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Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform/Phosphoinositide 3-kinase regulatory subunit 5
Ligand
BDBM50533531
Substrate
n/a
Meas. Tech.
ChEMBL_1925729 (CHEMBL4428801)
IC50
80±n/a nM
Citation
 Zhang, JQ; Luo, YJ; Xiong, YS; Yu, Y; Tu, ZC; Long, ZJ; Lai, XJ; Chen, HX; Luo, Y; Weng, J; Lu, G Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. J Med Chem 59:7268-74 (2016) [PubMed]  Article 
Target
Name:
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform/Phosphoinositide 3-kinase regulatory subunit 5
Synonyms:
PI3-kinase subunit gamma/Phosphoinositide 3-kinase regulatory subunit 5 | Phosphoinositide 3-Kinase (PI3K), gamma
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
Heterodimer of a catalytic subunit (PIK3CG/p120) and a regulatory (PIK3R5a/p101) subunit.
Components:
This complex has 2 components.
Component 1
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
  
Component 2
Name:
Phosphoinositide 3-kinase regulatory subunit 5
Synonyms:
IB PI3-kinase p101 subunit | PI3-kinase p101 subunit | PI3R5_HUMAN | PIK3R5 | Phosphatidylinositol-4,5-bisphosphate 3-kinase regulatory subunit | Phosphoinositide 3-Kinase (PI3K), gamma Chain B | Phosphoinositide 3-kinase regulatory subunit 5 | PtdIns-3-kinase p101 | p101-PI3K
Type:
Enzyme Subunit
Mol. Mass.:
97349.51
Organism:
Homo sapiens (Human)
Description:
Phosphoinositide 3-kinase regulatory subunit 5, p101-PI3K.
Residue:
880
Sequence:
MQPGATTCTEDRIQHALERCLHGLSLSRRSTSWSAGLCLNCWSLQELVSRDPGHFLILLEQILQKTREVQEKGTYDLLTPLALLFYSTVLCTPHFPPDSDLLLKAASTYHRFLTWPVPYCSICQELLTFIDAELKAPGISYQRLVRAEQGLPIRSHRSSTVTVLLLNPVEVQAEFLAVANKLSTPGHSPHSAYTTLLLHAFQATFGAHCDVPGLHCRLQAKTLAELEDIFTETAEAQELASGIGDAAEARRWLRTKLQAVGEKAGFPGVLDTAKPGKLHTIPIPVARCYTYSWSQDSFDILQEILLKEQELLQPGILGDDEEEEEEEEEVEEDLETDGHCAERDSLLSTSSLASHDSTLSLASSQASGPALSRHLLTSFVSGLSDGMDSGYVEDSEESSSEWPWRRGSQERRGHRRPGQKFIRIYKLFKSTSQLVLRRDSRSLEGSSDTALPLRRAGSLCSPLDEPVSPPSRAQRSRSLPQPKLGTQLPSWLLAPASRPQRRRPFLSGDEDPKASTLRVVVFGSDRISGKVARAYSNLRRLENNRPLLTRFFKLQFFYVPVKRSHGTSPGACPPPRSQTPSPPTDSPRHASPGELGTTPWEESTNDISHYLGMLDPWYERNVLGLMHLPPEVLCQQSLKAEAQALEGSPTQLPILADMLLYYCRFAARPVLLQVYQTELTFITGEKTTEIFIHSLELGHSAATRAIKASGPGSKRLGIDGDREAVPLTLQIIYSKGAISGRSRWSNLEKVCTSVNLNKACRKQEELDSSMEALTLNLTEVVKRQNSKSKKGFNQISTSQIKVDKVQIIGSNSCPFAVCLDQDERKILQSVVRCEVSPCYKPEKSDLSSPPQTPPDLPAQAAPDLCSLLCLPIMTFSGALP
  
Inhibitor
Name:
BDBM50533531
Synonyms:
CHEMBL4555071
Type:
Small organic molecule
Emp. Form.:
C26H29F3N8O4S
Mol. Mass.:
606.62
SMILES:
CS(=O)(=O)N1CCN(CC1)C(=O)c1ccc(Nc2nc(cc(n2)-c2cnc(N)cc2C(F)(F)F)N2CCOCC2)cc1
Structure:
Search PDB for entries with ligand similarity: