loratadine [Ligand Id: 7216] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL998 (Roletra, Claritin hives relief reditab, Clarityn rapide, Loratadine, Alavert, SCH-29851, Claritin hives relief, Claritin-D, Children's claritin, Claritin, BAY76-2211, Hay-rite, Loratadine redidose, Clarityne, SCH 29851, Claritin reditabs, Clarityn)
  • Farnesoid X receptor/Bile acid receptor FXR in Human [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
  • Histamine H1 receptor in Guinea pig [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
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  • PAF receptor/Platelet activating factor receptor in Human [ChEMBL: CHEMBL250] [GtoPdb: 334] [UniProtKB: P25105]
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  • K2P9.1/Potassium channel subfamily K member 9 in Human [ChEMBL: CHEMBL2321614] [GtoPdb: 520] [UniProtKB: Q9NPC2]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • B0AT2/Sodium-dependent neutral amino acid transporter B(0)AT2 in Human [ChEMBL: CHEMBL3351189] [GtoPdb: 940] [UniProtKB: Q9H2J7]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Farnesoid X receptor/Bile acid receptor FXR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
ChEMBL Antagonist activity at human GTS-tagged FXR after 20 mins by TR-FRET assay B 5.51 pIC50 3070 nM IC50 Bioorg. Med. Chem. (2013) 21: 4266-4278 [PMID:23688559]
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 7.8 pIC50 16 nM IC50 DrugMatrix in vitro pharmacology data
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 4.49 pKi 32022.8 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 4.41 pIC50 39086.6 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of human ERG in MCF7 cells B 6.76 pIC50 173.78 nM IC50 Eur. J. Med. Chem. (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL Inhibition of human ERG B 6.76 pIC50 173.78 nM IC50 Eur. J. Med. Chem. (2011) 46: 618-630 [PMID:21185626]
ChEMBL K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 F 6.76 pIC50 173 nM IC50 J. Med. Chem. (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 6.77 pIC50 169.82 nM IC50 Bioorg. Med. Chem. (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 6.77 pIC50 169.82 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibitory concentration against potassium channel HERG B 6.77 pIC50 169.82 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2886-2890 [PMID:15911273]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cells B 6.38 pKi 414 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 5591-5594 [PMID:15482930]
ChEMBL Displacement of [3H]mepyramine from human histamine H1 receptor expressed in Sf9 cells by scintillation counting method B 6.51 pKi 311 nM Ki J. Med. Chem. (2014) 57: 9473-9479 [PMID:25318072]
GtoPdb - - 7.43 pKi 37 nM Ki J Med Chem (2005) 48: 2154-66 [PMID:15771458]
ChEMBL Binding affinity for H1 histamine receptor expressed in CHO cells B 7.43 pKi 37 nM Ki J. Med. Chem. (2005) 48: 2154-2166 [PMID:15771458]
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 7.7 pKi 20 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibitory concentration against histamine H1 receptor B 6.54 pIC50 290 nM IC50 J. Med. Chem. (2005) 48: 6523-6543 [PMID:16220969]
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 6.77 pIC50 170 nM IC50 DrugMatrix in vitro pharmacology data
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand B 6.46 pKi 350 nM Ki J. Med. Chem. (1991) 34: 457-461 [PMID:1671420]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions B 7.14 pKd 72.44 nM Kd Bioorg. Med. Chem. Lett. (2015) 25: 1436-1442 [PMID:25752982]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin efflux (Daunorubicin: ? uM) in G185 cells F 4.94 pIC50 11400 nM IC50 Drug Metab. Dispos. (2001) 29: 1080-1083 [PMID:11454724]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
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 D10 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 Dd2 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 5.2 pIC50 6309.57 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 5.3 pIC50 5011.87 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 5.7 pIC50 1995.26 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
PAF receptor/Platelet activating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL250] [GtoPdb: 334] [UniProtKB: P25105]
ChEMBL Concentration required to cause 50% inhibition of platelet activating factor (PAF)-induced platelet aggregation of human platelet rich plasma when challenged with 25 nM PAF. F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (1991) 34: 457-461 [PMID:1671420]
K2P9.1/Potassium channel subfamily K member 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321614] [GtoPdb: 520] [UniProtKB: Q9NPC2]
ChEMBL Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay B 4.2 pIC50 63400 nM IC50 J Med Chem (2019) 62: 10044-10058 [PMID:31260312]
Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469]
ChEMBL Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay B 5.52 pEC50 3000 nM EC50 Bioorg. Med. Chem. (2013) 21: 4266-4278 [PMID:23688559]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.81 pKi 156 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.61 pIC50 245 nM IC50 DrugMatrix in vitro pharmacology data
B0AT2/Sodium-dependent neutral amino acid transporter B(0)AT2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3351189] [GtoPdb: 940] [UniProtKB: Q9H2J7]
ChEMBL Inhibition of eGFP-tagged human B0AT2 expressed in HEK293 cells measured within 10 mins by [3H]proline uptake assay B 5.4 pIC50 4000 nM IC50 J. Med. Chem. (2014) 57: 9473-9479 [PMID:25318072]
GtoPdb - - 5.4 pIC50 4000 nM IC50 J Med Chem (2014) 57: 9473-9 [PMID:25318072]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]