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ChEMBL ligand: CHEMBL119235 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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14-3-3 protein gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293296] [UniProtKB: P61981] | ||||||||
ChEMBL | Binding affinity to GST-tagged 14-3-3-gamma (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as inhibition of interaction with PRAS40 in African green monkey COS7 cells preincubated with protein followed by cell addition by ELISA | B | 4.79 | pIC50 | 16400 | nM | IC50 | J Med Chem (2018) 61: 3755-3778 [PMID:28968506] |
14-3-3 protein zeta/delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105899] [UniProtKB: P63104] | ||||||||
ChEMBL | Inhibition of PRAS40 binding to human GST-tagged 14-3-3 protein zeta/delta expressed in Escherichia coli BL21(DE3) by ELISA | B | 5.03 | pIC50 | 9300 | nM | IC50 | J Med Chem (2018) 61: 1276-1284 [PMID:29328660] |
ChEMBL | Binding affinity to GST-tagged 14-3-3-zeta (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as inhibition of interaction with PRAS40 in African green monkey COS7 cells preincubated with protein followed by cell addition by ELISA | B | 5.03 | pIC50 | 9300 | nM | IC50 | J Med Chem (2018) 61: 3755-3778 [PMID:28968506] |
P2X1/P2X purinoceptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5496] [GtoPdb: 478] [UniProtKB: P51576] | ||||||||
ChEMBL | Antagonist activity at recombinant mouse P2X1 receptor expressed in Xenopus oocytes assessed as inhibition of ATP-induced ion current preincubated for 20 mins followed by ATP addition by two-electrode voltage clamp assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Eur J Med Chem (2013) 70: 811-830 [PMID:24246730] |
P2X1/P2X purinoceptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2530] [GtoPdb: 478] [UniProtKB: P47824] | ||||||||
ChEMBL | Antagonist activity at recombinant rat P2X1 receptor expressed in Xenopus oocytes assessed as ion flux stimulation | B | 7.37 | pIC50 | 43 | nM | IC50 | Eur J Med Chem (2013) 70: 811-830 [PMID:24246730] |
GtoPdb | - | - | 8 | pIC50 | ~10 | nM | IC50 | J Med Chem (2001) 44: 340-9 [PMID:11462975] |
ChEMBL | Inhibition of inward ion current elicited by ATP at P2X1 receptor expressed in Xenopus oocytes | F | 8.03 | pIC50 | 9.4 | nM | IC50 | J Med Chem (2001) 44: 340-349 [PMID:11462975] |
P2X2/P2X purinoceptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2135] [GtoPdb: 479] [UniProtKB: P49653] | ||||||||
ChEMBL | Inhibition of inward ion current elicited by ATP at P2X2 receptor expressed in Xenopus oocytes | F | 4.92 | pIC50 | 11900 | nM | IC50 | J Med Chem (2001) 44: 340-349 [PMID:11462975] |
P2X3/P2X purinoceptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4824] [GtoPdb: 480] [UniProtKB: P49654] | ||||||||
ChEMBL | Inhibition of inward ion current elicited by ATP was determined at recombinant P2X3 receptor expressed in Xenopus oocytes | F | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2001) 44: 340-349 [PMID:11462975] |
P2X7/P2X purinoceptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572] | ||||||||
ChEMBL | Antagonist activity at P2X7 receptor (unknown origin) | B | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem (2013) 21: 2643-2650 [PMID:23510563] |
P2Y purinoceptor 1 in Turkey (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5720] [UniProtKB: P49652] | ||||||||
ChEMBL | Inhibition of 10 nM 2-MeS-ADP-stimulated phospholipase C in turkey erythrocyte membranes using [3H]inositol | F | 4 | pIC50 | 100000 | nM | IC50 | J Med Chem (2001) 44: 340-349 [PMID:11462975] |
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]