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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 |
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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]