GSK1482160 [Ligand Id: 10504] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1222883 (Gsk-1482160, Gsk1482160, GSK1482160)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
P2X7/P2X purinoceptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572]
GtoPdb Binding affinity determined in a radioligand binding assay. - 8.94 pKd 1.15 nM Kd J Nucl Med (2017) 58: 458-465 [PMID:27765863]
ChEMBL Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell membrane incubated for 1 hr by microplate scintillation counting method B 7.17 pKi 68 nM Ki J Med Chem (2020) 63: 2074-2094 [PMID:31525963]
ChEMBL Displacement of [3H]-A-804598 from human P2X7 receptor expressed in HEK293 cell membrane by in vitro binding assay B 8.24 pKi 5.7 nM Ki J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
ChEMBL Competitive displacement of [11C]GSK1482160 from human recombinant P2X7 receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method based radioligand competitive binding assay B 8.51 pKi 3.1 nM Ki Bioorg Med Chem Lett (2019) 29: 1476-1480 [PMID:31005444]
ChEMBL Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell membrane incubated for 1 hr by microplate scintillation counting method B 6.48 pIC50 332.4 nM IC50 J Med Chem (2020) 63: 2074-2094 [PMID:31525963]
GtoPdb - - 6.92 pIC50 119.3 nM IC50 J Med Chem (2020) 63: 2074-2094 [PMID:31525963]
ChEMBL Inhibition of human P2X7 expressed in human HEK293 cells assessed as reduction in BzATP-stimulated TO-PRO-3 incorporation preincubated with compound and TO-PRO-3 for 15 mins prior to BzATP addition and measured after 1 hr by Fluo-3AM dye based flow cytometry B 6.92 pIC50 119.3 nM IC50 J Med Chem (2020) 63: 2074-2094 [PMID:31525963]
ChEMBL Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis B 7.7 pIC50 20 nM IC50 J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
ChEMBL Displacement of [11C]GSK1482160 from human recombinant P2X7 receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method based radioligand competitive binding assay B 8.05 pIC50 8.9 nM IC50 Bioorg Med Chem Lett (2019) 29: 1476-1480 [PMID:31005444]
GtoPdb - - 8.5 pIC50 3.16 nM IC50 Bioorg Med Chem Lett (2010) 20: 5080-4 [PMID:20673717]
ChEMBL Inhibition of human P2X7 receptor by ethidium bromide release assay B 8.5 pIC50 3.16 nM IC50 Bioorg Med Chem Lett (2010) 20: 5080-5084 [PMID:20673717]
ChEMBL Antagonist activity at human recombinant P2X7 receptor expressed in HEK293 cells by ethidium accumulation assay F 8.5 pIC50 3.16 nM IC50 Bioorg Med Chem Lett (2010) 20: 6370-6374 [PMID:20934331]
P2X7/P2X purinoceptor 7 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5183] [GtoPdb: 484] [UniProtKB: Q9Z1M0]
ChEMBL Antagonist activity at mouse P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis B 5.64 pIC50 2300 nM IC50 J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
P2X7/P2X purinoceptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2496] [GtoPdb: 484] [UniProtKB: Q64663]
ChEMBL Displacement of [3H]-A-804598 from rat P2X7 receptor expressed in HEK293 cell membrane by in vitro binding assay B 6.29 pKi 510 nM Ki J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
ChEMBL Antagonist activity at rat P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis B 5.72 pIC50 1900 nM IC50 J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
ChEMBL Inhibition of rat P2X7 receptor by ethidium bromide release assay B 6.5 pIC50 316.23 nM IC50 Bioorg Med Chem Lett (2010) 20: 5080-5084 [PMID:20673717]
GtoPdb - - 6.5 pIC50 316 nM IC50 Bioorg Med Chem Lett (2010) 20: 5080-4 [PMID:20673717]
ChEMBL Antagonist activity at rat recombinant P2X7 receptor F 6.6 pIC50 251.19 nM IC50 Bioorg Med Chem Lett (2010) 20: 6370-6374 [PMID:20934331]

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]