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Target
Protein mono-ADP-ribosyltransferase PARP3
Ligand
BDBM50499822
Substrate
n/a
Meas. Tech.
ChEMBL_1541456 (CHEMBL3743827)
IC50
2800±n/a nM
Citation
 Johannes, JW; Almeida, L; Daly, K; Ferguson, AD; Grosskurth, SE; Guan, H; Howard, T; Ioannidis, S; Kazmirski, S; Lamb, ML; Larsen, NA; Lyne, PD; Mikule, K; Ogoe, C; Peng, B; Petteruti, P; Read, JA; Su, N; Sylvester, M; Throner, S; Wang, W; Wang, X; Wu, J; Ye, Q; Yu, Y; Zheng, X; Scott, DA Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering. Bioorg Med Chem Lett 25:5743-7 (2015) [PubMed]  Article 
Target
Name:
Protein mono-ADP-ribosyltransferase PARP3
Synonyms:
ADP-ribosyltransferase diphtheria toxin-like 3 | ADPRT-3 | ADPRT3 | ADPRTL3 | ARTD3 | IRT1 | NAD(+) ADP-ribosyltransferase 3 | PARP-3 | PARP3 | PARP3_HUMAN | Poly [ADP-ribose] polymerase 3 | Poly[ADP-ribose] synthase 3 | hPARP-3 | pADPRT-3
Type:
PROTEIN
Mol. Mass.:
60091.40
Organism:
Homo sapiens (Human)
Description:
ChEMBL_109545
Residue:
533
Sequence:
MAPKPKPWVQTEGPEKKKGRQAGREEDPFRSTAEALKAIPAEKRIIRVDPTCPLSSNPGTQVYEDYNCTLNQTNIENNNNKFYIIQLLQDSNRFFTCWNRWGRVGEVGQSKINHFTRLEDAKKDFEKKFREKTKNNWAERDHFVSHPGKYTLIEVQAEDEAQEAVVKVDRGPVRTVTKRVQPCSLDPATQKLITNIFSKEMFKNTMALMDLDVKKMPLGKLSKQQIARGFEALEALEEALKGPTDGGQSLEELSSHFYTVIPHNFGHSQPPPINSPELLQAKKDMLLVLADIELAQALQAVSEQEKTVEEVPHPLDRDYQLLKCQLQLLDSGAPEYKVIQTYLEQTGSNHRCPTLQHIWKVNQEGEEDRFQAHSKLGNRKLLWHGTNMAVVAAILTSGLRIMPHSGGRVGKGIYFASENSKSAGYVIGMKCGAHHVGYMFLGEVALGREHHINTDNPSLKSPPPGFDSVIARGHTEPDPTQDTELELDGQQVVVPQGQPVPCPEFSSSTFSQSEYLIYQESQCRLRYLLEVHL
  
Inhibitor
Name:
BDBM50499822
Synonyms:
CHEMBL3740897
Type:
Small organic molecule
Emp. Form.:
C24H20F4N6O2
Mol. Mass.:
500.4482
SMILES:
C[C@H]1Cn2c(CN1C(=O)c1cccc(c1)C(F)(F)c1n[nH]c(=O)c3ccccc13)nnc2C(C)(F)F |r|
Structure:
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