glibenclamide [Ligand Id: 2414] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL472 (Amglidia, Calabren, Cirara, Daonil, Diabeta, Diabetamide 2.5, Diabetamide 5, Euglucon, Glibenclamida, 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-26,452, U-26452) |
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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] |
| ChEMBL | Agonist activity at PPARgamma in human BMMSC cells assessed as promotion of adiponectin secretion by measuring increase in adiponectin level in presence of IDX medium by ELISA | B | 5.64 | pEC50 | 2300 | nM | EC50 | J Nat Prod (2023) 86: 138-148 [PMID:36529937] |
| 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] |
| Urokinase plasminogen activator surface receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4883] [UniProtKB: Q03405] | ||||||||
| ChEMBL | Binding affinity to uPAR H47C/N259C (unknown origin) mutant assessed as equilibrium dissociation constant by surface plasmon resonance (SPR) analysis relative to control | B | 4.39 | pKd | 40400 | nM | Kd | J Med Chem (2023) 66: 5415-5426 [PMID:36854648] |
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]
