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)
  • Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 in Human [ChEMBL: CHEMBL5925] [UniProtKB: P22413]
  • Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 in Rat [ChEMBL: CHEMBL4295913] [UniProtKB: Q924C3]
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  • P2Y1 receptor/Purinergic receptor P2Y1 in Human [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900]
  • P2Y1 receptor/Purinergic receptor P2Y1 in Rat [ChEMBL: CHEMBL2497] [GtoPdb: 323] [UniProtKB: P49651]
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  • P2Y11 receptor/Purinergic receptor P2Y11 in Human [ChEMBL: CHEMBL4867] [GtoPdb: 327] [UniProtKB: Q96G91]
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  • P2Y12 receptor/Purinergic receptor P2Y12 in Rat [ChEMBL: CHEMBL2188] [GtoPdb: 328] [UniProtKB: Q9EPX4]
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  • P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077]
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  • P2Y13 receptor in Human [GtoPdb: 329] [UniProtKB: Q9BPV8]
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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
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
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
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
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
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]