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Target
Mitogen-activated protein kinase 11
Ligand
BDBM50341346
Substrate
n/a
Meas. Tech.
ChEMBL_747813 (CHEMBL1781012)
Kd
8.7±n/a nM
Citation
Soth, M; Abbot, S; Abubakari, A; Arora, N; Arzeno, H; Billedeau, R; Dewdney, N; Durkin, K; Frauchiger, S; Ghate, M; Goldstein, DM; Hill, RJ; Kuglstatter, A; Li, F; Loe, B; McCaleb, K; McIntosh, J; Papp, E; Park, J; Stahl, M; Sung, ML; Suttman, R; Swinney, DC; Weller, P; Wong, B; Zecic, H; Gabriel, T 3-Amino-pyrazolo[3,4-d]pyrimidines as p38a kinase inhibitors: design and development to a highly selective lead. Bioorg Med Chem Lett 21:3452-6 (2011) [PubMed] Article
More Info.:
Target
Name:
Mitogen-activated protein kinase 11
Synonyms:
MAP kinase p38 | MAPK11 | MK11_HUMAN | Mitogen-activated protein kinase 11 | Mitogen-activated protein kinase p38 beta | PRKM11 | SAPK2 | SAPK2B | Stress-activated protein kinase 2 | p38 MAP kinase alpha/beta | p38-2 | p38-beta | p38b
Type:
Enzyme Catalytic Domain
Mol. Mass.:
41351.73
Organism:
Homo sapiens (Human)
Description:
gi_20128774
Residue:
364
Sequence:
MSGPRAGFYRQELNKTVWEVPQRLQGLRPVGSGAYGSVCSAYDARLRQKVAVKKLSRPFQSLIHARRTYRELRLLKHLKHENVIGLLDVFTPATSIEDFSEVYLVTTLMGADLNNIVKCQALSDEHVQFLVYQLLRGLKYIHSAGIIHRDLKPSNVAVNEDCELRILDFGLARQADEEMTGYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLQGKALFPGSDYIDQLKRIMEVVGTPSPEVLAKISSEHARTYIQSLPPMPQKDLSSIFRGANPLAIDLLGRMLVLDSDQRVSAAEALAHAYFSQYHDPEDEPEAEPYDESVEAKERTLEEWKELTYQEVLSFKPPEPPKPPGSLEIEQ
Inhibitor
Name:
BDBM50341346
Synonyms:
(R)-6-(2,4-difluorophenoxy)-8-methyl-2-(1-(methylsulfonyl)propan-2-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one | 6-(2,4-Difluorophenoxy)-2-((R)-2-methanesulfonyl-1-methyl-ethylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one | 6-(2,4-difluorophenoxy)-8-methyl-2-{[(1R)-1-methyl-2-(methylsulfonyl)ethyl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one | CHEMBL1232769
Type:
Small organic molecule
Emp. Form.:
C18H18F2N4O4S
Mol. Mass.:
424.422
SMILES:
C[C@H](CS(C)(=O)=O)Nc1ncc2cc(Oc3ccc(F)cc3F)c(=O)n(C)c2n1 |r|