Reaction Details |
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Target | Protein mono-ADP-ribosyltransferase PARP14 |
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Ligand | BDBM50238416 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1663208 (CHEMBL4012889) |
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IC50 | <5012±n/a nM |
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Citation | Thomson, DW; Wagner, AJ; Bantscheff, M; Benson, RE; Dittus, L; Duempelfeld, B; Drewes, G; Krause, J; Moore, JT; Mueller, K; Poeckel, D; Rau, C; Salzer, E; Shewchuk, L; Hopf, C; Emery, JG; Muelbaier, M Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines. J Med Chem60:5455-5471 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Protein mono-ADP-ribosyltransferase PARP14 |
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Name: | Protein mono-ADP-ribosyltransferase PARP14 |
Synonyms: | (ARTD8 or PARP14) | (ARTD8 or PARP14, Y1660L) | 2.4.2.- | 2.4.2.30 | ADP-ribosyltransferase diphtheria toxin-like 8 | ARTD8 | B aggressive lymphoma protein 2 | BAL2 | BAL2 | Human diphtheria toxin-like ADP-ribosyltransferase (ARTD8 or PARP14, Y1660L) | KIAA1268 | KIAA1268 GN | KIAA1268 GN | PAR14_HUMAN | PARP-14 | PARP14 | Poly [ADP-ribose] polymerase 14 | Synonyms=BAL2 |
Type: | n/a |
Mol. Mass.: | 202812.41 |
Organism: | Homo sapiens (Human) |
Description: | Q460N5 |
Residue: | 1801 |
Sequence: | MAVPGSFPLLVEGSWGPDPPKNLNTKLQMYFQSPKRSGGGECEVRQDPRSPSRFLVFFYP
EDVRQKVLERKNHELVWQGKGTFKLTVQLPATPDEIDHVFEEELLTKESKTKEDVKEPDV
SEELDTKLPLDGGLDKMEDIPEECENISSLVAFENLKANVTDIMLILLVENISGLSNDDF
QVEIIRDFDVAVVTFQKHIDTIRFVDDCTKHHSIKQLQLSPRLLEVTNTIRVENLPPGAD
DYSLKLFFENPYNGGGRVANVEYFPEESSALIEFFDRKVLDTIMATKLDFNKMPLSVFPY
YASLGTALYGKEKPLIKLPAPFEESLDLPLWKFLQKKNHLIEEINDEMRRCHCELTWSQL
SGKVTIRPAATLVNEGRPRIKTWQADTSTTLSSIRSKYKVNPIKVDPTMWDTIKNDVKDD
RILIEFDTLKEMVILAGKSEDVQSIEVQVRELIESTTQKIKREEQSLKEKMIISPGRYFL
LCHSSLLDHLLTECPEIEICYDRVTQHLCLKGPSADVYKAKCEIQEKVYTMAQKNIQVSP
EIFQFLQQVNWKEFSKCLFIAQKILALYELEGTTVLLTSCSSEALLEAEKQMLSALNYKR
IEVENKEVLHGKKWKGLTHNLLKKQNSSPNTVIINELTSETTAEVIITGCVKEVNETYKL
LFNFVEQNMKIERLVEVKPSLVIDYLKTEKKLFWPKIKKVNVQVSFNPENKQKGILLTGS
KTEVLKAVDIVKQVWDSVCVKSVHTDKPGAKQFFQDKARFYQSEIKRLFGCYIELQENEV
MKEGGSPAGQKCFSRTVLAPGVVLIVQQGDLARLPVDVVVNASNEDLKHYGGLAAALSKA
AGPELQADCDQIVKREGRLLPGNATISKAGKLPYHHVIHAVGPRWSGYEAPRCVYLLRRA
VQLSLCLAEKYKYRSIAIPAISSGVFGFPLGRCVETIVSAIKENFQFKKDGHCLKEIYLV
DVSEKTVEAFAEAVKTVFKATLPDTAAPPGLPPAAAGPGKTSWEKGSLVSPGGLQMLLVK
EGVQNAKTDVVVNSVPLDLVLSRGPLSKSLLEKAGPELQEELDTVGQGVAVSMGTVLKTS
SWNLDCRYVLHVVAPEWRNGSTSSLKIMEDIIRECMEITESLSLKSIAFPAIGTGNLGFP
KNIFAELIISEVFKFSSKNQLKTLQEVHFLLHPSDHENIQAFSDEFARRANGNLVSDKIP
KAKDTQGFYGTVSSPDSGVYEMKIGSIIFQVASGDITKEEADVIVNSTSNSFNLKAGVSK
AILECAGQNVERECSQQAQQRKNDYIITGGGFLRCKNIIHVIGGNDVKSSVSSVLQECEK
KNYSSICLPAIGTGNAKQHPDKVAEAIIDAIEDFVQKGSAQSVKKVKVVIFLPQVLDVFY
ANMKKREGTQLSSQQSVMSKLASFLGFSKQSPQKKNHLVLEKKTESATFRVCGENVTCVE
YAISWLQDLIEKEQCPYTSEDECIKDFDEKEYQELNELQKKLNINISLDHKRPLIKVLGI
SRDVMQARDEIEAMIKRVRLAKEQESRADCISEFIEWQYNDNNTSHCFNKMTNLKLEDAR
REKKKTVDVKINHRHYTVNLNTYTATDTKGHSLSVQRLTKSKVDIPAHWSDMKQQNFCVV
ELLPSDPEYNTVASKFNQTCSHFRIEKIERIQNPDLWNSYQAKKKTMDAKNGQTMNEKQL
FHGTDAGSVPHVNRNGFNRSYAGKNAVAYGKGTYFAVNANYSANDTYSRPDANGRKHVYY
VRVLTGIYTHGNHSLIVPPSKNPQNPTDLYDTVTDNVHHPSLFVAFYDYQAYPEYLITFR
K
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BDBM50238416 |
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n/a |
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Name | BDBM50238416 |
Synonyms: | CHEMBL4087470 |
Type | Small organic molecule |
Emp. Form. | C23H20N10O |
Mol. Mass. | 452.4713 |
SMILES | O=C(N1CCN(CC1)c1ncccn1)c1ccc(Nc2nc3ccccc3n3nnnc23)cc1 |
Structure |
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