[3H]αβ-meATP [Ligand Id: 5405] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL132722 (Alpha,beta-MeATP)
  • 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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  • P2Y12 receptor/Purinergic receptor P2Y12 in Rat [ChEMBL: CHEMBL2188] [GtoPdb: 328] [UniProtKB: Q9EPX4]
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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 ATP as substrate after 30 mins by capillary electrophoresis method B 4.57 pKi 26900 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 4.89 pKi 13000 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'-AMP as substrate after 30 mins by capillary electrophoresis method B 5.09 pKi 8190 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 5.48 pKi 3320 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 5.66 pKi 2200 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 6.7 pEC50 200 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 4 pEC50 100000 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 6.13 pEC50 740 nM EC50 J. Med. Chem. (2002) 45: 4057-4093 [PMID:12213051]
P2X4/P2X purinoceptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2818] [GtoPdb: 481] [UniProtKB: P51577]
ChEMBL Antagonist activity against recombinant rat P2X purinoceptor 4 (P2X4) at 30 uM, expressed in Xenopus oocytes F 4.48 pEC50 33000 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 5.15 pEC50 >7000 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 5.1 pEC50 >8000 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 against recombinant human P2X purinoceptor 7 (P2X7) F 4 pEC50 >100000 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 4 pEC50 >100000 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]

ChEMBL data shown on this page come from version 28:

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]