decynium 22 [Ligand Id: 8482] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1197556 (GNF-Pf-1919, GNF-Pf-4440, NSC-97374) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay | F | 6.21 | pEC50 | 618 | nM | EC50 | Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783] |
| ChEMBL | NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay | F | 6.26 | pEC50 | 544 | nM | EC50 | Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783] |
| ChEMBL | NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay | F | 6.72 | pEC50 | 188.7 | nM | EC50 | Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783] |
| ChEMBL | NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay | F | 7.18 | pEC50 | 65.8 | nM | EC50 | Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783] |
| Quinone reductase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3959] [UniProtKB: P16083] | ||||||||
| ChEMBL | Inhibition of human recombinant NQO2 | B | 5.57 | pIC50 | 2700 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7331-7336 [PMID:21074425] |
| 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 MPP+ uptake in Xenopus laevis oocytes | F | 5.36 | pKi | 4400 | nM | Ki | Mol Pharmacol (1997) 51: 913-921 [PMID:9187257] |
| ChEMBL | TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells | F | 5.56 | pKi | 2730 | nM | Ki | J Pharmacol Exp Ther (1998) 286: 354-361 [PMID:9655880] |
| ChEMBL | TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT1-expressing HEK293 cells | F | 6.01 | pIC50 | 980 | nM | IC50 | Br J Pharmacol (2002) 136: 829-836 [PMID:12110607] |
| 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 MPP+ uptake in OCT1-expressing HEK293 cells | F | 6.3 | pKi | 500 | nM | Ki | Naunyn Schmiedebergs Arch Pharmacol (1996) 354: 320-326 [PMID:8878062] |
| ChEMBL | TP_TRANSPORTER: inhibition of TEA uptake in Xenopus laevis oocytes | F | 6.44 | pKi | 360 | nM | Ki | Nature (1994) 372: 549-552 [PMID:7990927] |
| Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244] | ||||||||
| GtoPdb | Measuring inhibition of tetraethylammonium (TEA) uptake via OCT2 expressed in Xenopus oocytes. | - | 7 | pKi | 100 | nM | Ki | DNA Cell Biol (1997) 16: 871-81 [PMID:9260930] |
| ChEMBL | TP_TRANSPORTER: inhibition of TEA uptake in Xenopus laevis oocytes | F | 7 | pKi | 100 | nM | Ki | DNA Cell Biol (1997) 16: 871-881 [PMID:9260930] |
| ChEMBL | TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT2-expressing HEK293 cells | F | 5.95 | pIC50 | 1130 | nM | IC50 | Br J Pharmacol (2002) 136: 829-836 [PMID:12110607] |
| 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 (TEA: 100 uM) in Xenopus laevis oocytes | F | 4.86 | pIC50 | 13800 | nM | IC50 | Biochim Biophys Acta (1999) 1417: 224-231 [PMID:10082798] |
| Organic cation transporter 3/Solute carrier family 22 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT3-expressing HEK293 cells | F | 7.05 | pIC50 | 90 | nM | IC50 | Br J Pharmacol (2002) 136: 829-836 [PMID:12110607] |
| Plasma membrane monoamine transporter in Human [GtoPdb: 1120] [UniProtKB: Q7RTT9] | ||||||||
| GtoPdb | - | - | 7 | pKi | 100 | nM | Ki |
Mol Pharmacol (2005) 68: 1397-407 [PMID:16099839]; Clin Pharmacol Ther (2016) 100: 489-499 [PMID:27506881] |
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]
