Target
Phosphatidylinositol 3-kinase regulatory subunit beta
Ligand
BDBM362107
Substrate
n/a
Meas. Tech.
TR-FRET assays for PI3K isoforms
IC50
1000±n/a nM
Citation
 Du, ZEvarts, JKaplan, JKim, MNaduthambi, DPatel, LPerreault, SPhillips, BWPhillips, GStevens, KLTreiberg, JAVan Veldhuizen, JWatkins, WJYeung, SC Phosphatidylinositol 3-kinase inhibitors US Patent  US10221197 Publication Date 3/5/2019 
Target
Name:
Phosphatidylinositol 3-kinase regulatory subunit beta
Synonyms:
P85B_HUMAN | PI3-kinase regulatory subunit beta | PI3-kinase subunit p85-beta | PI3K regulatory subunit beta | PIK3R2 | Phosphatidylinositol 3-kinase 85 kDa regulatory subunit beta | PtdIns-3-kinase regulatory subunit beta | PtdIns-3-kinase regulatory subunit p85-beta
Type:
Enzyme Subunit
Mol. Mass.:
81542.75
Organism:
Homo sapiens (Human)
Description:
O00459
Residue:
728
Sequence:
MAGPEGFQYRALYPFRRERPEDLELLPGDVLVVSRAALQALGVAEGGERCPQSVGWMPGLNERTRQRGDFPGTYVEFLGPVALARPGPRPRGPRPLPARPRDGAPEPGLTLPDLPEQFSPPDVAPPLLVKLVEAIERTGLDSESHYRPELPAPRTDWSLSDVDQWDTAALADGIKSFLLALPAPLVTPEASAEARRALREAAGPVGPALEPPTLPLHRALTLRFLLQHLGRVASRAPALGPAVRALGATFGPLLLRAPPPPSSPPPGGAPDGSEPSPDFPALLVEKLLQEHLEEQEVAPPALPPKPPKAKPASTVLANGGSPPSLQDAEWYWGDISREEVNEKLRDTPDGTFLVRDASSKIQGEYTLTLRKGGNNKLIKVFHRDGHYGFSEPLTFCSVVDLINHYRHESLAQYNAKLDTRLLYPVSKYQQDQIVKEDSVEAVGAQLKVYHQQYQDKSREYDQLYEEYTRTSQELQMKRTAIEAFNETIKIFEEQGQTQEKCSKEYLERFRREGNEKEMQRILLNSERLKSRIAEIHESRTKLEQQLRAQASDNREIDKRMNSLKPDLMQLRKIRDQYLVWLTQKGARQKKINEWLGIKNETEDQYALMEDEDDLPHHEERTWYVGKINRTQAEEMLSGKRDGTFLIRESSQRGCYACSVVVDGDTKHCVIYRTATGFGFAEPYNLYGSLKELVLHYQHASLVQHNDALTVTLAHPVRAPGPGPPPAAR
  
Inhibitor
Name:
BDBM362107
Synonyms:
(S)-1-(3-(2-(1-((6-amino-5-cyanopyrimidin-4-yl)amino)ethyl)-5-chloro-4-oxoquinazolin-3(4H)-yl)phenyl)-3-(2-chlorophenyl)urea | US10221197, Compound 100 | US10221197, Compound 113
Type:
Small organic molecule
Emp. Form.:
C29H21ClF3N9O2
Mol. Mass.:
619.984
SMILES:
C[C@H](Nc1ncnc(N)c1C#N)c1nc2cccc(Cl)c2c(=O)n1-c1cccc(NC(=O)Nc2ccccc2C(F)(F)F)c1 |r|
Structure:
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