NGB 2904 [Ligand Id: 6674] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL300780
  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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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 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]