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Target
Non-receptor tyrosine-protein kinase TYK2
Ligand
BDBM406663
Substrate
n/a
Meas. Tech.
ChEMBL_2193380 (CHEMBL5105740)
IC50
110±n/a nM
Citation
Leit, S; Greenwood, JR; Mondal, S; Carriero, S; Dahlgren, M; Harriman, GC; Kennedy-Smith, JJ; Kapeller, R; Lawson, JP; Romero, DL; Toms, AV; Shelley, M; Wester, RT; Westlin, W; McElwee, JJ; Miao, W; Edmondson, SD; Masse, CE Potent and selective TYK2-JH1 inhibitors highly efficacious in rodent model of psoriasis. Bioorg Med Chem Lett 73:0 (2022) [PubMed] Article
More Info.:
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:
BDBM406663
Synonyms:
US10336752, Compound 1 | US10336752, Compound 2 | US10336752, Compound 4 | US10336752, Compound 5 | US10336752, Compound 6 | US11040967, Compound 6
Type:
Small organic molecule
Emp. Form.:
C24H20F2N4O2
Mol. Mass.:
434.438
SMILES:
Fc1cccc(F)c1-c1cc(Nc2ccc(cc2)C(=O)N2CCCC2)c2C(=O)NCc2n1