sumanirole [Ligand Id: 3949] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL419792 (Pnu-95666, PNU-95666E, Sumanirole) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Displacement of [3H]N-methylspiperone from human D2 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter | B | 4.79 | pKi | 16300 | nM | Ki | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Displacement of [3H]-(R)-(+)-7-OH-DPAT from human dopamine D2 receptor expressed in HEK293 cell membranes after 90 mins by micro beta scintillation counting analysis | B | 7.33 | pKi | 46.3 | nM | Ki | J Med Chem (2017) 60: 2890-2907 [PMID:28300398] |
| ChEMBL | Displacement of [3H]7-OH-DPAT from human D2 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter | B | 7.77 | pKi | 17.1 | nM | Ki | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Binding affinity towards Dopamine receptor D2 by displacement of [3H]U-86170. | B | 8.05 | pKi | 9 | nM | Ki | J Med Chem (1997) 40: 639-646 [PMID:9057850] |
| GtoPdb | - | - | 8.1 | pKi | 9 | nM | Ki | J Pharmacol Exp Ther (2005) 314: 1248-56 [PMID:15980060] |
| ChEMBL | Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assay | B | 6.26 | pEC50 | 543.3 | nM | EC50 | J Med Chem (2017) 60: 2890-2907 [PMID:28300398] |
| ChEMBL | Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay | B | 6.3 | pEC50 | 501.2 | nM | EC50 | J Med Chem (2017) 60: 2890-2907 [PMID:28300398] |
| ChEMBL | In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D2 using FLIPR assay | F | 6.78 | pEC50 | 165 | nM | EC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| ChEMBL | Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assay | B | 7.13 | pEC50 | 74.8 | nM | EC50 | J Med Chem (2017) 60: 2890-2907 [PMID:28300398] |
| ChEMBL | Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry | B | 7.19 | pEC50 | 64.7 | nM | EC50 | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay | B | 7.22 | pEC50 | 60.1 | nM | EC50 | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay | F | 7.49 | pEC50 | 32.2 | nM | EC50 | J Med Chem (2017) 60: 2890-2907 [PMID:28300398] |
| ChEMBL | Agonist activity at recombinant human D2 receptor expressing in CHO cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation by beta plate counter | B | 8.34 | pEC50 | 4.6 | nM | EC50 | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assay | F | 7.46 | pEC50 | 35 | nM | EC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| ChEMBL | In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay | F | 7.97 | pEC50 | 10.8 | nM | EC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Displacement of [3H]N-methylspiperone from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter | B | 5.2 | pKi | 6330 | nM | Ki | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Binding affinity towards Dopamine receptor D3 by displacement of [3H](+)-7-OH-DPAT. | B | 5.63 | pKi | 2333 | nM | Ki | J Med Chem (1997) 40: 639-646 [PMID:9057850] |
| ChEMBL | Displacement of [3H]-(R)-(+)-7-OH-DPAT from human dopamine D3 receptor expressed in HEK293 cell membranes after 90 mins by micro beta scintillation counting analysis | B | 6.24 | pKi | 573 | nM | Ki | J Med Chem (2017) 60: 2890-2907 [PMID:28300398] |
| ChEMBL | Displacement of [3H]7-OH-DPAT from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter | B | 6.26 | pKi | 546 | nM | Ki | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry | B | 6.17 | pEC50 | 669 | nM | EC50 | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay | B | 6.73 | pEC50 | 186 | nM | EC50 | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| 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 | 7.14 | pKi | 73 | nM | Ki | J Med Chem (1997) 40: 639-646 [PMID:9057850] |
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]
