Reaction Details
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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
Ligand
BDBM25045
Substrate
n/a
Meas. Tech.
ChEMBL_438489 (CHEMBL887589)
IC50
250±n/a nM
Citation
Hayakawa, M; Kaizawa, H; Moritomo, H; Koizumi, T; Ohishi, T; Yamano, M; Okada, M; Ohta, M; Tsukamoto, S; Raynaud, FI; Workman, P; Waterfield, MD; Parker, P Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem Lett 17:2438-42 (2007) [PubMed] Article More Info.:
Target
Name:
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
Synonyms:
PI3-kinase p110 subunit gamma | PI3-kinase subunit p120-gamma | PI3Kgamma | PIK3CG | PK3CG_HUMAN | Phosphatidylinositol 4,5-biphosphate 3-kinase catalytic subunit gamma (PIK3CG) | Phosphatidylinositol 4,5-bisphosphate 3-kinase (PI3K) | Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit gamma (PI3K gamma) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma (PI3Kgamma) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (PI3K gamma) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (PI3K) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (PI3Kgamma) | Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | Phosphoinositide 3-Kinase (PI3K), gamma Chain A | Phosphoinositide 3-kinases gamma (PI3K gamma) | Phosphoinositide-3-kinase (PI3K gamma) | p120-PI3K
Type:
Enzyme Subunit
Mol. Mass.:
126470.30
Organism:
Homo sapiens (Human)
Description:
P48736
Residue:
1102
Sequence:
MELENYKQPVVLREDNCRRRRRMKPRSAAASLSSMELIPIEFVLPTSQRKCKSPETALLHVAGHGNVEQMKAQVWLRALETSVAADFYHRLGPHHFLLLYQKKGQWYEIYDKYQVVQTLDCLRYWKATHRSPGQIHLVQRHPPSEESQAFQRQLTALIGYDVTDVSNVHDDELEFTRRGLVTPRMAEVASRDPKLYAMHPWVTSKPLPEYLWKKIANNCIFIVIHRSTTSQTIKVSPDDTPGAILQSFFTKMAKKKSLMDIPESQSEQDFVLRVCGRDEYLVGETPIKNFQWVRHCLKNGEEIHVVLDTPPDPALDEVRKEEWPLVDDCTGVTGYHEQLTIHGKDHESVFTVSLWDCDRKFRVKIRGIDIPVLPRNTDLTVFVEANIQHGQQVLCQRRTSPKPFTEEVLWNVWLEFSIKIKDLPKGALLNLQIYCGKAPALSSKASAESPSSESKGKVQLLYYVNLLLIDHRFLLRRGEYVLHMWQISGKGEDQGSFNADKLTSATNPDKENSMSISILLDNYCHPIALPKHQPTPDPEGDRVRAEMPNQLRKQLEAIIATDPLNPLTAEDKELLWHFRYESLKHPKAYPKLFSSVKWGQQEIVAKTYQLLARREVWDQSALDVGLTMQLLDCNFSDENVRAIAVQKLESLEDDDVLHYLLQLVQAVKFEPYHDSALARFLLKRGLRNKRIGHFLFWFLRSEIAQSRHYQQRFAVILEAYLRGCGTAMLHDFTQQVQVIEMLQKVTLDIKSLSAEKYDVSSQVISQLKQKLENLQNSQLPESFRVPYDPGLKAGALAIEKCKVMASKKKPLWLEFKCADPTALSNETIGIIFKHGDDLRQDMLILQILRIMESIWETESLDLCLLPYGCISTGDKIGMIEIVKDATTIAKIQQSTVGNTGAFKDEVLNHWLKEKSPTEEKFQAAVERFVYSCAGYCVATFVLGIGDRHNDNIMITETGNLFHIDFGHILGNYKSFLGINKERVPFVLTPDFLFVMGTSGKKTSPHFQKFQDICVKAYLALRHHTNLLIILFSMMLMTGMPQLTSKEDIEYIRDALTVGKNEEDAKKYFLDQIEVCRDKGWTVQFNWFLHLVLGIKQGEKHSA
Inhibitor
Name:
BDBM25045
Synonyms:
3-(4-morpholin-4-ylpyrido[2,3]furo[2,4-b]pyrimidin-2-yl)phenol | 3-(4-morpholin-4-ylpyrido[3 ,2 :4,5]furo[3,2-d]pyrimidin-2-yl)phenol | 3-(4-morpholinopyrido[2,3]furo[2,4-b]pyrimidin-2-yl)phenol | 3-[4-(4-morpholinyl)-2-pyrido[2,3]furo[2,4-b]pyrimidinyl]phenol | 3-[6-(morpholin-4-yl)-8-oxa-3,5,10-triazatricyclo[7.4.0.0^{2,7}]trideca-1(9),2,4,6,10,12-hexaen-4-yl]phenol | CHEMBL538346 | PI-103 | US9637488, PI-103 | cid_9884685 | mTOR Inhibitor, PI103 | pyridofuropyrimidine derivative, 2
Type:
Small organic molecule
Emp. Form.:
C19H16N4O3
Mol. Mass.:
348.3553
SMILES:
Oc1cccc(c1)-c1nc(N2CCOCC2)c2oc3ncccc3c2n1
Structure:
