ipragliflozin [Ligand Id: 9394] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2018096 (ASP-1941, Ipragliflozin) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Sodium/glucose cotransporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4979] [GtoPdb: 915] [UniProtKB: P13866] | ||||||||
| ChEMBL | Inhibition of human SGLT1 | B | 5.73 | pIC50 | 1876 | nM | IC50 | Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053] |
| GtoPdb | Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing hSGLT1. | - | 5.73 | pIC50 | 1876 | nM | IC50 | Naunyn Schmiedebergs Arch Pharmacol (2012) 385: 423-36 [PMID:22139434] |
| ChEMBL | Inhibition of SGLT1 (unknown origin) | B | 5.72 | pEC50 | 1900 | nM | EC50 | J Med Chem (2020) 63: 5031-5073 [PMID:31930920] |
| Sodium/glucose cotransporter 1 in Mouse [GtoPdb: 915] [UniProtKB: Q8C3K6] | ||||||||
| GtoPdb | Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing mSGLT1. | - | 5.86 | pIC50 | 1380 | nM | IC50 | Naunyn Schmiedebergs Arch Pharmacol (2012) 385: 423-36 [PMID:22139434] |
| Sodium/glucose cotransporter 1 in Rat [GtoPdb: 915] [UniProtKB: P53790] | ||||||||
| GtoPdb | Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing rSGLT1. | - | 5.93 | pIC50 | 1166 | nM | IC50 | Naunyn Schmiedebergs Arch Pharmacol (2012) 385: 423-36 [PMID:22139434] |
| Sodium/glucose cotransporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639] | ||||||||
| ChEMBL | Inhibition of SGLT2 (unknown origin) | B | 8.08 | pIC50 | 8.4 | nM | IC50 | Bioorg Med Chem (2018) 26: 3947-3952 [PMID:29954682] |
| GtoPdb | Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing hSGLT2. | - | 8.13 | pIC50 | 7.38 | nM | IC50 | Naunyn Schmiedebergs Arch Pharmacol (2012) 385: 423-36 [PMID:22139434] |
| ChEMBL | Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]AMG accumulation after 2 hrs by scintillation counting | B | 8.13 | pIC50 | 7.4 | nM | IC50 | Bioorg Med Chem (2012) 20: 3263-3279 [PMID:22507206] |
| ChEMBL | Inhibition of recombinant human full-length SGLT2 expressed in CHO cells assessed as decrease in [14C]-AMG uptake measured after 2 hrs by topcount scintillation counting method | B | 8.13 | pIC50 | 7.4 | nM | IC50 | Medchemcomm (2018) 9: 1273-1281 [PMID:30151080] |
| ChEMBL | Inhibition of human SGLT2 | B | 8.13 | pIC50 | 7.38 | nM | IC50 | Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053] |
| ChEMBL | Inhibition of SGLT2 (unknown origin) | B | 8.13 | pEC50 | 7.4 | nM | EC50 | J Med Chem (2020) 63: 5031-5073 [PMID:31930920] |
| Sodium/glucose cotransporter 2 in Mouse [GtoPdb: 916] [UniProtKB: Q923I7] | ||||||||
| GtoPdb | Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing mSGLT2. | - | 8.25 | pIC50 | 5.64 | nM | IC50 | Naunyn Schmiedebergs Arch Pharmacol (2012) 385: 423-36 [PMID:22139434] |
| Sodium/glucose cotransporter 2 in Rat [GtoPdb: 916] [UniProtKB: P53792] | ||||||||
| GtoPdb | Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing rSGLT2. | - | 8.2 | pIC50 | 6.37 | nM | IC50 | Naunyn Schmiedebergs Arch Pharmacol (2012) 385: 423-36 [PMID:22139434] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
