Target
Non-receptor tyrosine-protein kinase TYK2
Ligand
BDBM50261270
Substrate
n/a
Meas. Tech.
ChEMBL_1695702 (CHEMBL4046592)
EC50
200±n/a nM
Citation
 Liang, JVan Abbema, ABalazs, MBarrett, KBerezhkovsky, LBlair, WSChang, CDelarosa, DDeVoss, JDriscoll, JEigenbrot, CGoodacre, SGhilardi, NMacLeod, CJohnson, ABir Kohli, PLai, YLin, ZMantik, PMenghrajani, KNguyen, HPeng, ISambrone, AShia, SSmith, JSohn, STsui, VUltsch, MWilliams, KWu, LCYang, WZhang, BMagnuson, S Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model. Bioorg Med Chem Lett 27:4370-4376 (2017) [PubMed]  Article 
Target
Name:
Non-receptor tyrosine-protein kinase TYK2
Synonyms:
Non-receptor tyrosine-protein kinase TYK2 (TYK2) | TYK2 | TYK2_HUMAN | Tyrosine-protein kinase TYK2
Type:
Protein
Mol. Mass.:
133666.03
Organism:
Homo sapiens (Human)
Description:
P29597
Residue:
1187
Sequence:
MPLRHWGMARGSKPVGDGAQPMAAMGGLKVLLHWAGPGGGEPWVTFSESSLTAEEVCIHIAHKVGITPPCFNLFALFDAQAQVWLPPNHILEIPRDASLMLYFRIRFYFRNWHGMNPREPAVYRCGPPGTEASSDQTAQGMQLLDPASFEYLFEQGKHEFVNDVASLWELSTEEEIHHFKNESLGMAFLHLCHLALRHGIPLEEVAKKTSFKDCIPRSFRRHIRQHSALTRLRLRNVFRRFLRDFQPGRLSQQMVMVKYLATLERLAPRFGTERVPVCHLRLLAQAEGEPCYIRDSGVAPTDPGPESAAGPPTHEVLVTGTGGIQWWPVEEEVNKEEGSSGSSGRNPQASLFGKKAKAHKAVGQPADRPREPLWAYFCDFRDITHVVLKEHCVSIHRQDNKCLELSLPSRAAALSFVSLVDGYFRLTADSSHYLCHEVAPPRLVMSIRDGIHGPLLEPFVQAKLRPEDGLYLIHWSTSHPYRLILTVAQRSQAPDGMQSLRLRKFPIEQQDGAFVLEGWGRSFPSVRELGAALQGCLLRAGDDCFSLRRCCLPQPGETSNLIIMRGARASPRTLNLSQLSFHRVDQKEITQLSHLGQGTRTNVYEGRLRVEGSGDPEEGKMDDEDPLVPGRDRGQELRVVLKVLDPSHHDIALAFYETASLMSQVSHTHLAFVHGVCVRGPENIMVTEYVEHGPLDVWLRRERGHVPMAWKMVVAQQLASALSYLENKNLVHGNVCGRNILLARLGLAEGTSPFIKLSDPGVGLGALSREERVERIPWLAPECLPGGANSLSTAMDKWGFGATLLEICFDGEAPLQSRSPSEKEHFYQRQHRLPEPSCPQLATLTSQCLTYEPTQRPSFRTILRDLTRLQPHNLADVLTVNPDSPASDPTVFHKRYLKKIRDLGEGHFGKVSLYCYDPTNDGTGEMVAVKALKADCGPQHRSGWKQEIDILRTLYHEHIIKYKGCCEDQGEKSLQLVMEYVPLGSLRDYLPRHSIGLAQLLLFAQQICEGMAYLHAQHYIHRDLAARNVLLDNDRLVKIGDFGLAKAVPEGHEYYRVREDGDSPVFWYAPECLKEYKFYYASDVWSFGVTLYELLTHCDSSQSPPTKFLELIGIAQGQMTVLRLTELLERGERLPRPDKCPCEVYHLMKNCWETEASFRPTFENLIPILKTVHEKYQGQAPSVFSVC
  
Inhibitor
Name:
BDBM50261270
Synonyms:
CHEMBL4093872
Type:
Small organic molecule
Emp. Form.:
C20H17Cl2N7O
Mol. Mass.:
442.301
SMILES:
Clc1cccc(Cl)c1-c1nc2ccnc(Nc3cc(ncn3)N3CCOCC3)c2[nH]1
Structure:
Search PDB for entries with ligand similarity: