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-26,452, U-26452)
ABCB11/Bile salt export pump in Human [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342] ABCB11/Bile salt export pump in Rat [ChEMBL: CHEMBL2073674] [GtoPdb: 778] [UniProtKB: O70127] There should be some charts here, you may need to enable JavaScript!
CDGSH iron-sulfur domain-containing protein 1 in Human [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45] There should be some charts here, you may need to enable JavaScript!
CFTR/Cystic fibrosis transmembrane conductance regulator in Human [ChEMBL: CHEMBL4051] [GtoPdb: 707] [UniProtKB: P13569] There should be some charts here, you may need to enable JavaScript!
CYP2C9/Cytochrome P450 2C9 in Human [ChEMBL: CHEMBL3397] [GtoPdb: 1326] [UniProtKB: P11712] There should be some charts here, you may need to enable JavaScript!
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
Mitochondrial complex V; ATP synthase in Bovine [ChEMBL: CHEMBL612444] [UniProtKB: P00829, P05630, P05631, P05632] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
Peptide transporter 2/Oligopeptide transporter, kidney isoform in Rat [ChEMBL: CHEMBL3325] [GtoPdb: 985] [UniProtKB: Q63424] There should be some charts here, you may need to enable JavaScript!
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum [ChEMBL: CHEMBL364] There should be some charts here, you may need to enable JavaScript!
Peptide transporter 1/Solute carrier family 15 member 1 in Rat [ChEMBL: CHEMBL2073691] [GtoPdb: 984] [UniProtKB: P51574] There should be some charts here, you may need to enable JavaScript!
Organic anion transporter 1/Solute carrier family 22 member 6 in Rat [ChEMBL: CHEMBL1777665] [GtoPdb: 1025] [UniProtKB: O35956] There should be some charts here, you may need to enable JavaScript!
Organic anion transporter 2/Solute carrier family 22 member 7 in Rat [ChEMBL: CHEMBL2073671] [GtoPdb: 1026] [UniProtKB: Q5RLM2] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
ABCC9/Kir6.2/Sulfonylurea receptor 2, Kir6.2 in Human [ChEMBL: CHEMBL2095198] [GtoPdb: 2746, 442] [UniProtKB: O60706, Q14654] ABCC9/Kir6.2 in Mouse [GtoPdb: 2746, 442] [UniProtKB: P70170, Q61743] There should be some charts here, you may need to enable JavaScript!

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 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]