ropinirole [Ligand Id: 7295] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL589 (NSC-758917, Requip, Ropinirole, SK&F 101468) |
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| 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 | F | 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 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]
