GSK1331268 [Ligand Id: 6253] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL595759 (GSK1331268)
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
Created with Highcharts 10.3.3ValuesChart context menuDopamine D2 receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
Created with Highcharts 10.3.3ValuesChart context menuDopamine D3 receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
Created with Highcharts 10.3.3ValuesChart context menuDopamine D4 receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
Created with Highcharts 10.3.3ValuesChart context menuMetabotropic glutamate receptor 2pKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
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 Antagonist activity at human D2 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay F 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2010) 20: 759-762 [PMID:20005096]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Antagonist activity at human D3 receptor expressed in CHO cells co-expressing G0 by [35S]GTPgammaS binding assay F 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2010) 20: 759-762 [PMID:20005096]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay F 5.6 pKi 2511.89 nM Ki Bioorg Med Chem Lett (2010) 20: 759-762 [PMID:20005096]
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
ChEMBL Agonist activity at human mGluR2 expressed in CHO cells co-expressing Ga16 G-protein assessed as glutamate-induced response by FLIPR assay F 5.9 pEC50 1258.93 nM EC50 Bioorg Med Chem Lett (2010) 20: 759-762 [PMID:20005096]
GtoPdb - - 6.9 pEC50 125 nM EC50 Bioorg Med Chem Lett (2010) 20: 759-62 [PMID:20005096]
ChEMBL Positive modulation of human mGluR2 expressed in CHO cells co-expressing Ga16 G-protein assessed as glutamate-induced response by FLIPR assay B 6.9 pEC50 125.89 nM EC50 Bioorg Med Chem Lett (2010) 20: 759-762 [PMID:20005096]

ChEMBL data shown on this page come from version 35:

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]