cetirizine [Ligand Id: 1222] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1000 (AC-170, Cetiderm, Cetirizine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 4.5 | pIC50 | 31622.78 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
| ChEMBL | Inhibition of human Potassium channel HERG expressed in mammalian cells | B | 4.52 | pIC50 | 30199.52 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512] |
| ChEMBL | Inhibitory concentration against potassium channel HERG | B | 4.52 | pIC50 | 30199.52 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
| ChEMBL | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | B | 4.52 | pIC50 | 30199.52 | nM | IC50 | Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342] |
| ChEMBL | Inhibition of human ERG potassium channel in HEK293 cells by patch clamp assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5507-5512 [PMID:16931010] |
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | Displacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation counting | B | 7.1 | pKi | 79.43 | nM | Ki | Nat Chem Biol (2005) 1: 98-103 [PMID:16408006] |
| ChEMBL | Displacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation counting | B | 7.2 | pKi | 63.1 | nM | Ki | Nat Chem Biol (2005) 1: 98-103 [PMID:16408006] |
| ChEMBL | Displacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation counting | B | 7.2 | pKi | 63.1 | nM | Ki | Nat Chem Biol (2005) 1: 98-103 [PMID:16408006] |
| ChEMBL | Displacement of [3H]mepyramine from human histamine H1 receptor S3.36A mutant expressed in COS-7 cells by liquid scintillation counting | B | 7.3 | pKi | 50.12 | nM | Ki | Nat Chem Biol (2005) 1: 98-103 [PMID:16408006] |
| ChEMBL | Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting | B | 7.3 | pKi | 50.12 | nM | Ki | Nat Chem Biol (2005) 1: 98-103 [PMID:16408006] |
| ChEMBL | Displacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation counting | B | 7.5 | pKi | 31.62 | nM | Ki | Nat Chem Biol (2005) 1: 98-103 [PMID:16408006] |
| ChEMBL | Displacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation counting | B | 7.5 | pKi | 31.62 | nM | Ki | Nat Chem Biol (2005) 1: 98-103 [PMID:16408006] |
| ChEMBL | In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 2265-2268 [PMID:15081022] |
| ChEMBL | Inhibition constant against histamine H1 receptor | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
| ChEMBL | Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cells | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5591-5594 [PMID:15482930] |
| GtoPdb | - | - | 8.2 | pKi | - | - | - | Eur J Biochem (1994) 224: 489-95 [PMID:7925364] |
| ChEMBL | Binding affinity for human Histamine H1 receptor in CHO K1 cells | B | 8.23 | pKi | 5.89 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1083-1085 [PMID:15686917] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | DNDI: Malaria in Vitro, 72 hour | F | 4.7 | pIC50 | 19980 | nM | IC50 | Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning |
| TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] | ||||||||
| ChEMBL | Binding affinity to human recombinant Tie2 by SPR assay | B | 4.05 | pKd | 90000 | nM | Kd | Bioorg Med Chem Lett (2012) 22: 2388-2392 [PMID:22406116] |
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]
