αβ-methyleneADP [Ligand Id: 5092] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL583969
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  • 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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Ecto-5'-Nucleotidase/5`-nucleotidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5957] [GtoPdb: 1232] [UniProtKB: P21589]
ChEMBL Inhibition of native CD73 in human MDA-MB-231 cell membrane preparations [3H]AMP as substrate incubated for 25 mins by scintillation counting method B 6.68 pKi 207 nM Ki J Med Chem (2020) 63: 2941-2957 [PMID:32045236]
ChEMBL Inhibition of purified recombinant soluble human CD73 expressed in Sf9 cells [3H]AMP as substrate incubated for 25 mins by scintillation counting method B 7.05 pKi 88.4 nM Ki J Med Chem (2020) 63: 2941-2957 [PMID:32045236]
ChEMBL Inhibition of human CD73 B 7.05 pKi 88.4 nM Ki J Med Chem (2020) 63: 3935-3955 [PMID:32212732]
ChEMBL Inhibition of CD73 in human NCI-H292 cells assessed as reduction in conversion of AMP to adenosine incubated for 30 mins by malachite green reagent based assay B 4.63 pIC50 23600 nM IC50 Eur J Med Chem (2018) 157: 1051-1055 [PMID:30176535]
ChEMBL Inhibition of CD73 in human MDA-MB-231 cells assessed as reduction in conversion of AMP to adenosine incubated for 30 mins by malachite green reagent based assay B 4.67 pIC50 21400 nM IC50 Eur J Med Chem (2018) 157: 1051-1055 [PMID:30176535]
ChEMBL Inhibition of recombinant CD73 (27 to 549 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of AMP to adenosine incubated for 1 min followed by AMP addition measured after 3.5 mins by malachite green reagent based assay B 5.42 pIC50 3800 nM IC50 Eur J Med Chem (2018) 157: 1051-1055 [PMID:30176535]
GtoPdb - - 8.7 pIC50 - - - Biochemistry (1975) 14: 2362-6 [PMID:1169962]
Ecto-5'-Nucleotidase/5`-nucleotidase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075214] [GtoPdb: 1232] [UniProtKB: P21588]
ChEMBL Inhibition of purified recombinant soluble rat CD73 expressed in Sf9 cells [3H]AMP as substrate incubated for 25 mins by scintillation counting method B 6.71 pKi 197 nM Ki J Med Chem (2020) 63: 2941-2957 [PMID:32045236]
ChEMBL Inhibition of recombinant rat C-terminal His-tagged soluble form of CD73 expressed in baculovirus infected Sf9 insect cells using [2,8-3H]AMP as substrate measured after 25 mins by scintillation counting method B 6.78 pKi 167 nM Ki J Med Chem (2019) 62: 3677-3695 [PMID:30895781]
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 4.59 pKi 25800 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 4.61 pKi 24300 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 4.78 pKi 16500 nM Ki MedChemComm (2017) 8: 823-840
ChEMBL Competitive-inhibition of recombinant human NPP1 expressed in HEK293 cell membranes using p-Nph-5'-TMP as substrate pretreated for 10 mins followed by substrate addition and measured after 60 mins by capillary electrophoresis method B 4.78 pKi 16500 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 5.89 pKi 1280 nM Ki MedChemComm (2017) 8: 823-840
Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295913] [UniProtKB: Q924C3]
ChEMBL Mixed-inhibition of Wistar rat NPP1 using p-Nph-5'-TMP as substrate measured after 5 mins by UPLC method B 5.02 pKi 9600 nM Ki MedChemComm (2017) 8: 823-840

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]