lansoprazole [Ligand Id: 7208] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL480 (A-65006, AG-1749, Agopton, Lansoprazol, Lansoprazole, Lansox, Lanzoprazole, Lanzor, Limpidex, NSC-758638, Ogast, Ogastoro, Opiren, Prevacid, Prevacid 24 hr, Prevacid Delayed Release, Prevacid iv, Prevacid Solutab, Prevonco, Takepron, Zoton) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
| ChEMBL | Inhibition of human ABCG2 expressed in human HEK293 cells membrane vesicles mediated transport of 3[H]-MTX for 2 mins using [3H]-methotrexate as substrate by rapid filtration technique | B | 4.84 | pIC50 | 14400 | nM | IC50 | Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322] |
| CYP2C19/Cytochrome P450 2C19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3622] [GtoPdb: 1328] [UniProtKB: P33261] | ||||||||
| ChEMBL | DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) | B | 6.47 | pIC50 | 336.7 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635] | ||||||||
| ChEMBL | DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) | B | 5.27 | pIC50 | 5314.8 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Endo-beta-N-acetylglucosaminidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5172] [UniProtKB: Q8NFI3] | ||||||||
| ChEMBL | Inhibition of recombinant human C-MYC/DDK-tagged ENGase expressed in HEK293T cells using heat inactivated bovine ribonuclease B as substrate pretreated for 15 mins followed by substrate addition after 90 mins by SDS-PAGE analysis | B | 4.61 | pIC50 | 24380 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2962-2966 [PMID:28512024] |
| fatty acid synthase/Fatty acid synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4158] [GtoPdb: 2608] [UniProtKB: P49327] | ||||||||
| ChEMBL | Inhibition of purified recombinant FASN TE activity (unknown origin) using 4-MUH as substrate preincubated for 30 mins before substrate addition measured after 1 hr by fluorescence assay | B | 5.28 | pKi | 5300 | nM | Ki | J Med Chem (2015) 58: 778-784 [PMID:25513712] |
| ChEMBL | Inhibition of human FASN enoyl reductase activity using crotonyl CoA as substrate assessed as inhibition of substrate hydrolysis measured every 1 min for 10 mins in the presence of NADPH by fluorescence based assay | B | 5.77 | pKi | 1700 | nM | Ki | J Med Chem (2022) 65: 13681-13691 [PMID:36257066] |
| ChEMBL | Inhibition of FASN in human PANC1 cells assessed as inhibition of [14C]acetate incorporation preincubated for 4 hrs before [14C]acetate addition measured after 2 hrs by scintillation counting | B | 4.03 | pIC50 | 93000 | nM | IC50 | J Med Chem (2015) 58: 778-784 [PMID:25513712] |
| ChEMBL | Inhibition of purified recombinant FASN TE activity (unknown origin) using 4-MUH as substrate preincubated for 30 mins before substrate addition measured after 1 hr by fluorescence assay | B | 4.33 | pIC50 | 46700 | nM | IC50 | J Med Chem (2015) 58: 778-784 [PMID:25513712] |
| indoleamine 2,3-dioxygenase 1/Indoleamine 2,3-dioxygenase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075294] [GtoPdb: 2829] [UniProtKB: P28776] | ||||||||
| ChEMBL | Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis | B | 4.03 | pIC50 | 94000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7641-7646 [PMID:23122865] |
| indoleamine 2,3-dioxygenase 2/Indoleamine 2,3-dioxygenase 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189159] [GtoPdb: 3019] [UniProtKB: Q8R0V5] | ||||||||
| ChEMBL | Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis | B | 5.09 | pIC50 | 8200 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7641-7646 [PMID:23122865] |
| Microtubule-associated protein tau in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293224] [UniProtKB: P10636] | ||||||||
| ChEMBL | Binding affinity to heparin induced human Tau 441 at 50 pM to 500 nM after 30 mins | B | 8.6 | pKi | 2.5 | nM | Ki | ACS Med Chem Lett (2012) 3: 936-941 [PMID:24900410] |
| NG,NG-Dimethylarginine dimethylaminohydrolase 1/N(G),N(G)-dimethylarginine dimethylaminohydrolase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6036] [GtoPdb: 1247] [UniProtKB: O94760] | ||||||||
| ChEMBL | Inhibition of recombinant human DDAH1 expressed in Escherichia coli BL21 Star (DE3) using ADMA as substrate assessed as decrease in citrulline production after 4 hrs by colorimetric method | B | 4.29 | pIC50 | 51000 | nM | IC50 | WO-2014160947-A1. Dimethylarginine Dimethylaminohydrolase inhibitors and methods of use thereof (2014) |
| ChEMBL | Inhibition of recombinant human DDAH1 by HTS analysis | B | 4.29 | pIC50 | 51000 | nM | IC50 | Bioorg Med Chem (2022) 72: 116970-116970 [PMID:36063653] |
| ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells | F | 4.2 | pIC50 | 62800 | nM | IC50 | Naunyn Schmiedebergs Arch Pharmacol (2001) 364: 551-557 [PMID:11770010] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antimicrobial activity against Plasmodium falciparum | F | 4.96 | pIC50 | 11000 | nM | IC50 | Bioorg Med Chem (2010) 18: 2225-2231 [PMID:20185316] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ATP4A/ATP4B/Potassium-transporting ATPase in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095173] [GtoPdb: 849, 851] [UniProtKB: P20648, P51164] | ||||||||
| ChEMBL | In vitro evaluation for the inhibition of H+/K+ ATPase at pH < 3 in the gastric glands of isolated rabbit stomach. | B | 6.4 | pIC50 | 398.11 | nM | IC50 | J Med Chem (1992) 35: 1049-1057 [PMID:1313110] |
| Replicase polyprotein 1ab in Middle East respiratory syndrome-related coronavirus (isolate UnitedKingdom/H123990006/2012) (Betacoronavirus England 1) (Humancoronavirus EMC) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295557] [UniProtKB: K9N7C7] | ||||||||
| ChEMBL | MERS_3CL Pro protease inhibition IC50 by FRET kind of response from peptide substrate | F | 5 | pIC50 | >10000 | nM | IC50 | Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen |
| CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523582] [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1] | ||||||||
| ChEMBL | SARS-CoV-2 3CL-Pro protease inhibition IC50 determined by FRET kind of response from peptide substrate | F | 5.8 | pIC50 | 1600 | nM | IC50 | Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen |
| ChEMBL | SARS-CoV-2 3CL-Pro protease inhibition IC50 determined by FRET kind of response from peptide substrate | F | 6.41 | pIC50 | 390 | nM | IC50 | Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen |
| sodium/potassium-transporting ATPase subunit α-1/sodium/potassium-transporting ATPase subunit β-1/sodium/potassium-transporting ATPase subunit α-3/sodium/potassium-transporting ATPase subunit β-2/sodium/potassium-transporting ATPase subunit α-2/sodium/potassium-transporting ATPase subunit β-3/sodium/potassium-transporting ATPase subunit γ/sodium/potassium-transporting ATPase subunit α-4/Sodium/potassium-transporting ATPase in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095186] [GtoPdb: 833, 837, 835, 838, 834, 839, 2610, 836] [UniProtKB: P05023, P05026, P13637, P14415, P50993, P54709, P54710, Q13733] | ||||||||
| ChEMBL | In vitro evaluation for its ability to inhibit the Na+/K+ ATPase at pH 7.4. | B | 4.4 | pIC50 | 39810.72 | nM | IC50 | J Med Chem (1992) 35: 1049-1057 [PMID:1313110] |
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]
