AZ10606120 [Ligand Id: 9021] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL562308 |
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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 | Measuring binding of [3H]-AZ10606120 to human P2X7 receptors | - | 8.85 | pKd | 1.4 | nM | Kd | Br J Pharmacol (2008) 153: 737-50 [PMID:18071294] |
| ChEMBL | Antagonist activity at human P2X7R transfected in HEK293 cells assessed as inhibition of ATP-mediated calcium influx measured after 10 mins by YOPRO-1 dye uptake assay | B | 4.04 | pIC50 | 92000 | nM | IC50 | J Nat Prod (2019) 82: 2559-2567 [PMID:31532206] |
| ChEMBL | Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake | F | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2009) 52: 3123-3141 [PMID:19191585] |
| ChEMBL | Antagonist activity at human P2X7R transfected in HEK293 cells | B | 8 | pIC50 | 10 | nM | IC50 | J Nat Prod (2019) 82: 2559-2567 [PMID:31532206] |
| P2X7 in Rat [GtoPdb: 484] [UniProtKB: Q64663] | ||||||||
| GtoPdb | Measuring binding of [3H]-AZ10606120 to rat P2X7 receptors | - | 8.72 | pKd | 1.9 | nM | Kd | Br J Pharmacol (2008) 153: 737-50 [PMID:18071294] |
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]
