Reaction Details
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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
Ligand
BDBM415499
Substrate
n/a
Meas. Tech.
Scintillation Proximity Assay
IC50
300±n/a nM
Citation
Li, Y; Metcalf, BW; Combs, AP Pyrimidinones as PI3K inhibitors US Patent US10829502 Publication Date 11/10/2020 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:
BDBM415499
Synonyms:
6-(2-chlorophenyl)-3-methyl-7-[1-(9H-purin-6-ylamino)ethyl]-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one trifluoroacetic acid salt | US10428087, Example 43 | US10829502, Example 43-1 | US11401280, Example 43-1
Type:
Small organic molecule
Emp. Form.:
C20H16ClN7OS
Mol. Mass.:
437.905
SMILES:
C[C@@H](Nc1ncnc2[nH]cnc12)c1nc2scc(C)n2c(=O)c1-c1ccccc1Cl |r,wU:1.0,(3.23,1.21,;1.9,.45,;1.9,-1.09,;3.24,-1.86,;4.57,-1.09,;5.91,-1.86,;5.91,-3.4,;4.57,-4.17,;4.25,-5.68,;2.72,-5.84,;2.09,-4.43,;3.24,-3.4,;.57,1.22,;-.76,.45,;-2.1,1.22,;-3.56,.74,;-4.47,1.99,;-3.56,3.23,;-3.96,4.72,;-2.1,2.76,;-.76,3.53,;-.76,5.06,;.57,2.76,;1.9,3.53,;3.24,2.76,;4.57,3.53,;4.57,5.07,;3.24,5.84,;1.9,5.07,;.57,5.84,)|
Structure:
