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ChEMBL ligand: CHEMBL180010 (PG-01037) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Inhibition of [3H]YM-09151-2 binding to human Dopamine D2L receptor expressed in CHO cells | B | 6.97 | pKi | 106 | nM | Ki | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
ChEMBL | Binding affinity for human dopamine D2 receptor | B | 7.03 | pKi | 93.3 | nM | Ki | J Med Chem (2005) 48: 839-848 [PMID:15689168] |
ChEMBL | Inhibition of [125I]IABN binding to human Dopamine D2L receptor expressed in HEK 293 cells | B | 7.03 | pKi | 93.3 | nM | Ki | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
ChEMBL | Displacement of [125I]IABN from human dopamine D2 receptor expressed in HEK293 cells | B | 7.03 | pKi | 93.3 | nM | Ki | J Med Chem (2007) 50: 4135-4146 [PMID:17672446] |
ChEMBL | Displacement of [125I]-IABN from human dopamine D2L receptor expressed in HEK293 cells after 60 mins by gamma counting | B | 7.03 | pKi | 93.3 | nM | Ki | J Med Chem (2011) 54: 3581-3594 [PMID:21495689] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cells | B | 7.13 | pKi | 74 | nM | Ki | J Med Chem (2015) 58: 5361-5380 [PMID:25826710] |
ChEMBL | Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D2 receptor | F | 7.09 | pIC50 | 80.9 | nM | IC50 | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
ChEMBL | Antagonist activity at human dopamine D2 receptor expressed in HEK293 cells by mitogenesis assay | F | 7.09 | pIC50 | 80.9 | nM | IC50 | J Med Chem (2007) 50: 4135-4146 [PMID:17672446] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | Inhibition of [3H]YM-09151-2 binding to human Dopamine D3 receptor expressed in CHO cells | B | 8.68 | pKi | 2.11 | nM | Ki | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
ChEMBL | Binding affinity for human dopamine D3 receptor | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2005) 48: 839-848 [PMID:15689168] |
ChEMBL | Inhibition of [125I]IABN binding to human Dopamine D3 receptor expressed in HEK 293 cells | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
ChEMBL | Displacement of [125I]IABN from human dopamine D3 receptor expressed in HEK293 cells | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2007) 50: 4135-4146 [PMID:17672446] |
ChEMBL | Displacement of [125I]-IABN from human dopamine D3 receptor expressed in HEK293 cells after 60 mins by gamma counting | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2011) 54: 3581-3594 [PMID:21495689] |
GtoPdb | - | - | 9.2 | pKi | - | - | - | J Med Chem (2007) 50: 4135-46 [PMID:17672446] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cells | B | 9.5 | pKi | 0.32 | nM | Ki | J Med Chem (2015) 58: 5361-5380 [PMID:25826710] |
ChEMBL | Mitogenic stimulation or antagonism of 30 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor | F | 8.52 | pIC50 | 3.01 | nM | IC50 | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
ChEMBL | Antagonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay | F | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2007) 50: 4135-4146 [PMID:17672446] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells | B | 6.26 | pKi | 550 | nM | Ki | J Med Chem (2015) 58: 5361-5380 [PMID:25826710] |
ChEMBL | Binding affinity for human dopamine D4 receptor | B | 6.43 | pKi | 375 | nM | Ki | J Med Chem (2005) 48: 839-848 [PMID:15689168] |
ChEMBL | Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells | B | 6.43 | pKi | 375 | nM | Ki | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
ChEMBL | Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells | B | 6.43 | pKi | 375 | nM | Ki | J Med Chem (2007) 50: 4135-4146 [PMID:17672446] |
ChEMBL | Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting | B | 6.43 | pKi | 375 | nM | Ki | J Med Chem (2011) 54: 3581-3594 [PMID:21495689] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | Binding affinity to human 5HT1A receptor | B | 7.07 | pKi | 85.4 | nM | Ki | J Med Chem (2007) 50: 4135-4146 [PMID:17672446] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
ChEMBL | Binding affinity to human 5HT2A receptor | B | 7.2 | pKi | 62.4 | nM | Ki | J Med Chem (2007) 50: 4135-4146 [PMID:17672446] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
ChEMBL | Binding affinity to human 5HT2C receptor | B | 7.33 | pKi | 47 | nM | Ki | J Med Chem (2007) 50: 4135-4146 [PMID:17672446] |
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]