Reaction Details |
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Target | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform |
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Ligand | BDBM50573180 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2119125 (CHEMBL4828191) |
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IC50 | 251±n/a nM |
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Citation | Down, K; Amour, A; Anderson, NA; Barton, N; Campos, S; Cannons, EP; Clissold, C; Convery, MA; Coward, JJ; Doyle, K; Duempelfeld, B; Edwards, CD; Goldsmith, MD; Krause, J; Mallett, DN; McGonagle, GA; Patel, VK; Rowedder, J; Rowland, P; Sharpe, A; Sriskantharajah, S; Thomas, DA; Thomson, DW; Uddin, S; Hamblin, JN; Hessel, EM Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3K? with a Novel Binding Mode. J Med Chem64:13780-13792 (2021) [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 gamma isoform |
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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: | MELENYKQPVVLREDNCRRRRRMKPRSAAASLSSMELIPIEFVLPTSQRKCKSPETALLH
VAGHGNVEQMKAQVWLRALETSVAADFYHRLGPHHFLLLYQKKGQWYEIYDKYQVVQTLD
CLRYWKATHRSPGQIHLVQRHPPSEESQAFQRQLTALIGYDVTDVSNVHDDELEFTRRGL
VTPRMAEVASRDPKLYAMHPWVTSKPLPEYLWKKIANNCIFIVIHRSTTSQTIKVSPDDT
PGAILQSFFTKMAKKKSLMDIPESQSEQDFVLRVCGRDEYLVGETPIKNFQWVRHCLKNG
EEIHVVLDTPPDPALDEVRKEEWPLVDDCTGVTGYHEQLTIHGKDHESVFTVSLWDCDRK
FRVKIRGIDIPVLPRNTDLTVFVEANIQHGQQVLCQRRTSPKPFTEEVLWNVWLEFSIKI
KDLPKGALLNLQIYCGKAPALSSKASAESPSSESKGKVQLLYYVNLLLIDHRFLLRRGEY
VLHMWQISGKGEDQGSFNADKLTSATNPDKENSMSISILLDNYCHPIALPKHQPTPDPEG
DRVRAEMPNQLRKQLEAIIATDPLNPLTAEDKELLWHFRYESLKHPKAYPKLFSSVKWGQ
QEIVAKTYQLLARREVWDQSALDVGLTMQLLDCNFSDENVRAIAVQKLESLEDDDVLHYL
LQLVQAVKFEPYHDSALARFLLKRGLRNKRIGHFLFWFLRSEIAQSRHYQQRFAVILEAY
LRGCGTAMLHDFTQQVQVIEMLQKVTLDIKSLSAEKYDVSSQVISQLKQKLENLQNSQLP
ESFRVPYDPGLKAGALAIEKCKVMASKKKPLWLEFKCADPTALSNETIGIIFKHGDDLRQ
DMLILQILRIMESIWETESLDLCLLPYGCISTGDKIGMIEIVKDATTIAKIQQSTVGNTG
AFKDEVLNHWLKEKSPTEEKFQAAVERFVYSCAGYCVATFVLGIGDRHNDNIMITETGNL
FHIDFGHILGNYKSFLGINKERVPFVLTPDFLFVMGTSGKKTSPHFQKFQDICVKAYLAL
RHHTNLLIILFSMMLMTGMPQLTSKEDIEYIRDALTVGKNEEDAKKYFLDQIEVCRDKGW
TVQFNWFLHLVLGIKQGEKHSA
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BDBM50573180 |
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n/a |
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Name | BDBM50573180 |
Synonyms: | CHEMBL4175737 |
Type | Small organic molecule |
Emp. Form. | C28H34FN5O5S |
Mol. Mass. | 571.663 |
SMILES | COc1ncc(cc1S(=O)(=O)Nc1ccnc(c1)-c1ccc(CN2C[C@H](C)O[C@H](C)C2)cc1F)N1CCOCC1 |r| |
Structure |
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