Ki Summary

Reaction Details

Report a problem with these data

Target

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

Ligand

BDBM118248

Substrate

n/a

Meas. Tech.

Enzyme Assay

IC50

14±n/a nM

Citation

Cooke, NG; Fernandes Gomes Dos Santos, P; Graveleau, N; Hebach, C; Högenauer, K; Hollingworth, G; Smith, AB; Soldermann, N; Stowasser, F; Strang, R; Tufilli, N; Von Matt, A; Wolf, R; Zecri, F Tetrahydro-pyrido-pyrimidine derivatives US Patent US8653092 Publication Date 2/18/2014

More Info.:

Get all data from this article, Assay Method

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:

BDBM118248

Synonyms:

US8653092, 15

Type:

Small organic molecule

Emp. Form.:

C24H31N5O4

Mol. Mass.:

453.534

SMILES:

COC1CC(C1)C(=O)N1CC[C@@H](C1)Oc1ncnc2CCN(Cc12)c1cnc(OC)c(C)c1 |r,wD:11.14,(9,5.87,;8.61,4.38,;7.12,3.98,;6.35,2.65,;5.02,3.42,;5.79,4.75,;3.53,3.02,;2.44,4.11,;3.13,1.53,;4.03,.29,;3.13,-.96,;1.66,-.48,;1.66,1.06,;.33,-1.25,;.33,-2.79,;1.66,-3.56,;1.66,-5.1,;.33,-5.87,;-1,-5.1,;-2.34,-5.87,;-3.67,-5.1,;-3.67,-3.56,;-2.34,-2.79,;-1,-3.56,;-5,-2.79,;-5,-1.25,;-6.34,-.48,;-7.67,-1.25,;-9,-.48,;-9,1.06,;-7.67,-2.79,;-9,-3.56,;-6.34,-3.56,)|

Structure: