Ki Summary

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Target

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

Ligand

BDBM358754

Substrate/Competitor

n/a

Meas. Tech.

ADP-Glo Format PI3K Assay

IC50

0.700±n/a nM

Citation

Bhide, RS; Batt, DG; Cherney, RJ; Cornelius, LA; Liu, Q; Marcoux, D; Neels, J; Poss, MA; Ruan, Z; Shi, Q; Srivastava, AS; Qin, L; Tino, JA; Watterson, SH Bicyclic heteroaryl amine compounds US Patent US10214537 Publication Date 2/26/2019

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

BDBM358754

n/a

Name

BDBM358754

Synonyms:

4-acetyl-1-(3-(4-amino-5-chloro-6- fluoropyrrolo[2,1-f][1,2,4]triaizn-7-yl)- 2-fluorophenyl)-3,3- dimethylpiperazin-2-one-5,5,6,6-d4 | US10214537, Example 833

Type

Small organic molecule

Emp. Form.

C20H19ClF2N6O2

Mol. Mass.

448.854

SMILES

CC(=O)N1CCN(C(=O)C1(C)C)c1cccc(-c2c(F)c(Cl)c3c(N)ncnn23)c1F |(6.04,-5.05,;5.64,-3.56,;6.73,-2.47,;4.15,-3.16,;3.06,-4.25,;1.57,-3.85,;1.18,-2.36,;2.27,-1.27,;1.87,.21,;3.75,-1.67,;3.75,-.13,;5.24,-1.27,;-.31,-1.96,;-1.4,-3.05,;-2.89,-2.65,;-3.29,-1.17,;-2.2,-.08,;-2.6,1.41,;-1.69,2.66,;-.15,2.66,;-2.6,3.9,;-1.83,5.24,;-4.06,3.43,;-5.39,4.2,;-5.39,5.74,;-6.73,3.43,;-6.73,1.89,;-5.39,1.12,;-4.06,1.89,;-.71,-.48,;.38,.61,)|

Structure