2MeSATP [Ligand Id: 1711] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL336208 (2-MeSATP, 2-Methylthioadenosine 5'-Triphosphate, 2-(Methylthio)-Adenosinetriphosphate) |
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5925] [UniProtKB: P22413] | ||||||||
| ChEMBL | Competitive-inhibition of recombinant human N-terminal His-tagged soluble NPP1 (Val191 to Leu591 residues) expressed in mouse NSO cells using p-Nph-5'-AMP as substrate after 30 mins by capillary electrophoresis method | B | 4.4 | pKi | 39900 | nM | Ki | Medchemcomm (2017) 8: 823-840 [PMID:30108800] |
| ChEMBL | Competitive-inhibition of recombinant human N-terminal His-tagged soluble NPP1 (Val191 to Leu591 residues) expressed in mouse NSO cells using ATP as substrate by capillary electrophoresis method | B | 4.6 | pKi | 25300 | nM | Ki | Medchemcomm (2017) 8: 823-840 [PMID:30108800] |
| ChEMBL | Competitive-inhibition of recombinant human N-terminal His-tagged soluble NPP1 (Val191 to Leu591 residues) expressed in mouse NSO cells using ATP as substrate after 30 mins by capillary electrophoresis method | B | 4.67 | pKi | 21300 | nM | Ki | Medchemcomm (2017) 8: 823-840 [PMID:30108800] |
| ChEMBL | Competitive-inhibition of recombinant human N-terminal His-tagged soluble NPP1 (Val191 to Leu591 residues) expressed in mouse NSO cells using p-Nph-5'-TMP as substrate after 15 mins by capillary electrophoresis method | B | 5.35 | pKi | 4470 | nM | Ki | Medchemcomm (2017) 8: 823-840 [PMID:30108800] |
| Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295913] [UniProtKB: Q924C3] | ||||||||
| ChEMBL | Competitive-inhibition of Wistar rat NPP1 using p-Nph-5'-TMP as substrate measured after 5 mins by UPLC method | B | 4.69 | pKi | 20500 | nM | Ki | Medchemcomm (2017) 8: 823-840 [PMID:30108800] |
| P2X1/P2X purinoceptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2094] [GtoPdb: 478] [UniProtKB: P51575] | ||||||||
| ChEMBL | Antagonist activity against recombinant human P2X purinoceptor 1 (P2X1 ) | F | 7.27 | pEC50 | 54 | 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 | Antagonist activity against recombinant rat receptor P2X purinoceptor 2 (P2X2) at 10 uM, expressed in Xenopus oocytes | F | 5.82 | pEC50 | 1500 | 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 against recombinant human P2X purinoceptor 3 (P2X3 ) | F | 6.46 | pEC50 | 350 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2X4/P2X purinoceptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2104] [GtoPdb: 481] [UniProtKB: Q99571] | ||||||||
| ChEMBL | Antagonist activity at human P2X4 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx compound preincubated for 30 mins before ATP treatment by Fluo-4 AM fluorescence method | F | 5 | pEC50 | 10000 | nM | EC50 | J Med Chem (2012) 55: 9576-9588 [PMID:23075067] |
| ChEMBL | Antagonist activity against recombinant human P2X purinoceptor 4 (P2X4) | F | 6 | pEC50 | 1000 | 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 | Antagonist activity at mouse P2X4 receptor by cell-based calcium influx assay | F | 5 | pEC50 | 10000 | nM | EC50 | J Med Chem (2012) 55: 9576-9588 [PMID:23075067] |
| P2X4/P2X purinoceptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2818] [GtoPdb: 481] [UniProtKB: P51577] | ||||||||
| ChEMBL | Antagonist activity at rat P2X4 receptor by cell-based calcium influx assay | F | 5 | pEC50 | 10000 | nM | EC50 | J Med Chem (2012) 55: 9576-9588 [PMID:23075067] |
| ChEMBL | Antagonist activity against recombinant rat P2X purinoceptor 4 (P2X4) at 30 uM, expressed in Xenopus oocytes | F | 5.13 | pEC50 | 7400 | 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 | 6 | pEC50 | 1000 | 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 | Antagonist activity against recombinant rat P2X purinoceptor 6 (P2X6 ) | F | 6.22 | pEC50 | 600 | 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 | Evaluated for agonist activity against phospholipase C coupled P2Y purinoceptor 1 (P2Y1) of turkey erythrocytes | F | 8.1 | pEC50 | 8 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| ChEMBL | Activation of Purinoceptor P2Y1-mediated phospholipase C in turkey erythrocyte membranes | B | 8.1 | pEC50 | 8 | nM | EC50 | J Med Chem (2002) 45: 2090-2100 [PMID:11985476] |
| P2Y1 receptor/Purinergic receptor P2Y1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900] | ||||||||
| GtoPdb | - | - | 5.2 | pKi | - | - | - | Mol Pharmacol (1998) 53: 727-33 [PMID:9547364] |
| GtoPdb | - | - | 7.6 | pIC50 | - | - | - |
Br J Pharmacol (1997) 121: 338-44 [PMID:9154346]; Mol Pharmacol (2002) 62: 1249-57 [PMID:12391289] |
| ChEMBL | Accumulation of inositol phosphate in 1321N1 astrocytoma cells expressing human P2Y1 purinoceptor | B | 7.47 | pEC50 | 34 | nM | EC50 | J Med Chem (2002) 45: 2090-2100 [PMID:11985476] |
| P2Y1 receptor/Purinergic receptor P2Y1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2497] [GtoPdb: 323] [UniProtKB: P49651] | ||||||||
| ChEMBL | Concentration required for calcium mobilization at rat purinergic 2Y1 receptor expressed in HEK 293 cells | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2004) 47: 4405-4416 [PMID:15317453] |
| P2Y11 receptor/Purinergic receptor P2Y11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4867] [GtoPdb: 327] [UniProtKB: Q96G91] | ||||||||
| GtoPdb | - | - | 4.3 | pEC50 | - | - | - | Br J Pharmacol (1999) 128: 1199-206 [PMID:10578132] |
| ChEMBL | Agonist activity against phospholipase C coupled human P2Y purinoceptor 11 (P2Y11) | F | 4.3 | pEC50 | 50000 | 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 | 8.96 | pEC50 | 1.1 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077] | ||||||||
| GtoPdb | - | - | 4 | pEC50 | - | - | - | Biochem Biophys Res Commun (1996) 222: 303-8 [PMID:8670200] |
| ChEMBL | The compound was evaluated for agonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 6 (P2Y6) | F | 4 | pEC50 | 100000 | nM | EC50 | J Med Chem (2002) 45: 4057-4093 [PMID:12213051] |
| P2Y13 receptor in Human [GtoPdb: 329] [UniProtKB: Q9BPV8] | ||||||||
| GtoPdb | - | - | 7.7 | 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]
