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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 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]