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ChEMBL ligand: CHEMBL3039507 (Inpefa, LP-802034, LX-4211, LX4211, Sar-439954, Sar439954, Sotagliflozin, Zynquista) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Sodium/glucose cotransporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4979] [GtoPdb: 915] [UniProtKB: P13866] | ||||||||
GtoPdb | - | - | 7.44 | pIC50 | 36 | nM | IC50 | Clin Pharmacol Ther (2012) 92: 158-69 [PMID:22739142] |
ChEMBL | Inhibition of human HA-tagged SGLT1 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method | B | 7.44 | pIC50 | 36.2 | nM | IC50 | J Med Chem (2017) 60: 710-721 [PMID:28045524] |
ChEMBL | Inhibition of SGLT1 (unknown origin) | B | 7.44 | pIC50 | 36 | nM | IC50 | Medchemcomm (2018) 9: 1273-1281 [PMID:30151080] |
ChEMBL | Inhibition of SGLT1 (unknown origin) | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127387-127387 [PMID:32738984] |
ChEMBL | Inhibition of human SGLT1 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method | B | 7.46 | pIC50 | 34.6 | nM | IC50 | J Med Chem (2017) 60: 4173-4184 [PMID:28447791] |
ChEMBL | Inhibition of human SGLT1 | B | 7.46 | pIC50 | 34.6 | nM | IC50 | J Med Chem (2017) 60: 4173-4184 [PMID:28447791] |
ChEMBL | Inhibition of human SGLT1 | B | 7.46 | pIC50 | 34.6 | nM | IC50 | Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053] |
Sodium/glucose cotransporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639] | ||||||||
GtoPdb | - | - | 8.74 | pIC50 | 1.8 | nM | IC50 | Clin Pharmacol Ther (2012) 92: 158-69 [PMID:22739142] |
ChEMBL | Inhibition of SGLT2 (unknown origin) | B | 8.74 | pIC50 | 1.8 | nM | IC50 | Medchemcomm (2018) 9: 1273-1281 [PMID:30151080] |
ChEMBL | Inhibition of SGLT2 (unknown origin) | B | 8.74 | pIC50 | 1.8 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127387-127387 [PMID:32738984] |
ChEMBL | Inhibition of human SGLT2 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2017) 60: 4173-4184 [PMID:28447791] |
ChEMBL | Inhibition of human SGLT2 | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2017) 60: 4173-4184 [PMID:28447791] |
ChEMBL | Inhibition of human SGLT2 | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]