glibenclamide [Ligand Id: 2414] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL472 (Calabren, Cirara, Daonil, Diabeta, Diabetamide 2.5, Diabetamide 5, Euglucon, Glibenclamide, Glibenclamidum, Gliken, Glybenclamide, Glyburide, Glyburide (micronized), Glynase, Glynase Prestab, HB 419, HB-419, Lederglib, Libanil, Malix, Micronase, NSC-759618, Semi-daonil, U-26,45, U-26452, U-26,452)
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  • CDGSH iron-sulfur domain-containing protein 1 in Human [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45]
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  • CFTR/Cystic fibrosis transmembrane conductance regulator in Human [ChEMBL: CHEMBL4051] [GtoPdb: 707] [UniProtKB: P13569]
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  • NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Human [ChEMBL: CHEMBL1741208] [GtoPdb: 1770] [UniProtKB: Q96P20]
  • NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Mouse [ChEMBL: CHEMBL3779755] [GtoPdb: 1770] [UniProtKB: Q8R4B8]
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  • Peptide transporter 2/Oligopeptide transporter, kidney isoform in Rat [ChEMBL: CHEMBL3325] [GtoPdb: 985] [UniProtKB: Q63424]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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  • Peptide transporter 1/Solute carrier family 15 member 1 in Rat [ChEMBL: CHEMBL2073691] [GtoPdb: 984] [UniProtKB: P51574]
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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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  • Organic anion transporter 2/Solute carrier family 22 member 7 in Rat [ChEMBL: CHEMBL2073671] [GtoPdb: 1026] [UniProtKB: Q5RLM2]
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  • ATP-binding cassette, sub-family C (CFTR/MRP), member 8/Kir6.2/Sulfonylurea receptor 1, Kir6.2 in Human [ChEMBL: CHEMBL2096972] [GtoPdb: 2594, 442] [UniProtKB: Q09428, Q14654]
  • ATP-binding cassette, sub-family C (CFTR/MRP), member 8/Kir6.2 in Mouse [GtoPdb: 2594, 442] [UniProtKB: Q61743]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342]
ChEMBL TP_TRANSPORTER: inhibition of Taurocholate uptake(Glibenclamide 30uM, 50 % of control) in membrane vesicles prepared from High Five cells infected with the ABCB11 baculovirus F 4.56 pKi 27500 nM Ki Gastroenterology (2002) 123: 1649-1658 [PMID:12404239]
ChEMBL Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake B 5.28 pIC50 5300 nM IC50 Drug Metab. Dispos. (2012) 40: 130-138 [PMID:21965623]
ABCB11/Bile salt export pump in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073674] [GtoPdb: 778] [UniProtKB: O70127]
ChEMBL TP_TRANSPORTER: inhibition of Taurocholate uptake in membrane vesicles from Bsep-expressing Sf9 cells F 5.21 pKi 6100 nM Ki Gastroenterology (2000) 118: 422-430 [PMID:10648470]
ChEMBL TP_TRANSPORTER: inhibition of Taurocholate uptake (Taurocholate: 1 uM) in liver canalicular membrane vesicle from female rat F 4.8 pIC50 15700 nM IC50 Toxicology (2001) 167: 83-98 [PMID:11557132]
ChEMBL TP_TRANSPORTER: inhibition of Taurocholate uptake (Taurocholate: 1 uM) in liver canalicular membrane vesicle from male rat F 5.07 pIC50 8600 nM IC50 Toxicology (2001) 167: 83-98 [PMID:11557132]
ChEMBL Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake B 5.55 pIC50 2800 nM IC50 Drug Metab. Dispos. (2012) 40: 130-138 [PMID:21965623]
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 5.78 pKi 1671 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 4.41 pIC50 39100 nM IC50 Bioorg Med Chem Lett (2016) 26: 5350-5353 [PMID:27687671]
CFTR/Cystic fibrosis transmembrane conductance regulator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4051] [GtoPdb: 707] [UniProtKB: P13569]
GtoPdb - - 4.66 pKi 21800 nM Ki J Gen Physiol (1992) 100: 573-91 [PMID:1281220]
ChEMBL Inhibition of wild type CFTR expressed in CHO cells by [125I]iodide efflux assay B 4.82 pIC50 15000 nM IC50 Eur. J. Med. Chem. (2011) 46: 1935-1941 [PMID:21397997]
CYP2C9/Cytochrome P450 2C9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3397] [GtoPdb: 1326] [UniProtKB: P11712]
ChEMBL DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.8 pIC50 1602 nM IC50 DrugMatrix in vitro pharmacology data
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG in MCF7 cells B 4.13 pIC50 74131.02 nM IC50 Eur. J. Med. Chem. (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL Inhibition of human ERG B 4.13 pIC50 74131.02 nM IC50 Eur. J. Med. Chem. (2011) 46: 618-630 [PMID:21185626]
ChEMBL K+ channel blocking activity in neuroblastoma cells expressing HERG Kv11.1 F 4.13 pIC50 74000 nM IC50 J. Med. Chem. (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL Inhibition of human ERG potassium channel B 4.13 pIC50 74000 nM IC50 Bioorg. Med. Chem. (2008) 16: 4107-4119 [PMID:18243713]
Mitochondrial complex V; ATP synthase in Bovine (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL612444] [UniProtKB: P00829, P05630, P05631, P05632]
ChEMBL Inhibitory concentration towards rat mitochondrial F1F0 ATP hydrolase using a pyruvate kinase / lactate dehydrogenase system B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2004) 47: 1081-1084 [PMID:14971888]
NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741208] [GtoPdb: 1770] [UniProtKB: Q96P20]
ChEMBL Inhibition of NLRP3 in LPS activated human monocytes after 30 mins by ELISA analysis in presence of ATP B 4.92 pIC50 12000 nM IC50 J. Med. Chem. (2016) 59: 1691-1710 [PMID:26422006]
NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3779755] [GtoPdb: 1770] [UniProtKB: Q8R4B8]
ChEMBL Inhibition of NLRP3 inflammasome activation in LPS-primed mouse bone marrow derived macrophages preincubated for 15 mins followed by addition of ATP and measured after 30 mins by immunoblotting analysis B 5 pIC50 10000 nM IC50 Eur J Med Chem (2020) 185: 111822-111822 [PMID:31699536]
Peptide transporter 2/Oligopeptide transporter, kidney isoform in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3325] [GtoPdb: 985] [UniProtKB: Q63424]
ChEMBL TP_TRANSPORTER: inhibition of Gly-Sar uptake in PEPT2-expressing LLC-PK1 cells F 5.11 pKi 7800 nM Ki Br. J. Pharmacol. (1999) 128: 1159-1164 [PMID:10578127]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Binding affinity to PPARgamma (unknown origin) by TR-FRET assay B 6.18 pKi 660 nM Ki J Nat Prod (2019) 82: 259-264 [PMID:30672698]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL DNDI: Malaria in Vitro, 72 hour F 4.42 pIC50 38260 nM IC50 Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning
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]
Peptide transporter 1/Solute carrier family 15 member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073691] [GtoPdb: 984] [UniProtKB: P51574]
ChEMBL TP_TRANSPORTER: inhibition of Gly-Sar uptake in PEPT1-expressing LLC-PK1 cells F 4.6 pKi 25000 nM Ki Br. J. Pharmacol. (1999) 128: 1159-1164 [PMID:10578127]
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 5.8 pKi 1600 nM Ki Eur. J. Pharmacol. (2000) 398: 193-197 [PMID:10854830]
Organic anion transporter 2/Solute carrier family 22 member 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073671] [GtoPdb: 1026] [UniProtKB: Q5RLM2]
ChEMBL TP_TRANSPORTER: inhibition of Salicylate uptake in Oat2-expressing LLC PK1 cells F 4.91 pKi 12300 nM Ki Jpn. Pharmacol. Ther. (2001) 29: S101-S104
ATP-binding cassette, sub-family C (CFTR/MRP), member 8/Kir6.2/Sulfonylurea receptor 1, Kir6.2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096972] [GtoPdb: 2594, 442] [UniProtKB: Q09428, Q14654]
ChEMBL Inhibition of human SUR1/Kir6.2 expressed in CHO cells B 8.37 pIC50 4.3 nM IC50 J. Med. Chem. (2001) 44: 1627-1653 [PMID:11356099]
ATP-binding cassette, sub-family C (CFTR/MRP), member 8/Kir6.2 in Mouse [GtoPdb: 2594, 442] [UniProtKB: Q61743]
GtoPdb - - 5.7 pIC50 - - - Science (1995) 270: 1166-70 [PMID:7502040];
Neuron (1996) 16: 1011-7 [PMID:8630239]
ABCC9/Kir6.2/Sulfonylurea receptor 2, Kir6.2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095198] [GtoPdb: 2746, 442] [UniProtKB: O60706, Q14654]
ChEMBL Binding affinity was determined by displacement of [3H]P1075 from its binding sites in canine cardiac membranes B 6.89 pKi 130 nM Ki J. Med. Chem. (1998) 41: 271-275 [PMID:9464357]
ChEMBL Inhibition of human SUR2A/Kir6.2 expressed in Xenopus oocytes B 6.66 pIC50 220 nM IC50 J. Med. Chem. (2001) 44: 1627-1653 [PMID:11356099]
ABCC9/Kir6.2 in Mouse [GtoPdb: 2746, 442] [UniProtKB: P70170, Q61743]
GtoPdb - - 5.7 pIC50 - - - Science (1995) 270: 1166-70 [PMID:7502040];
Neuron (1996) 16: 1011-7 [PMID:8630239]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]