azelastine [Ligand Id: 7121] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL639 (Azelastine, NSC-758971) |
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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 | F | 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 | F | 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 | F | 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 | F | 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 | J Appl Toxicol (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 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]
