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ChEMBL ligand: CHEMBL300780 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
ChEMBL | Compound was evaluated for binding affinity against Dopamine receptor D1 transfected in CHO cell membranes | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2715-2718 [PMID:9873609] |
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 | 6.16 | pKi | 698 | nM | Ki | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
ChEMBL | Compound was evaluated for binding affinity against Dopamine receptor D2 subtype from primate | B | 6.66 | pKi | 217 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2715-2718 [PMID:9873609] |
ChEMBL | Inhibition of [125I]IABN binding to human Dopamine D2L receptor expressed in HEK 293 cells | B | 6.95 | pKi | 112 | nM | Ki | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
ChEMBL | Displacement of [125I]-IABN from human dopamine D2L receptor expressed in HEK293 cells after 60 mins by gamma counting | B | 6.95 | pKi | 112 | nM | Ki | J Med Chem (2011) 54: 3581-3594 [PMID:21495689] |
ChEMBL | Displacement of [125I]ABN from human dopamine D2L receptor expressed in HEK293 cells after 60 mins by gamma counting analysis | B | 6.95 | pKi | 112 | nM | Ki | Bioorg Med Chem (2013) 21: 2988-2998 [PMID:23618707] |
ChEMBL | Displacement of [125I]IABN from human dopamine D2 receptor expressed in HEK293 cells | B | 6.95 | pKi | 112 | nM | Ki | J Med Chem (2007) 50: 4135-4146 [PMID:17672446] |
ChEMBL | Binding affinity for human dopamine D2 receptor | B | 6.95 | pKi | 112 | nM | Ki | J Med Chem (2005) 48: 839-848 [PMID:15689168] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cells | B | 7.26 | pKi | 54.7 | 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 | 5.89 | pIC50 | 1280 | 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 | 5.89 | pIC50 | 1280 | nM | IC50 | J Med Chem (2007) 50: 4135-4146 [PMID:17672446] |
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
ChEMBL | Binding affinity towards rat Dopamine receptor D2 in Sf9 cells expressing in recombinant baculovirus (Bv) using [125I]IABN as radioligand | B | 6.04 | pKi | 911 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2179-2183 [PMID:12798330] |
ChEMBL | Inhibition of [125I]IABN binding to rat Dopamine D2L receptor expressed in HEK 293 cells | B | 6.04 | pKi | 911 | nM | Ki | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
ChEMBL | Binding affinity at dopamine receptor D2 on Sf9 cells by [125I]IABN displacement. | B | 6.66 | pKi | 217 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 195-202 [PMID:14684327] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assay | F | 8.7 | pKd | 2 | nM | Kd | J Med Chem (2005) 48: 7919-7922 [PMID:16335915] |
ChEMBL | Inhibition of [3H]YM-09151-2 binding to human Dopamine D3 receptor expressed in CHO cells | B | 8.57 | pKi | 2.7 | 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 after 60 mins by gamma counting | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2011) 54: 3581-3594 [PMID:21495689] |
ChEMBL | Binding affinity for human dopamine D3 receptor | B | 8.7 | pKi | 2 | 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 | 8.7 | pKi | 2 | 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 | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2007) 50: 4135-4146 [PMID:17672446] |
ChEMBL | Displacement of [3H]spiroperidol from cloned human dopamine receptor D3 in CHO cell membrane | B | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2005) 48: 7919-7922 [PMID:16335915] |
GtoPdb | - | - | 8.8 | pKi | - | - | - | CNS Drug Rev (2007) 13: 240-59 [PMID:17627675] |
ChEMBL | Compound was evaluated for binding affinity against human Dopamine receptor D3 transfected in CHO cell membranes to stimulate [3H]thymidine uptake | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2715-2718 [PMID:9873609] |
ChEMBL | Displacement of [125I]ABN from human dopamine D3 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem (2013) 21: 2988-2998 [PMID:23618707] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cells | B | 9.63 | pKi | 0.23 | 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 | 7.84 | pIC50 | 14.4 | 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 | 7.84 | pIC50 | 14.4 | nM | IC50 | J Med Chem (2007) 50: 4135-4146 [PMID:17672446] |
ChEMBL | Antagonist activity against 100 nM quinpirole-stimulated mitogenesis in CHO cells expressing human dopamine D3 receptor | F | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
ChEMBL | Binding affinity at dopamine receptor D3 on Sf9 cells by [125I]IABN displacement. | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 195-202 [PMID:14684327] |
ChEMBL | Binding affinity towards rat Dopamine receptor D3 in Sf9 cells expressing in recombinant baculovirus (Bv) using [125I]IABN as radioligand | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2179-2183 [PMID:12798330] |
ChEMBL | Inhibition of [125I]IABN binding to rat Dopamine D3 receptor expressed in HEK 293 cells | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | Compound was evaluated for binding affinity against human Dopamine receptor D4 transfected in CHO cell membranes | B | 5.3 | pKi | >5000 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2715-2718 [PMID:9873609] |
ChEMBL | Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells | B | 5.3 | pKi | >5000 | nM | Ki | J Med Chem (2005) 48: 3663-3679 [PMID:15916415] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells | B | 5.44 | pKi | 3670 | nM | Ki | J Med Chem (2015) 58: 5361-5380 [PMID:25826710] |
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
ChEMBL | Compound was evaluated for binding affinity against human Dopamine receptor D5 transfected in CHO cell membranes | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2715-2718 [PMID:9873609] |
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 | 5.69 | pKi | 2040 | 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 | 6.17 | pKi | 679 | 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 | 6.39 | pKi | 411 | 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]