ARL 67156 [Ligand Id: 9030] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1206141
  • ectonucleoside triphosphate diphosphohydrolase 1/Ectonucleoside triphosphate diphosphohydrolase 1 in Human [ChEMBL: CHEMBL5722] [GtoPdb: 2888] [UniProtKB: P49961]
  • ectonucleoside triphosphate diphosphohydrolase 1 in Rat [GtoPdb: 2888] [UniProtKB: P97687]
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  • Ectonucleoside triphosphate diphosphohydrolase 3 in Human [ChEMBL: CHEMBL5897] [UniProtKB: O75355]
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  • Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 in Human [ChEMBL: CHEMBL5925] [UniProtKB: P22413]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ectonucleoside triphosphate diphosphohydrolase 1/Ectonucleoside triphosphate diphosphohydrolase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5722] [GtoPdb: 2888] [UniProtKB: P49961]
ChEMBL Competitive inhibition of human CD39 using ATP as substrate preincubated for 3 mins followed by substrate addition and measured after 15 mins by Dixon and Cornish-Bowden plot analysis B 4.96 pKi 11000 nM Ki J Med Chem (2020) 63: 13444-13465 [PMID:32786396]
ectonucleoside triphosphate diphosphohydrolase 1 in Rat [GtoPdb: 2888] [UniProtKB: P97687]
GtoPdb - - 4.57 pKi 27000 nM Ki J Med Chem (2008) 51: 4518-28 [PMID:18630897]
Ectonucleoside triphosphate diphosphohydrolase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5897] [UniProtKB: O75355]
ChEMBL Competitive inhibition of human NTPDase3 using ATP as substrate preincubated for 3 mins followed by substrate addition and measured after 15 mins by Dixon and Cornish-Bowden plot analysis B 4.74 pKi 18000 nM Ki J Med Chem (2020) 63: 13444-13465 [PMID:32786396]
Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5925] [UniProtKB: P22413]
ChEMBL Competitive inhibition of human NPP1 transfected in HEK293 cells using p-Nph-5'-TMP as substrate preincubated for 3 mins followed by substrate addition measured after 15 mins by Cornish-Bowden plot analysis B 4.92 pKi 12000 nM Ki Bioorg Med Chem (2016) 24: 3157-3165 [PMID:27265686]
ChEMBL Competitive-inhibition of recombinant human NPP1 expressed in HEK293 cell membranes using p-Nph-5'-TMP as substrate pretreated for 3 mins followed by substrate addition and measured after 15 mins by HPLC method B 4.92 pKi 12000 nM Ki Medchemcomm (2017) 8: 823-840 [PMID:30108800]
ChEMBL Competitive inhibition of human NPP1 using pnp-TMP as substrate preincubated for 3 mins followed by substrate addition and measured after 15 mins by Dixon and Cornish-Bowden plot analysis B 4.92 pKi 12000 nM Ki J Med Chem (2020) 63: 13444-13465 [PMID:32786396]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]