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 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]
