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Target
Sodium/glucose cotransporter 1
Ligand
BDBM20877
Substrate
BDBM20876
Meas. Tech.
SGLT Binding Assay
pH
7.2±n/a
Temperature
295.15±n/a K
EC50
211±29 nM
Citation
Meng, W; Ellsworth, BA; Nirschl, AA; McCann, PJ; Patel, M; Girotra, RN; Wu, G; Sher, PM; Morrison, EP; Biller, SA; Zahler, R; Deshpande, PP; Pullockaran, A; Hagan, DL; Morgan, N; Taylor, JR; Obermeier, MT; Humphreys, WG; Khanna, A; Discenza, L; Robertson, JG; Wang, A; Han, S; Wetterau, JR; Janovitz, EB; Flint, OP; Whaley, JM; Washburn, WN Discovery of Dapagliflozin: A Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes. J Med Chem 51:1145-9 (2008) [PubMed] Article
More Info.:
Target
Name:
Sodium/glucose cotransporter 1
Synonyms:
High affinity sodium-glucose cotransporter | NAGT | Na(+)/glucose cotransporter 1 | SC5A1_HUMAN | SGLT1 | SLC5A1 | Sodium-dependent glucose cotransporter 1 (SGLT1) | Sodium/glucose cotransporter 1 | Sodium/glucose cotransporter 1 (SGLT1) | Solute carrier family 5 member 1
Type:
Protein
Mol. Mass.:
73503.78
Organism:
Homo sapiens (Human)
Description:
P13866
Residue:
664
Sequence:
MDSSTWSPKTTAVTRPVETHELIRNAADISIIVIYFVVVMAVGLWAMFSTNRGTVGGFFLAGRSMVWWPIGASLFASNIGSGHFVGLAGTGAASGIAIGGFEWNALVLVVVLGWLFVPIYIKAGVVTMPEYLRKRFGGQRIQVYLSLLSLLLYIFTKISADIFSGAIFINLALGLNLYLAIFLLLAITALYTITGGLAAVIYTDTLQTVIMLVGSLILTGFAFHEVGGYDAFMEKYMKAIPTIVSDGNTTFQEKCYTPRADSFHIFRDPLTGDLPWPGFIFGMSILTLWYWCTDQVIVQRCLSAKNMSHVKGGCILCGYLKLMPMFIMVMPGMISRILYTEKIACVVPSECEKYCGTKVGCTNIAYPTLVVELMPNGLRGLMLSVMLASLMSSLTSIFNSASTLFTMDIYAKVRKRASEKELMIAGRLFILVLIGISIAWVPIVQSAQSGQLFDYIQSITSYLGPPIAAVFLLAIFWKRVNEPGAFWGLILGLLIGISRMITEFAYGTGSCMEPSNCPTIICGVHYLYFAIILFAISFITIVVISLLTKPIPDVHLYRLCWSLRNSKEERIDLDAEEENIQEGPKETIEIETQVPEKKKGIFRRAYDLFCGLEQHGAPKMTEEEEKAMKMKMTDTSEKPLWRTVLNVNGIILVTVAVFCHAYFA
Inhibitor
Name:
BDBM20877
Synonyms:
3-(1-benzofuran-5-yl)-1-(2-hydroxy-4-methyl-6-{[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}phenyl)propan-1-one | CHEMBL183937 | JMC511145 Compound 2 | O-glucoside, 2 | T-1095A
Type:
Small organic molecule
Emp. Form.:
C24H26O9
Mol. Mass.:
458.4578
SMILES:
Cc1cc(O)c(C(=O)CCc2ccc3occc3c2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1