procainamide [Ligand Id: 4811] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL640 (Procainamide, Procapan, Pronestyl-SR, Pronestyl, Procan, Procanbid, NSC-27461)
  • acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
  • Acetylcholinesterase in Bovine [ChEMBL: CHEMBL4768] [UniProtKB: P23795]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
  • Organic cation transporter 1/Solute carrier family 22 member 1 in Mouse [ChEMBL: CHEMBL2073664] [GtoPdb: 1019] [UniProtKB: O08966]
  • Organic cation transporter 1/Solute carrier family 22 member 1 in Rat [ChEMBL: CHEMBL2073670] [GtoPdb: 1019] [UniProtKB: Q63089]
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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Human [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
  • Organic cation transporter 2/Solute carrier family 22 member 2 in Rat [ChEMBL: CHEMBL1770032] [GtoPdb: 1020] [UniProtKB: Q9R0W2]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL Binding affinity against Acetylcholinesterase of human RBC B 6 pKi 1000 nM Ki J. Med. Chem. (1997) 40: 3009-3013 [PMID:9301662]
ChEMBL Binding affinity against Acetylcholinesterase of purified Octopus brain (OB) B 6 pKi 1000 nM Ki J. Med. Chem. (1997) 40: 3009-3013 [PMID:9301662]
ChEMBL Inhibition of Acetylcholinesterase from human red blood cells B 6 pIC50 1000 nM IC50 J. Med. Chem. (1997) 40: 3009-3013 [PMID:9301662]
ChEMBL Inhibition of Acetylcholinesterase activity from octopus brain B 6 pIC50 1000 nM IC50 J. Med. Chem. (1997) 40: 3009-3013 [PMID:9301662]
Acetylcholinesterase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4768] [UniProtKB: P23795]
ChEMBL Binding affinity against Acetylcholinesterase of purified calf forebrain (CFB) B 6 pKi 1000 nM Ki J. Med. Chem. (1997) 40: 3009-3013 [PMID:9301662]
ChEMBL Inhibition of Acetylcholinesterase activity of calf forebrain B 6.3 pIC50 500 nM IC50 J. Med. Chem. (1997) 40: 3009-3013 [PMID:9301662]
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells F 4.13 pKi 73900 nM Ki J. Pharmacol. Exp. Ther. (1998) 286: 354-361 [PMID:9655880]
Organic cation transporter 1/Solute carrier family 22 member 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073664] [GtoPdb: 1019] [UniProtKB: O08966]
ChEMBL TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in Xenopus laevis oocytes F 5.41 pIC50 3900 nM IC50 Biochem. Biophys. Res. Commun. (2002) 296: 644-650 [PMID:12176030]
Organic cation transporter 1/Solute carrier family 22 member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073670] [GtoPdb: 1019] [UniProtKB: Q63089]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing MDCK cells F 4.33 pKi 47000 nM Ki Pharm. Res. (2001) 18: 1528-1534 [PMID:11758759]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake in Xenopus laevis oocytes F 4.89 pKi 13000 nM Ki Nature (1994) 372: 549-552 [PMID:7990927]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake (in the absence of bicarbonate) (TEA: 20 uM) in OCT1-expressing HEK293 cells F 4.92 pIC50 12000 nM IC50 J. Pharmacol. Exp. Ther. (2002) 303: 959-968 [PMID:12438515]
ChEMBL TP_TRANSPORTER: inhibition pramipexole uptake in rOCT1-injected oocytes F 5.11 pIC50 7700 nM IC50 Drug Metab. Dispos. (2005) 33: 495-499 [PMID:15640376]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake (in the presence of bicarbonate) (TEA: 20 uM) in OCT1-expressing HEK293 cells F 5.15 pIC50 7000 nM IC50 J. Pharmacol. Exp. Ther. (2002) 303: 959-968 [PMID:12438515]
Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake in Xenopus laevis oocytes F 4.3 pKi 50000 nM Ki DNA Cell Biol. (1997) 16: 871-881 [PMID:9260930]
Organic cation transporter 2/Solute carrier family 22 member 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770032] [GtoPdb: 1020] [UniProtKB: Q9R0W2]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake in OCT2-expressing MDCK cells F 4.44 pKi 36000 nM Ki Pharm. Res. (2001) 18: 1528-1534 [PMID:11758759]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake (in the presence of bicarbonate) (TEA: 20 uM) in OCT2-expressing HEK293 cells F 4.05 pIC50 90000 nM IC50 J. Pharmacol. Exp. Ther. (2002) 303: 959-968 [PMID:12438515]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]