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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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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]