Reaction Details |
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Target | Protein mono-ADP-ribosyltransferase PARP3 [R100H] |
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Ligand | BDBM50316226 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_628374 (CHEMBL1115412) |
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IC50 | 1300±n/a nM |
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Citation | Jones, P; Altamura, S; Boueres, J; Ferrigno, F; Fonsi, M; Giomini, C; Lamartina, S; Monteagudo, E; Ontoria, JM; Orsale, MV; Palumbi, MC; Pesci, S; Roscilli, G; Scarpelli, R; Schultz-Fademrecht, C; Toniatti, C; Rowley, 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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More Info.: | Get all data from this article, Assay Method |
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Protein mono-ADP-ribosyltransferase PARP3 [R100H] |
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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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BDBM50316226 |
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n/a |
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Name | BDBM50316226 |
Synonyms: | (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide | CHEMBL1094636 | MK-4827 | Niraparib |
Type | Small organic molecule |
Emp. Form. | C19H20N4O |
Mol. Mass. | 320.3883 |
SMILES | NC(=O)c1cccc2cn(nc12)-c1ccc(cc1)[C@@H]1CCCNC1 |r| |
Structure |
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