ChEMBL ligand: CHEMBL583969
Ecto-5'-Nucleotidase/5`-nucleotidase in Human [ChEMBL: CHEMBL5957] [GtoPdb: 1232] [UniProtKB: P21589] Ecto-5'-Nucleotidase/5`-nucleotidase in Mouse [ChEMBL: CHEMBL4680034] [GtoPdb: 1232] [UniProtKB: Q61503] Ecto-5'-Nucleotidase/5`-nucleotidase in Rat [ChEMBL: CHEMBL1075214] [GtoPdb: 1232] [UniProtKB: P21588] There should be some charts here, you may need to enable JavaScript!
ectonucleoside triphosphate diphosphohydrolase 1/Ectonucleoside triphosphate diphosphohydrolase 1 in Mouse [ChEMBL: CHEMBL4739681] [GtoPdb: 2888] [UniProtKB: P55772] There should be some charts here, you may need to enable JavaScript!
Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 in Human [ChEMBL: CHEMBL5925] [UniProtKB: P22413] Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 in Rat [ChEMBL: CHEMBL4295913] [UniProtKB: Q924C3] There should be some charts here, you may need to enable JavaScript!

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 CD73 in human melanoma 1539 cells using AMP substrate by capillary electrophoresis assay	B	6.29	pKi	510	nM	Ki	J Med Chem (2020) 63: 13444-13465 [PMID:32786396]
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 recombinant soluble CD73 assessed as inhibition constant by radiometric assay	B	7.05	pKi	88.4	nM	Ki	J Med Chem (2022) 65: 2409-2433 [PMID:35080883]
ChEMBL	Inhibition of CD73 (unknown origin)	B	7.05	pKi	88.4	nM	Ki	Bioorg Med Chem (2022) 59: 116672-116672 [PMID:35217359]
ChEMBL	Inhibition of human CD73 using AMP as substrate by Malachite green phosphate reagent-based assay	B	7.05	pKi	88.4	nM	Ki	J Med Chem (2020) 63: 11448-11468 [PMID:32614585]
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 human CD73	B	5.22	pIC50	6090	nM	IC50	J Med Chem (2023) 66: 345-370 [PMID:36529947]
ChEMBL	Inhibition of human CD73	B	5.4	pIC50	3970	nM	IC50	Bioorg Med Chem Lett (2021) 34: 127758-127758 [PMID:33359608]
ChEMBL	Inhibition of human CD73 assessed as reduction in inorganic phosphate release upon substrate hydrolysis using AMP/ATP as substrate incubated for 1 hr followed by substrate addition and measured after 2 hrs by malachite green reagent based colorimetric assay	B	5.4	pIC50	3970	nM	IC50	Bioorg Med Chem (2022) 59: 116672-116672 [PMID:35217359]
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]
ChEMBL	Inhibition of human C-terminal His6-tagged CD73 expressed in CHO cells preincubated for 15 mins followed by AMP addition and measured after 10 mins by malachite green reagent based assay	B	5.58	pIC50	2653	nM	IC50	J Med Chem (2020) 63: 10433-10459 [PMID:32865411]
ChEMBL	Inhibition of recombinant human CD73 using AMP as substrate incubated for 120 mins by CellTiter-Glo assay	B	5.6	pIC50	2500	nM	IC50	J Med Chem (2020) 63: 13444-13465 [PMID:32786396]
ChEMBL	Inhibition of recombinant human CD73 using AMP as substrate incubated for 90 mins by malachite green colorimetric assay	B	5.96	pIC50	1100	nM	IC50	J Med Chem (2020) 63: 13444-13465 [PMID:32786396]
ChEMBL	Inhibition of human CD73 using AMP as substrate by Malachite green phosphate reagent-based assay	B	6.73	pIC50	187	nM	IC50	J Med Chem (2020) 63: 11448-11468 [PMID:32614585]
ChEMBL	Inhibition of human C-terminal His6-tagged CD73 expressed in HEK293F cells using [15N]5-AMP as substrate preincubated for 1 hr followed by substrate addition and measured after 8 mins by MS/MS assay	B	7.22	pIC50	60	nM	IC50	J Med Chem (2020) 63: 13444-13465 [PMID:32786396]
ChEMBL	Inhibition of human CD73 expressed in CHO cells using AMP as substrate preincubated for 10 mins followed by substrate addition and measured every minute for 10 to 20 mins by PNP coupled enzyme assay	B	7.3	pIC50	50	nM	IC50	J Med Chem (2020) 63: 13444-13465 [PMID:32786396]
GtoPdb	-	-	8.7	pIC50	-	-	-	Biochemistry (1975) 14: 2362-6 [PMID:1169962]
ChEMBL	Inhibition of CD73 in human NCI-H1568 cells assessed as reduction in AMP-induced ADO expression preincubated for 15 mins followed by AMP addition and measured after 1 hr by LC-MS/MS analysis	B	4.79	pEC50	16268	nM	EC50	J Med Chem (2020) 63: 10433-10459 [PMID:32865411]
Ecto-5'-Nucleotidase/5`-nucleotidase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4680034] [GtoPdb: 1232] [UniProtKB: Q61503]
ChEMBL	Inhibition of mouse CD73	B	5.33	pIC50	4630	nM	IC50	Bioorg Med Chem Lett (2021) 34: 127758-127758 [PMID:33359608]
ChEMBL	Inhibition of mouse CD73 assessed as reduction in inorganic phosphate release upon substrate hydrolysis using AMP/ATP as substrate incubated for 1 hr followed by substrate addition and measured after 2 hrs by malachite green reagent based colorimetric assay	B	5.33	pIC50	4630	nM	IC50	Bioorg Med Chem (2022) 59: 116672-116672 [PMID:35217359]
Ecto-5'-Nucleotidase/5`-nucleotidase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075214] [GtoPdb: 1232] [UniProtKB: P21588]
ChEMBL	Inhibition of rat CD73 expressed in baculovirus infected insect cells using AMP substrate by capillary electrophoresis assay	B	6.06	pKi	870	nM	Ki	J Med Chem (2020) 63: 13444-13465 [PMID:32786396]
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]
ectonucleoside triphosphate diphosphohydrolase 1/Ectonucleoside triphosphate diphosphohydrolase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4739681] [GtoPdb: 2888] [UniProtKB: P55772]
ChEMBL	Inhibition of mouse CD39	B	4	pIC50	>100000	nM	IC50	Bioorg Med Chem Lett (2021) 34: 127758-127758 [PMID:33359608]
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 [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	4.61	pKi	24300	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	4.78	pKi	16500	nM	Ki	Medchemcomm (2017) 8: 823-840 [PMID:30108800]
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 [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	5.89	pKi	1280	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	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 [PMID:30108800]

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]