Ki Summary

Reaction Details

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Target

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

Ligand

BDBM295058

Substrate/Competitor

n/a

Meas. Tech.

TR-FRET Adapta Assay for PI 3-Kinase Gamma (E), PI 3-Kinase Delta (F)

7.5±n/a

IC50

270±n/a nM

Comments

extracted

Citation

Bellenie, BR; Bloomfield, GC; Bruce, I; Culshaw, AJ; Hall, EC; Hollingworth, GJ; Neef, J; Spendiff, M; Watson, SJ Amino pyridine derivatives as phosphatidylinositol 3-kinase inhibitors US Patent US10112926 Publication Date 10/30/2018

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

BDBM295058

n/a

Name

BDBM295058

Synonyms:

US10112926, Example 12 | trans 3-[6-Amino-5-(3-methyl-[1,2,4]oxadiazol-5-yl)-pyridin-3-yl]-N-(4-hydroxy-cyclohexyl)-4-methyl-benzenesulfonamide, hydrochloride salt

Type

Small organic molecule

Emp. Form.

C21H25N5O4S

Mol. Mass.

443.519

SMILES

Cc1noc(n1)-c1cc(cnc1N)-c1cc(ccc1C)S(=O)(=O)N[C@H]1CC[C@H](O)CC1 |r,wU:24.26,wD:27.30,(7.05,-.65,;6.28,.68,;7.19,1.93,;6.28,3.17,;4.82,2.69,;4.82,1.15,;3.48,3.47,;2.15,2.69,;.82,3.47,;.82,5,;2.15,5.78,;3.48,5,;4.82,5.78,;-.52,2.69,;-.52,1.15,;-1.85,.38,;-3.19,1.15,;-3.19,2.69,;-1.85,3.47,;-1.85,5,;-1.85,-1.15,;-.31,-1.15,;-3.39,-1.15,;-1.85,-2.69,;-3.19,-3.47,;-3.19,-5,;-4.52,-5.78,;-5.85,-5,;-7.19,-5.78,;-5.85,-3.47,;-4.52,-2.69,)|

Structure