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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL640 (Novocainamide, NSC-27461, Procainamide, Procan, Procanbid, Procapan, Pronestyl, Pronestyl-SR, Sp 100 (pharmaceutical))
  • acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
  • Acetylcholinesterase in Bovine [ChEMBL: CHEMBL4768] [UniProtKB: P23795]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • TAS2R9 in Human [GtoPdb: 665] [UniProtKB: Q9NYW1]
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
acetylcholinesterase (Yt 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]
TAS2R9 in Human [GtoPdb: 665] [UniProtKB: Q9NYW1]
GtoPdb - - 2.55 pEC50 2800000 nM EC50 PLoS One (2008) 3: e3974 [PMID:19092995]

ChEMBL data shown on this page come from version 33:

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]