PG01037 [Ligand Id: 6675] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL180010
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/D(3) dopamine receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/D(4) dopamine receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/5-hydroxytryptamine receptor 1A 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/5-hydroxytryptamine receptor 2A 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/5-hydroxytryptamine receptor 2C 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]
D2 receptor/D(2) dopamine 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/D(3) dopamine 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/D(4) dopamine 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]

ChEMBL data shown on this page come from version 36:

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]