ChEMBL ligand: CHEMBL998 (Alavert, BAY76-2211, Children's claritin, Claritin, Claritin-D, Claritin hives relief, Claritin hives relief reditab, Claritin reditabs, Clarityn, Clarityne, Clarityn rapide, Hay-rite, Loratadine, Loratadine redidose, NSC-758628, Roletra, SCH 29851, SCH-29851)
Farnesoid X receptor/Bile acid receptor FXR in Human [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1] There should be some charts here, you may need to enable JavaScript!
CYP2C19/Cytochrome P450 2C19 in Human [ChEMBL: CHEMBL3622] [GtoPdb: 1328] [UniProtKB: P33261] There should be some charts here, you may need to enable JavaScript!
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum [ChEMBL: CHEMBL364] There should be some charts here, you may need to enable JavaScript!
PAF receptor/Platelet activating factor receptor in Human [ChEMBL: CHEMBL250] [GtoPdb: 334] [UniProtKB: P25105] There should be some charts here, you may need to enable JavaScript!
K2P9.1/Potassium channel subfamily K member 9 in Human [ChEMBL: CHEMBL2321614] [GtoPdb: 520] [UniProtKB: Q9NPC2] There should be some charts here, you may need to enable JavaScript!
Pregnane X receptor in Human [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469] There should be some charts here, you may need to enable JavaScript!
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] There should be some charts here, you may need to enable JavaScript!
B0AT2/Sodium-dependent neutral amino acid transporter B(0)AT2 in Human [ChEMBL: CHEMBL3351189] [GtoPdb: 940] [UniProtKB: Q9H2J7] There should be some charts here, you may need to enable JavaScript!
TRPV2 in Human [GtoPdb: 508] [UniProtKB: Q9Y5S1] There should be some charts here, you may need to enable JavaScript!

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 to human H1 histamine receptor expressed in CHO cells after 1 hr by calcium 5 dye-based FLIPR assay	B	6.72	pKd	190	nM	Kd	J Med Chem (2020) 63: 7268-7292 [PMID:32462865]
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]
TRPV2 in Human [GtoPdb: 508] [UniProtKB: Q9Y5S1]
GtoPdb	-	-	5.52	pIC50	3000	nM	IC50	Eur J Pharmacol (2022) 928: 175086 [PMID:35714693]

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]