Reaction Details Report a problem with these data
Target
Phosphatidylinositol 4-kinase beta
Ligand
BDBM489258
Substrate
n/a
Meas. Tech.
ChEMBL_2145020 (CHEMBL5029300)
IC50
501±n/a nM
Citation
Perry, MWD; Björhall, K; Bold, P; Br?lls, M; Börjesson, U; Carlsson, J; Chang, HA; Chen, Y; Eriksson, A; Fihn, BM; Fransson, R; Fredlund, L; Ge, H; Huang, H; Karabelas, K; Lamm Bergström, E; Lever, S; Lindmark, H; Mogemark, M; Nikitidis, A; Palmgren, AP; Pemberton, N; Petersen, J; Rodrigo Blomqvist, M; Smith, RW; Thomas, MJ; Ullah, V; Tyrchan, C; Wennberg, T; Westin Eriksson, A; Yang, W; Zhao, S; Öster, L Discovery of AZD8154, a Dual PI3K?? Inhibitor for the Treatment of Asthma. J Med Chem 64:8053-8075 (2021) [PubMed] Article
More Info.:
Target
Name:
Phosphatidylinositol 4-kinase beta
Synonyms:
NPIK | PI4-kinase beta subunit | PI4K-beta | PI4K92 | PI4KB | PI4KB_HUMAN | PI4Kbeta | PIK4B | PIK4CB | Phosphatidylinositol 4-kinase beta | Phosphatidylinositol 4-kinase, PI4K | PtdIns 4-kinase beta
Type:
Protein
Mol. Mass.:
91373.30
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
816
Sequence:
MGDTVVEPAPLKPTSEPTSGPPGNNGGSLLSVITEGVGELSVIDPEVAQKACQEVLEKVKLLHGGVAVSSRGTPLELVNGDGVDSEIRCLDDPPAQIREEEDEMGAAVASGTAKGARRRRQNNSAKQSWLLRLFESKLFDISMAISYLYNSKEPGVQAYIGNRLFCFRNEDVDFYLPQLLNMYIHMDEDVGDAIKPYIVHRCRQSINFSLQCALLLGAYSSDMHISTQRHSRGTKLRKLILSDELKPAHRKRELPSLSPAPDTGLSPSKRTHQRSKSDATASISLSSNLKRTASNPKVENEDEELSSSTESIDNSFSSPVRLAPEREFIKSLMAIGKRLATLPTKEQKTQRLISELSLLNHKLPARVWLPTAGFDHHVVRVPHTQAVVLNSKDKAPYLIYVEVLECENFDTTSVPARIPENRIRSTRSVENLPECGITHEQRAGSFSTVPNYDNDDEAWSVDDIGELQVELPEVHTNSCDNISQFSVDSITSQESKEPVFIAAGDIRRRLSEQLAHTPTAFKRDPEDPSAVALKEPWQEKVRRIREGSPYGHLPNWRLLSVIVKCGDDLRQELLAFQVLKQLQSIWEQERVPLWIKPYKILVISADSGMIEPVVNAVSIHQVKKQSQLSLLDYFLQEHGSYTTEAFLSAQRNFVQSCAGYCLVCYLLQVKDRHNGNILLDAEGHIIHIDFGFILSSSPRNLGFETSAFKLTTEFVDVMGGLDGDMFNYYKMLMLQGLIAARKHMDKVVQIVEIMQQGSQLPCFHGSSTIRNLKERFHMSMTEEQLQLLVEQMVDGSMRSITTKLYDGFQYLTNGIM
Inhibitor
Name:
BDBM489258
Synonyms:
2-[(1S)-1-Cyclopropylethyl]-6-(4-methyl-2-{[6-(3-oxomorpholin-4-yl)pyridin-2-yl]amino}-1,3-thiazol-5-yl)-N-(oxetan-3-yl)-3-oxo-2,3-dihydro-1H-isoindole-4-sulfonamide | US10961236, Example 31
Type:
Small organic molecule
Emp. Form.:
C29H32N6O6S2
Mol. Mass.:
624.731
SMILES:
C[C@@H](C1CC1)N1Cc2cc(cc(c2C1=O)S(=O)(=O)NC1COC1)-c1sc(Nc2cccc(n2)N2CCOCC2=O)nc1C |r|