A740003 [Ligand Id: 4119] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL255787 (A-740003) |
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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] | ||||||||
| ChEMBL | Displacement of [3H]-A-804598 from human P2X7 receptor expressed in HEK293 cell membrane by in vitro binding assay | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (2021) 64: 4891-4902 [PMID:33822617] |
| ChEMBL | Antagonist activity at human P2X7R expressed in HEK293 cells assessed as inhibition of ATP-induced ethidium iodide uptake preincubated for 5 mins followed by ATP induction and measured after 25 mins by fluorescence assay | B | 6.12 | pIC50 | 750 | nM | IC50 | Bioorg Med Chem (2019) 27: 1449-1455 [PMID:30528164] |
| ChEMBL | Antagonist activity at human P2X7R expressed in differentiated human THP-1 cells assessed as reduction in BzATP induced IL-1beta release incubated for 30 mins followed by BzATP addition and measured for 30 mins by ELISA | B | 6.81 | pIC50 | 156 | nM | IC50 | Bioorg Med Chem Lett (2021) 51: 128361-128361 [PMID:34543755] |
| ChEMBL | Antagonist activity at human recombinant P2X7 receptor expressed in human THP1 cells assessed as inhibition of BzATP-induced IL1-beta release by enzyme-linked immunosorbent assay | F | 6.81 | pIC50 | 156 | nM | IC50 | Bioorg Med Chem (2009) 17: 4861-4865 [PMID:19540765] |
| ChEMBL | Antagonist activity at human P2X7R expressed in HEK293 cells assessed as inhibition of ATP-induced ethidium iodide uptake preincubated for 10 mins followed by ATP induction measured after 25 mins by fluorescence assay | B | 6.96 | pIC50 | 109 | nM | IC50 | Eur J Med Chem (2018) 143: 1361-1372 [PMID:29133043] |
| ChEMBL | Antagonist activity at human recombinant P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of BzATP-induced pore formation flux by fluorometric assay | F | 7.04 | pIC50 | 92 | nM | IC50 | Bioorg Med Chem (2009) 17: 4861-4865 [PMID:19540765] |
| ChEMBL | Antagonist activity at human P2X7R expressed in differentiated human THP-1 cells assessed as reduction in BzATP induced YO-PRO uptake by cells incubated for 10 mins followed by compound addition and measured for 50 mins by fluorescence based analysis | B | 7.04 | pIC50 | 92 | nM | IC50 | Bioorg Med Chem Lett (2021) 51: 128361-128361 [PMID:34543755] |
| ChEMBL | Antagonist activity at human P2X7 receptor | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2016) 59: 7410-7430 [PMID:27427902] |
| ChEMBL | Antagonist activity at P2X7 receptor in LPS/IFNc-differentiated human THP-1 cells assessed as inhibition of ATP-induced IL-1beta release preincubated for 30 mins followed by LPS stimulation for 4 hrs using cells treated with ATP for 30 mins by ELISA | B | 7.05 | pIC50 | 89 | nM | IC50 | Eur J Med Chem (2017) 139: 698-717 [PMID:28858765] |
| ChEMBL | Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of ATP-induced ethidium iodide uptake preincubated for 10 mins followed by ATP addition measured after 20 mins by spectrofluorometric analysis | B | 7.07 | pIC50 | 86 | nM | IC50 | Eur J Med Chem (2017) 139: 698-717 [PMID:28858765] |
| ChEMBL | Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of ATP-induced IL-1beta release preincubated for 30 mins followed by ATP addition measured after 30 mins by ELISA | B | 7.09 | pIC50 | 82 | nM | IC50 | Eur J Med Chem (2017) 139: 698-717 [PMID:28858765] |
| 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 | 7.09 | pIC50 | 81 | nM | IC50 | J Med Chem (2021) 64: 4891-4902 [PMID:33822617] |
| ChEMBL | Antagonist activity at human recombinant P2X7 receptor assessed as inhibition of calcium flux by FLIPR assay | F | 7.36 | pIC50 | 44 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2093-2096 [PMID:18272365] |
| ChEMBL | Antagonist activity at human recombinant P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of agonist-induced calcium flux by fluorometric assay | F | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem (2009) 17: 4861-4865 [PMID:19540765] |
| GtoPdb | - | - | 7.4 | pIC50 | 40 | nM | IC50 | J Pharmacol Exp Ther (2006) 319: 1376-85 [PMID:16982702] |
| ChEMBL | Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake | F | 7.4 | pIC50 | 39.81 | nM | IC50 | J Med Chem (2009) 52: 3123-3141 [PMID:19191585] |
| ChEMBL | Antagonist activity at human cloned P2X7 receptor expressed in HEK293 cells assessed as inhibition of calcium flux by FLIPR assay | F | 7.4 | pIC50 | 39.81 | nM | IC50 | J Med Chem (2009) 52: 3366-3376 [PMID:19397270] |
| P2X7/P2X purinoceptor 7 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5183] [GtoPdb: 484] [UniProtKB: Q9Z1M0] | ||||||||
| ChEMBL | Antagonist activity at P2X7R in Swiss Webster mouse peritoneal macrophages assessed as inhibition of ATP-induced propidium iodide uptake preincubated for 10 mins followed by ATP induction measured after 25 mins by fluorescence assay | B | 6.05 | pIC50 | 897 | nM | IC50 | Eur J Med Chem (2018) 143: 1361-1372 [PMID:29133043] |
| 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 | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (2021) 64: 4891-4902 [PMID:33822617] |
| ChEMBL | Antagonist activity at P2X7 receptor in LPS/IFNc-differentiated Swiss mouse peritoneal macrophages assessed as inhibition of ATP-induced IL-1beta release preincubated for 30 mins followed by LPS stimulation for 4 hrs using cells treated with ATP for 15 mins by ELISA | B | 6.95 | pIC50 | 112 | nM | IC50 | Eur J Med Chem (2017) 139: 698-717 [PMID:28858765] |
| ChEMBL | Antagonist activity at P2X7 receptor in Swiss mouse peritoneal macrophages assessed as inhibition of BzATP-induced ethidium iodide uptake after 30 mins by spectrofluorometric analysis | B | 7.2 | pIC50 | 63.33 | nM | IC50 | Eur J Med Chem (2017) 139: 698-717 [PMID:28858765] |
| ChEMBL | Antagonist activity at P2X7 receptor in Swiss mouse peritoneal macrophages assessed as inhibition of BzATP-induced current at holding potential of -60 mV preincubated for 5 mins followed by BzATP addition measured after 5 mins by Whole cell patch-clamp analysis | B | 7.33 | pIC50 | 46.91 | nM | IC50 | Eur J Med Chem (2017) 139: 698-717 [PMID:28858765] |
| 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 | 7.23 | pKi | 59 | nM | Ki | J Med Chem (2021) 64: 4891-4902 [PMID:33822617] |
| ChEMBL | Antagonist activity at rat cloned P2X7 receptor expressed in HEK293 cells assessed as inhibition of calcium flux by FLIPR assay | F | 7.7 | pIC50 | 19.95 | nM | IC50 | J Med Chem (2009) 52: 3366-3376 [PMID:19397270] |
| ChEMBL | Activity at rat P2X7 receptor expressed in HEK cells assessed as effect on BzATP-induced ethidium uptake | B | 7.7 | pIC50 | 19.95 | nM | IC50 | J Med Chem (2009) 52: 3123-3141 [PMID:19191585] |
| ChEMBL | Antagonist activity at rat recombinant P2X7 receptor assessed as inhibition of calcium flux by FLIPR assay | F | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2093-2096 [PMID:18272365] |
| ChEMBL | Antagonist activity at rat recombinant P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of agonist-induced calcium flux by fluorometric assay | F | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem (2009) 17: 4861-4865 [PMID:19540765] |
| 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 | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2021) 64: 4891-4902 [PMID:33822617] |
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]
