glucose dextrose BDBM34103 D-glucose
CHEMBL458193 2,3-hexahydroxydiphenoyl-D-glucose 2,3-O-(S)-hexahydroxydiphenoyl-D-glucose 2,3-(S)-hexahydroxydiphenoyl-D-glucose BDBM50250987 2, 3-(S)-hexahydroxydiphenoyl-D-glucose
(glucose)n glycogen BDBM24362
UDPG BDBM50423218 Udp-Glucose URIDINE DIPHOSPHATE GLUCOSE 5''-Diphosphoglucose Uridine-5''-Diphosphoglucose
BDBM197174 Glucose-6-phosphate (G6P)
Uridine-5'-glucose-1'-tetraphosphate BDBM50270545 CHEMBL499138
BDBM420321 Penta-O-galloyl-beta-D-glucose hydrate
BDBM50319133 3-Phenacyluridine5'-Glucose-1'-triphosphate TriethylammoniumSalt CHEMBL1083262
2, 6-di-O-galloyl-D-glucose BDBM50269545 CHEMBL458684
5-Iodouridine 5'-Glucose-1'-triphosphate TriethylammoniumSalt BDBM50319127 CHEMBL1083261
BDBM50308980 6-O-Octylsulfonyl-D-glucose-2,4-bisphosphate CHEMBL600442
BDBM50308981 CHEMBL600243 6-O-Hexylsulfonyl-D-glucose-2,4-bisphosphate
BDBM741327 BCN-NHC2H4CO- (glucose) SG4-P9 US20250161476, LP# LP18
CHEMBL1614854 beta-D-glucopyranose Glucoside BDBM50240803 beta-D-glucose
CHEMBL454230 Uridine-5'-(2'-deoxy-glucose)-6'-tetraphosphate BDBM50270548
CHEMBL590082 BDBM50308978 6-O-Ethylsulfonyl-D-glucose-2,4-bisphosphate
CHEMBL590347 6-O-Dodecylsulfonyl-D-glucose-2,4-bisphosphate BDBM50308979
N4-Methoxycytidine 5'-Glucose-1'-triphosphate TriethylammoniumSalt CHEMBL1083264 BDBM50319136
US20250161476, LP# LP20 BDBM741329 DIBAC-suc- (glucose) SG4-P9
BDBM226188 dihydrodehydrodiconifeyl alcohol 9'-O-β-D-glucose (19)
BDBM50319134 Uridine 5'-Glucose-1'-alpha,beta-methylenetriphosphate TriethylammoniumSalt CHEMBL1083263
cori ester glucose-1-phosphate alpha-glucose-1-phosphate {[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}phosphonic acid BDBM23188
P1-Uridine 5'-P3-[1]Glucose-1'-Triphosphate TriethylammoniumSalt BDBM50319132 CHEMBL1083260
uridine 5'-[3-alpha-D-glucopyranosyl dihydrogen diphosphate] UDP-alpha-D-glucose BDBM50209659
Sulpiride-d Sulpiride-low,(-) Sulpiride-R Sulpiride-high,(-) BDBM81775
CHEMBL498485 Icaritin 3-hydroxy-7-o-beta-glucose-8-prenyl-4'-methoxy Chrysin BDBM50272527
1,2,6-tris-O-galloyl-beta-D-glucose BDBM50250504 CHEMBL447974 1,2,6-tris-O-(3,4,5-trihydroxybenzoyl)-beta-D-glucopyranose
BDBM645364 pinocembrin 7-O-(3$#8243;- galloyl-4$#8243;,6$#8243;-(S)- hexahydroxydiphenoyl)- beta-D-glucose (PGHG) US20240016777, Table3.6
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- Peters, JU; Kühne, H; Dehmlow, H; Grether, U; Conte, A; Hainzl, D; Hertel, C; Kratochwil, NA; Otteneder, M; Narquizian, R; Panousis, CG; Ricklin, F; Röver, S Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: optimization of in vitro activity. Bioorg Med Chem Lett 20: 5426-30 (2010)
- Park, JD; Kim, DH Reversed hydroxamate-bearing thermolysin inhibitors mimic a high-energy intermediate along the enzyme-catalyzed proteolytic reaction pathway. Bioorg Med Chem Lett 13: 3161-6 (2003)
- Podust, LM; von Kries, JP; Eddine, AN; Kim, Y; Yermalitskaya, LV; Kuehne, R; Ouellet, H; Warrier, T; Alteköster, M; Lee, JS; Rademann, J; Oschkinat, H; Kaufmann, SH; Waterman, MR Small-molecule scaffolds for CYP51 inhibitors identified by high-throughput screening and defined by X-ray crystallography. Antimicrob Agents Chemother 51: 3915-23 (2007)
- Smith, AL; Stevenson, GI; Lewis, S; Patel, S; Castro, JL Solid-phase synthesis of 2,3-disubstituted indoles: discovery of a novel, high-affinity, selective h5-HT2A antagonist. Bioorg Med Chem Lett 10: 2693-6 (2000)
- Ryu, H; Jin, MK; Kim, SY; Choi, HK; Kang, SU; Kang, DW; Lee, J; Pearce, LV; Pavlyukovets, VA; Morgan, MA; Tran, R; Toth, A; Lundberg, DJ; Blumberg, PM Stereospecific high-affinity TRPV1 antagonists: chiral N-(2-Benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues. J Med Chem 51: 57-67 (2008)
- Kaushik, D; Kaur, A; Patil, MT; Sihag, B; Piplani, S; Sakala, I; Honda-Okubo, Y; Ramakrishnan, S; Petrovsky, N; Salunke, DB Structure-Activity Relationships toward the Identification of a High-Potency Selective Human Toll-like Receptor-7 Agonist. J Med Chem 67: 8346-8360
- Yu, J; Luo, L; Hu, T; Cui, Y; Sun, X; Gou, W; Hou, W; Li, Y; Sun, T Structure-based design, synthesis, and evaluation of inhibitors with high selectivity for PARP-1 over PARP-2. Eur J Med Chem 227: (2022)
- Ghosh, AK; Gemma, S; Simoni, E; Baldridge, A; Walters, DE; Ide, K; Tojo, Y; Koh, Y; Amano, M; Mitsuya, H Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands. Bioorg Med Chem Lett 20: 1241-6 (2010)
- Ghosh, AK; Lee, HY; Thompson, WJ; Culberson, C; Holloway, MK; McKee, SP; Munson, PM; Duong, TT; Smith, AM; Darke, PL The development of cyclic sulfolanes as novel and high-affinity P2 ligands for HIV-1 protease inhibitors. J Med Chem 37: 1177-88 (1994)
- Holmes, IP; Blunt, RJ; Lorthioir, OE; Blowers, SM; Gribble, A; Payne, AH; Stansfield, IG; Wood, M; Woollard, PM; Reavill, C; Howes, CM; Micheli, F; Di Fabio, R; Donati, D; Terreni, S; Hamprecht, D; Arista, L; Worby, A; Watson, SP The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure. Bioorg Med Chem Lett 20: 2013-6 (2010)
- Zheng, W; Padia, J; Urban, DJ; Jadhav, A; Goker-Alpan, O; Simeonov, A; Goldin, E; Auld, D; LaMarca, ME; Inglese, J; Austin, CP; Sidransky, E Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease. Proc Natl Acad Sci U S A 104: 13192-7 (2007)
- Chang, LL; Ashton, WT; Flanagan, KL; Chen, TB; O'Malley, SS; Zingaro, GJ; Siegl, PK; Kivlighn, SD; Lotti, VJ; Chang, RS Triazolinone biphenylsulfonamides as angiotensin II receptor antagonists with high affinity for both the AT1 and AT2 subtypes. J Med Chem 37: 4464-78 (1995)
- Skolnick, P; Hu, RJ; Cook, CM; Hurt, SD; Trometer, JD; Liu, R; Huang, Q; Cook, JM [3H]RY 80: A high-affinity, selective ligand for gamma-aminobutyric acidA receptors containing alpha-5 subunits. J Pharmacol Exp Ther 283: 488-93 (1997)
- Semple, G; Ren, A; Fioravanti, B; Pereira, G; Calderon, I; Choi, K; Xiong, Y; Shin, YJ; Gharbaoui, T; Sage, CR; Morgan, M; Xing, C; Chu, ZL; Leonard, JN; Grottick, AJ; Al-Shamma, H; Liang, Y; Demarest, KT; Jones, RM Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control. Bioorg Med Chem Lett 21: 3134-41 (2011)
- Chang, CC; Chao, YS; Chen, CT; Chiu, CH; Chu, KF; Hsiao, WC; Hsieh, CJ; Yuan, MC; Hsieh, TC; Huang, CY; Hung, MS; Lee, JC; Liu, YW; Song, JS; Tsai, CH; Wang, MH; Wu, SH; Yao, CH; Yeh, TK Discovery of novel N-ß-D-xylosylindole derivatives as sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the management of hyperglycemia in diabetes. J Med Chem 54: 166-78 (2011)
- PubChem, PC Dose Response orthogonal kinetic assay utilizing the direct detection of NADPH for uHTS small molecule inhibitors of Plasmodium falciparum Glucose-6-phosphate dehydrogenase PubChem Bioassay (2011)
- ChEMBL_486571 (CHEMBL1018340) Inhibition of rat intestinal maltase assessed as glucose release by Glucose B-test
- ChEMBL_486577 (CHEMBL1020971) Inhibition of rat intestinal sucrase assessed as glucose release by Glucose B-test
- ChEMBL_486579 (CHEMBL1020973) Inhibition of rat intestinal isomaltase assessed as glucose release by Glucose B-test
- ChEMBL_501266 (CHEMBL976168) Inhibition of glucose-6-phosphatase
- ChEMBL_1664958 (CHEMBL4014754) Activation of recombinant human glucokinase assessed as conversion of D-glucose to D-glucose-6-phosphate in presence of 2.5 mM glucose by G6PDH coupled spectrophotometric assay
- ChEMBL_1664960 (CHEMBL4014756) Activation of recombinant human glucokinase assessed as conversion of D-glucose to D-glucose-6-phosphate in presence of 10 mM glucose by G6PDH coupled spectrophotometric assay
- ChEMBL_1664995 (CHEMBL4014791) Activation of recombinant human glucokinase assessed as conversion of D-glucose to D-glucose-6-phosphate in presence of 10 mM glucose by G6PDH coupled spectrophotometric assay
- ChEMBL_545872 (CHEMBL1034387) Inhibition of yeast alpha-glucosidase assessed as D-glucose release after 30 mins by Glucose B-test
- ChEMBL_545873 (CHEMBL1034388) Inhibition of rat intestinal maltase assessed as D-glucose release after 30 mins by Glucose B-test
- ChEMBL_545875 (CHEMBL1034390) Inhibition of Caldocellum saccharolyticum beta-glucosidase assessed as D-glucose release after 30 mins by Glucose B-test
- ChEMBL_545874 (CHEMBL1034389) Inhibition of rat liver lysosome alpha-glucosidase assessed as D-glucose release after 30 mins by Glucose B-test
- ChEMBL_565878 (CHEMBL959301) Activation of human glucokinase by glucose-6-phosphate dehydrogenase coupled continuous spectrophotometric assay in presence of 2.5 mM glucose
- ChEMBL_565879 (CHEMBL959302) Activation of human glucokinase by glucose-6-phosphate dehydrogenase coupled continuous spectrophotometric assay in presence of 10 mM glucose
- ChEMBL_1924594 (CHEMBL4427550) Activation of human recombinant glucokinase using 5 mM glucose monitored over 5 mins in presence of NAD+ and glucose 6-phosphate 4% human serum albumin by glucose 6-phosphate dehydrogenase coupled assay
- ChEMBL_447975 (CHEMBL898227) Inhibition of glucose 6 phosphate translocase 1
- ChEMBL_575563 (CHEMBL1036406) Inhibition of rat liver glucose-6-phosphatase
- ChEMBL_1519497 (CHEMBL3625683) Inhibition of rat intestinal Maltase using maltose as substrate assessed as glucose release after 10 mins by glucose oxidase method
- ChEMBL_1519498 (CHEMBL3625684) Inhibition of rat intestinal Sucrase using sucrose as substrate assessed as glucose release after 40 mins by glucose oxidase method
- Inhibition Assay Inhibition assay using glucose-1-phosphate thymidylyltransferase (RmlA).
- ChEMBL_1554316 (CHEMBL3766855) Inhibition of glycogen phosphorylase in human hepatocytes assessed as decrease in glucagon stimulated glucose release after 3 hrs by glucose oxidase method
- ChEMBL_1924392 (CHEMBL4427348) Activation of human recombinant glucokinase using 5 mM glucose as substrate in presence of NAD+ by glucose 6-phosphate dehydrogenase coupled assay
- ChEMBL_602872 (CHEMBL1065927) Activation of human liver glucokinase expressed in CHO cells at 2.5 mM glucose concentration by glucose-6-phosphate coupled continuous spectrophotometric assay
- ChEMBL_602874 (CHEMBL1038417) Activation of human liver glucokinase expressed in CHO cells at 10 mM glucose concentration by glucose-6-phosphate coupled continuous spectrophotometric assay
- ChEMBL_1554315 (CHEMBL3766854) Inhibition of glycogen phosphorylase in Wistar rat hepatocytes assessed as decrease in glucagon stimulated glucose release after 3 hrs by glucose oxidase method
- ChEMBL_1297748 (CHEMBL3131380) Activation of glucokinase (unknown origin) using glucose as substrate
- ChEMBL_304261 (CHEMBL829031) Effective concentration for glucokinase activation with 5 mM glucose
- ChEMBL_304263 (CHEMBL829033) Effective concentration for glucokinase activation with 15 mM glucose
- ChEMBL_424350 (CHEMBL909553) Inhibition of human liver GPa in presence of glucose
- ChEMBL_424351 (CHEMBL909554) Inhibition of human liver GPa in absence of glucose
- ChEMBL_1924593 (CHEMBL4427549) Activation of human recombinant glucokinase using 5 mM glucose monitored over 5 mins in presence of NAD+ by glucose 6-phosphate dehydrogenase coupled assay
- ChEMBL_1924393 (CHEMBL4427349) Activation of human recombinant glucokinase using 5 mM glucose as substrate in presence of NAD+ and 4% HSA by glucose 6-phosphate dehydrogenase coupled assay
- ChEMBL_34553 (CHEMBL646886) Inhibition of yeast alpha-glucosidase after addition of D-glucose
- ChEMBL_491666 (CHEMBL946384) Inhibition of human glycogen phosphorylase alpha in presence of glucose
- ChEMBL_491667 (CHEMBL946385) Inhibition of human glycogen phosphorylase alpha in absence of glucose
- ChEMBL_550868 (CHEMBL1007667) Inhibition of Wistar rat intestinal isomaltase by glucose B-test
- ChEMBL_566717 (CHEMBL961709) Inhibition of human kidney SGLT2 assessed as renal glucose reabsorption
- ChEMBL_2248960 (CHEMBL5163170) Positive allosteric modulator activity at GLP-1R in rat INS1 beta-cells assessed potentiation of GLP-1(7-36)NH2 induced insulin secretion incubated for 30 mins in presence of high glucose condition by ELISA
- High Through-Put Fluorescence Assay A fluorometric high through-put assay for inhibitor towards human liver cathepsin D from Calbiochem.
- ChEMBL_1436697 (CHEMBL3384773) Activation of purified human glucokinase isoform 3 (13 to 466 aa) using 5 mM glucose by spectrophotometry in presence of NAD+ and glucose 6-phosphate dehydrogenase
- ChEMBL_1554117 (CHEMBL3768919) Activation of recombinant human glucokinase assessed as NADPH formation using glucose as substrate incubated for 30 mins in presence of NADP+ and glucose 6-phosphate dehydrogenase
- ChEMBL_1645848 (CHEMBL3994904) Inhibition of sucrase in rat small intestinal mucosa assessed as reduction in glucose production using sucrose as substrate measured after 40 mins by glucose oxidase assay
- ChEMBL_1758345 (CHEMBL4193353) Activation of recombinant human liver glucokinase 2 assessed as assessed as reduction in Km for glucose in presence of 5 mM glucose by G6PDH coupled assay
- ChEMBL_1909269 (CHEMBL4411715) Inhibition of glucose-6-phosphatase in rat H42E cells using glucose-6-phosphate as substrate preincubated overnight followed by substrate addition and measured after 40 mins
- ChEMBL_566832 (CHEMBL957641) Activation of flag-tagged human recombinant liver glucokinase expressed in Escherichia coli by glucose-6-phosphate dehydrogenase coupled continuous spectrophotometric assay in presence of 2.5 mM glucose
- ChEMBL_566834 (CHEMBL957643) Activation of flag-tagged human recombinant liver glucokinase expressed in Escherichia coli by glucose-6-phosphate dehydrogenase coupled continuous spectrophotometric assay in presence of 10 mM glucose
- ChEMBL_576767 (CHEMBL1032034) Activation of flag-tagged human recombinant liver glucokinase expressed in Escherichia coli by glucose-6-phosphate dehydrogenase coupled continuous spectrophotometric assay in presence of 2.5 mM glucose
- ChEMBL_576768 (CHEMBL1032035) Activation of flag-tagged human recombinant liver glucokinase expressed in Escherichia coli by glucose-6-phosphate dehydrogenase coupled continuous spectrophotometric assay in presence of 10 mM glucose
- ChEMBL_2152934 (CHEMBL5037481) Inhibition of CDK9 (unknown origin) in high presence of high ATP incubated for 25 min by TR-FRET assay
- ChEMBL_557775 (CHEMBL953284) Inhibition of human liver glycogen phosphorylase a in absence of glucose
- ChEMBL_557776 (CHEMBL953285) Inhibition of human liver glycogen phosphorylase a in presence of glucose
- ChEMBL_701783 (CHEMBL1656920) Inhibition of sucrase in mouse intestinal input by glucose release assay
- ChEMBL_701784 (CHEMBL1656921) Inhibition of lactase in mouse intestinal input by glucose release assay
- ChEMBL_701785 (CHEMBL1656922) Inhibition of maltase in mouse intestinal input by glucose release assay
- ChEMBL_750244 (CHEMBL1788085) Activation of human recombinant glucokinase using 6.5 mM glucose by spectrophotometry
- ChEMBL_873671 (CHEMBL2188787) Agonist activity at rat P2Y1R assessed as glucose-dependent insulin secretion
- ChEMBL_935336 (CHEMBL2318453) Induction of human hepatic glucokinase activity at 5 mM glucose concentration
- ChEMBL_935338 (CHEMBL2318649) Induction of human pancreatic glucokinase activity at 5 mM glucose concentration
- Biological Assays The SGLT2 functional assay was designed to detect the inhibition of methyl-alpha-D glucopyranoside (AMG a non-metabolizable form of glucose) uptake via the SGLT2 transporter. The SGLT2 transporter recovers glucose from the proximal tubules of the kidney; its inhibition results in sugar wasted in the urine. The positive control compound, Phlorizin, is a known inhibitor of glucose uptake for SGLT2 and was used for comparing the high percent effect of SGLT2 inhibition of the test compounds.
- ChEBML_274 Inhibition constant of high-affinity 5-HT uptake
- ChEMBL_217034 (CHEMBL821568) Inhibition constant of high-affinity choline uptake
- ChEMBL_621738 (CHEMBL1108470) Inhibition of JNK1 by high throughput screening
- ChEMBL_621739 (CHEMBL1108471) Inhibition of JNK3 by high throughput screening
- ChEMBL_621740 (CHEMBL1108472) Inhibition of p38alpha by high throughput screening
- ChEMBL_62802 (CHEMBL674115) Inhibition constant of high-affinity dopamine uptake
- ChEMBL_798646 (CHEMBL1942635) Inhibition of BRAF by high-throughput assay
- ChEMBL_979855 (CHEMBL2422398) Inhibition of Fas-mediated cell death in oxygen and glucose deprived rat H9c2 cells treated 30 mins before oxygen and glucose deprivation measured after 6 hrs by DAPI staining
- High-Throughput Assay Please see Hutti, et al., (2012). Development of a High-Throughput Assay for Identifying Inhibitors of TBK1 and IKKε.
- ChEMBL_1339208 (CHEMBL3243402) Activation of recombinant human pancreatic glucokinase using 10 mM glucose by spectrophotometry
- ChEMBL_2284250 Inhibition of FBPase in rat Primary hepatocyte assessed as reduction in glucose production
- ChEMBL_338364 (CHEMBL866544) Inhibition of D-glucose uptake mediated by PfHT expressed in Xenopus oocytes
- ChEMBL_745322 (CHEMBL1775397) Activation of FFA1 in mouse islets assessed as glucose-dependent insulin secretion
- ChEMBL_858378 (CHEMBL2168593) Activation of human recombinant glucokinase using 6.5 mM glucose by spectrophotometric analysis
- ChEMBL_974049 (CHEMBL2410527) Activation of human recombinant glucokinase by matrix assay in presence of glucose
- ChEMBL_1878663 (CHEMBL4380057) Inhibition of human recombinant CYP1B1 using 7-ethoxyresorufin as substrate in presence of glucose-6-phosphate, glucose-6-phosphate dehydrogenase and NADPH-generating system incubated for 35 mins by fluorometry
- ChEMBL_1878664 (CHEMBL4380058) Inhibition of human recombinant CYP1A1 using 7-ethoxyresorufin as substrate in presence of glucose-6-phosphate, glucose-6-phosphate dehydrogenase and NADPH-generating system incubated for 15 mins by fluorometry
- ChEMBL_1878665 (CHEMBL4380059) Inhibition of human recombinant CYP1A2 using 7-ethoxyresorufin as substrate in presence of glucose-6-phosphate, glucose-6-phosphate dehydrogenase and NADPH-generating system incubated for 50 mins by fluorometry
- ChEBML_210738 Inhibition of NGF high affinity receptor tyrosine kinase TrkA
- ChEMBL_274 (CHEMBL615714) Inhibition constant of high-affinity 5-HT uptake
- ChEMBL_553586 (CHEMBL958769) Inhibition of aromatase by fluorimetric high throughput method
- ChEMBL_766202 (CHEMBL1826222) Inhibition of human TCPTP by high-throughput screening
- ChEMBL_766203 (CHEMBL1826223) Inhibition of human SHP1 by high-throughput screening
- ChEMBL_766204 (CHEMBL1826224) Inhibition of human SHP2 by high-throughput screening
- ChEMBL_839821 (CHEMBL2089922) Inhibition of CYP1A2 by high-throughput fluorescence assay
- ChEMBL_839822 (CHEMBL2089923) Inhibition of CYP2C9 by high-throughput fluorescence assay
- ChEMBL_839823 (CHEMBL2089924) Inhibition of CYP2C19 by high-throughput fluorescence assay
- ChEMBL_839824 (CHEMBL2089925) Inhibition of CYP2D6 by high-throughput fluorescence assay
- ChEMBL_839825 (CHEMBL2089926) Inhibition of CYP3A4 by high-throughput fluorescence assay
- ChEMBL_850936 (CHEMBL2157031) Binding affinity to TRKA by high throughput assay
- ChEMBL_850938 (CHEMBL2157033) Binding affinity to PI3Kalpha by high throughput assay
- ChEMBL_851044 (CHEMBL2157424) Inhibition of KIT by high throughput binding assay
- ChEMBL_861570 (CHEMBL2174511) Inhibition of SIRT1 by high throughput screening assay
- ChEMBL_873555 (CHEMBL2187472) Agonist activity at alpha4beta2 nAChR high sensitivity form
- ChEMBL_1436698 (CHEMBL3384774) Activation of purified human glucokinase isoform 3 (13 to 466 aa) using 5 mM glucose by spectrophotometry in presence of NAD+ and glucose 6-phosphate dehydrogenase in presence of 4% HSA
- ChEMBL_588966 (CHEMBL1056161) Activation of N-terminal His-tagged human recombinant liver glucokinase expressed in Escherichia coli BL21 (DE3) by glucose-6-phosphate dehydrogenase coupled continuous spectrophotometric assay in presence of 2.5 mM glucose
- ChEMBL_588968 (CHEMBL1056163) Activation of N-terminal His-tagged human recombinant liver glucokinase expressed in Escherichia coli BL21 (DE3) by glucose-6-phosphate dehydrogenase coupled continuous spectrophotometric assay in presence of 10 mM glucose
- ChEBML_71573 Inhibition of [125I]7-IHPP-Fsk binding to glucose transporter of human erythrocyte membrane
- ChEMBL_1518286 (CHEMBL3620261) Antagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assay
- ChEMBL_202730 (CHEMBL809058) Binding affinity against Sodium/glucose co-transporter of isolated renal brush border membranes.
- ChEMBL_438958 (CHEMBL889301) Inhibition of cPEPCK in rat H4IIE cells assessed as effect on glucose production
- ChEMBL_456667 (CHEMBL924048) Inhibition of [3H]glucose uptake at mammalian GLUT1 expressed in Xenopus laevis oocytes
- ChEMBL_744250 (CHEMBL1772057) Inhibition of rat small intestinal maltase after 30 mins by glucose-oxidase method
- ChEMBL_744251 (CHEMBL1772058) Inhibition of rat small intestinal sucrase after 30 mins by glucose-oxidase method
- ChEMBL_744252 (CHEMBL1772059) Inhibition of rat small intestinal isomaltase after 30 mins by glucose-oxidase method
- ChEMBL_857274 (CHEMBL2160769) Inhibition of rat small intestinal isomaltase after 30 mins by glucose-oxidase method
- ChEMBL_857275 (CHEMBL2160770) Inhibition of rat small intestinal sucrase after 30 mins by glucose-oxidase method
- ChEMBL_857276 (CHEMBL2160771) Inhibition of rat small intestinal maltase after 30 mins by glucose-oxidase method
- ChEMBL_1767894 (CHEMBL4220006) Agonist activity at B6D2F1 mouse insulin receptor assessed as increase in glucose incorporation into lipid phase after 2 hrs in presence of D-[3-3H]glucose by TopCount microplate scintillation counting method
- ChEMBL_1850639 (CHEMBL4351263) Inhibition of human ERG by high-throughput electrophysiology assay
- ChEMBL_2068301 (CHEMBL4723554) Binding affinity to dopamine D2 (high) receptor (unknown origin)
- ChEMBL_2452046 Inhibition of MNK1 (unknown origin) by high-throughput screening assay
- ChEMBL_2452047 Inhibition of MNK2 (unknown origin) by high-throughput screening assay
- ChEMBL_2500630 Inhibition of PDE9A (unknown origin) by high-throughput screening analysis
- ChEMBL_457249 (CHEMBL941735) Binding to high affinity site of human serum albumin
- ChEMBL_52871 (CHEMBL666230) Inhibitory activity against dihydrofolate reductase in mammalians. (high potency)
- ChEMBL_675462 (CHEMBL1273599) Displacement of high affinity TRAP form human platelet PAR1
- ChEMBL_741955 (CHEMBL1768607) Binding affinity to CDK11 by high-throughput binding assay
- ChEMBL_741959 (CHEMBL1768719) Binding affinity to mTOR by high-throughput binding assay
- ChEMBL_741962 (CHEMBL1768722) Binding affinity to PIK3CA by high-throughput binding assay
- ChEMBL_741964 (CHEMBL1768724) Binding affinity to PIK3CB by high-throughput binding assay
- ChEMBL_831960 (CHEMBL2065218) Inhibition of PI3Kgamma by high throughput chemoproteomics binding assay
- ChEMBL_831961 (CHEMBL2065219) Inhibition of PI3Kdelta by high throughput chemoproteomics binding assay
- ChEMBL_831962 (CHEMBL2065220) Inhibition of PI3Kalpha by high throughput chemoproteomics binding assay
- ChEMBL_831963 (CHEMBL2065221) Inhibition of PI3Kbeta by high throughput chemoproteomics binding assay
- High Throughput Screening (HTS) by Fluorescence Polarization (pH = 5.0) pH = 5.0.
- High Throughput Screening (HTS) by Fluorescence Polarization (pH = 5.9) pH = 5.9.
- High Throughput Screening (HTS) by Fluorescence Polarization (pH = 7.0) pH = 7.0.
- ChEMBL_1279808 (CHEMBL3095509) Activation of glucokinase in rat INS-1 cells assessed as glucose-stimulated insulin secretion
- ChEMBL_1554435 (CHEMBL3767566) Competitive inhibition of rabbit muscle glycogen phosphorylase b in presence of glucose 1-phosphate
- ChEMBL_456666 (CHEMBL924047) Inhibition of [3H]glucose uptake at Plasmodium falciparum HT expressed in Xenopus laevis oocytes
- ChEMBL_542431 (CHEMBL1011499) Inhibition of human G6PDH using glucose-6-phosphate as substrate by Lineweaver-Burke plot
- ChEMBL_626547 (CHEMBL1108920) Inhibition of human SGLT2 expressed in CHOK1 cells assessed as inhibition of glucose uptake
- ChEMBL_626548 (CHEMBL1108921) Inhibition of human SGLT1 expressed in CHOK1 cells assessed as inhibition of glucose uptake
- ChEMBL_775861 (CHEMBL1912402) Inhibition of GCS assessed as amount of UDP-glucose consumed during enzyme-catalyzed reaction
- ChEMBL_862643 (CHEMBL2174116) Inhibition of human glucose-6-phosphate dehydrogenase after 90 mins by resazurin/diaphorasecoupled assay
- ChEMBL_862644 (CHEMBL2174117) Inhibition of Plasmodium falciparum glucose-6-phosphate dehydrogenase after 45 mins by orthogonal assay
- ChEMBL_62884 (CHEMBL673594) In vitro binding affinity to rat striatal Dopamine receptor D2 was determined using the agonist [3H]quinpirole to label the high affinity state (D2 high)
- High Throughput Screening (HTS) Assa A high throughput screening (HTS) assay and together with NCATS screened over 350,000 compounds in attempt to identify novel GLS inhibitor structures.
- ChEMBL_1619019 (CHEMBL3861188) Inhibition of human recombinant liver glycogen phosphorylase A expressed in baculovirus infected Sf9 insect cells assessed as release of phosphate from glucose-1- phosphate in presence of 7.5 mM glucose by malachite green based assay
- ChEMBL_1282959 (CHEMBL3100278) Inhibition of AKT1 (unknown origin) by high-throughput screen assay
- ChEMBL_1434164 (CHEMBL3383972) Inhibition of CYP1A2 (unknown origin) by high throughput fluorescence assay
- ChEMBL_1434165 (CHEMBL3383973) Inhibition of CYP2C9 (unknown origin) by high throughput fluorescence assay
- ChEMBL_1434166 (CHEMBL3383974) Inhibition of CYP2C19 (unknown origin) by high throughput fluorescence assay
- ChEMBL_1434167 (CHEMBL3383975) Inhibition of CYP2D6 (unknown origin) by high throughput fluorescence assay
- ChEMBL_1434168 (CHEMBL3383976) Inhibition of CYP3A4 (unknown origin) by high throughput fluorescence assay
- ChEMBL_1980150 (CHEMBL4613412) Inhibition of CDK1 (unknown origin) in presence of high ATP
- ChEMBL_1980151 (CHEMBL4613413) Inhibition of CDK7 (unknown origin) in presence of high ATP
- ChEMBL_1980152 (CHEMBL4613414) Inhibition of CDK2 (unknown origin) in presence of high ATP
- ChEMBL_1980153 (CHEMBL4613415) Inhibition of CDK9 (unknown origin) in presence of high ATP
- ChEMBL_1990087 (CHEMBL4623822) Inhibition of human ERG by Ionworks high-throughput electrophysiology method
- ChEMBL_2196802 (CHEMBL5109318) Inhibition of CDK12 (unknown origin) in presence of high ATP
- ChEMBL_2196806 (CHEMBL5109322) Inhibition of CDK9 (unknown origin) in presence of high ATP
- ChEMBL_2196807 (CHEMBL5109323) Inhibition of CDK7 (unknown origin) in presence of high ATP
- ChEMBL_2196808 (CHEMBL5109324) Inhibition of CDK2 (unknown origin) in presence of high ATP
- ChEMBL_2196809 (CHEMBL5109325) Inhibition of CDK1 (unknown origin) in presence of high ATP
- ChEMBL_2472607 Inhibition of HDAC8 (unknown origin) by SAMDI high throughput mass spectrometry
- ChEMBL_469820 (CHEMBL933387) Inhibition of full length iNOS by high-throughput oxymyoglobin assay
- ChEMBL_52982 (CHEMBL664189) Inhibitory activity against dihydrofolate reductase in Pneumocystis carinii. (high potency)
- ChEMBL_595792 (CHEMBL1048799) Inhibition of Trypanosoma cruzi cruzain by quantitative high throughput screening
- ChEMBL_61476 (CHEMBL672527) Binding affinity on High Affinity Site of Dopamine receptor D2L
- ChEMBL_61805 (CHEMBL670558) Binding Affinity on High Affinity Site of Dopamine receptor D2S
- ChEMBL_1619017 (CHEMBL3861186) Inhibition of rabbit muscle glycogen phosphorylase b using alpha-D-glucose-1-phosphate as substrate
- ChEMBL_206287 (CHEMBL808824) Inhibition of Sucrase in rat intestinal brush border membranes by D-glucose oxidase-peroxidase method
- ChEMBL_306715 (CHEMBL832300) Inhibitory concentration against human glutathione reductase in the absence of glucose-6-phosphate dehydrogenase (G6PDH)
- ChEMBL_479543 (CHEMBL931539) Agonist activity at glucocorticoid receptor assessed as glucose response element transcriptional transactivation by luciferase assay
- ChEMBL_498540 (CHEMBL973516) Inhibition of GluT1-mediated [14C]D-glucose uptake in Wistar rat brain by perfusion technique
- ChEMBL_527710 (CHEMBL975068) Inhibition of topoisomerase 1 in Saccharomyces cerevisiae RS321N in glucose medium by microtiter plate assay
- ChEMBL_542429 (CHEMBL1010666) Inhibition of Trypanosoma brucei G6PDH using glucose-6-phosphate as substrate by Lineweaver-Burke plot
- ChEMBL_556521 (CHEMBL956516) Inhibition of rabbit muscle glycogen phosphorylase assessed as release of phosphate from glucose 1 phosphate
- ChEMBL_800636 (CHEMBL1947668) Activation of SUR1 in rat pancreatic islets assessed as inhibition of glucose-induced insulin secretion
- ChEMBL_859947 (CHEMBL2167350) Inhibition of GCS assessed as amount of UDP glucose after 3 hrs by Fluorometry analysis
- ChEMBL_862647 (CHEMBL2174120) Inhibition of Plasmodium falciparum glucose-6-phosphate dehydrogenase after 2 hrs by resazurin/diaphorasecoupled assay
- ChEMBL_959585 (CHEMBL2382530) Agonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretion
- ChEMBL_2027541 (CHEMBL4681699) Inhibition of active recombinant human N-terminal His-tagged 11-betaHSD1 expressed in Escherichia coli using cortisone, NADPH and glucose-6-phosphate incubated for 2 hrs by glucose-6-phosphate dehydrogenase based coupled HTRF immuno-competitive assay
- Metabolic Measurements Glucose in tail blood was measured using a glucometer (One-Touch Basic; Lifescan, CA). For glucose tolerance tests (GTTs), mice were fasted for 10 hours and then injected with 20% D-glucose (2 mg/g body weight) and the blood glucose was monitored immediately before and at 15, 30, 60 and 120 mins following the injection. For insulin tolerance tests (ITTs), 4-h fasted animals were given insulin (0.75 mU/g) and blood glucose was measured immediately before and at 30, 60 and 120 minutes postinjection. Serum insulin, cholesterol, triglycerides (Stanbio Labs, TX), BDNF (Abnova), IGF1 and IGFBPs (R&D Systems) were determined by enzyme-linked immunosorbent assay.
- ChEBML_217497 Inhibition of human lung high-affinity cGMP phosphodiesterases (0.5-2 uM/L)
- ChEMBL_1290535 (CHEMBL3119984) Binding affinity to high-affinity state of D2L receptor (unknown origin)
- ChEMBL_1362781 (CHEMBL3295224) Inhibition of human recombinant PDE4B at high-affinity rolipram binding site
- ChEMBL_166352 (CHEMBL775439) Inhibition of high affinity dopamine uptake at concentration of 1 uM
- ChEMBL_1765499 (CHEMBL4200746) Displacement of [3H]dofetilide from human ERG by high throughput assay
- ChEMBL_1904571 (CHEMBL4406929) Inhibition of human ERG by high throughput automated patch clamp method
- ChEMBL_216905 (CHEMBL821923) Inhibition of high affinity choline uptake at concentration of 1 uM
- ChEMBL_217811 (CHEMBL821718) Inhibition of high affinity radioligand binding to human alphaV-beta3 integrin
- ChEMBL_2273330 Inhibition of DC-SIGN (unknown origin) by high-throughput ELLA-type assay
- ChEMBL_32655 (CHEMBL642823) Inhibition of high affinity radioligand binding to human alphaV-beta3 integrin
- ChEMBL_753217 (CHEMBL1799372) Inhibition of Mycobacterium tuberculosis pantothenate synthetase by high throughput screening method
- ChEMBL_766205 (CHEMBL1826326) Inhibition of human LAR catalytic domain 1 by high-throughput screening
- High-Throughput Circadian Assay Per2 Assay for Evaluating the Potency of Test Compounds.
- ChEBML_71686 Compound was evaluated for inhibition of Glucose-6-Phosphatase from Triton X-100 disrupted pig liver microsomes.
- ChEMBL_101863 (CHEMBL710106) Inhibition of Glycosidases (maltase) in rat intestinal brush border membranes by D-glucose oxidase-peroxidase method
- ChEMBL_1495696 (CHEMBL3578684) Activation of recombinant human pancreatic glucokinase using 10 mM glucose as substrate by G6PDH coupled assay
- ChEMBL_1546979 (CHEMBL3748082) Binding affinity to Salmonella typhi glucose-1-phosphate cytidylyl-transferase assessed as dissociation constant by spectrophotometry
- ChEMBL_208284 (CHEMBL813582) Inhibition of Glycosidases (trehalase)in rat intestinal brush border membranes by D-glucose oxidase-peroxidase method
- ChEMBL_515050 (CHEMBL1034792) Inhibition of human liver glycogen phosphorylase A by fluorescence intensity endpoint assay in presence of glucose
- ChEMBL_515051 (CHEMBL1034793) Inhibition of human liver glycogen phosphorylase A by fluorescence intensity endpoint assay in absence of glucose
- ChEMBL_599699 (CHEMBL1045565) Inhibition of GLUT2-mediated [14C]D-glucose uptake in human MCF7 cells by liquid scintillation counting
- ChEMBL_748047 (CHEMBL1781588) Activation of His-tagged recombinant glucokinase expressed in Escherichia coli using [14C]-glucose substrate by spectrophotometrically
- ChEMBL_759809 (CHEMBL1809870) Antiglycation activity in bovine serum albumin assessed as inhibition of fructosamines formation in presence of glucose
- ChEMBL_858381 (CHEMBL2168596) Activation of glucokinase in rat INS-1 cells assessed as stimulation of glucose-induced insulin secretion
- ChEMBL_88829 (CHEMBL698884) Inhibition of Glycosidases (isomaltase)in rat intestinal brush border membranes by D-glucose oxidase-peroxidase method
- ChEMBL_96426 (CHEMBL706374) Inhibition of Glycosidases (lactase)in rat intestinal brush border membranes by D-glucose oxidase-peroxidase method
- ChEMBL_984799 (CHEMBL2432301) Allosteric activation of human glucokinase using glucose as substrate measured every 10 secs for 5 mins
- ChEMBL_1279734 (CHEMBL3095124) Inhibition of GLUT1 in human H1299 cells assessed as inhibition of 2-deoxy-D-[3H]-glucose uptake incubated for 15 mins prior to 2-deoxy-D-[3H]-glucose addition measured after 30 mins by liquid scintillation counting analysis
- ChEMBL_1828995 (CHEMBL4328869) Inhibition of C-terminal 6-His tagged recombinant Clostridium difficile toxin B glucosyltransferase domain assessed as reduction in UDP-glucose hydrolysis activity using UDP-glucose substrate and ADP Alexa633 tracer incubated for 3 hrs by fluorescence polarization assay
- ChEBML_62329 Inhibition of high affinity uptake of [3H]dopamine into striatal nerve endings (synaptosomes)
- ChEMBL_1440951 (CHEMBL3375801) Inhibition of wild-type EGFR (unknown origin) by high-throughput biochemical screening
- ChEMBL_1440975 (CHEMBL3375825) Inhibition of EGFR L858R mutant (unknown origin) by high-throughput biochemical screening
- ChEMBL_273 (CHEMBL615713) Inhibition of high affinity 5-HT uptake at concentration of 1 uM
- ChEMBL_61479 (CHEMBL672381) Binding Affinity was tested on High Affinity Site of Dopamine receptor D2L
- ChEMBL_61807 (CHEMBL672954) Binding Affinity was tested on High Affinity Site of Dopamine receptor D2S
- ChEMBL_62971 (CHEMBL677461) Inhibition of high affinity DA uptake into rat synaptosomes using [3H]DA
- ChEMBL_61464 (CHEMBL671445) Affinity of compound for D2 receptor in rat striatal membrane determined for agonist state (high affinity state, D2 High) [3H]quinpirole as radioligand (in the absence of GTP and sodium)
- ChEMBL_101864 (CHEMBL710107) Inhibition of Glycosidases (maltase) in rat intestinal brush border membranes by D-glucose oxidase-peroxidase method maltase
- ChEMBL_1554222 (CHEMBL3766261) Inhibition of rat intestinal sucrase using sucrose as substrate incubated for 30 mins by glucose-oxidase method
- ChEMBL_31929 (CHEMBL642972) Compound was tested for the inhibition of the rat lens aldose reductase using the substrate as glucose.
- ChEMBL_477692 (CHEMBL931372) Inhibition of Trypanosoma cruzi hexokinase in presence of ATP, 2 mM D-glucose and 3 mM MgCl2
- ChEMBL_477693 (CHEMBL931373) Inhibition of Trypanosoma cruzi hexokinase in presence of D-glucose, 1 mM ATP and 3 mM MgCl2
- ChEMBL_664635 (CHEMBL1260349) Inhibition of human recombinant N-terminal domain of maltase-glucoamylase after 60 mins by glucose oxidase assay
- ChEMBL_684093 (CHEMBL1286470) Inhibition of human recombinant N-terminal subunit of maltase-glucoamylase after 60 mins by glucose oxidase assay
- ChEMBL_71572 (CHEMBL684233) Binding activity against Glucose transporter in human erythrocyte membrane using [125I]7-IHPP-Fsk as the radioligand.
- ChEMBL_885380 (CHEMBL2215682) Activation of recombinant rat glucokinase assessed measuring rate of glucose 6-phosphate formation using G6PDH/NADP coupling
- ChEMBL_885387 (CHEMBL2216128) Activation of recombinant human glucokinase assessed measuring rate of glucose 6-phosphate formation using G6PDH/NADP coupling
- ChEMBL_1717901 (CHEMBL4132901) Antagonist activity at human GLUT1 expressed in HEK293 cells transfected with GLUT1 shRNA assessed as inhibition of [3H]2-deoxy-D-glucose uptake preincubated for 5 mins followed by [3H]2-deoxy-D-glucose addition and measured after 6 mins
- ChEMBL_1717902 (CHEMBL4132902) Antagonist activity at human GLUT3 expressed in HEK293 cells transfected with GLUT1 shRNA assessed as inhibition of [3H]2-deoxy-D-glucose uptake preincubated for 5 mins followed by [3H]2-deoxy-D-glucose addition and measured after 6 mins
- ChEMBL_1717903 (CHEMBL4132903) Antagonist activity at human GLUT4 expressed in HEK293 cells transfected with GLUT1 shRNA assessed as inhibition of [3H]2-deoxy-D-glucose uptake preincubated for 5 mins followed by [3H]2-deoxy-D-glucose addition and measured after 6 mins
- ChEMBL_1717904 (CHEMBL4132904) Antagonist activity at human GLUT8 expressed in HEK293 cells transfected with GLUT1 shRNA assessed as inhibition of [3H]2-deoxy-D-glucose uptake preincubated for 5 mins followed by [3H]2-deoxy-D-glucose addition and measured after 6 mins
- ChEMBL_1453753 (CHEMBL3364468) Inhibition of Wistar rat intestinal maltase assessed as inhibition of D-glucose release after 30 mins by spectrophotometry
- ChEMBL_1454615 (CHEMBL3366727) Inhibition of Wistar rat intestinal isomaltase assessed as inhibition of D-glucose release after 30 mins by spectrophotometry
- ChEMBL_1454616 (CHEMBL3366728) Inhibition of Wistar rat intestinal sucrase assessed as inhibition of D-glucose release after 30 mins by spectrophotometry
- ChEMBL_1583831 (CHEMBL3815263) Inhibition of rat small intestinal sucrase using sucrose as substrate incubated for 30 mins by glucose-oxidase method
- ChEMBL_1583832 (CHEMBL3815264) Inhibition of rat small intestinal isomaltase using isomaltose as substrate incubated for 30 mins by glucose-oxidase method
- ChEMBL_1630545 (CHEMBL3873251) Competitive inhibition of rabbit muscle glycogen phosphorylase-b in presence of varying glucose-1-phosphate levels and NADP
- ChEMBL_208279 (CHEMBL813414) Inhibitory activity measured against trehalase of porcine kidney by colorimetric assay using the D-glucose oxidase-peroxidase method
- ChEMBL_216816 (CHEMBL816395) Inhibitory activity measured against alpha-glucosidase of rice by colorimetric assay using the D-glucose oxidase-peroxidase method
- ChEMBL_2222060 (CHEMBL5135394) Inhibition of rat intestinal maltase assessed as release of D-glucose using maltose as substrate by colorimetric analysis
- ChEMBL_34390 (CHEMBL649260) Inhibitory activity measured against alpha-glucosidase of rice by colorimetric assay using the D-glucose oxidase-peroxidase method
- ChEMBL_477720 (CHEMBL931369) Inhibition of glycosomal Trypanosoma cruzi hexokinase in presence of ATP, 2 mM D-glucose and 3 mM MgCl2
- ChEMBL_477721 (CHEMBL927019) Inhibition of glycosomal Trypanosoma cruzi hexokinase in presence of D-glucose, 1 mM ATP and 3 mM MgCl2
- ChEMBL_599700 (CHEMBL1045566) Inhibition of GLUT2-mediated [14C]D-glucose uptake in human MDA-MB-231 cells by liquid scintillation counting
- ChEMBL_620083 (CHEMBL1108551) Inhibition of rabbit muscle glycogen phosphorylase assessed as release of phosphate from glucose-1-phosphate after 25 mins
- ChEMBL_639182 (CHEMBL1168035) Inhibition of rice alpha-glucosidase assessed as D-glucose release at pH 5 after 10 to 30 mins
- In Vitro Inhibition Assay In vitro inhibition assay using human nampt, NMN adenylytransferase (nmant1)and UDP-glucose dehdryogenase (ugdh) genes.
- ChEMBL_1670145 (CHEMBL4020033) Competitive inhibition of human liver glycogen phosphorylase-a assessed as release of inorganic phosphate using varying levels of glucose-1-phosphate and constant concentration of AMP and glycogen preincubated for 15 mins with AMP and glycogen followed by glucose-1-phosphate addition
- ChEMBL_1670148 (CHEMBL4020036) Competitive inhibition of rabbit muscle glycogen phosphorylase-b in presence of varying levels of glucose-1-phosphate and constant concentration of glycogen and AMP preincubated for 15 mins with AMP and glycogen followed by glucose-1-phosphate addition by Lineweaver-Burk plot method
- ChEMBL_1670149 (CHEMBL4020037) Competitive inhibition of rabbit muscle glycogen phosphorylase-a in presence of varying levels of glucose-1-phosphate and constant concentration of glycogen and AMP preincubated for 15 mins with AMP and glycogen followed by glucose-1-phosphate addition by Lineweaver-Burk plot method
- ChEMBL_1752667 (CHEMBL4187427) Inhibition of C-terminal 6-His tagged recombinant Clostridium difficile toxin B catalytic fragment (Met1 to Leu543 residues) assessed as reduction in glucosyltransferase domain UDP-glucose hydrolysis activity using UDP-glucose and ADP Alexa633 tracer incubated fore 3 hrs by fluorescence polarization assay
- ChEMBL_1440949 (CHEMBL3375799) Inhibition of EGFR T790M/L858R mutant (unknown origin) by high-throughput biochemical screening
- ChEMBL_177939 (CHEMBL785010) Inhibition of high affinity neuronal GABA uptake by synaptosomes of rat brain membrane
- ChEMBL_201804 (CHEMBL872698) Inhibition of high affinity serotonin uptake into rat synaptosomes using [3H]5-HT
- ChEMBL_2046360 (CHEMBL4701059) Antagonist activity at adenosine 2A receptor (unknown origin) in presence of high adenosine
- ChEMBL_2339761 Induction of ERalpha Y537N mutant degradation in human MCF cells high content imaging assay
- ChEMBL_2380159 Inhibition of HEPTP (unknown origin) using pNPP as substrate by high-throughput screening assay
- ChEMBL_2480698 Inhibition of Staphylococcus aureus pyruvate carboxylase by FVB based high-throughput fixed time assay
- ChEMBL_499368 (CHEMBL1015820) Inhibition of delta-(5)-desaturase in mouse ABMC7 cells by high throughput radioassay
- ChEMBL_499369 (CHEMBL1015821) Inhibition of delta-(6)-desaturase in mouse ABMC7 cells by high throughput radioassay
- ChEMBL_555399 (CHEMBL964796) Binding affinity to L-FABP high binding affinity site by titration calorimetry method
- ChEMBL_574490 (CHEMBL1030329) Inhibition of HIV1 recombinant integrase by electrochemiluminescent-based high-throughput strand transfer assay
- ChEMBL_575565 (CHEMBL1036408) Inhibition of human recombinant DNMT1 expressed in baculovirus infected high five insect cells
- ChEMBL_575566 (CHEMBL1036409) Inhibition of human recombinant DNMT3b2 expressed in baculovirus infected high five insect cells
- ChEMBL_61175 (CHEMBL670990) Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
- ChEMBL_62118 (CHEMBL879553) Binding Affinity was tested on the high affinity site of Dopamine receptor D3
- ChEMBL_62329 (CHEMBL674268) Inhibition of high affinity uptake of [3H]dopamine into striatal nerve endings (synaptosomes)
- ChEMBL_718440 (CHEMBL1680104) Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
- ChEMBL_988770 (CHEMBL2439143) Inhibition of wild type human FLT3 by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_988771 (CHEMBL2439144) Inhibition of wild type human IKKa by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_988772 (CHEMBL2439145) Inhibition of wild type human IKKb by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_988775 (CHEMBL2439148) Inhibition of wild type human ABL1 by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_988776 (CHEMBL2439149) Inhibition of wild type human ZAP70 by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_988777 (CHEMBL2439150) Inhibition of wild type human TRKB by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_988778 (CHEMBL2439151) Inhibition of wild type human TRKA by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_988899 (CHEMBL2439753) Inhibition of wild type human SYK by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_988900 (CHEMBL2439754) Inhibition of wild type human SGK1 by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_988902 (CHEMBL2439756) Inhibition of wild type human ROCK2 by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_988903 (CHEMBL2439757) Inhibition of wild type human ROCK1 by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_988905 (CHEMBL2439759) Inhibition of wild type human MEKK2 by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_988907 (CHEMBL2439761) Inhibition of wild type human IGF1R by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_988908 (CHEMBL2439762) Inhibition of wild type human IR by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_988911 (CHEMBL2439765) Inhibition of wild type human ERK2 by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_988913 (CHEMBL2439767) Inhibition of wild type human CDK1 by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_1554437 (CHEMBL3767568) Competitive inhibition of rabbit muscle glycogen phosphorylase b by Lineweaver-Burk plot analysis in presence of glucose 1-phosphate
- ChEMBL_1558648 (CHEMBL3771525) Inhibition of rabbit muscle glycogen phosphorylase-a assessed as formation of inorganic phosphate from glucose-1-phosphate by colorimetry
- ChEMBL_1583833 (CHEMBL3815265) Inhibition of human small intestine microsomal maltase using maltose as substrate incubated for 30 mins by glucose-oxidase method
- ChEMBL_2270628 Inhibition of PFKFB3 in human HCT-116 cells assessed as inhibition of glucose induced lactate production by absorbance based analysis
- ChEMBL_2476702 Inhibition of rat intestinal alpha-glucosidase using p-nitrophenyl glycoside as substrate assessed as D-glucose release by colorimetric analysis
- ChEMBL_479545 (CHEMBL931541) Antagonist activity at glucocorticoid receptor assessed as inhibition of dexamethasone-induced glucose response element transcriptional transactivation by luciferase assay
- ChEMBL_499902 (CHEMBL978960) Inhibition of 1,3-beta-D-glucan synthase EMFR-S678P mutant from Aspergillus fumigatus assessed as incorporation of [3H]glucose
- ChEMBL_595113 (CHEMBL1050600) Inhibition of rabbit muscle glycogen phosphorylase A assessed as release of phosphate from glucose-1-phosphate after 25 mins
- ChEMBL_70513 (CHEMBL679754) Inhibitory activity measured against alpha-galactosidase of coffee bean by colorimetric assay using the D-glucose oxidase-peroxidase method
- ChEMBL_762684 (CHEMBL1817502) Inhibition of rabbit muscle glycogen phosphorylase 1a assessed as release of phosphate from glucose-1- phosphate after 20 mins
- ChEMBL_762685 (CHEMBL1817503) Inhibition of human liver glycogen phosphorylase 1a assessed as release of phosphate from glucose-1- phosphate after 20 mins
- ChEMBL_1290539 (CHEMBL3119988) Displacement of [3H]-iodosulpiride from recombinant high-affinity state of human dopamine D2L receptor
- ChEMBL_1440976 (CHEMBL3375826) Inhibition of EGFR del746 to 750 mutant (unknown origin) by high-throughput biochemical screening
- ChEMBL_1456348 (CHEMBL3368357) Inhibition of human CYP2D6 after 20 to 50 mins by high-throughput fluorescence assay
- ChEMBL_192993 (CHEMBL803575) Displacement of [3H]rolipram from high affinity binding site (HARBS) in rat brain membrane.
- ChEMBL_2273485 Inhibition of recombinant STAT3 (unknown origin) incubated for 30 mins by high-throughput fluorescence microscopy
- ChEMBL_2339760 Induction of wild type ERalpha degradation in human MCF cells by high content imaging assay
- ChEMBL_2452098 Inhibition of eIF4E/eIF4G (unknown origin) interaction by TR-FRET-based high-throughput screening analysis
- ChEMBL_514924 (CHEMBL972650) Inhibition of adenylate binding site of Photuris pennsylvanica luciferase by quantitative high throughput screening
- ChEMBL_514925 (CHEMBL972651) Inhibition of adenylate binding site of Photinus pyralis luciferase by quantitative high throughput screening
- ChEMBL_885045 (CHEMBL2211769) Inhibition of recombinant PTP1B using para-nitrophenylphosphate as substrate by high throughput screening assay
- ChEMBL_988912 (CHEMBL2439766) Inhibition of wild type human c-MET by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_1445934 (CHEMBL3377918) Activation of human recombinant Glucokinase measured over 5 mins by G6-PD coupled assay in presence of 5 mM glucose
- ChEMBL_1455264 (CHEMBL3362270) Agonist activity at mouse FFA4 receptor in mouse MIN6 cells assessed as induction of glucose-induced insulin secretion by AlphaLISA
- ChEMBL_1541190 (CHEMBL3745192) Displacement of UDP-[3H]glucose from beta-1,3-glucan synthase in Candida albicans MY1055 microsomal membranes incubated for 2 hrs
- ChEMBL_1557478 (CHEMBL3771809) Competitive inhibition of rabbit muscle glycogen phosphorylase-b using alpha-D-glucose-1-phosphate as substrate by Dixon plot analysis
- ChEMBL_1623252 (CHEMBL3865604) Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
- ChEMBL_1821937 (CHEMBL4321597) Inhibition of HK2 (unknown origin) using glucose-6-phosphate dehydrogenase as substrate preincubated for 10 mins followed by substrate addition
- ChEMBL_2164214 (CHEMBL5049075) Inhibition of human GCS using C8-ceramide and UDP-glucose as substrate incubated for 1 hr by RapidFire mass spectrometry
- ChEMBL_2164220 (CHEMBL5049081) Inhibition of mouse GCS using C8-ceramide and UDP-glucose as substrate incubated for 1 hr by RapidFire mass spectrometry
- ChEMBL_2226820 (CHEMBL5140333) Inhibition of rat small intestinal maltase assessed as reduction of D-glucose release using maltose as substrate by colorimetric analysis
- ChEMBL_2335138 Inhibition of GLUT1 in human MCF7 cells assessed as ATP production incubated for 24 hrs in presence of 0.1 mM glucose
- ChEMBL_2335139 Inhibition of GLUT1 in human MCF7 cells assessed as ATP production incubated for 24 hrs in presence of 10 mM glucose
- ChEMBL_308699 (CHEMBL834934) In vitro inhibition of Na-dependent [14C]AMG uptake in CHO-K1 cells expressing human sodium glucose co-transporter 1
- ChEMBL_308700 (CHEMBL834935) In vitro inhibition of Na-dependent [14C]AMG uptake in CHO-K1 cells expressing human sodium glucose co-transporter 2
- ChEMBL_31457 (CHEMBL643939) Inhibition of aldose reductase activity was measured on partially purified bovine lens preparations incubated in presence of 50 mM glucose.
- ChEMBL_33948 (CHEMBL884024) Inhibitory activity measured against alpha-L-fucosidase of bovine epididymis by colorimetric assay using the D-glucose oxidase-peroxidase method
- ChEMBL_33966 (CHEMBL649591) Inhibitory activity measured against alpha-L-fucosidase of bovine epididymis by colorimetric assay using the D-glucose oxidase-peroxidase method
- ChEMBL_34094 (CHEMBL649723) Inhibitory activity measured against alpha-L-fucosidase of rat epididymis by colorimetric assay using the D-glucose oxidase-peroxidase method
- ChEMBL_34419 (CHEMBL649423) Inhibitory activity measured against alpha-glucosidase of rat intestinal isomaltase by colorimetric assay using the D-glucose oxidase-peroxidase method
- ChEMBL_34420 (CHEMBL649424) Inhibitory activity measured against alpha-glucosidase of rat intestinal maltase by colorimetric assay using the D-glucose oxidase-peroxidase method
- ChEMBL_34421 (CHEMBL649425) Inhibitory activity measured against alpha-glucosidase of rat intestinal sucrase by colorimetric assay using the D-glucose oxidase-peroxidase method
- ChEMBL_34526 (CHEMBL648167) Inhibitory activity measured against alpha-glucosidase of rat liver lysosomal by colorimetric assay using the D-glucose oxidase-peroxidase method
- ChEMBL_584072 (CHEMBL1058313) Activation of flag-tagged recombinant human liver glucokinase expressed in Escherichia coli assessed as glucose-6-phosphate dehydrogenase by spectrophotometry
- ChEMBL_659928 (CHEMBL1247186) Inhibition of GLUT1-mediated [3H]2-deoxy-glucose uptake in rat L6 cells after 15 mins by liquid scintillation counting
- ChEMBL_830545 (CHEMBL2061357) Inhibition of rat intestinal maltase using maltose as substrate preincubated for 10 mins before substrate addition by glucose oxidase method
- ChEMBL_959319 (CHEMBL2384006) Activation of human recombinant muscle GYS1 expressed in insect sf9 cells using glycogen and UDP-glucose as substrates by spectrophotometry
- ChEMBL_99040 (CHEMBL712593) In vitro inhibitory activity against recombinant human liver glycogen phosphorylase a (rHLGPa) catalyzed release of phosphate from glucose-1-phosphate.
- ChEMBL_2521267 Inhibition of human GLUT4 expressed in CHO cells assessed as reduction in glucose uptake by measuring decrease in ATP production preincubated for 20 mins followed by glucose addition and measured after 15 mins in presence of oxidative phosphorylation inhibitor rotenone by CellTiter-Glo Luminescent Cell Viability Assay
- ChEBML_58211 The compound was evaluated for the binding affinity towards Dopamine receptor D2 at high affinity state
- ChEMBL_1440950 (CHEMBL3375800) Inhibition of EGFR T790M/del746 to 750 mutant (unknown origin) by high-throughput biochemical screening
- ChEMBL_1501100 (CHEMBL3587448) Inhibition of GST-tagged PTP1B (unknown origin) by pNPP catalysis based colorimetric high throughput assay
- ChEMBL_1891115 (CHEMBL4392942) Inhibition of recombinant human Kv1.5 expressed in CHO cells by IonWork high-throughput electrophysiology assay
- ChEMBL_198048 (CHEMBL805175) Inhibition of high affinity re-uptake of [3H]5-HT (serotonin) into nerve ending synaptosomes
- ChEMBL_2297887 Binding affinity to human recombinant PTGER2 assessed as dissociation constant by high throughput fluorescence polarization assay
- ChEMBL_578460 (CHEMBL1062264) Inhibition of human NEU3 transiently transfected in HEK293T cells by fluorimetric high-performance liquid chromatography
- ChEMBL_61177 (CHEMBL872781) Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
- ChEMBL_61466 (CHEMBL671447) Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D2L
- ChEMBL_61478 (CHEMBL672529) Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D2L
- ChEMBL_61806 (CHEMBL872880) Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D2S
- ChEMBL_62120 (CHEMBL673441) Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D3
- ChEMBL_69801 (CHEMBL678749) Inhibition of [3H]flunitrazepam binding to high affinity GABA-A receptor of rat hippocampal membranes
- ChEMBL_988916 (CHEMBL2439770) Inhibition of wild type human Aurora kinase B by high throughput ATP-[33P] radiolabeled assay
- ChEMBL_988917 (CHEMBL2439771) Inhibition of wild type human Aurora kinase A by high throughput ATP-[33P] radiolabeled assay
- UNG Inhibition Assay Inhibition of human uracil DNA glycosylase using high-throughput fluorescent molecular beacon DNA substrate.
- SyncroPatch 384 (Nanion) High Throughput Electrophysiology Assay Solutions were of the following composition:Earle's balanced salt solution (in mM): 135 NaCl, 5.4 KCl, 5 Glucose, 2 CaCl2), 1 MgCl2, 5 HEPES, pH 7.4. Seal enhancer solution (in mM): 90 NaCl, 3 KCl, 35 CaCl2), 10 MgCl2, 10 HEPES, pH 7.4. Extracellular recording solution (in mM): 71 NaCl, 70 NMDG, 13 KCl, 5 Glucose, 2 CaCl2), 1 MgCl2, 10 HEPES, pH 7.4. Intracellular recording solution (in mM): 130 KF, 20 KCl, 4 EGTA, 10 HEPES, 2 EDTA, 0.01 Escin, pH 7.2.