indacaterol [Ligand Id: 7455] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1095777 (Indacaterol, QAB149, QAB-149, QABI49)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
  • 7.04
1 CHEMBL1095777_lig_chart_1 Beta-1 adrenergic receptor Human
There should be some charts here, you may need to enable JavaScript!
  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
  • Beta-2 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4]
  • 0
2 CHEMBL1095777_lig_chart_2 Beta-2 adrenergic receptor HumanGuinea pig
There should be some charts here, you may need to enable JavaScript!
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • This target only has 0 pki data point
  • 0
3 CHEMBL1095777_lig_chart_3 Dopamine D2 receptor Human
There should be some charts here, you may need to enable JavaScript!
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
  • This target only has 1 pki data point
  • 5.98
4 CHEMBL1095777_lig_chart_4 Dopamine D3 receptor Human
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
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 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 15.9 nM Ki Bioorg Med Chem Lett (2012) 22: 6280-5 [PMID:22932315]
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]
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]
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]
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 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]

ChEMBL data shown on this page come from version 28:

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]