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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL300780
  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
There should be some charts here, you may need to enable JavaScript!
  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
There should be some charts here, you may need to enable JavaScript!
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 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]