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Target
Phosphatidylinositol 3-kinase regulatory subunit alpha
Ligand
BDBM272997
Substrate
n/a
Meas. Tech.
TBD
Ki
0.102±n/a nM
Citation
 Braun, M; Garland, K; Hanan, E; Purkey, H; Staben, ST; Heald, RA; Knight, J; Macleod, C; Lu, A; Wu, G; Yeap, SK Tricyclic PI3K inhibitor compounds and methods of use US Patent  US10435414 Publication Date 10/8/2019
Target
Name:
Phosphatidylinositol 3-kinase regulatory subunit alpha
Synonyms:
GRB1 | P85A_HUMAN | PI3-kinase class I | PI3-kinase p85 subunit alpha | PI3-kinase p85-alpha subunit | PI3-kinase p85-subunit alpha | PI3-kinase subunit p85-alpha | PI3K | PIK3CG/PIK3R1 | PIK3R1 | Phosphatidylinositol 3-kinase 85 kDa regulatory subunit alpha (PI3K alpha) | Phosphatidylinositol 3-kinase regulatory subunit alpha (PI3K p85-alpha) | Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1) | Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3RI) | Phosphatidylinositol 3-kinase regulatory subunit alpha isoform 1 (PI3 Kinase alpha) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3Kalpha p85alpha) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3Kalpha) | Phosphoinositide 3-Kinase (PI3K) Chain B | PtdIns-3-kinase p85-alpha | p84 alpha | p85 alpha
Type:
Protein
Mol. Mass.:
83592.82
Organism:
Homo sapiens (Human)
Description:
P27986
Residue:
724
Sequence:
MSAEGYQYRALYDYKKEREEDIDLHLGDILTVNKGSLVALGFSDGQEARPEEIGWLNGYNETTGERGDFPGTYVEYIGRKKISPPTPKPRPPRPLPVAPGSSKTEADVEQQALTLPDLAEQFAPPDIAPPLLIKLVEAIEKKGLECSTLYRTQSSSNLAELRQLLDCDTPSVDLEMIDVHVLADAFKRYLLDLPNPVIPAAVYSEMISLAPEVQSSEEYIQLLKKLIRSPSIPHQYWLTLQYLLKHFFKLSQTSSKNLLNARVLSEIFSPMLFRFSAASSDNTENLIKVIEILISTEWNERQPAPALPPKPPKPTTVANNGMNNNMSLQDAEWYWGDISREEVNEKLRDTADGTFLVRDASTKMHGDYTLTLRKGGNNKLIKIFHRDGKYGFSDPLTFSSVVELINHYRNESLAQYNPKLDVKLLYPVSKYQQDQVVKEDNIEAVGKKLHEYNTQFQEKSREYDRLYEEYTRTSQEIQMKRTAIEAFNETIKIFEEQCQTQERYSKEYIEKFKREGNEKEIQRIMHNYDKLKSRISEIIDSRRRLEEDLKKQAAEYREIDKRMNSIKPDLIQLRKTRDQYLMWLTQKGVRQKKLNEWLGNENTEDQYSLVEDDEDLPHHDEKTWNVGSSNRNKAENLLRGKRDGTFLVRESSKQGCYACSVVVDGEVKHCVINKTATGYGFAEPYNLYSSLKELVLHYQHTSLVQHNDSLNVTLAYPVYAQQRR
  
Inhibitor
Name:
BDBM272997
Synonyms:
(R)-2-(4-(1-(2- aminooxazolo[4,5- b]pyridin-5-yl)- 7,8,9,10-tetrahydro-6- oxa-2,10a- diazacycloocta[cd]inden- 4-yl)-1H-pyrazol-1- yl)butanamide | US10065970, Example 302 | US10065970, Example 312 | US10435414, Example 302
Type:
Small organic molecule
Emp. Form.:
C24H24N8O3
Mol. Mass.:
472.4992
SMILES:
CC[C@H](C(N)=O)n1cc(cn1)-c1cc2OCCCCn3c(nc(c1)c23)-c1ccc2oc(N)nc2n1 |r|
Structure:
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