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 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]
