omeprazole [Ligand Id: 4279] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1503 (Antra, H 168/68, H-168/68, Losec, Losec mups, Mezzopram, Mopral, NSC-751450, NSC-759192, Omeprazol, Omeprazole, Omeran, Prilosec, Zanprol) |
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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 | 4.75 | pIC50 | 17600 | nM | IC50 | Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322] |
| BB3 receptor/Bombesin receptor subtype-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4080] [GtoPdb: 40] [UniProtKB: P32247] | ||||||||
| ChEMBL | Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay | F | 4.85 | pEC50 | 14000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5451-5455 [PMID:18818070] |
| 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 | 4.6 | pIC50 | 25000 | 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 | 5.47 | pKi | 3400 | nM | Ki | 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 | 4.53 | pIC50 | 29600 | nM | IC50 | J Med Chem (2015) 58: 778-784 [PMID:25513712] |
| glutathione S-transferase omega 1/Glutathione transferase omega 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3174] [GtoPdb: 3110] [UniProtKB: P78417] | ||||||||
| ChEMBL | Inhibition of GSTO1-1 (unknown origin) by enzymatic assay | B | 5.34 | pIC50 | 4600 | nM | IC50 | J Med Chem (2018) 61: 7448-7470 [PMID:29652143] |
| 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 | 4.7 | pIC50 | 20000 | nM | IC50 | WO-2014160947-A1. Dimethylarginine Dimethylaminohydrolase inhibitors and methods of use thereof (2014) |
| ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
| ChEMBL | Concentration required for 50% inhibition at binding site of human P-Glycoprotein (P-gp) in one-affinity model | B | 4.01 | pIC50 | 97200 | nM | IC50 | J Med Chem (2002) 45: 5671-5686 [PMID:12477351] |
| ChEMBL | Concentration required for 50% inhibition at binding site of human P-Glycoprotein (P-gp) in one-affinity model | B | 4.04 | pIC50 | 91200 | nM | IC50 | J Med Chem (2002) 45: 5671-5686 [PMID:12477351] |
| ChEMBL | Concentration required for 50% inhibition at binding site of human P-Glycoprotein (P-gp) in one-affinity model | B | 4.05 | pIC50 | 89000 | nM | IC50 | J Med Chem (2002) 45: 5671-5686 [PMID:12477351] |
| ChEMBL | TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells | F | 4.75 | pIC50 | 17700 | nM | IC50 | Naunyn Schmiedebergs Arch Pharmacol (2001) 364: 551-557 [PMID:11770010] |
| Plasmodium (target type: ORGANISM) [ChEMBL: CHEMBL4888483] | ||||||||
| ChEMBL | Antimalarial activity against Plasmodium | F | 6 | pIC50 | <1000 | nM | IC50 | Eur J Med Chem (2020) 195: 112275-112275 [PMID:32283298] |
| Plasmodium berghei (target type: ORGANISM) [ChEMBL: CHEMBL612653] | ||||||||
| ChEMBL | HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells | F | 6.17 | pIC50 | 680 | nM | IC50 | Proc Natl Acad Sci U S A (2012) 109: 8511-8516 [PMID:22586124] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antimicrobial activity against Plasmodium falciparum | F | 4.12 | pIC50 | 76000 | nM | IC50 | Bioorg Med Chem (2010) 18: 2225-2231 [PMID:20185316] |
| ChEMBL | HARVARD: Inhibition of blood stage Plasmodium falciparum 3D7 infection | F | 4.3 | pIC50 | >50000 | nM | IC50 | Proc Natl Acad Sci U S A (2012) 109: 8511-8516 [PMID:22586124] |
| ChEMBL | HARVARD: Inhibition of blood stage Plasmodium falciparum Dd2 infection | F | 4.3 | pIC50 | >50000 | nM | IC50 | Proc Natl Acad Sci U S A (2012) 109: 8511-8516 [PMID:22586124] |
| ChEMBL | DNDI: Malaria in Vitro, 72 hour | F | 4.88 | pIC50 | 13230 | nM | IC50 | Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning |
| ATP4A/ATP4B/Potassium-transporting ATPase in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095173] [GtoPdb: 849, 851] [UniProtKB: P20648, P51164] | ||||||||
| ChEMBL | Compound was tested in vitro for H+/K+ ATPase activity in rabbit stomach preparations | B | 4.65 | pIC50 | 22400 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2819-2822 [PMID:10522698] |
| ChEMBL | Inhibition of H+/K+ ATPase activity in buffered solution (pH 7.4) | B | 5.42 | pIC50 | 3800 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1909-1912 [PMID:9873457] |
| ChEMBL | In vitro inhibitory activity against H+/K+ ATPase prepared from canine fundic mucosa | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (1988) 31: 1215-1220 [PMID:2836591] |
| ChEMBL | In vitro evaluation for the inhibition of H+/K+ ATPase at pH < 3 in the gastric glands of isolated rabbit stomach. | B | 6.3 | pIC50 | 501.19 | nM | IC50 | J Med Chem (1992) 35: 1049-1057 [PMID:1313110] |
| ChEMBL | Inhibition of [14C]aminopyrine (AP) accumulation stimulated by dibutyryl cyclic AMP in isolated rabbit parietal cells | F | 6.43 | pIC50 | 370 | nM | IC50 | J Med Chem (1997) 40: 313-321 [PMID:9022797] |
| ChEMBL | Antisecretory activity evaluated by the inhibition of 14C -AP uptake in isolated rabbit parietal cells stimulated by dibutyryl cyclic adenosine 3', 5' -monophosphate (dcAMP) | F | 6.55 | pIC50 | 280 | nM | IC50 | J Med Chem (1988) 31: 1778-1785 [PMID:2842503] |
| ChEMBL | Antisecretory activity evaluated by the inhibition of 14C -AP uptake in isolated rabbit parietal cells stimulated by exogenous histamine | F | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (1988) 31: 1778-1785 [PMID:2842503] |
| Potassium-transporting ATPase in Pig (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095228] [UniProtKB: P18434, P19156] | ||||||||
| ChEMBL | Activity was evaluated by measuring the inhibition of isolated hog H+/K+ ATPase | B | 4.3 | pIC50 | 50000 | nM | IC50 | J Med Chem (1991) 34: 1049-1062 [PMID:1848293] |
| ChEMBL | In vitro inhibition against H+/K+ ATPase from porcine gastric mucosal membrane vesicles | B | 5.42 | pIC50 | 3800 | nM | IC50 | J Med Chem (1996) 39: 596-604 [PMID:8558532] |
| 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 | 4.5 | pIC50 | 31622.78 | 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]
