Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T30085 | Target Info | |||
| Target Name | Sodium/glucose cotransporter 2 (SGLT2) | ||||
| Synonyms |
Solute carrier family 5 member 2; Na(+)/glucose cotransporter 2; Low affinity sodium-glucose cotransporter
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| Target Type | Successful Target | ||||
| Gene Name | SLC5A2 | ||||
| Biochemical Class | Solute:sodium symporter | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 25 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Phlorizin
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Investigative | Compound Info | ||
| Synonyms |
Phlorizin; Phloridzin; 60-81-1; Phlorhizin; Phlorizoside; Floridzin; Phlorrhizin; Phloretin 2'-glucoside; Phlorrhizen; Phloridzosid; Phlorizine; UNII-CU9S17279X; Phloretin-2'-O-beta-glucoside; AI3-19835; NSC 2833; Phloridzin dihydrate; EINECS 200-487-1; Phloretin-2'-beta-glucoside; CHEBI:8113; CHEMBL245067; IOUVKUPGCMBWBT-QNDFHXLGSA-N; CU9S17279X; 2'-(beta-D-Glucopyranosyloxy)-4',6'-dihydroxy-3-(4-hydroxyphenyl)propiophenone; 1-[2-(beta-D-Glucopyranosyloxy)-4,6-dihydroxyphenyl]-3-(4-hydroxyphenyl)-1-propanone; 1-Propanone, 1-(2-(b
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| Activity |
IC50 = 100000 nM
|
[1] | |||
| Compound Name |
1-(2-Imino-3-(2-(piperidin-1-yl)ethyl)-2,3-dihydrobenzo[d]imidazol-1-yl)-3,3-dimethylbutan-2-ol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL397851; ChemDiv3_001291; Oprea1_794919; Oprea1_839452; HMS1476K15; BDBM50346272; STK037997; AKOS000591510; AKOS021987392; MCULE-7620191138; IDI1_020257; EU-0036627; AB00096972-01
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| Activity |
EC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
(2S,3R,4R,5R)-2-[4-Chloro-3-[(4-fluorophenyl)methyl]phenyl]-5-[(1R)-1,2-dihydroxyethyl]oxolane-3,4-diol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440375; BDBM50442483
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| Activity |
EC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
[3-(4-Chloro-benzyl)-2-imino-2,3-dihydro-benzoimidazol-1-yl]-acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1782544; CBMicro_033035; Oprea1_357869; Oprea1_376180; ZINC4639093; BDBM50346262; STK059078; AKOS001489023; MCULE-7790568083; [3-(4-chlorobenzyl)-2-imino-2,3-dihydro-1H-benzimidazol-1-yl]acetic acid; 2-(3-(4-chlorobenzyl)-2-imino-2,3-dihydro-1H-benzo[d]imidazol-1-yl)acetic acid
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| Activity |
EC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
(2S,3R,4R,5R)-2-[4-Chloro-3-[(4-phenoxyphenyl)methyl]phenyl]-5-[(1R)-1,2-dihydroxyethyl]oxolane-3,4-diol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440377; BDBM50442482
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| Activity |
EC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
3-Benzyl-4-hydroxy-1-(beta-D-xylopyranosyl)-1H-indole
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1650483; BDBM50335127
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| Activity |
EC50 ~ 50000 nM
|
[4] | |||
| Compound Name |
(2S,3R,4R,5R)-2-[3-(1,3-Benzodioxol-5-ylmethyl)-4-chlorophenyl]-5-[(1R)-1,2-dihydroxyethyl]oxolane-3,4-diol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440379; BDBM50442481
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| Activity |
EC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
CID 73357151
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440380; BDBM50442480
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| Activity |
EC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
(2S,3R,4R,5R)-2-[4-Chloro-3-[(3-methoxyphenyl)methyl]phenyl]-5-[(1R)-1,2-dihydroxyethyl]oxolane-3,4-diol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440372; BDBM50442485
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|
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| Activity |
EC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
2-(3-Benzyl-2-imino-2,3-dihydro-benzoimidazol-1-yl)-ethanol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1623333; MLS000071043; SMR000009266; ChemDiv2_000594; Oprea1_689255; Oprea1_860807; BDBM33493; cid_6603635; HMS1370K22; STK039644; ZINC19805360; AKOS000560365; MCULE-4611952995; EU-0038938; AB00089204-01; 2-(3-benzyl-2-iminobenzimidazol-1-yl)ethanol;hydrochloride; 2-(3-benzyl-2-imino-2,3-dihydro-1H-benzimidazol-1-yl)ethanol; 2-(3-benzyl-2-imino-benzimidazol-1-yl)ethanol;hydrochloride; 2-[2-imino-3-(phenylmethyl)-1-benzimidazolyl]ethanol;hydrochloride; 2-[2-azanylidene-3-(phenylmethyl)benzimidazol-1-yl]ethanol;hydrochloride
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| Activity |
EC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
(2S,3R,4R,5R)-2-[4-Chloro-3-[(2-methoxyphenyl)methyl]phenyl]-5-[(1R)-1,2-dihydroxyethyl]oxolane-3,4-diol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440373; BDBM50442484
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|
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| Activity |
EC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
2',4',6'-Trihydroxy-4-fluorochalcone
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL334384; BDBM50235123; (E)-2',4',6'-Trihydroxy-4-fluorochalcone; 4-FLUORO-2',4',6'-TRIHYDROXYCHALCONE; 4-FLUORO-2'',4'',6''-TRIHYDROXYCHALCONE
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| Activity |
IC50 = 51700 nM
|
[5] | |||
| Compound Name |
(2R,3S,4S,5R,6S)-2-(Hydroxymethyl)-6-[[5-propan-2-yl-4-[[2-(trifluoromethyl)phenyl]methyl]-1H-pyrazol-3-yl]oxy]oxane-3,4,5-triol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2160190; BDBM50394547
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| Activity |
IC50 = 60500 nM
|
[6] | |||
| Compound Name |
CID 69516839
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2159090; SCHEMBL5644192; BDBM50394552
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| Activity |
IC50 = 64700 nM
|
[6] | |||
| Compound Name |
2-[[5-Propan-2-yl-3-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-1H-pyrazol-4-yl]methyl]benzonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2159432; BDBM50394543
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|
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| Activity |
IC50 = 65700 nM
|
[6] | |||
| Compound Name |
4-(2-Benzyloxybenzyl)-3-(beta-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazole
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2159091; SCHEMBL5643805; BDBM50394531
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| Activity |
IC50 = 74000 nM
|
[6] | |||
| Compound Name |
3-(beta-D-Glucopyranosyloxy)-4-(2-hydroxybenzyl)-5-isopropyl-1H-pyrazole
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2160187; SCHEMBL5643566; BDBM50394544
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|
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| Activity |
IC50 = 75900 nM
|
[6] | |||
| Compound Name |
Methyl (14E)-19-[(acetyloxy)methyl]-14-ethylidene-6-methoxy-2-methyl-18-oxa-2,12-diazahexacyclo[9.6.1.1^{9,15}.0^{1,9}.0^{3,8}.0^{12,17}]nonadeca-3(8),4,6-triene-19-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL590530; BDBM50308534
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|
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| Activity |
IC50 = 78000 nM
|
[1] | |||
| Compound Name |
(2R,3S,4R,5R,6S)-2-(Hydroxymethyl)-6-[3-[(1-methylbenzimidazol-2-yl)methyl]phenyl]oxane-3,4,5-triol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2018089; SCHEMBL12426148; BDBM50381536
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|
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
(2R,3S,4R,5R,6S)-2-(Hydroxymethyl)-6-[3-(pyrazin-2-ylmethyl)phenyl]oxane-3,4,5-triol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2018083; SCHEMBL12426124; BDBM50381543
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|
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
3H-Pyrazol-3-one, 1,2-dihydro-((4-(methylthio)phenyl)methyl)-5-(trifluoromethyl)-
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|
Investigative | Compound Info | ||
| Synonyms |
Way 123783; 3H-Pyrazol-3-one,1,2-dihydro-4-[[4-(methylthio)phenyl]methyl]-5-(trifluoromethyl)-; ACMC-20n6ht; CHEMBL3918460; CTK4C7502
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| Compound Name |
Methyl (14E)-19-[(benzyloxy)methyl]-14-ethylidene-6-methoxy-2-methyl-18-oxa-2,12-diazahexacyclo[9.6.1.1^{9,15}.0^{1,9}.0^{3,8}.0^{12,17}]nonadeca-3(8),4,6-triene-19-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL590772; BDBM50308536
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(2S,3R,4R,5S,6R)-2-[4-Chloro-3-[(4-methoxynaphthalen-1-yl)methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1808385; BDBM50349231
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|
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| Activity |
IC50 ~ 100000 nM
|
[9] | |||
| Compound Name |
(2R,3S,4R,5R,6S)-2-(Hydroxymethyl)-6-[3-(pyridin-2-ylmethyl)phenyl]oxane-3,4,5-triol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2018082; SCHEMBL12426065; BDBM50381542
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
(2S,3R,4S,5S,6R)-2-[[5-Cyclopropyl-4-[(2-phenylmethoxyphenyl)methyl]-1H-pyrazol-3-yl]oxy]-6-(hydroxymethyl)oxane-3,4,5-triol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2159089; BDBM50394551
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|
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| Activity |
IC50 = 156000 nM
|
[6] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(2R,3S,4S,5R,6S)-2-(Hydroxymethyl)-6-[[4-[(2-methoxyphenyl)methyl]-5-propan-2-yl-1H-pyrazol-3-yl]oxy]oxane-3,4,5-triol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2160188; BDBM50394545
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| Activity |
IC50 = 204000 nM
|
[6] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Alstiphyllanines E-H, picraline and ajmaline-type alkaloids from Alstonia macrophylla inhibiting sodium glucose cotransporter. Bioorg Med Chem. 2010 Mar 15;18(6):2152-2158. | ||||
| REF 2 | Discovery of non-glycoside sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors by ligand-based virtual screening. J Med Chem. 2010 Dec 23;53(24):8770-4. | ||||
| REF 3 | Synthesis and biological evaluation of novel C-aryl d-glucofuranosides as sodium-dependent glucose co-transporter 2 inhibitors. Bioorg Med Chem. 2013 Nov 1;21(21):6282-91. | ||||
| REF 4 | Discovery of novel N--D-xylosylindole derivatives as sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the management of hyperglycemia in diabetes. J Med Chem. 2011 Jan 13;54(1):166-78. | ||||
| REF 5 | Targeting Type 2 Diabetes with C-Glucosyl Dihydrochalcones as Selective Sodium Glucose Co-Transporter 2 (SGLT2) Inhibitors: Synthesis and Biological Evaluation. J Med Chem. 2017 Jan 26;60(2):568-579. | ||||
| REF 6 | Structure-activity relationship studies of 4-benzyl-1H-pyrazol-3-yl -d-glucopyranoside derivatives as potent and selective sodium glucose co-transporter 1 (SGLT1) inhibitors with therapeutic activity on postprandial hyperglycemia. Bioorg Med Chem. 2012 Nov 15;20(22):6598-612. | ||||
| REF 7 | Discovery of Ipragliflozin (ASP1941): a novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus. Bioorg Med Chem. 2012 May 15;20(10):3263-79. | ||||
| REF 8 | US patent application no. 20040063646A1, Glucopyranosyloxypyrazole derivatives and use thereof in medicines | ||||
| REF 9 | C-aryl glucosides substituted at the 4'-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4465-70. | ||||
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