indacaterol [Ligand Id: 7455] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1095777 (Indacaterol, Indacterol, Onbrez, QAB-149, QAB149, QABI49) |
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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 | PDSP Secondary Binding target: ADRA1A - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.45 | pKi | 355.59 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | PDSP Secondary Binding target: ADRA1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.36 | pKi | 4322.65 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| ChEMBL | PDSP Secondary Binding target: ADRA1D - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.14 | pKi | 731.31 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
| GtoPdb | - | - | 6.7 | pKi | 180 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 6280-5 [PMID:22932315] |
| ChEMBL | Displacement of [3H]CGP12177 from human beta-1 adrenoceptor | B | 7.04 | pKi | 91.4 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 5302-5307 [PMID:20655218] |
| ChEMBL | Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay | B | 7.04 | pKi | 91 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4341-4347 [PMID:25065493] |
| ChEMBL | Binding affinity to beta1 adrenoceptor | B | 6.5 | pIC50 | 316.23 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 689-695 [PMID:22079756] |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | PDSP Secondary Binding target: ADRB2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.97 | pKi | 105.96 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| ChEMBL | Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay | B | 7.12 | pKi | 76 | nM | Ki | J Med Chem (2010) 53: 3675-3684 [PMID:20402514] |
| ChEMBL | Displacement of [3H]CGP12177 from human beta2 adrenoceptor | B | 7.69 | pKi | 20.6 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 5302-5307 [PMID:20655218] |
| ChEMBL | Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay | B | 7.69 | pKi | 20.6 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4341-4347 [PMID:25065493] |
| GtoPdb | - | - | 7.8 | pKi | - | - | - |
Bioorg Med Chem Lett (2012) 22: 6280-5 [PMID:22932315]; J Pharmacol Exp Ther (2006) 317: 762-70 [PMID:16434564] |
| ChEMBL | GPCR PRESTO-Tango dose-response in agonist mode with target: ADRB2 | F | 7.08 | pEC50 | 83.28 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| ChEMBL | Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry | F | 7.8 | pEC50 | 15.85 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 689-695 [PMID:22079756] |
| ChEMBL | Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay | F | 7.96 | pEC50 | 11 | nM | EC50 | J Med Chem (2010) 53: 3675-3684 [PMID:20402514] |
| GtoPdb | - | - | 8.1 | pEC50 | - | - | - | J Pharmacol Exp Ther (2006) 317: 762-70 [PMID:16434564] |
| ChEMBL | Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level | F | 8.82 | pEC50 | 1.5 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4341-4347 [PMID:25065493] |
| ChEMBL | Agonist activity at beta2 adrenoceptor (unknown origin) | F | 9.1 | pEC50 | 0.79 | nM | EC50 | J Med Chem (2020) 63: 15218-15242 [PMID:33213146] |
| Beta-2 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4] | ||||||||
| ChEMBL | Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins | F | 8.1 | pIC50 | 7.9 | nM | IC50 | J Med Chem (2010) 53: 3675-3684 [PMID:20402514] |
| ChEMBL | Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction | B | 8.1 | pIC50 | 7.9 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4341-4347 [PMID:25065493] |
| CYP1B1/Cytochrome P450 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4878] [GtoPdb: 1320] [UniProtKB: Q16678] | ||||||||
| ChEMBL | Inhibition of human CYP1B1 using 7-ethyl-O-resorufin as substrate incubated for 30 mins in presence of NADPH by EROD assay | B | 4.23 | pIC50 | 59200 | nM | IC50 | Eur J Med Chem (2020) 193: 112235-112235 [PMID:32203789] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Activity at human D2R expressed in CHO cells by radiolabelled [35S]GTPgammaS assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4341-4347 [PMID:25065493] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | PDSP Secondary Binding target: DRD3 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.87 | pKi | 1339.37 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| ChEMBL | Displacement of [125I]7-HO-PIPAT from human D3R expressed in HEK cells | B | 5.98 | pKi | 1048 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4341-4347 [PMID:25065493] |
| DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
| ChEMBL | PDSP Secondary Binding target: SLC6A3 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 7.12 | pKi | 75.02 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | PDSP Secondary Binding target: SLC6A2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.25 | pKi | 568.66 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| Serine/arginine-rich splicing factor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5169149] [UniProtKB: Q13247] | ||||||||
| ChEMBL | Inhibition of SRSF6 (unknown origin) | B | 4.72 | pIC50 | 19010 | nM | IC50 | Bioorg Med Chem (2022) 70: 116921-116921 [PMID:35863237] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | PDSP Secondary Binding target: HTR2A - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.69 | pKi | 2019.53 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | PDSP Secondary Binding target: HTR2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.74 | pKi | 1800.32 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | PDSP Secondary Binding target: HTR6 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5 | pKi | >10000 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | PDSP Secondary Binding target: SLC6A4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.11 | pKi | 770.02 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] | ||||||||
| ChEMBL | PDSP Secondary Binding target: TMEM97 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.97 | pKi | 106.86 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
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]
