furosemide [Ligand Id: 4839] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL35 (Aluzine 20, Aluzine 40, Aluzine 500, Aquamed, Disal, Diuresal, Dryptal, Froop, Frumax, Frumil, Frusemide, Frusetic, Frusid, Frusol, Furosemide, Furosemidum, Hydroled, Lasix, Lasix ret, LB-502, Logirene, Marsemide, Mirfat, NSC-269420, Oedemex, Rusyde, Tenkofruse) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| hydroxysteroid 11-beta dehydrogenase 1/11-beta-hydroxysteroid dehydrogenase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4235] [GtoPdb: 2763] [UniProtKB: P28845] | ||||||||
| ChEMBL | Inhibition of human 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH | B | 5.42 | pIC50 | 3760 | nM | IC50 | Eur J Med Chem (2009) 44: 1167-1171 [PMID:18653260] |
| hydroxysteroid 11-beta dehydrogenase 1/11-beta-hydroxysteroid dehydrogenase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3910] [GtoPdb: 2763] [UniProtKB: P50172] | ||||||||
| ChEMBL | Inhibition of mouse 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH | B | 5.42 | pIC50 | 3760 | nM | IC50 | Eur J Med Chem (2009) 44: 1167-1171 [PMID:18653260] |
| Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745] | ||||||||
| ChEMBL | Binding affinity against adenosine A1 receptor in guinea pig forebrain membranes using N6-[3H]cyclohexyladenosine as radioligand | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (1992) 35: 3066-3075 [PMID:1501234] |
| Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of Taurocholate uptake in NTCP-expressing HeLa cells | F | 4.82 | pIC50 | 15000 | nM | IC50 | J Pharmacol Exp Ther (1999) 291: 1204-1209 [PMID:10565843] |
| carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915] | ||||||||
| ChEMBL | Inhibition of human recombinant full length CA1 by stopped-flow CO2 hydration method | B | 7.21 | pKi | 62 | nM | Ki | Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014] |
| carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918] | ||||||||
| ChEMBL | Inhibition of human recombinant full length CA2 by stopped-flow CO2 hydration method | B | 7.19 | pKi | 65 | nM | Ki | Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014] |
| carbonic anhydrase 4/Carbonic anhydrase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748] | ||||||||
| ChEMBL | Inhibition of human recombinant full length CA4 by stopped-flow CO2 hydration method | B | 6.25 | pKi | 564 | nM | Ki | Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014] |
| carbonic anhydrase 9/Carbonic anhydrase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790] | ||||||||
| ChEMBL | Inhibition of human recombinant CA9 catalytic domain by stopped-flow CO2 hydration method | B | 6.38 | pKi | 420 | nM | Ki | Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014] |
| carbonic anhydrase 5A/Carbonic anhydrase VA in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218] | ||||||||
| ChEMBL | Inhibition of human recombinant full length CA5A by stopped-flow CO2 hydration method | B | 6.3 | pKi | 499 | nM | Ki | Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014] |
| Carbonic anhydrase VB in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3969] [UniProtKB: Q9Y2D0] | ||||||||
| ChEMBL | Inhibition of human recombinant full length CA5B by stopped-flow CO2 hydration method | B | 6.49 | pKi | 322 | nM | Ki | Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014] |
| Carbonic anhydrase VI in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3025] [UniProtKB: P23280] | ||||||||
| ChEMBL | Inhibition of human recombinant full length CA6 by stopped-flow CO2 hydration method | B | 6.61 | pKi | 245 | nM | Ki | Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014] |
| carbonic anhydrase 7/Carbonic anhydrase VII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166] | ||||||||
| ChEMBL | Inhibition of human recombinant full length CA7 by stopped-flow CO2 hydration method | B | 6.29 | pKi | 513 | nM | Ki | Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014] |
| carbonic anhydrase 12/Carbonic anhydrase XII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570] | ||||||||
| ChEMBL | Inhibition of human recombinant CA12 catalytic domain by stopped-flow CO2 hydration method | B | 6.58 | pKi | 261 | nM | Ki | Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014] |
| carbonic anhydrase 13/Carbonic anhydrase XIII in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2186] [GtoPdb: 2748] [UniProtKB: Q9D6N1] | ||||||||
| ChEMBL | Inhibition of mouse recombinant full length CA13 by stopped-flow CO2 hydration method | B | 6.26 | pKi | 550 | nM | Ki | Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014] |
| carbonic anhydrase 14/Carbonic anhydrase XIV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3510] [GtoPdb: 2598] [UniProtKB: Q9ULX7] | ||||||||
| ChEMBL | Inhibition of human recombinant full length CA14 by stopped-flow CO2 hydration method | B | 7.28 | pKi | 52 | nM | Ki | Bioorg Med Chem (2009) 17: 1214-1221 [PMID:19119014] |
| CDGSH iron-sulfur domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45] | ||||||||
| ChEMBL | Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis | B | 5.64 | pKi | 2285 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 5350-5353 [PMID:27687671] |
| ChEMBL | Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay | B | 4.27 | pIC50 | 53460 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5350-5353 [PMID:27687671] |
| GPR35/G-protein coupled receptor 35 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97] | ||||||||
| ChEMBL | Displacement of [3H]PSB-13253 from human recombinant GPR35 exprssed in CHO cells by liquid scintillation counting analysis | B | 5.49 | pKi | 3270 | nM | Ki | J Med Chem (2013) 56: 7084-7099 [PMID:23888932] |
| ChEMBL | Agonist activity at C-terminal beta-galactosidase tagged human recombinant GPR35 expressed in CHO cells after 90 mins by beta-arrestin recruitment assay | B | 4.95 | pEC50 | 11200 | nM | EC50 | J Med Chem (2013) 56: 7084-7099 [PMID:23888932] |
| ChEMBL | Agonist activity at human GPR35 by Ca+2 release assay | B | 5.21 | pEC50 | 6200 | nM | EC50 | J Med Chem (2013) 56: 7084-7099 [PMID:23888932] |
| GtoPdb | - | - | 5.63 | pEC50 | - | - | - | Pharmacology (2012) 89: 13-7 [PMID:22236570] |
| Holo-[acyl-carrieir-protein] synthase in Bacillus subtilis (strain 168) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4734] [UniProtKB: P96618] | ||||||||
| ChEMBL | Inhibitory activity against Bacillus subtilis AcpS by HTRF assay | B | 4.9 | pIC50 | 12700 | nM | IC50 | J Med Chem (2005) 48: 7960-7969 [PMID:16335920] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 4.8 | pIC50 | 15848.93 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| Organic anion transporter 1/Solute carrier family 22 member 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1777665] [GtoPdb: 1025] [UniProtKB: O35956] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of PAH uptake in Xenopus laevis oocytes | F | 5.02 | pKi | 9500 | nM | Ki | J Pharmacol Exp Ther (2000) 295: 261-265 [PMID:10991988] |
| OATP2A1/Solute carrier organic anion transporter family member 2A1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073680] [GtoPdb: 1223] [UniProtKB: Q00910] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of PGF2alpha uptake in PGT-expressing HeLa cells | F | 4.33 | pKi | 47000 | nM | Ki | Science (1995) 268: 866-869 [PMID:7754369] |
| Kidney-specific Na-K-Cl symporter in Human [GtoPdb: 968] [UniProtKB: Q13621] | ||||||||
| GtoPdb | - | - | 5.15 | pIC50 | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2002) 365: 193-9 [PMID:11882915] |
| Basolateral Na-K-Cl symporter in Human [GtoPdb: 969] [UniProtKB: P55011] | ||||||||
| GtoPdb | - | - | 5.13 | pIC50 | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2002) 365: 193-9 [PMID:11882915] |
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]
