PF-04905428 [Ligand Id: 9062] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1823817 (Ce 224535, Ce-224535, CE 224,535, CE-224,535, CE224535) |
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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 | Antagonist activity at human P2X7 receptor in expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2018) 151: 462-481 [PMID:29649742] |
| ChEMBL | Antagonist activity at human P2X7 receptor | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2016) 59: 7410-7430 [PMID:27427902] |
| ChEMBL | Antagonist activity at P2X7 receptor expressed in HEK293 cells assessed as inhibition of ATP-induced YOPRO-1 uptake | F | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3708-3711 [PMID:21565499] |
| ChEMBL | Antagonist activity at P2X7 receptor in human LPS-stimulated monocytes assessed as inhibition of ATP-induced IL1-beta release by ELISA | F | 8.85 | pIC50 | 1.4 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3708-3711 [PMID:21565499] |
| ChEMBL | Antagonist activity against human P2X7 receptor assessed as inhibition of IL-1beta production by cell based assay | B | 8.85 | pIC50 | 1.4 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3157-3163 [PMID:26099534] |
| ChEMBL | Antagonist activity at P2X7R expressed in LPS-activated human monocytes assessed as inhibition of ATP-induced IL1-beta release in presence of low serum concentration | F | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 5475-5479 [PMID:21782426] |
| ChEMBL | Antagonist activity at P2X7 receptor in human LPS-stimulated monocytes assessed as inhibition of ATP-induced IL1-beta release by ELISA in presence of human blood | F | 9.1 | pIC50 | 0.8 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3708-3711 [PMID:21565499] |
| 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 | 9.12 | pIC50 | 0.76 | nM | IC50 | J Med Chem (2021) 64: 4891-4902 [PMID:33822617] |
| 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 | 6.18 | pIC50 | 660 | 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 | 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 | 6.33 | pIC50 | 470 | 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]
