Target
Protein mono-ADP-ribosyltransferase TIPARP
Ligand
BDBM476803
Substrate
n/a
Meas. Tech.
Enzymatic Assay
IC50
<100±n/a nM
Citation
 Vasbinder, MMSchenkel, LBSwinger, KKKuntz, KW Pyridazinones as PARP7 inhibitors US Patent  US10870641 Publication Date 12/22/2020 
Target
Name:
Protein mono-ADP-ribosyltransferase TIPARP
Synonyms:
ADP-ribosyltransferase diphtheria toxin-like 14 | ARTD14 | PARP-7 | PARP7 | PARPT_HUMAN | Poly [ADP-ribose] polymerase 7 | TCDD-inducible poly [ADP-ribose] polymerase | TIPARP
Type:
Protein
Mol. Mass.:
76228.44
Organism:
Human
Description:
Q7Z3E1
Residue:
657
Sequence:
MEMETTEPEPDCVVQPPSPPDDFSCQMRLSEKITPLKTCFKKKDQKRLGTGTLRSLRPILNTLLESGSLDGVFRSRNQSTDENSLHEPMMKKAMEINSSCPPAENNMSVLIPDRTNVGDQIPEAHPSTEAPERVVPIQDHSFPSETLSGTVADSTPAHFQTDLLHPVSSDVPTSPDCLDKVIDYVPGIFQENSFTIQYILDTSDKLSTELFQDKSEEASLDLVFELVNQLQYHTHQENGIEICMDFLQGTCIYGRDCLKHHTVLPYHWQIKRTTTQKWQSVFNDSQEHLERFYCNPENDRMRMKYGGQEFWADLNAMNVYETTEFDQLRRLSTPPSSNVNSIYHTVWKFFCRDHFGWREYPESVIRLIEEANSRGLKEVRFMMWNNHYILHNSFFRREIKRRPLFRSCFILLPYLQTLGGVPTQAPPPLEATSSSQIICPDGVTSANFYPETWVYMHPSQDFIQVPVSAEDKSYRIIYNLFHKTVPEFKYRILQILRVQNQFLWEKYKRKKEYMNRKMFGRDRIINERHLFHGTSQDVVDGICKHNFDPRVCGKHATMFGQGSYFAKKASYSHNFSKKSSKGVHFMFLAKVLTGRYTMGSHGMRRPPPVNPGSVTSDLYDSCVDNFFEPQIFVIFNDDQSYPYFVIQYEEVSNTVSI
  
Inhibitor
Name:
BDBM476803
Synonyms:
US10870641, Example 79B | US10870641, Example 79C | US10870641, Example 79D | US11014913, Example 79C
Type:
Small organic molecule
Emp. Form.:
C28H26F3N7O3
Mol. Mass.:
565.5463
SMILES:
FC(F)(F)c1c(cn[nH]c1=O)N1Cc2ccccc2[C@@H]1COC\C=C\C(=O)N1CCN(CC1)c1ccc(cn1)C#N |r|
Structure:
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