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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 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]