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Target
Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit delta isoform
Ligand
BDBM185152
Substrate
n/a
Meas. Tech.
Invitrogen SelectScreen Enzymatic Assay
IC50
856±0.0 nM
Citation
 Liu, F; Wang, J; Yang, X; Li, B; Wu, H; Qi, S; Chen, C; Liu, X; Yu, K; Wang, W; Zhao, Z; Wang, A; Chen, Y; Wang, L; Gray, NS; Liu, J; Zhang, X; Liu, Q Discovery of a Highly Selective STK16 Kinase Inhibitor. ACS Chem Biol 11:1537-43 (2016) [PubMed]  Article
Target
Name:
Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit delta isoform
Synonyms:
PI3-kinase p110-delta/p85-alpha | PI3-kinase p110-delta/p85-alpha subunit | PI3-kinase subunit p110 delta/p85 alpha | PI3K p110delta/p85alpha (Human) | PIK3CD/PIK3R1 | Phosphoinositide 3-Kinase (PI3K), delta | p110delta/p85alpha
Type:
Heterodimer of a p110 (catalytic) and a p85 (regulatory) subunit
Mol. Mass.:
n/a
Description:
Recombinant human p110delta was coexpressed in an Sf9 baculovirus system with the p85alpha regulatory subunit and purified as GST-fusion protein using affinity chromatography on glutathione-sepharose.
Components:
This complex has 2 components.
Component 1
Name:
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
Synonyms:
PI3-kinase p110 subunit delta | PI3-kinase p110-delta subunit | PI3-kinase subunit p110-delta | PI3K | PIK3CD | PK3CD_HUMAN | Phosphatidylinositol 4,5-biphosphate 3-kinase catalytic subunit delta (PIK3CD) | Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit delta | Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit delta (PI3K delta) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic (PI3K) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta (PI3Kdelta) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform ( PI3K-delta) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PI3K delta) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PI3K) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PI3K-delta) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PI3Kd) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PI3Kdelta)
Type:
Enzyme Subunit
Mol. Mass.:
119489.41
Organism:
Homo sapiens (Human)
Description:
O00329
Residue:
1044
Sequence:
MPPGVDCPMEFWTKEENQSVVVDFLLPTGVYLNFPVSRNANLSTIKQLLWHRAQYEPLFHMLSGPEAYVFTCINQTAEQQELEDEQRRLCDVQPFLPVLRLVAREGDRVKKLINSQISLLIGKGLHEFDSLCDPEVNDFRAKMCQFCEEAAARRQQLGWEAWLQYSFPLQLEPSAQTWGPGTLRLPNRALLVNVKFEGSEESFTFQVSTKDVPLALMACALRKKATVFRQPLVEQPEDYTLQVNGRHEYLYGSYPLCQFQYICSCLHSGLTPHLTMVHSSSILAMRDEQSNPAPQVQKPRAKPPPIPAKKPSSVSLWSLEQPFRIELIQGSKVNADERMKLVVQAGLFHGNEMLCKTVSSSEVSVCSEPVWKQRLEFDINICDLPRMARLCFALYAVIEKAKKARSTKKKSKKADCPIAWANLMLFDYKDQLKTGERCLYMWPSVPDEKGELLNPTGTVRSNPNTDSAAALLICLPEVAPHPVYYPALEKILELGRHSECVHVTEEEQLQLREILERRGSGELYEHEKDLVWKLRHEVQEHFPEALARLLLVTKWNKHEDVAQMLYLLCSWPELPVLSALELLDFSFPDCHVGSFAIKSLRKLTDDELFQYLLQLVQVLKYESYLDCELTKFLLDRALANRKIGHFLFWHLRSEMHVPSVALRFGLILEAYCRGSTHHMKVLMKQGEALSKLKALNDFVKLSSQKTPKPQTKELMHLCMRQEAYLEALSHLQSPLDPSTLLAEVCVEQCTFMDSKMKPLWIMYSNEEAGSGGSVGIIFKNGDDLRQDMLTLQMIQLMDVLWKQEGLDLRMTPYGCLPTGDRTGLIEVVLRSDTIANIQLNKSNMAATAAFNKDALLNWLKSKNPGEALDRAIEEFTLSCAGYCVATYVLGIGDRHSDNIMIRESGQLFHIDFGHFLGNFKTKFGINRERVPFILTYDFVHVIQQGKTNNSEKFERFRGYCERAYTILRRHGLLFLHLFALMRAAGLPELSCSKDIQYLKDSLALGKTEEEALKHFRVKFNEALRESWKTKVNWLAHNVSKDNRQ
  
Component 2
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:
BDBM185152
Synonyms:
STK16-IN-1
Type:
Small organic molecule
Emp. Form.:
C16H10FN3O2
Mol. Mass.:
295.2679
SMILES:
Oc1cc(ccc1F)-n1c2c3cc[nH]c3ncc2ccc1=O
Structure:
Search PDB for entries with ligand similarity: