bumetanide [Ligand Id: 4837] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1072 (Betinex, Bumetanide, Bumex, Burinex, Lixil, RO 10-6338, RO-10-6338, RO-106338, S-95008., S95008.)
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  • Basolateral Na-K-Cl symporter/Solute carrier family 12 member 2 in Human [ChEMBL: CHEMBL1615383] [GtoPdb: 969] [UniProtKB: P55011]
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  • Organic anion transporter 1/Solute carrier family 22 member 6 in Rat [ChEMBL: CHEMBL1777665] [GtoPdb: 1025] [UniProtKB: O35956]
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  • GPR35 in Human [GtoPdb: 102] [UniProtKB: Q9HC97]
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  • Kidney-specific Na-K-Cl symporter in Human [GtoPdb: 968] [UniProtKB: Q13621]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
AQP4/Aquaporin-4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5291512] [GtoPdb: 691] [UniProtKB: P47863]
ChEMBL Inhibition of rat AQP4 water channel expressed in Xenopus laevis oocytes assessed as inhibition of AQP1-mediated osmotic swelling incubated for 1 to 2 hrs by videomicroscopy analysis B 4 pIC50 100000 nM IC50 Eur J Med Chem (2020) 208: 112855-112855 [PMID:33007663]
Basolateral Na-K-Cl symporter/Solute carrier family 12 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1615383] [GtoPdb: 969] [UniProtKB: P55011]
GtoPdb - - 5.6 pIC50 - - - Naunyn Schmiedebergs Arch Pharmacol (2002) 365: 193-9 [PMID:11882915]
ChEMBL Inhibition of NKCC1 in human HT-29 cells assessed as inhibition of rubidium uptake incubated for 20 min by atomic absorption spectroscopy B 5.81 pIC50 1540 nM IC50 Eur J Med Chem (2020) 208: 112855-112855 [PMID:33007663]
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 5.26 pKi 5500 nM Ki J Pharmacol Exp Ther (2000) 295: 261-265 [PMID:10991988]
GPR35 in Human [GtoPdb: 102] [UniProtKB: Q9HC97]
GtoPdb - - 5.54 pEC50 - - - Pharmacology (2012) 89: 13-7 [PMID:22236570]
Kidney-specific Na-K-Cl symporter in Human [GtoPdb: 968] [UniProtKB: Q13621]
GtoPdb - - 6.48 pIC50 - - - Naunyn Schmiedebergs Arch Pharmacol (2002) 365: 193-9 [PMID:11882915]

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]