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 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]
