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ChEMBL ligand: CHEMBL640 (Novocainamide, NSC-27461, Procainamide, Procan, Procanbid, Procapan, Pronestyl, Pronestyl-SR, Sp 100 (pharmaceutical)) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]