azelastine [Ligand Id: 7121] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL639 (Azelastina, 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] |
| ChEMBL | Antagonist activity against recombinant human adrenergic alpha1A receptor expressed in Rat1 cells incubated for 30 mins by FLIPR analysis | B | 7.3 | pKi | 50.12 | nM | Ki | ACS Med Chem Lett (2017) 8: 577-581 [PMID:28523114] |
| 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] |
| ChEMBL | Antagonist activity against recombinant human adrenergic alpha1B receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis | B | 7.3 | pKi | 50.12 | nM | Ki | ACS Med Chem Lett (2017) 8: 577-581 [PMID:28523114] |
| 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 potency at human H1 receptor | B | 9.7 | pKd | 0.2 | nM | Kd | ACS Med Chem Lett (2017) 8: 577-581 [PMID:28523114] |
| 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] |
| ChEMBL | Antagonist activity against recombinant human H1 receptor expressed in CHO cells incubated for 30 mins by FLIPR analysis | B | 8.9 | pKi | 1.26 | nM | Ki | ACS Med Chem Lett (2017) 8: 577-581 [PMID:28523114] |
| 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 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]
