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TargetProtein mono-ADP-ribosyltransferase PARP3 [R100H]
LigandBDBM50316226
Substrate/Competitorn/a
Meas. Tech.ChEMBL_628374 (CHEMBL1115412)
IC50 1300±n/a nM
Citation Jones, PAltamura, SBoueres, JFerrigno, FFonsi, MGiomini, CLamartina, SMonteagudo, EOntoria, JMOrsale, MVPalumbi, MCPesci, SRoscilli, GScarpelli, RSchultz-Fademrecht, CToniatti, CRowley, M Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem52:7170-85 (2009) [PubMed]  Article
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Protein mono-ADP-ribosyltransferase PARP3 [R100H]
Name:Protein mono-ADP-ribosyltransferase PARP3 [R100H]
Synonyms:(ARTD3 or PARP3) | ADP-ribosyltransferase diphtheria toxin-like 3 | ADPRT3 | ADPRTL3 | Human diphtheria toxin-like ADP-ribosyltransferase (ARTD3 or PARP3) | PARP3 | PARP3_HUMAN | Poly [ADP-ribose] polymerase 3 | Poly [ADP-ribose] polymerase 3 (PARP-3) | Poly(ADP-ribose) polymerase-3 (ARTD3/PARP3)
Type:PROTEIN
Mol. Mass.:60071.85
Organism:Homo sapiens (Human)
Description:Q9Y6F1[R100H]
Residue:533
Sequence:
MAPKPKPWVQTEGPEKKKGRQAGREEDPFRSTAEALKAIPAEKRIIRVDPTCPLSSNPGT
QVYEDYNCTLNQTNIENNNNKFYIIQLLQDSNRFFTCWNHWGRVGEVGQSKINHFTRLED
AKKDFEKKFREKTKNNWAERDHFVSHPGKYTLIEVQAEDEAQEAVVKVDRGPVRTVTKRV
QPCSLDPATQKLITNIFSKEMFKNTMALMDLDVKKMPLGKLSKQQIARGFEALEALEEAL
KGPTDGGQSLEELSSHFYTVIPHNFGHSQPPPINSPELLQAKKDMLLVLADIELAQALQA
VSEQEKTVEEVPHPLDRDYQLLKCQLQLLDSGAPEYKVIQTYLEQTGSNHRCPTLQHIWK
VNQEGEEDRFQAHSKLGNRKLLWHGTNMAVVAAILTSGLRIMPHSGGRVGKGIYFASENS
KSAGYVIGMKCGAHHVGYMFLGEVALGREHHINTDNPSLKSPPPGFDSVIARGHTEPDPT
QDTELELDGQQVVVPQGQPVPCPEFSSSTFSQSEYLIYQESQCRLRYLLEVHL
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  Blast E-value cutoff:
BDBM50316226
n/a
NameBDBM50316226
Synonyms:(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide | CHEMBL1094636 | MK-4827 | Niraparib
TypeSmall organic molecule
Emp. Form.C19H20N4O
Mol. Mass.320.3883
SMILESNC(=O)c1cccc2cn(nc12)-c1ccc(cc1)[C@@H]1CCCNC1 |r|
Structure
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