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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 |
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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 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 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 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 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]