niraparib
Niraparib is an inhibitor of poly(ADP-ribose) polymerase (PARP) enzymes, PARP-1 and PARP-2, which play a role in DNA repair. In vitro studies have shown that niraparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, apoptosis and cell death. Increased niraparib-induced cytotoxicity was observed in tumor cell lines with or without deficiencies in BRCA1/2. Niraparib decreased tumor growth in mouse xenograft models of human cancer cell lines with deficiencies in BRCA1/2 and in human patient-derived xenograft tumor models with homologous recombination deficiency that had either mutated or wild type BRCA1/2.
Ligand Summary
UNII: HMC2H89N35
PubChem: 24958200
Guide to Pharmacology: 8275
ChEMBL: CHEMBL1094636
DrugCentral: 5222
LyCHI: 4262PFAPFBJK
Target Activities
PARP1
Poly [ADP-ribose] polymerase 1
16 Activities
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1 – 10 of 16
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 8.42 | |||||
IC50 | 8.7 | J. Med. Chem., (2015) 58:8:3302 | ||||
IC50 | 8.49 | J. Med. Chem., (2009) 52:22:7170 | ||||
Ki | 8.49 | Eur J Med Chem, (2019) 165:None:198 | ||||
IC50 | 8.42 | Bioorg Med Chem Lett, (2016) 26:16:4127 | ||||
IC50 | 8.42 | Eur J Med Chem, (2019) 165:None:198 | ||||
IC50 | 8.09 | J. Med. Chem., (2016) 59:1:335 | ||||
IC50 | 7.79 | J Med Chem, (2017) 60:4:1262 | ||||
IC50 | 7.78 | J Med Chem, (2017) 60:4:1262 | ||||
IC50 | 7.52 | Bioorg. Med. Chem. Lett., (2014) 24:2:462 | ||||
PARP2
Poly [ADP-ribose] polymerase 2
7 Activities
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1 – 7 of 7
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 8.68 | |||||
IC50 | 8.68 | J. Med. Chem., (2009) 52:22:7170 | ||||
IC50 | 8.68 | Eur J Med Chem, (2019) 165:None:198 | ||||
Ki | 8.4 | Eur J Med Chem, (2019) 165:None:198 | ||||
IC50 | 7.82 | J Med Chem, (2017) 60:4:1262 | ||||
IC50 | 7.81 | J Med Chem, (2017) 60:4:1262 | ||||
IC50 | 8.68 | INHIBITOR | ||||
PARP4
Poly [ADP-ribose] polymerase 4
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 6.48 | J. Med. Chem., (2009) 52:22:7170 | ||||
IC50 | 6.35 | J Med Chem, (2017) 60:4:1262 | ||||
IC50 | 6.35 | J Med Chem, (2017) 60:4:1262 | ||||
IC50 | 6.48 | |||||
PARP12
Poly [ADP-ribose] polymerase 12
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 7.1 | J Med Chem, (2017) 60:4:1262 | ||||
IC50 | 6.1 | J Med Chem, (2017) 60:4:1262 | ||||
IC50 | 7.1 | |||||
PARP3
Poly [ADP-ribose] polymerase 3
2 Activities
TNKS
Tankyrase-1
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 6.24 | J. Med. Chem., (2009) 52:22:7170 | ||||
IC50 | 6.24 | |||||