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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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
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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 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]