Reaction Details
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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
Ligand
BDBM261143
Substrate
n/a
Meas. Tech.
Scintillation Proximity Assay
IC50
<10±n/a nM
Citation
Li, Y; Yao, W; Combs, AP; Mei, S; Glenn, J; Maduskuie, Jr., TP; Sparks, RB Heterocyclylamines as PI3K inhibitors US Patent US10646492 Publication Date 5/12/2020 More Info.:
Target
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
Inhibitor
Name:
BDBM261143
Synonyms:
3-{3-[1-(4-Amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-methoxy-6-methylphenyl}cyclobutanol trifluoroacetate | US10376513, Example 166 | US10646492, Example 166 | US11433071, Example 166 | US9707233, 166 | US9730939, Example 166 | US9932341, Example 166
Type:
Small organic molecule
Emp. Form.:
C20H24ClN5O2
Mol. Mass.:
401.89
SMILES:
COc1c(cc(Cl)c(C)c1C1CC(O)C1)C(C)n1nc(C)c2c(N)ncnc12 |(.77,1.41,;-.56,2.18,;-1.9,1.41,;-1.9,-.13,;-3.23,-.9,;-4.56,-.13,;-5.9,-.9,;-4.56,1.41,;-5.9,2.18,;-3.23,2.18,;-3.23,3.72,;-2.14,4.81,;-3.23,5.9,;-3.23,7.44,;-4.32,4.81,;-.56,-.9,;.77,-.13,;-.56,-2.44,;-1.81,-3.34,;-1.33,-4.81,;-2.1,-6.14,;.21,-4.81,;1.24,-5.95,;.84,-7.44,;2.74,-5.63,;3.22,-4.17,;2.19,-3.02,;.68,-3.34,)|
Structure:
