PPADS [Ligand Id: 1725] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL69234 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295913] [UniProtKB: Q924C3] | ||||||||
| ChEMBL | Inhibition of NPP1 in Wistar rat C6 cells using [gamma-32P]ATP as substrate pretreated for 30 mins followed by substrate addition and measured after 90 mins by TLC analysis | B | 4.92 | pIC50 | 12000 | nM | IC50 | Medchemcomm (2017) 8: 823-840 [PMID:30108800] |
| P2X1/P2X purinoceptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5496] [GtoPdb: 478] [UniProtKB: P51576] | ||||||||
| ChEMBL | Antagonist activity at mouse P2X1 receptor | B | 7 | pIC50 | 99 | 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 | Compound was tested in a functional ion channel assay of ATP-induced current at recombinant rat P2X1 receptor expressed in Xenopus oocytes. | B | 4.01 | pIC50 | 98500 | nM | IC50 | J Med Chem (1998) 41: 2201-2206 [PMID:9632352] |
| ChEMBL | Antagonist activity at rat P2X1 receptor | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2020) 63: 6164-6178 [PMID:32345019] |
| ChEMBL | Inhibition of inward ion current elicited by ATP at P2X1 receptor expressed in Xenopus oocytes | F | 7 | pIC50 | 99 | nM | IC50 | J Med Chem (2001) 44: 340-349 [PMID:11462975] |
| ChEMBL | The compound was evaluated for antagonist activity against recombinant rat P2X purinoceptor 1 (P2X1) at 1 uM, expressed in Xenopus oocytes | F | 7 | pEC50 | 99 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2X2/P2X purinoceptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2531] [GtoPdb: 479] [UniProtKB: Q9UBL9] | ||||||||
| ChEMBL | Antagonist activity against human P2X2R stably transfected in human 1321N1 cells incubated for 30 mins by Fura-2 AM staining based calcium influx assay | B | 5.69 | pIC50 | 2020 | nM | IC50 | Eur J Med Chem (2022) 238: 114491-114491 [PMID:35660250] |
| 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 | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2001) 44: 340-349 [PMID:11462975] |
| ChEMBL | The compound was evaluated for antagonist activity against recombinant rat receptor P2X purinoceptor 2 (P2X2) at 30 uM, expressed in Xenopus oocytes | F | 4.92 | pEC50 | 12000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2X3/P2X purinoceptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2998] [GtoPdb: 480] [UniProtKB: P56373] | ||||||||
| ChEMBL | Antagonist activity at human P2X3 receptor | B | 6.62 | pIC50 | 240 | nM | IC50 | Eur J Med Chem (2013) 70: 811-830 [PMID:24246730] |
| ChEMBL | Antagonist activity against recombinant human P2X purinoceptor 3 (P2X3 ) | F | 5.77 | pEC50 | 1700 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| ChEMBL | The compound was evaluated for antagonist activity against recombinant rat P2X purinoceptor 3 (P2X3) at 10 uM, expressed in Xenopus oocytes | F | 6.62 | pEC50 | 240 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| 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 | 6.62 | pIC50 | 240 | nM | IC50 | J Med Chem (2001) 44: 340-349 [PMID:11462975] |
| P2X4/P2X purinoceptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2104] [GtoPdb: 481] [UniProtKB: Q99571] | ||||||||
| ChEMBL | Inhibition of inward ion current elicited by ATP at human P2X4 receptor (mutant type) | F | 4.56 | pIC50 | 27500 | nM | IC50 | J Med Chem (2001) 44: 340-349 [PMID:11462975] |
| GtoPdb | - | - | 5 | pIC50 | 10000 | nM | IC50 | Br J Pharmacol (2000) 129: 388-94 [PMID:10694247] |
| ChEMBL | Antagonist activity against human P2X4R stably transfected in human 1321N1 cells incubated for 30 mins by Fura-2 AM staining based calcium influx assay | B | 5.21 | pIC50 | 6100 | nM | IC50 | Eur J Med Chem (2022) 238: 114491-114491 [PMID:35660250] |
| ChEMBL | Antagonist activity against recombinant human P2X purinoceptor 4 (P2X4) | F | 5 | pEC50 | 10000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2X4/P2X purinoceptor 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176849] [GtoPdb: 481] [UniProtKB: Q9JJX6] | ||||||||
| ChEMBL | Inhibition of inward ion current elicited by ATP at mouse P2X4 receptor (mutant type) | F | 4.68 | pIC50 | 21000 | nM | IC50 | J Med Chem (2001) 44: 340-349 [PMID:11462975] |
| GtoPdb | - | - | 5 | pIC50 | 10000 | nM | IC50 | Br J Pharmacol (2000) 129: 388-94 [PMID:10694247] |
| P2X4/P2X purinoceptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2818] [GtoPdb: 481] [UniProtKB: P51577] | ||||||||
| ChEMBL | Inhibition of inward ion current elicited by ATP at rat P2X4 receptor (mutant type) | F | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (2001) 44: 340-349 [PMID:11462975] |
| ChEMBL | Antagonist activity against recombinant rat P2X purinoceptor 4 (P2X4) at 3 uM, expressed in Xenopus oocytes | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2X5/P2X purinoceptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4942] [GtoPdb: 482] [UniProtKB: Q93086] | ||||||||
| ChEMBL | Antagonist activity against human P2X5R stably transfected in human 1321N1 cells incubated for 30 mins by Fura-2 AM staining based calcium influx assay | B | 5.07 | pIC50 | 8450 | nM | IC50 | Eur J Med Chem (2022) 238: 114491-114491 [PMID:35660250] |
| P2X5/P2X purinoceptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2495] [GtoPdb: 482] [UniProtKB: P51578] | ||||||||
| ChEMBL | Antagonist activity against recombinant rat P2X purinoceptor 5 (P2X5) | F | 5.59 | pEC50 | 2600 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2X6/P2X purinoceptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2122] [GtoPdb: 483] [UniProtKB: P51579] | ||||||||
| ChEMBL | Inhibition of inward ion current elicited by ATP at rat P2X6 receptor (mutant type) | F | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2001) 44: 340-349 [PMID:11462975] |
| ChEMBL | Antagonist activity against recombinant rat P2X purinoceptor 6 (P2X6 ) | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2X7/P2X purinoceptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572] | ||||||||
| ChEMBL | Antagonist activity at recombinant human P2X7 receptor assessed as inhibition of BzATP-mediated Yo-Pro uptake measured for 1 hr by FLIPR assay | B | 5.93 | pIC50 | 1180 | nM | IC50 | Eur J Med Chem (2013) 70: 811-830 [PMID:24246730] |
| P2X7/P2X purinoceptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2496] [GtoPdb: 484] [UniProtKB: Q64663] | ||||||||
| ChEMBL | The compound was evaluated for antagonist activity against recombinant rat P2X purinoceptor 7 (P2X7) | F | 4.21 | pEC50 | 62000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| 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 | 4.78 | pIC50 | 16600 | nM | IC50 | J Med Chem (2001) 44: 340-349 [PMID:11462975] |
| P2Y1 receptor/Purinergic receptor P2Y1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900] | ||||||||
| GtoPdb | - | - | 5.2 | pKi | - | - | - | Mol Pharmacol (2002) 62: 1249-57 [PMID:12391289] |
| ChEMBL | Evaluated for agonist activity against phospholipase C coupled P2Y purinoceptor 1 (P2Y1) of rat erythrocytes | F | 4.74 | pEC50 | 18200 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| ChEMBL | Evaluated for agonist activity against phospholipase C coupled P2Y purinoceptor 1 (P2Y1) of human erythrocytes | F | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2Y12 receptor/Purinergic receptor P2Y12 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2188] [GtoPdb: 328] [UniProtKB: Q9EPX4] | ||||||||
| ChEMBL | Antagonist activity against phospholipase C coupled rat P2Y purinoceptor 12 (P2Y12) | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2Y2 receptor/Purinergic receptor P2Y2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231] | ||||||||
| ChEMBL | Evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 2 (P2Y2) | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2Y4 receptor/Pyrimidinergic receptor P2Y4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2123] [GtoPdb: 325] [UniProtKB: P51582] | ||||||||
| GtoPdb | - | - | 5 | pEC50 | - | - | - | Purinergic Signal (2009) 5: 75-89 [PMID:18600475] |
| ChEMBL | The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4) | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2Y6 receptor in Human [GtoPdb: 326] [UniProtKB: Q15077] | ||||||||
| P2Y13 receptor in Human [GtoPdb: 329] [UniProtKB: Q9BPV8] | ||||||||
| GtoPdb | - | - | 4.9 | pIC50 | - | - | - | Mol Pharmacol (2003) 64: 104-12 [PMID:12815166] |
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]
