αβ-meATP [Ligand Id: 4093] 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 [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 4.89 pKi 13000 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'-AMP as substrate after 30 mins by capillary electrophoresis method B 5.09 pKi 8190 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 5.48 pKi 3320 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 5.66 pKi 2200 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 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 in Human [GtoPdb: 481] [UniProtKB: Q99571]
GtoPdb - - 4.7 pEC50 19952 nM EC50 Br J Pharmacol (2000) 129: 388-94 [PMID:10694247]
P2X4 in Mouse [GtoPdb: 481] [UniProtKB: Q9JJX6]
GtoPdb - - 5.2 pEC50 6309 nM EC50 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 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 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]