KIDNEY TUBULES; and the interstitium. Clinical signs include persistent PROTEINURIA, from microalbuminuria progressing to ALBUMINURIA of greater than 300 mg/24 h, leading to reduced GLOMERULAR FILTRATION RATE and END-STAGE RENAL DISEASE.		02.4820
Diabetic Cardiomyopathies
Diabetes complications in which VENTRICULAR REMODELING in the absence of CORONARY ATHEROSCLEROSIS and hypertension results in cardiac dysfunctions, typically LEFT VENTRICULAR DYSFUNCTION. The changes also result in myocardial hypertrophy, myocardial necrosis and fibrosis, and collagen deposition due to impaired glucose tolerance.		02.110
Neurovisceral Storage Disease with Vertical Supranuclear Ophthalmoplegia
[description not available]		02.0810
Niemann-Pick Disease, Type C
An autosomal recessive lipid storage disorder that is characterized by accumulation of CHOLESTEROL and SPHINGOMYELINS in cells of the VISCERA and the CENTRAL NERVOUS SYSTEM. Type C (or C1) and type D are allelic disorders caused by mutation of the NPC1 gene, which encodes a protein that mediates intracellular cholesterol transport from LYSOSOMES. Clinical signs include hepatosplenomegaly and chronic neurological symptoms. Type D is a variant in people with a Nova Scotia ancestry.		02.0810
Deficiency, Vitamin E
[description not available]		02.0810
Dementias, Transmissible
[description not available]		02.110
Malignant Melanoma
[description not available]		02.4920
Metastase
[description not available]		02.110
Cancer of Skin
[description not available]		02.4920
Melanoma
A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)		02.4920
Neoplasm Metastasis
The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.		02.110
Skin Neoplasms
Tumors or cancer of the SKIN.		02.4920
Diffuse Cutaneous Systemic Sclerosis
[description not available]		02.1110
Cirrhosis
[description not available]		02.1110
Dermatoses
[description not available]		02.1110
Fibrosis
Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.		02.1110
Skin Diseases
Diseases involving the DERMIS or EPIDERMIS.		02.1110
Scleroderma, Diffuse
A rapid onset form of SYSTEMIC SCLERODERMA with progressive widespread SKIN thickening over the arms, the legs and the trunk, resulting in stiffness and disability.		02.1110
Age-Related Memory Disorders
[description not available]		02.7630
Memory Disorders
Disturbances in registering an impression, in the retention of an acquired impression, or in the recall of an impression. Memory impairments are associated with DEMENTIA; CRANIOCEREBRAL TRAUMA; ENCEPHALITIS; ALCOHOLISM (see also ALCOHOL AMNESTIC DISORDER); SCHIZOPHRENIA; and other conditions.		02.7630
Airway Remodeling
The structural changes in the number, mass, size and/or composition of the airway tissues.		07.110
Asthma, Bronchial
[description not available]		02.110
Asthma
A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).		07.110
Amentia
[description not available]		02.110
Dementia
An acquired organic mental disorder with loss of intellectual abilities of sufficient severity to interfere with social or occupational functioning. The dysfunction is multifaceted and involves memory, behavior, personality, judgment, attention, spatial relations, language, abstract thought, and other executive functions. The intellectual decline is usually progressive, and initially spares the level of consciousness.		07.110
Autoimmune Disease
[description not available]		02.110
Autoimmune Diseases
Disorders that are characterized by the production of antibodies that react with host tissues or immune effector cells that are autoreactive to endogenous peptides.		02.110
Uveitis
Inflammation of part or all of the uvea, the middle (vascular) tunic of the eye, and commonly involving the other tunics (sclera and cornea, and the retina). (Dorland, 27th ed)		02.110
Kahler Disease
[description not available]		02.110
Multiple Myeloma
A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.		02.110
Heart Disease, Ischemic
[description not available]		02.110
Myocardial Ischemia
A disorder of cardiac function caused by insufficient blood flow to the muscle tissue of the heart. The decreased blood flow may be due to narrowing of the coronary arteries (CORONARY ARTERY DISEASE), to obstruction by a thrombus (CORONARY THROMBOSIS), or less commonly, to diffuse narrowing of arterioles and other small vessels within the heart. Severe interruption of the blood supply to the myocardial tissue may result in necrosis of cardiac muscle (MYOCARDIAL INFARCTION).		02.110
Mastitis
INFLAMMATION of the BREAST, or MAMMARY GLAND.		02.110
Fetal Growth Restriction
[description not available]		02.110
Fetal Growth Retardation
Failure of a FETUS to attain expected GROWTH.		02.110
Cancer of Prostate
[description not available]		03.5680
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		03.5680
Aortic Diseases
Pathological processes involving any part of the AORTA.		02.1110
Acute Kidney Failure
[description not available]		02.1110
Acute Kidney Injury
Abrupt reduction in kidney function. Acute kidney injury encompasses the entire spectrum of the syndrome including acute kidney failure; ACUTE KIDNEY TUBULAR NECROSIS; and other less severe conditions.		02.1110
Cerebral Pseudosclerosis
[description not available]		02.1310
Hepatolenticular Degeneration
A rare autosomal recessive disease characterized by the deposition of copper in the BRAIN; LIVER; CORNEA; and other organs. It is caused by defects in the ATP7B gene encoding copper-transporting ATPase 2 (EC 3.6.3.4), also known as the Wilson disease protein. The overload of copper inevitably leads to progressive liver and neurological dysfunction such as LIVER CIRRHOSIS; TREMOR; ATAXIA and intellectual deterioration. Hepatic dysfunction may precede neurologic dysfunction by several years.		02.1310
Brain Hemorrhage, Cerebral
[description not available]		02.1310
Cerebral Hemorrhage
Bleeding into one or both CEREBRAL HEMISPHERES including the BASAL GANGLIA and the CEREBRAL CORTEX. It is often associated with HYPERTENSION and CRANIOCEREBRAL TRAUMA.		02.1310
Diabetes Insipidus
A disease that is characterized by frequent urination, excretion of large amounts of dilute URINE, and excessive THIRST. Etiologies of diabetes insipidus include deficiency of antidiuretic hormone (also known as ADH or VASOPRESSIN) secreted by the NEUROHYPOPHYSIS, impaired KIDNEY response to ADH, and impaired hypothalamic regulation of thirst.		02.1310
Elevated Cholesterol
[description not available]		04.1331
Hypercholesterolemia
A condition with abnormally high levels of CHOLESTEROL in the blood. It is defined as a cholesterol value exceeding the 95th percentile for the population.		04.1331
Biliary Calculi
[description not available]		02.1310
Gallstones
Solid crystalline precipitates in the BILIARY TRACT, usually formed in the GALLBLADDER, resulting in the condition of CHOLELITHIASIS. Gallstones, derived from the BILE, consist mainly of calcium, cholesterol, or bilirubin.		02.1310
Colitis
Inflammation of the COLON section of the large intestine (INTESTINE, LARGE), usually with symptoms such as DIARRHEA (often with blood and mucus), ABDOMINAL PAIN, and FEVER.		02.1310
Autism
[description not available]		02.1310
Autistic Disorder
A disorder beginning in childhood. It is marked by the presence of markedly abnormal or impaired development in social interaction and communication and a markedly restricted repertoire of activity and interest. Manifestations of the disorder vary greatly depending on the developmental level and chronological age of the individual. (DSM-V)		02.1310
Delayed Effects, Prenatal Exposure
[description not available]		02.4820
Blood Pressure, High
[description not available]		02.1510
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		02.1510
Alveolitis, Fibrosing
[description not available]		02.1310
Pulmonary Fibrosis
A process in which normal lung tissues are progressively replaced by FIBROBLASTS and COLLAGEN causing an irreversible loss of the ability to transfer oxygen into the bloodstream via PULMONARY ALVEOLI. Patients show progressive DYSPNEA finally resulting in death.		02.1310
Dyslipidemia
[description not available]		03.8740
Dyslipidemias
Abnormalities in the serum levels of LIPIDS, including overproduction or deficiency. Abnormal serum lipid profiles may include high total CHOLESTEROL, high TRIGLYCERIDES, low HIGH DENSITY LIPOPROTEIN CHOLESTEROL, and elevated LOW DENSITY LIPOPROTEIN CHOLESTEROL.		03.8740
7-Dehydrocholesterol Reductase Deficiency
[description not available]		02.0410
Smith-Lemli-Opitz Syndrome
An autosomal recessive disorder of CHOLESTEROL metabolism. It is caused by a deficiency of 7-dehydrocholesterol reductase, the enzyme that converts 7-dehydrocholesterol to cholesterol, leading to an abnormally low plasma cholesterol. This syndrome is characterized by multiple CONGENITAL ABNORMALITIES, growth deficiency, and INTELLECTUAL DISABILITY.		02.0410
Hepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted
[description not available]		02.0410
Hepatitis C
INFLAMMATION of the LIVER in humans caused by HEPATITIS C VIRUS, a single-stranded RNA virus. Its incubation period is 30-90 days. Hepatitis C is transmitted primarily by contaminated blood parenterally and is often associated with transfusion and intravenous drug abuse. However, in a significant number of cases, the source of hepatitis C infection is unknown.		02.0410
Neuroblastoma
A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)		02.0410
Hepatoblastoma
A malignant neoplasm occurring in young children, primarily in the liver, composed of tissue resembling embryonal or fetal hepatic epithelium, or mixed epithelial and mesenchymal tissues. (Stedman, 25th ed)		02.0510
Arthritis, Degenerative
[description not available]		02.4620
Osteoarthritis
A progressive, degenerative joint disease, the most common form of arthritis, especially in older persons. The disease is thought to result not from the aging process but from biochemical changes and biomechanical stresses affecting articular cartilage. In the foreign literature it is often called osteoarthrosis deformans.		02.4620
Adenoma, beta-Cell
[description not available]		02.4420
Cancer of Pancreas
[description not available]		02.4420
Insulinoma
A benign tumor of the PANCREATIC BETA CELLS. Insulinoma secretes excess INSULIN resulting in HYPOGLYCEMIA.		02.4420
Pancreatic Neoplasms
Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).		02.4420
Compensatory Hyperinsulinemia
A GLUCOSE-induced HYPERINSULINEMIA, a marker of insulin-resistant state. It is a mechanism to compensate for reduced sensitivity to insulin.		02.4520
Hyperinsulinism
A syndrome with excessively high INSULIN levels in the BLOOD. It may cause HYPOGLYCEMIA. Etiology of hyperinsulinism varies, including hypersecretion of a beta cell tumor (INSULINOMA); autoantibodies against insulin (INSULIN ANTIBODIES); defective insulin receptor (INSULIN RESISTANCE); or overuse of exogenous insulin or HYPOGLYCEMIC AGENTS.		02.4520
Ovarian Hyperstimulation Syndrome, Familial Gestational Spontaneous
[description not available]		02.0510
Ovarian Hyperstimulation Syndrome
A complication of OVULATION INDUCTION in infertility treatment. It is graded by the severity of symptoms which include OVARY enlargement, multiple OVARIAN FOLLICLES; OVARIAN CYSTS; ASCITES; and generalized EDEMA. The full-blown syndrome may lead to RENAL FAILURE, respiratory distress, and even DEATH. Increased capillary permeability is caused by the vasoactive substances, such as VASCULAR ENDOTHELIAL GROWTH FACTORS, secreted by the overly-stimulated OVARIES.		02.0510
Calcification, Pathologic
[description not available]		02.0510
Calcinosis
Pathologic deposition of calcium salts in tissues.		02.0510
Allergic Encephalomyelitis
[description not available]		02.4420
MS (Multiple Sclerosis)
[description not available]		02.7430
Multiple Sclerosis
An autoimmune disorder mainly affecting young adults and characterized by destruction of myelin in the central nervous system. Pathologic findings include multiple sharply demarcated areas of demyelination throughout the white matter of the central nervous system. Clinical manifestations include visual loss, extra-ocular movement disorders, paresthesias, loss of sensation, weakness, dysarthria, spasticity, ataxia, and bladder dysfunction. The usual pattern is one of recurrent attacks followed by partial recovery (see MULTIPLE SCLEROSIS, RELAPSING-REMITTING), but acute fulminating and chronic progressive forms (see MULTIPLE SCLEROSIS, CHRONIC PROGRESSIVE) also occur. (Adams et al., Principles of Neurology, 6th ed, p903)		02.7430
Cerebral Infarction, Middle Cerebral Artery
[description not available]		02.0510
Apoplexy
[description not available]		02.7530
Infarction, Middle Cerebral Artery
NECROSIS occurring in the MIDDLE CEREBRAL ARTERY distribution system which brings blood to the entire lateral aspects of each CEREBRAL HEMISPHERE. Clinical signs include impaired cognition; APHASIA; AGRAPHIA; weak and numbness in the face and arms, contralaterally or bilaterally depending on the infarction.		02.0510
Stroke
A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)		02.7530
Cardiac Hypertrophy
Enlargement of the HEART due to chamber HYPERTROPHY, an increase in wall thickness without an increase in the number of cells (MYOCYTES, CARDIAC). It is the result of increase in myocyte size, mitochondrial and myofibrillar mass, as well as changes in extracellular matrix.		02.4620
Cardiomegaly
Enlargement of the HEART, usually indicated by a cardiothoracic ratio above 0.50. Heart enlargement may involve the right, the left, or both HEART VENTRICLES or HEART ATRIA. Cardiomegaly is a nonspecific symptom seen in patients with chronic systolic heart failure (HEART FAILURE) or several forms of CARDIOMYOPATHIES.		02.4620
Hormone-Dependent Neoplasms
[description not available]		02.4420
Adjuvant Arthritis
[description not available]		02.4420
Rheumatoid Arthritis
[description not available]		02.4620
Arthritis, Rheumatoid
A chronic systemic disease, primarily of the joints, marked by inflammatory changes in the synovial membranes and articular structures, widespread fibrinoid degeneration of the collagen fibers in mesenchymal tissues, and by atrophy and rarefaction of bony structures. Etiology is unknown, but autoimmune mechanisms have been implicated.		02.4620
Cancer of Ovary
[description not available]		02.4620
Ovarian Neoplasms
Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.		02.4620
B-Cell Chronic Lymphocytic Leukemia
[description not available]		02.0510
Leukemia, Lymphocytic, Chronic, B-Cell
A chronic leukemia characterized by abnormal B-lymphocytes and often generalized lymphadenopathy. In patients presenting predominately with blood and bone marrow involvement it is called chronic lymphocytic leukemia (CLL); in those predominately with enlarged lymph nodes it is called small lymphocytic lymphoma. These terms represent spectrums of the same disease.		02.0510
Dyskinesia Syndromes
[description not available]		02.0510
Infectious Myelitis
[description not available]		02.0510
Injuries, Spinal Cord
[description not available]		02.0510
Movement Disorders
Syndromes which feature DYSKINESIAS as a cardinal manifestation of the disease process. Included in this category are degenerative, hereditary, post-infectious, medication-induced, post-inflammatory, and post-traumatic conditions.		02.0510
Spinal Cord Injuries
Penetrating and non-penetrating injuries to the spinal cord resulting from traumatic external forces (e.g., WOUNDS, GUNSHOT; WHIPLASH INJURIES; etc.).		02.0510
Morbid Obesity
[description not available]		02.0510
Weight Reduction
[description not available]		02.0510
Obesity, Morbid
The condition of weighing two, three, or more times the ideal weight, so called because it is associated with many serious and life-threatening disorders. In the BODY MASS INDEX, morbid obesity is defined as having a BMI greater than 40.0 kg/m2.		02.0510
Weight Loss
Decrease in existing BODY WEIGHT.		02.0510
Injury, Ischemia-Reperfusion
[description not available]		02.0510
Reperfusion Injury
Adverse functional, metabolic, or structural changes in tissues that result from the restoration of blood flow to the tissue (REPERFUSION) following ISCHEMIA.		02.0510
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		02.0510
Pleurisy
INFLAMMATION of PLEURA, the lining of the LUNG. When PARIETAL PLEURA is involved, there is pleuritic CHEST PAIN.		02.0510
Experimental Lung Inflammation
Inflammation of any part, segment or lobe, of the lung parenchyma.		02.0510
Pneumonia
Infection of the lung often accompanied by inflammation.		02.0510
Left Ventricular Hypertrophy
[description not available]		02.0510
Hypertrophy, Left Ventricular
Enlargement of the LEFT VENTRICLE of the heart. This increase in ventricular mass is attributed to sustained abnormal pressure or volume loads and is a contributor to cardiovascular morbidity and mortality.		02.0510
Edema-Proteinuria-Hypertension Gestosis
[description not available]		02.7530
Pre-Eclampsia
A complication of PREGNANCY, characterized by a complex of symptoms including maternal HYPERTENSION and PROTEINURIA with or without pathological EDEMA. Symptoms may range between mild and severe. Pre-eclampsia usually occurs after the 20th week of gestation, but may develop before this time in the presence of trophoblastic disease.		02.7530
Hemorrhagic Shock
[description not available]		02.0610
Heart Valve Diseases
Pathological conditions involving any of the various HEART VALVES and the associated structures (PAPILLARY MUSCLES and CHORDAE TENDINEAE).		02.0510
Brain Swelling
[description not available]		02.0710
Cerebral Ischemia
[description not available]		02.0710
Brain Edema
Increased intracellular or extracellular fluid in brain tissue. Cytotoxic brain edema (swelling due to increased intracellular fluid) is indicative of a disturbance in cell metabolism, and is commonly associated with hypoxic or ischemic injuries (see HYPOXIA, BRAIN). An increase in extracellular fluid may be caused by increased brain capillary permeability (vasogenic edema), an osmotic gradient, local blockages in interstitial fluid pathways, or by obstruction of CSF flow (e.g., obstructive HYDROCEPHALUS). (From Childs Nerv Syst 1992 Sep; 8(6):301-6)		02.0710
Brain Ischemia
Localized reduction of blood flow to brain tissue due to arterial obstruction or systemic hypoperfusion. This frequently occurs in conjunction with brain hypoxia (HYPOXIA, BRAIN). Prolonged ischemia is associated with BRAIN INFARCTION.		02.0710
Adenocarcinoma, Basal Cell
[description not available]		02.0710
Adenocarcinoma
A malignant epithelial tumor with a glandular organization.		02.0710
Genetic Predisposition
[description not available]		02.0610
Carcinoma, Lewis Lung
A carcinoma discovered by Dr. Margaret R. Lewis of the Wistar Institute in 1951. This tumor originated spontaneously as a carcinoma of the lung of a C57BL mouse. The tumor does not appear to be grossly hemorrhagic and the majority of the tumor tissue is a semifirm homogeneous mass. (From Cancer Chemother Rep 2 1972 Nov;(3)1:325) It is also called 3LL and LLC and is used as a transplantable malignancy.		02.0710
Cancer of the Uterus
[description not available]		02.0710
Placenta Diseases
Pathological processes or abnormal functions of the PLACENTA.		02.0710
Choriocarcinoma
A malignant metastatic form of trophoblastic tumors. Unlike the HYDATIDIFORM MOLE, choriocarcinoma contains no CHORIONIC VILLI but rather sheets of undifferentiated cytotrophoblasts and syncytiotrophoblasts (TROPHOBLASTS). It is characterized by the large amounts of CHORIONIC GONADOTROPIN produced. Tissue origins can be determined by DNA analyses: placental (fetal) origin or non-placental origin (CHORIOCARCINOMA, NON-GESTATIONAL).		02.0710
Uterine Neoplasms
Tumors or cancer of the UTERUS.		02.0710
Cardiovascular Stroke
[description not available]		02.0710
Myocardial Infarction
NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).		02.0710
Hypermelanosis
[description not available]		02.0810
Hyperpigmentation
Excessive pigmentation of the skin, usually as a result of increased epidermal or dermal melanin pigmentation, hypermelanosis. Hyperpigmentation can be localized or generalized. The condition may arise from exposure to light, chemicals or other substances, or from a primary metabolic imbalance.		02.0810
Anoxia, Brain
[description not available]		02.0810
Carotid Arteriopathies, Traumatic
[description not available]		02.0210
Hyperplasia
An increase in the number of cells in a tissue or organ without tumor formation. It differs from HYPERTROPHY, which is an increase in bulk without an increase in the number of cells.		02.0210
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		02.0210
A-alphalipoprotein Neuropathy
[description not available]		02.0310
Impaired Glucose Tolerance
[description not available]		02.0310
Glucose Intolerance
A pathological state in which BLOOD GLUCOSE level is less than approximately 140 mg/100 ml of PLASMA at fasting, and above approximately 200 mg/100 ml plasma at 30-, 60-, or 90-minute during a GLUCOSE TOLERANCE TEST. This condition is seen frequently in DIABETES MELLITUS, but also occurs with other diseases and MALNUTRITION.		02.0310
Niemann-Pick Disease
[description not available]		02.0310
Niemann-Pick Diseases
A group of autosomal recessive disorders in which harmful quantities of lipids accumulate in the viscera and the central nervous system. They can be caused by deficiencies of enzyme activities (SPHINGOMYELIN PHOSPHODIESTERASE) or defects in intracellular transport, resulting in the accumulation of SPHINGOMYELINS and CHOLESTEROL. There are various subtypes based on their clinical and genetic differences.		02.0310
Acute-Phase Reaction
An early local inflammatory reaction to insult or injury that consists of fever, an increase in inflammatory humoral factors, and an increased synthesis by hepatocytes of a number of proteins or glycoproteins usually found in the plasma.		02.0310
Hyperhomocysteinemia
Condition in which the plasma levels of homocysteine and related metabolites are elevated (		02.0310
Cell Transformation, Neoplastic
Cell changes manifested by escape from control mechanisms, increased growth potential, alterations in the cell surface, karyotypic abnormalities, morphological and biochemical deviations from the norm, and other attributes conferring the ability to invade, metastasize, and kill.		02.0410
Apolipoprotein B-100, Familial Defective
[description not available]		02.0410
Hyperlipoproteinemia Type II
A group of familial disorders characterized by elevated circulating cholesterol contained in either LOW-DENSITY LIPOPROTEINS alone or also in VERY-LOW-DENSITY LIPOPROTEINS (pre-beta lipoproteins).		02.0410
Infections, Klebsiella
[description not available]		02.0410
Klebsiella Infections
Infections with bacteria of the genus KLEBSIELLA.		02.0410
Diabetic Angiopathies
VASCULAR DISEASES that are associated with DIABETES MELLITUS.		02.0410