Reaction Details |
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Target | Protein mono-ADP-ribosyltransferase PARP14 |
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Ligand | BDBM50461017 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1770603 (CHEMBL4222715) |
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IC50 | 1000±n/a nM |
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Citation | Moustakim, M; Riedel, K; Schuller, M; Gehring, AP; Monteiro, OP; Martin, SP; Fedorov, O; Heer, J; Dixon, DJ; Elkins, JM; Knapp, S; Bracher, F; Brennan, PE Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2. Bioorg Med Chem26:2965-2972 (2018) [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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BDBM50461017 |
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n/a |
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Name | BDBM50461017 |
Synonyms: | CHEMBL4229283 |
Type | Small organic molecule |
Emp. Form. | C26H21N3O |
Mol. Mass. | 391.4644 |
SMILES | Cc1ccc(CC(=O)Nc2ccccc2-c2cccc3c4ccccc4[nH]c23)cn1 |
Structure |
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