AZ10606120 [Ligand Id: 9021] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL562308 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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]
