ropinirole [Ligand Id: 7295] 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: CHEMBL589 (SK&F-101468, Ropinirole, Requip)
  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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]
  • Dopamine D2 receptor in Bovine [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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]
  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
There should be some charts here, you may need to enable JavaScript!
  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
There should be some charts here, you may need to enable JavaScript!
  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Binding affinity to human dopamine D1 receptor B 4.49 pKi 32500 nM Ki MedChemComm (2014) 5: 891-898
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [3H]spiperone form human cloned dopamine D2L receptor expressed in CHO cells B 6.16 pKi 691.83 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 2133-2138 [PMID:19324548]
GtoPdb - - 8.14 pKi 7.2 nM Ki J. Med. Chem. (1997) 40: 639-46 [PMID:9057850]
ChEMBL Binding affinity towards Dopamine receptor D2 by displacement of [3H]U-86170. B 8.14 pKi 7.2 nM Ki J. Med. Chem. (1997) 40: 639-646 [PMID:9057850]
ChEMBL Binding affinity to human dopamine D2 receptor B 8.43 pKi 3.7 nM Ki MedChemComm (2014) 5: 891-898
ChEMBL Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assay B 6.48 pEC50 330 nM EC50 J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding F 6.52 pEC50 304 nM EC50 J. Med. Chem. (2010) 53: 1023-1037 [PMID:20038106]
ChEMBL Agonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay F 6.52 pEC50 304 nM EC50 J. Med. Chem. (2010) 53: 2114-2125 [PMID:20146482]
ChEMBL Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding F 6.52 pEC50 304 nM EC50 Bioorg. Med. Chem. (2010) 18: 5661-5674 [PMID:20605099]
ChEMBL Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay F 6.52 pEC50 304 nM EC50 J. Med. Chem. (2015) 58: 718-738 [PMID:25490054]
ChEMBL Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay F 6.52 pEC50 302 nM EC50 J. Med. Chem. (2015) 58: 718-738 [PMID:25490054]
ChEMBL Agonist activity at human D2SR expressed in HEK293 cells incubated for 5 hrs by beta-Arrestin 2 recruitment assay B 7.05 pEC50 89 nM EC50 Bioorg Med Chem (2017) 25: 5613-5628 [PMID:28870802]
ChEMBL Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay B 7.05 pEC50 89 nM EC50 J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation F 7.08 pEC50 83 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 6691-6696 [PMID:17976986]
ChEMBL Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay B 7.52 pEC50 30 nM EC50 J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay B 8.19 pEC50 6.46 nM EC50 US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
ChEMBL Displacement of [3H]spiroperidol from homogenized bovine pituitary Dopamine receptor D2 B 5.17 pIC50 6810 nM IC50 J. Med. Chem. (1987) 30: 1166-1176 [PMID:2955118]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Displacement of [3H]spiperone from rat D2 receptor expressed in HEK293 cells B 5.57 pKi 2674 nM Ki Bioorg. Med. Chem. (2010) 18: 5661-5674 [PMID:20605099]
ChEMBL Displacement of [3H]spiperone from rat cloned dopamine D2L receptor expressed in HEK293 cells after 1 hr B 5.57 pKi 2674 nM Ki Bioorg. Med. Chem. (2013) 21: 3164-3174 [PMID:23623679]
ChEMBL Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting B 5.74 pIC50 1803 nM IC50 Med Chem Res (2004) 13: 25-33
ChEMBL Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min F 7.12 pEC50 75.5 nM EC50 Med Chem Res (2004) 13: 25-33
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Agonist activity at dopamine D3 receptor (unknown origin) B 7.21 pKi 61 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 5586-5591 [PMID:24012118]
ChEMBL Displacement of [3H]spiperone form human cloned dopamine D3 receptor expressed in CHO cells B 7.44 pKi 36.31 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 2133-2138 [PMID:19324548]
GtoPdb - - 7.72 pKi 19 nM Ki J. Med. Chem. (1997) 40: 639-46 [PMID:9057850]
ChEMBL Binding affinity towards Dopamine receptor D3 by displacement of [3H](+)-7-OH-DPAT. B 7.72 pKi 19 nM Ki J. Med. Chem. (1997) 40: 639-646 [PMID:9057850]
ChEMBL Binding affinity to human dopamine D3 receptor B 8.54 pKi 2.9 nM Ki MedChemComm (2014) 5: 891-898
ChEMBL Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding F 7.72 pEC50 19.2 nM EC50 J. Med. Chem. (2010) 53: 1023-1037 [PMID:20038106]
ChEMBL Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay F 7.99 pEC50 10.3 nM EC50 J. Med. Chem. (2010) 53: 2114-2125 [PMID:20146482]
ChEMBL Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding F 7.99 pEC50 10.3 nM EC50 Bioorg. Med. Chem. (2010) 18: 5661-5674 [PMID:20605099]
ChEMBL Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation F 8.4 pEC50 4 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 6691-6696 [PMID:17976986]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL Displacement of [3H]spiperone from rat D3 receptor expressed in HEK293 cells B 7.53 pKi 29.3 nM Ki Bioorg. Med. Chem. (2010) 18: 5661-5674 [PMID:20605099]
ChEMBL Displacement of [3H]spiperone from rat cloned dopamine D3 receptor expressed in HEK293 cells after 1 hr B 7.53 pKi 29.3 nM Ki Bioorg. Med. Chem. (2013) 21: 3164-3174 [PMID:23623679]
ChEMBL Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting B 6.97 pIC50 107 nM IC50 Med Chem Res (2004) 13: 25-33
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Binding affinity to human dopamine D4 receptor B 8.11 pKi 7.8 nM Ki MedChemComm (2014) 5: 891-898
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
ChEMBL Binding affinity to human dopamine D5 receptor B 4.38 pKi 41211 nM Ki MedChemComm (2014) 5: 891-898
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity towards Serotonin 5-hydroxytryptamine 1A receptor by displacement of [3H]-(+)-8-OH-DPAT. B 5.77 pKi 1706 nM Ki J. Med. Chem. (1997) 40: 639-646 [PMID:9057850]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay B 6.85 pEC50 141.25 nM EC50 US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)

ChEMBL data shown on this page come from version 27:

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]