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ChEMBL ligand: CHEMBL3137320 (BMN 673, BMN-673, LT-673, Talazoparib) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG by cell based assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2016) 59: 335-357 [PMID:26652717] |
poly(ADP-ribose) polymerase 1/Poly [ADP-ribose] polymerase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3105] [GtoPdb: 2771] [UniProtKB: P09874] | ||||||||
ChEMBL | Inhibition of human PARP1 using [3H]NAD as substrate after 1 min by microplate scintillation counting analysis | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2016) 59: 335-357 [PMID:26652717] |
ChEMBL | Inhibition of PARP1 (unknown origin) after 1 min in presence of NAD by top count analysis | B | 8.92 | pKi | 1.2 | nM | Ki | Eur J Med Chem (2019) 165: 198-215 [PMID:30684797] |
ChEMBL | Inhibition of PARP1 (unknown origin) by ELISA | B | 8.14 | pIC50 | 7.2 | nM | IC50 | Eur J Med Chem (2017) 138: 514-531 [PMID:28692916] |
ChEMBL | Inhibition of N-terminal GST-tagged human full length PARP1 (2 to 1041 residues) expressed in baculovirus infected Sf9 cells using histone mixture (H2A and H2B) and biotinylated NAD+ as substrate in presence of activated DNA incubated for 60 mins by chemiluminescence assay | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem (2020) 28: 115819-115819 [PMID:33120078] |
ChEMBL | Inhibition of PARP1 (unknown origin) | B | 9.22 | pIC50 | 0.6 | nM | IC50 | J Med Chem (2015) 58: 3302-3314 [PMID:25761096] |
ChEMBL | Inhibition of PARP1 (unknown origin) | B | 9.24 | pIC50 | 0.58 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4127-4132 [PMID:27353531] |
ChEMBL | Inhibition of human PARP1 using [3H]NAD as substrate after 1 min by microplate scintillation counting analysis | B | 9.24 | pIC50 | 0.57 | nM | IC50 | J Med Chem (2016) 59: 335-357 [PMID:26652717] |
ChEMBL | Inhibition of PARP1 (unknown origin) after 1 min in presence of NAD by top count analysis | B | 9.24 | pIC50 | 0.57 | nM | IC50 | Eur J Med Chem (2019) 165: 198-215 [PMID:30684797] |
ChEMBL | Inhibition of human PARP-1 catalytic domain (662 to 1011 residues) expressed in Escherichia coli BL21(DE3) cells incubated for 0.5 hrs by fluorescence polarization assay based DNA trapping activity assay | B | 8.49 | pEC50 | 3.2 | nM | EC50 | J Med Chem (2020) 63: 15541-15563 [PMID:33264017] |
poly(ADP-ribose) polymerase 2/Poly [ADP-ribose] polymerase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5366] [GtoPdb: 2772] [UniProtKB: Q9UGN5] | ||||||||
ChEMBL | Inhibition of PARP2 (unknown origin) after 1 min in presence of NAD by top count analysis | B | 9.05 | pKi | 0.9 | nM | Ki | Eur J Med Chem (2019) 165: 198-215 [PMID:30684797] |
ChEMBL | Inhibition of human PARP2 using [3H]NAD as substrate after 1 min by microplate scintillation counting analysis | B | 9.07 | pKi | 0.85 | nM | Ki | J Med Chem (2016) 59: 335-357 [PMID:26652717] |
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]