Reaction Details
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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
Ligand
BDBM489228
Substrate
n/a
Meas. Tech.
ChEMBL_2145003 (CHEMBL5029283)
IC50
1.000000±n/a nM
Citation
Perry, MWD; Björhall, K; Bold, P; Br?lls, M; Börjesson, U; Carlsson, J; Chang, HA; Chen, Y; Eriksson, A; Fihn, BM; Fransson, R; Fredlund, L; Ge, H; Huang, H; Karabelas, K; Lamm Bergström, E; Lever, S; Lindmark, H; Mogemark, M; Nikitidis, A; Palmgren, AP; Pemberton, N; Petersen, J; Rodrigo Blomqvist, M; Smith, RW; Thomas, MJ; Ullah, V; Tyrchan, C; Wennberg, T; Westin Eriksson, A; Yang, W; Zhao, S; Öster, L Discovery of AZD8154, a Dual PI3K?? Inhibitor for the Treatment of Asthma. J Med Chem 64:8053-8075 (2021) [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:
BDBM489228
Synonyms:
N-{6-[(5-{2-[(1S)-1-Cyclopropylethyl]-7-(methylsulfonyl)-1-oxo-2,3-dihydro-1H-isoindol-5-yl}-4-methyl-1,3-thiazol-2-yl)amino]pyridin-2-yl}acetamide | US10961236, Example 2
Type:
Small organic molecule
Emp. Form.:
C25H27N5O4S2
Mol. Mass.:
525.643
SMILES:
C[C@@H](C1CC1)N1Cc2cc(cc(c2C1=O)S(C)(=O)=O)-c1sc(Nc2cccc(NC(C)=O)n2)nc1C |r|
Structure:
