Reaction Details |
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Target | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform |
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Ligand | BDBM50232430 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1647802 (CHEMBL3996858) |
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IC50 | 4.0±n/a nM |
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Citation | Qin, LY; Ruan, Z; Cherney, RJ; Dhar, TGM; Neels, J; Weigelt, CA; Sack, JS; Srivastava, AS; Cornelius, LAM; Tino, JA; Stefanski, K; Gu, X; Xie, J; Susulic, V; Yang, X; Yarde-Chinn, M; Skala, S; Bosnius, R; Goldstein, C; Davies, P; Ruepp, S; Salter-Cid, L; Bhide, RS; Poss, MA Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kd inhibitors. Bioorg Med Chem Lett27:855-861 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform |
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Name: | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform |
Synonyms: | PI3-kinase subunit delta | PI3K p110 delta/p85 alpha | PI3K-delta | PI3Kdelta | PK3CD_MOUSE | Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit delta | Pik3cd | PtdIns-3-kinase subunit delta | PtdIns-3-kinase subunit p110-delta | p110delta |
Type: | Enzyme |
Mol. Mass.: | 119725.20 |
Organism: | Mus musculus (Mouse) |
Description: | O35904 |
Residue: | 1043 |
Sequence: | MPPGVDCPMEFWTKEESQSVVVDFLLPTGVYLNFPVSRNANLSTIKQVLWHRAQYEPLFH
MLSDPEAYVFTCVNQTAEQQELEDEQRRLCDIQPFLPVLRLVAREGDRVKKLINSQISLL
IGKGLHEFDSLRDPEVNDFRTKMRQFCEEAAAHRQQLGWVEWLQYSFPLQLEPSARGWRA
GLLRVSNRALLVNVKFEGSEESFTFQVSTKDMPLALMACALRKKATVFRQPLVEQPEEYA
LQVNGRHEYLYGNYPLCHFQYICSCLHSGLTPHLTMVHSSSILAMRDEQSNPAPQVQKPR
AKPPPIPAKKPSSVSLWSLEQPFSIELIEGRKVNADERMKLVVQAGLFHGNEMLCKTVSS
SEVNVCSEPVWKQRLEFDISVCDLPRMARLCFALYAVVEKAKKARSTKKKSKKADCPIAW
ANLMLFDYKDQLKTGERCLYMWPSVPDEKGELLNPAGTVRGNPNTESAAALVIYLPEVAP
HPVYFPALEKILELGRHGERGRITEEELQLREILERRGSGELYEHEKDLVWKMRHEVQEH
FPEALARLLLVTKWNKHEDVAQMLYLLCSWPELPVLSALELLDFSFPDCYVGSFAIKSLR
KLTDDELFQYLLQLVQVLKYESYLDCELTKFLLGRALANRKIGHFLFWHLRSEMHVPSVA
LRFGLIMEAYCRGSTHHMKVLMKQGEALSKLKALNDFVKVSSQKTTKPQTKEMMHMCMRQ
ETYMEALSHLQSPLDPSTLLEEVCVEQCTFMDSKMKPLWIMYSSEEAGSAGNVGIIFKNG
DDLRQDMLTLQMIQLMDVLWKQEGLDLRMTPYGCLPTGDRTGLIEVVLHSDTIANIQLNK
SNMAATAAFNKDALLNWLKSKNPGEALDRAIEEFTLSCAGYCVATYVLGIGDRHSDNIMI
RESGQLFHIDFGHFLGNFKTKFGINRERVPFILTYDFVHVIQQGKTNNSEKFERFRGYCE
RAYTILRRHGLLFLHLFALMRAAGLPELSCSKDIQYLKDSLALGKTEEEALKHFRVKFNE
ALRESWKTKVNWLAHNVSKDNRQ
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BDBM50232430 |
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n/a |
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Name | BDBM50232430 |
Synonyms: | CHEMBL4061855 | US10214537, Example 262 |
Type | Small organic molecule |
Emp. Form. | C28H34N8O2 |
Mol. Mass. | 514.622 |
SMILES | C[C@H]1CN(C[C@@H](C)N1c1cccc(c1)-c1cc(-c2ccnn2C2CCOCC2)c2c(N)ncnn12)C(C)=O |r| |
Structure |
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