fluzoparib [Ligand Id: 13763] 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: CHEMBL3930624 (Fluzoparib, Fuzuloparib, Fuzuopali, HS-10160, HS10160, Shr3162, SHR-3162, SHR3162) |
|---|
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 |
|---|---|---|---|---|---|---|---|---|
| poly(ADP-ribose) polymerase 1/Poly [ADP-ribose] polymerase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3105] [GtoPdb: 2771] [UniProtKB: P09874] | ||||||||
| ChEMBL | HTF Homologous PARP Inhibition Assay: The tested compounds were dissolved in dimethylsulfoxide and then diluted with 1x buffer to the concentration desired in the experiment. 25 uL of a 200 nM NAD+ solution was added to a 96-well round bottomed plate, followed by the addition of 1 uL of tested compounds solution, and the control of replicate wells were installed. Then 25 uL of the reaction mixture containing DNA, PARP enzyme and reaction buffer was added into each well. After incubating for 30 minutes at room temperature, 50 uL of cycling reaction mixture was added into each well and incubated in the dark at room temperature for 15 to 40 minutes. Then 50 uL of stop solution was added into each well and the fluorescence values of each well were read on an ELISA (Ex544 nm, Em590 nm). | B | 7.99 | pIC50 | 10.2 | nM | IC50 | US-9273052-B2. Phthalazinone ketone derivative, preparation method thereof, and pharmaceutical use thereof (2016) |
| GtoPdb | - | - | 8.05 | pIC50 | 8.84 | nM | IC50 | J Med Chem (2023) 66: 14095-14115 [PMID:37843892] |
| ChEMBL | Inhibition of PARP1 (unknown origin) by ELISA | B | 8.84 | pIC50 | 1.46 | nM | IC50 | Eur J Med Chem (2020) 203: 112570-112570 [PMID:32717529] |
| ChEMBL | Inhibition of PARP1 (unknown origin) by ELISA | B | 8.84 | pIC50 | 1.46 | nM | IC50 | RSC Med Chem (2024) 15: 981-997 [PMID:38516606] |
| ChEMBL | Inhibition of PARP1 (unknown origin) using histone as substrate by ELISA | B | 8.84 | pIC50 | 1.46 | nM | IC50 | J Med Chem (2023) 66: 12284-12303 [PMID:37605459] |
| ChEMBL | Inhibition of PARP1 (unknown origin) | B | 8.84 | pIC50 | 1.46 | nM | IC50 | J Med Chem (2023) 66: 14095-14115 [PMID:37843892] |
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]
