talazoparib [Ligand Id: 8313] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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] |
| Mono [ADP-ribose] polymerase PARP16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105981] [UniProtKB: Q8N5Y8] | ||||||||
| ChEMBL | Binding affinity to PARP16 (unknown origin) assessed as apparent dissociation constant | B | 6 | pKd | 1000 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| poly(ADP-ribose) polymerase 1/Poly [ADP-ribose] polymerase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3105] [GtoPdb: 2771] [UniProtKB: P09874] | ||||||||
| ChEMBL | Binding affinity to PARP1 (unknown origin) assessed as apparent dissociation constant | B | 8.96 | pKd | 1.1 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| ChEMBL | Binding affinity to PARP1 (unknown origin) assessed as dissociation constant incubated for 30 mins by streptavidin pulldown based Western blot analysis | B | 9.22 | pKd | 0.6 | nM | Kd | Eur J Med Chem (2023) 252: 115300-115300 [PMID:36989813] |
| 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 | Binding affinity to PARP1 (unknown origin) assessed as inhibition constant | B | 9.24 | pKi | 0.58 | nM | Ki | Eur J Med Chem (2022) 230: 114109-114109 [PMID:35051747] |
| ChEMBL | Inhibition of human recombinant N-terminal 6His-6Lys-TEV tagged PARP1 full length expressed in pFastBac expression system incubated for 4 hrs by fluorescence anisotropy binding assay | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| 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 PARP1 (unknown origin) | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Eur J Med Chem (2023) 252: 115300-115300 [PMID:36989813] |
| 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 | 9.15 | pIC50 | 0.7 | nM | IC50 | J Med Chem (2023) 66: 14095-14115 [PMID:37843892] |
| 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) using NAD as substrate incubated for 1 min | B | 9.22 | pIC50 | 0.6 | nM | IC50 | J Med Chem (2022) 65: 6803-6825 [PMID:35442700] |
| ChEMBL | Inhibition of PARP1 (unknown origin) by ELISA | B | 9.22 | pIC50 | 0.6 | nM | IC50 | RSC Med Chem (2024) 15: 981-997 [PMID:38516606] |
| 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 recombinant PARP-1 (662 to 1011 residues) | B | 9.24 | pIC50 | 0.57 | nM | IC50 | J Med Chem (2016) 59: 9575-9598 [PMID:27416328] |
| 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) | B | 9.24 | pIC50 | 0.57 | nM | IC50 | Eur J Med Chem (2022) 230: 114109-114109 [PMID:35051747] |
| 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 family member 10/Poly [ADP-ribose] polymerase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2429708] [GtoPdb: 3267] [UniProtKB: Q53GL7] | ||||||||
| ChEMBL | Binding affinity to PARP10 (unknown origin) assessed as apparent dissociation constant | B | 5.24 | pKd | 5700 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| poly(ADP-ribose) polymerase family member 11/Poly [ADP-ribose] polymerase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2380189] [GtoPdb: 3268] [UniProtKB: Q9NR21] | ||||||||
| ChEMBL | Inhibition of human N-terminal FLAG-tagged/C-terminal His-tagged recombinant PARP11 (8 to 338 (end) residues) expressed in Sf9 cells | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2023) 66: 14095-14115 [PMID:37843892] |
| Poly [ADP-ribose] polymerase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2429709] [UniProtKB: Q9H0J9] | ||||||||
| ChEMBL | Binding affinity to PARP12 (unknown origin) assessed as apparent dissociation constant | B | 5 | pKd | >10000 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| poly(ADP-ribose) polymerase family member 14/Poly [ADP-ribose] polymerase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176777] [GtoPdb: 3269] [UniProtKB: Q460N5] | ||||||||
| ChEMBL | Binding affinity to PARP14 (unknown origin) assessed as apparent dissociation constant | B | 5 | pKd | >10000 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| poly(ADP-ribose) polymerase 2/Poly [ADP-ribose] polymerase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5366] [GtoPdb: 2772] [UniProtKB: Q9UGN5] | ||||||||
| ChEMBL | Binding affinity to PARP2 (unknown origin) assessed as apparent dissociation constant | B | 8.48 | pKd | 3.3 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| 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 | Inhibition of human recombinant N-terminal Avi-6His-TEV tagged PARP2 full length expressed in pFastBac expression system incubated for 4 hrs by fluorescence anisotropy binding assay | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| ChEMBL | Inhibition of PARP2 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2022) 230: 114109-114109 [PMID:35051747] |
| ChEMBL | Inhibition of PARP2 (unknown origin) | B | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (2023) 66: 14095-14115 [PMID:37843892] |
| ChEMBL | Inhibition of PARP2 (unknown origin) using NAD as substrate incubated for 1 min | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2022) 65: 6803-6825 [PMID:35442700] |
| poly (ADP-ribose) polymerase 3/Poly [ADP-ribose] polymerase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5083] [GtoPdb: 2864] [UniProtKB: Q9Y6F1] | ||||||||
| ChEMBL | Binding affinity to PARP3 (unknown origin) assessed as apparent dissociation constant | B | 7.62 | pKd | 24 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| Poly [ADP-ribose] polymerase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6142] [UniProtKB: Q9UKK3] | ||||||||
| ChEMBL | Binding affinity to PARP4 (unknown origin) assessed as apparent dissociation constant | B | 9.15 | pKd | 0.7 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| Poly [ADP-ribose] polymerase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3091262] [UniProtKB: Q8N3A8] | ||||||||
| ChEMBL | Binding affinity to PARP8 (unknown origin) assessed as apparent dissociation constant | B | 5.96 | pKd | 1100 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| tankyrase/Tankyrase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6164] [GtoPdb: 3108] [UniProtKB: O95271] | ||||||||
| ChEMBL | Binding affinity to PARP5a (unknown origin) assessed as apparent dissociation constant | B | 7.28 | pKd | 53 | nM | Kd | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
| ChEMBL | Binding affinity to TNKS1 (unknown origin) assessed as dissociation constant incubated for 30 mins by streptavidin pulldown based Western blot analysis | B | 7.85 | pKd | 14 | nM | Kd | Eur J Med Chem (2023) 252: 115300-115300 [PMID:36989813] |
| ChEMBL | Inhibition of human recombinant PARP5a (E1023 to T1327 amino acids) incubated for 4 hrs by fluorescence anisotropy binding assay | B | 5.72 | pIC50 | 1900 | nM | IC50 | J Med Chem (2021) 64: 14498-14512 [PMID:34570508] |
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]
