GSK1482160 [Ligand Id: 10504] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1222883 |
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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 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]
