azelastine [Ligand Id: 7121] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL639 (Azelastine)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Binding affinity to human adrenergic alpha1A receptor expressed in rat intact fibroblasts B 7.3 pKi 50.12 nM Ki J. Med. Chem. (2011) 54: 2183-2195 [PMID:21381763]
ChEMBL Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imaging F 7.3 pKi 50.12 nM Ki Bioorg. Med. Chem. (2012) 20: 6097-6108 [PMID:22985961]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptor B 7.3 pKi 50.12 nM Ki Bioorg Med Chem Lett (2017) 27: 4914-4919 [PMID:28958623]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Binding affinity to human adrenergic Alpha-1B receptor expressed in rat intact fibroblasts B 7.3 pKi 50.12 nM Ki J. Med. Chem. (2011) 54: 2183-2195 [PMID:21381763]
ChEMBL Antagonist activity at human adrenergic alpha1B receptor expressed in rat fibroblasts by by plate-based calcium imaging F 7.3 pKi 50.12 nM Ki Bioorg. Med. Chem. (2012) 20: 6097-6108 [PMID:22985961]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Displacement of labeled dofetilide human ERG B 7 pIC50 100 nM IC50 J. Med. Chem. (2011) 54: 2183-2195 [PMID:21381763]
ChEMBL Displacement of [3H]dofetilide from human ERG B 7 pIC50 100 nM IC50 Bioorg. Med. Chem. (2012) 20: 6097-6108 [PMID:22985961]
ChEMBL Displacement of [3H]-dofetilide from human ERG expressed in CHOK1 cell membranes incubated for 4 hrs in dark by luminescent assay B 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (2016) 26: 5855-5859 [PMID:27866818]
ChEMBL Displacement of [3H]-Dofetilide from recombinant human ERG expressed in CHOK1 cell membranes incubated for 4 hrs under dark condition by luminescence assay B 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (2017) 27: 4914-4919 [PMID:28958623]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization at 100 nM after 30 mins by FLIPR assay F 9.7 pKd 0.2 nM Kd J. Med. Chem. (2011) 54: 2183-2195 [PMID:21381763]
ChEMBL Antagonist activity against human CHO cells H1 receptor at 100 nM after 30 mins by FLIPR assay F 9.7 pKd 0.2 nM Kd Bioorg. Med. Chem. (2012) 20: 6097-6108 [PMID:22985961]
ChEMBL Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux at 100 nM preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay B 9.7 pKd 0.2 nM Kd Bioorg Med Chem Lett (2016) 26: 5855-5859 [PMID:27866818]
ChEMBL Antagonist activity at human histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced intracellular calcium mobilization at 100 nM pretreated for 30 mins followed by histamine addition measured for 1 min by Fluo-4-AM dye based FLIPR method B 9.7 pKd 0.2 nM Kd Bioorg Med Chem Lett (2017) 27: 4914-4919 [PMID:28958623]
ChEMBL Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular calcium mobilization by FLIPR assay F 8.9 pKi 1.26 nM Ki J. Med. Chem. (2011) 54: 2183-2195 [PMID:21381763]
GtoPdb - - 8.9 pKi 1.26 nM Ki J. Med. Chem. (2011) 54: 2183-95 [PMID:21381763]
ChEMBL Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay F 8.92 pKi 1.2 nM Ki Bioorg. Med. Chem. (2012) 20: 6097-6108 [PMID:22985961]
ChEMBL Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 30 mins followed by histamine addition by Fluo-4-AM dye based FLIPR assay B 8.92 pKi 1.2 nM Ki Bioorg Med Chem Lett (2016) 26: 5855-5859 [PMID:27866818]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Antagonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as inhibition of histamine-induced GTP-gammaS binding F 6.8 pKi 158.49 nM Ki J. Med. Chem. (2011) 54: 2183-2195 [PMID:21381763]
ChEMBL Antagonist activity at human H3 receptor expressed in CHO cells assessed as inhibition of histamine-induced GTPgamma[S] binding by scintillation proximity assay F 6.83 pKi 147.91 nM Ki Bioorg. Med. Chem. (2012) 20: 6097-6108 [PMID:22985961]
ChEMBL Antagonist activity at human Histamine H3 receptor expressed in CHO cell membranes assessed as inhibition of histamine-induced [35S]GTPgammaS binding after 2 to 6 hrs by scintillation proximity assay B 6.83 pKi 147.91 nM Ki Bioorg Med Chem Lett (2016) 26: 5855-5859 [PMID:27866818]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Displacement of [3H]AF-DX 384 from recombinant human M1 receptor expressed in CHO cells B 5.2 pIC50 6309.57 nM IC50 Bioorg Med Chem Lett (2017) 27: 4914-4919 [PMID:28958623]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.025 uM) in MDR1-expressing LLC-PK1 cells F 4.52 pIC50 30000 nM IC50 Eur. J. Pharm. Sci. (2001) 12: 505-513 [PMID:11231118]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells F 4.8 pIC50 16000 nM IC50 Eur. J. Pharm. Sci. (2001) 12: 505-513 [PMID:11231118]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cells B 7.7 pKi 19.95 nM Ki Bioorg Med Chem Lett (2017) 27: 4914-4919 [PMID:28958623]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Displacement of [3H]mesulergine from recombinant human 5-ht2C expressed in CHO cells B 6.3 pKi 501.19 nM Ki Bioorg Med Chem Lett (2017) 27: 4914-4919 [PMID:28958623]
Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
ChEMBL Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes F 4.69 pIC50 20200 nM IC50 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]
ChEMBL Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in guinea pig tracheal smooth muscle cells F 5.1 pIC50 8000 nM IC50 IC50 data for the L-type calcium channel extracted from a set of literature articles

ChEMBL data shown on this page come from version 26:

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]