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

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ChEMBL ligand: CHEMBL180010 (PG-01037)
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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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
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 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]