Ki Summary

Reaction Details

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Target

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform

Ligand

BDBM377060

Substrate/Competitor

n/a

Meas. Tech.

PI3Kdelta Scintillation Proximity Assay

IC50

<100±n/a nM

Citation

Combs, AP; Sparks, RB; Maduskuie, Jr., TP Bicyclic azaheterocyclobenzylamines as PI3K inhibitors US Patent US10259818 Publication Date 4/16/2019

More Info.:

Get all data from this article, Assay Method

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform

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:

MPPGVDCPMEFWTKEENQSVVVDFLLPTGVYLNFPVSRNANLSTIKQLLWHRAQYEPLFH
MLSGPEAYVFTCINQTAEQQELEDEQRRLCDVQPFLPVLRLVAREGDRVKKLINSQISLL
IGKGLHEFDSLCDPEVNDFRAKMCQFCEEAAARRQQLGWEAWLQYSFPLQLEPSAQTWGP
GTLRLPNRALLVNVKFEGSEESFTFQVSTKDVPLALMACALRKKATVFRQPLVEQPEDYT
LQVNGRHEYLYGSYPLCQFQYICSCLHSGLTPHLTMVHSSSILAMRDEQSNPAPQVQKPR
AKPPPIPAKKPSSVSLWSLEQPFRIELIQGSKVNADERMKLVVQAGLFHGNEMLCKTVSS
SEVSVCSEPVWKQRLEFDINICDLPRMARLCFALYAVIEKAKKARSTKKKSKKADCPIAW
ANLMLFDYKDQLKTGERCLYMWPSVPDEKGELLNPTGTVRSNPNTDSAAALLICLPEVAP
HPVYYPALEKILELGRHSECVHVTEEEQLQLREILERRGSGELYEHEKDLVWKLRHEVQE
HFPEALARLLLVTKWNKHEDVAQMLYLLCSWPELPVLSALELLDFSFPDCHVGSFAIKSL
RKLTDDELFQYLLQLVQVLKYESYLDCELTKFLLDRALANRKIGHFLFWHLRSEMHVPSV
ALRFGLILEAYCRGSTHHMKVLMKQGEALSKLKALNDFVKLSSQKTPKPQTKELMHLCMR
QEAYLEALSHLQSPLDPSTLLAEVCVEQCTFMDSKMKPLWIMYSNEEAGSGGSVGIIFKN
GDDLRQDMLTLQMIQLMDVLWKQEGLDLRMTPYGCLPTGDRTGLIEVVLRSDTIANIQLN
KSNMAATAAFNKDALLNWLKSKNPGEALDRAIEEFTLSCAGYCVATYVLGIGDRHSDNIM
IRESGQLFHIDFGHFLGNFKTKFGINRERVPFILTYDFVHVIQQGKTNNSEKFERFRGYC
ERAYTILRRHGLLFLHLFALMRAAGLPELSCSKDIQYLKDSLALGKTEEEALKHFRVKFN
EALRESWKTKVNWLAHNVSKDNRQ

BDBM377060

n/a

Name

BDBM377060

Synonyms:

US10259818, Example 42 | US9944646, Example 42

Type

Small organic molecule

Emp. Form.

C23H26ClFN6O3

Mol. Mass.

488.942

SMILES

CC(c1cc(Cl)c(F)c2CN(C[C@@H](C)Oc12)C1CC(C1)C(O)=O)n1nc(C)c2c(N)ncnc12 |r,wU:12.12,(2.11,-1.89,;.78,-2.66,;-.56,-1.89,;-1.89,-2.66,;-3.23,-1.89,;-4.56,-2.66,;-3.23,-.35,;-4.56,.42,;-1.89,.42,;-2.12,1.95,;-1.07,3.08,;.46,2.96,;1.33,1.69,;2.85,1.92,;.88,.22,;-.56,-.35,;-1.64,4.51,;-1.02,5.92,;-2.43,6.54,;-3.05,5.13,;-2.99,7.97,;-2.03,9.17,;-4.52,8.2,;.78,-4.2,;-.47,-5.1,;.01,-6.57,;-.9,-7.81,;1.55,-6.57,;2.58,-7.71,;2.1,-9.17,;4.08,-7.39,;4.56,-5.93,;3.53,-4.78,;2.02,-5.1,)|

Structure