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Target
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta
Ligand
BDBM25018
Substrate
BDBM15235
Meas. Tech.
Scintillation Proximity Assay
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
220±n/a nM
Citation
Hayakawa, M; Kawaguchi, K; Kaizawa, H; Koizumi, T; Ohishi, T; Yamano, M; Okada, M; Ohta, M; Tsukamoto, S; Raynaud, FI; Parker, P; Workman, P; Waterfield, MD Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem 15:5837-44 (2007) [PubMed] Article
More Info.:
Target
Name:
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta
Synonyms:
C2-PI3K | P3C2B_HUMAN | PI3K-C2beta | PIK3C2B | Phosphatidylinositol 4-phosphate 3-kinase C2 beta (PIK3C2B) | Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide | Phosphoinositide 3-Kinase (PI3K), C2beta | Phosphoinositide 3-Kinase-C2-beta | PtdIns-3-kinase C2 beta
Type:
Enzyme
Mol. Mass.:
184784.86
Organism:
Homo sapiens (Human)
Description:
O00750
Residue:
1634
Sequence:
MSSTQGNGEHWKSLESVGISRKELAMAEALQMEYDALSRLRHDKEENRAKQNADPSLISWDEPGVDFYSKPAGRRTDLKLLRGLSGSDPTLNYNSLSPQEGPPNHSTSQGPQPGSDPWPKGSLSGDYLYIFDGSDGGVSSSPGPGDIEGSCKKLSPPPLPPRASIWDTPPLPPRKGSPSSSKISQPSDINTFSLVEQLPGKLLEHRILEEEEVLGGGGQGRLLGSVDYDGINDAITRLNLKSTYDAEMLRDATRGWKEGRGPLDFSKDTSGKPVARSKTMPPQVPPRTYASRYGNRKNATPGKNRRISAAPVGSRPHTVANGHELFEVSEERDEEVAAFCHMLDILRSGSDIQDYFLTGYVWSAVTPSPEHLGDEVNLKVTVLCDRLQEALTFTCNCSSTVDLLIYQTLCYTHDDLRNVDVGDFVLKPCGLEEFLQNKHALGSHEYIQYCRKFDIDIRLQLMEQKVVRSDLARTVNDDQSPSTLNYLVHLQERPVKQTISRQALSLLFDTYHNEVDAFLLADGDFPLKADRVVQSVKAICNALAAVETPEITSALNQLPPCPSRMQPKIQKDPSVLAVRENREKVVEALTAAILDLVELYCNTFNADFQTAVPGSRKHDLVQEACHFARSLAFTVYATHRIPIIWATSYEDFYLSCSLSHGGKELCSPLQTRRAHFSKYLFHLIVWDQQICFPVQVNRLPRETLLCATLYALPIPPPGSSSEANKQRRVPEALGWVTTPLFNFRQVLTCGRKLLGLWPATQENPSARWSAPNFHQPDSVILQIDFPTSAFDIKFTSPPGDKFSPRYEFGSLREEDQRKLKDIMQKESLYWLTDADKKRLWEKRYYCHSEVSSLPLVLASAPSWEWACLPDIYVLLKQWTHMNHQDALGLLHATFPDQEVRRMAVQWIGSLSDAELLDYLPQLVQALKYECYLDSPLVRFLLKRAVSDLRVTHYFFWLLKDGLKDSQFSIRYQYLLAALLCCCGKGLREEFNRQCWLVNALAKLAQQVREAAPSARQGILRTGLEEVKQFFALNGSCRLPLSPSLLVKGIVPRDCSYFNSNAVPLKLSFQNVDPLGENIRVIFKCGDDLRQDMLTLQMIRIMSKIWVQEGLDMRMVIFRCFSTGRGRGMVEMIPNAETLRKIQVEHGVTGSFKDRPLADWLQKHNPGEDEYEKAVENFIYSCAGCCVATYVLGICDRHNDNIMLKTTGHMFHIDFGRFLGHAQMFGNIKRDRAPFVFTSDMAYVINGGDKPSSRFHDFVDLCCQAYNLIRKHTHLFLNLLGLMLSCGIPELSDLEDLKYVYDALRPQDTEANATTYFTRLIESSLGSVATKLNFFIHNLAQMKFTGSDDRLTLSFASRTHTLKSSGRISDVFLCRHEKIFHPNKGYIYVVKVMRENTHEATYIQRTFEEFQELHNKLRLLFPSSHLPSFPSRFVIGRSRGEAVAERRREELNGYIWHLIHAPPEVAECDLVYTFFHPLPRDEKAMGTSPAPKSSDGTWARPVGKVGGEVKLSISYKNNKLFIMVMHIRGLQLLQDGNDPDPYVKIYLLPDPQKTTKRKTKVARKTCNPTYNEMLVYDGIPKGDLQQRELQLSVLSEQGFWENVLLGEVNIRLRELDLAQEKTGWFALGSRSHGTL
Inhibitor
Name:
BDBM25018
Synonyms:
3-(4-morpholin-4-ylthieno[3,2-d]pyrimidin-2-yl)phenol | 3-[4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-2-yl]phenol | CHEMBL541643 | thieno[3,2-d]pyrimidine derivative, 1 | thienopyrimidine derivative, 1
Type:
Small organic molecule
Emp. Form.:
C16H15N3O2S
Mol. Mass.:
313.374
SMILES:
Oc1cccc(c1)-c1nc(N2CCOCC2)c2sccc2n1
Substrate
Name:
BDBM15235
Synonyms:
L-alpha-Phosphatidylinositol 4,5-bisphosphate | Phosphatidylinositol-4,5-bisphosphate (PIP2) | PtdInsP2
Type:
Small organic molecule
Emp. Form.:
C47H80O19P3
Mol. Mass.:
1042.0507
SMILES:
CCCCCCCCCCCCCCCCCC(=O)OCC(COP([O-])(=O)O[C@@H]1[C@H](O)[C@H](O)[C@@H](OP([O-])([O-])=O)[C@H](OP([O-])([O-])=O)[C@H]1O)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC