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 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]
