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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 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]