Reaction Details Report a problem with these data
Target
Sodium/glucose cotransporter 2
Ligand
BDBM20879
Substrate
BDBM20876
Meas. Tech.
SGLT Binding Assay
pH
7.2±n/a
Temperature
295.15±n/a K
EC50
1300±600 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 2
Synonyms:
Na(+)/glucose cotransporter 2 | SC5A2_HUMAN | SGLT2 | SLC5A2 | Sodium-Dependent Glucose Cotransporter 2 (SGLT2) | Sodium/glucose cotransporter 1 (SGLT1) | Solute carrier family 5 member 2
Type:
Protein
Mol. Mass.:
72902.00
Organism:
Homo sapiens (Human)
Description:
P31639
Residue:
672
Sequence:
MEEHTEAGSAPEMGAQKALIDNPADILVIAAYFLLVIGVGLWSMCRTNRGTVGGYFLAGRSMVWWPVGASLFASNIGSGHFVGLAGTGAASGLAVAGFEWNALFVVLLLGWLFAPVYLTAGVITMPQYLRKRFGGRRIRLYLSVLSLFLYIFTKISVDMFSGAVFIQQALGWNIYASVIALLGITMIYTVTGGLAALMYTDTVQTFVILGGACILMGYAFHEVGGYSGLFDKYLGAATSLTVSEDPAVGNISSFCYRPRPDSYHLLRHPVTGDLPWPALLLGLTIVSGWYWCSDQVIVQRCLAGKSLTHIKAGCILCGYLKLTPMFLMVMPGMISRILYPDEVACVVPEVCRRVCGTEVGCSNIAYPRLVVKLMPNGLRGLMLAVMLAALMSSLASIFNSSSTLFTMDIYTRLRPRAGDRELLLVGRLWVVFIVVVSVAWLPVVQAAQGGQLFDYIQAVSSYLAPPVSAVFVLALFVPRVNEQGAFWGLIGGLLMGLARLIPEFSFGSGSCVQPSACPAFLCGVHYLYFAIVLFFCSGLLTLTVSLCTAPIPRKHLHRLVFSLRHSKEEREDLDADEQQGSSLPVQNGCPESAMEMNEPQAPAPSLFRQCLLWFCGMSRGGVGSPPPLTQEEAAAAARRLEDISEDPSWARVVNLNALLMMAVAVFLWGFYA
Inhibitor
Name:
BDBM20879
Synonyms:
C-aryl glucoside, 5 | CHEMBL429911 | N-ethyl-2,6-dihydroxy-5-[(4-methoxyphenyl)methyl]-3-[(2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]benzamide
Type:
Small organic molecule
Emp. Form.:
C23H29NO9
Mol. Mass.:
463.4777
SMILES:
CCNC(=O)c1c(O)c(Cc2ccc(OC)cc2)cc([C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1O