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Literature summary extracted from

  • Karcher, S.C.; Laufer, S.A.
    Aza-analogue dibenzepinone scaffolds as p38 mitogen-activated protein kinase inhibitors: design, synthesis, and biological data of inhibitors with improved physicochemical properties (2009), J. Med. Chem., 52, 1778-1782.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.11.24 medicine p38 mitogen-activated protein kinase is a promising target for the treatment of chronic inflammatory diseases such as rheumatoid arthritis Mammalia

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.24 2-[(2,4-difluorophenyl)amino]-10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-one
-
 Mammalia
2.7.11.24 2-[(2,4-difluorophenyl)amino]-5H-dibenzo[a,d][7]annulen-5-one
-
 Mammalia
2.7.11.24 2-[(2-amino-4-fluorophenyl)amino]-10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-one
-
 Mammalia
2.7.11.24 2-[(2-aminophenyl)amino]-10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-one
-
 Mammalia
2.7.11.24 2-[(2-aminophenyl)amino]-5H-dibenzo[a,d][7]annulen-5-one
-
 Mammalia
2.7.11.24 3-[(2,4-difluorophenyl)amino]dibenzo[b,e]oxepin-11(6H)-one
-
 Mammalia
2.7.11.24 3-[(2-amino-4-fluorophenyl)amino]dibenzo[b,e]oxepin-11(6H)-one
-
 Mammalia
2.7.11.24 3-[(2-aminophenyl)amino]dibenzo[b,e]oxepin-11(6H)-one
-
 Mammalia
2.7.11.24 8-[(2,4-difluorophenyl)amino]-10,11-dihydro-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one
-
 Mammalia
2.7.11.24 8-[(2,4-difluorophenyl)amino]-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one
-
 Mammalia
2.7.11.24 8-[(2,4-difluorophenyl)amino][1]benzoxepino[3,4-b]pyridin-5(11H)-one
-
 Mammalia
2.7.11.24 8-[(2-amino-4-fluorophenyl)amino]-10,11-dihydro-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one
-
 Mammalia
2.7.11.24 8-[(2-amino-4-fluorophenyl)amino][1]benzoxepino[3,4-b]pyridin-5(11H)-one
-
 Mammalia
2.7.11.24 8-[(2-aminophenyl)amino]-10,11-dihydro-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one
-
 Mammalia
2.7.11.24 8-[(2-aminophenyl)amino]-11H-benzo[5,6]cyclohepta[1,2-c]pyridin-11-one
-
 Mammalia
2.7.11.24 8-[(2-aminophenyl)amino]-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-one
-
 Mammalia
2.7.11.24 8-[(2-aminophenyl)amino]-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one
-
 Mammalia
2.7.11.24 8-[(2-aminophenyl)amino][1]benzoxepino[3,4-b]pyridin-5(11H)-one
-
 Mammalia
2.7.11.24 SB203580
-
 Mammalia

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.24 ATP + a protein Mammalia
-
 ADP + a phosphoprotein
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.24 Mammalia
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.24 ATP + a protein
-
 Mammalia ADP + a phosphoprotein
-
 ?
2.7.11.24 ATP + ATF-2 substrate in kinase activity assay Mammalia ADP + phosphorylated ATF-2
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.24 MAP kinase
-
 Mammalia
2.7.11.24 mitogen-activated kinase
-
 Mammalia
2.7.11.24 p38 mitogen-activated protein kinase
-
 Mammalia

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.24 ATP
-
 Mammalia

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.24 0.00004
-
-
 Mammalia 3-[(2-amino-4-fluorophenyl)amino]dibenzo[b,e]oxepin-11(6H)-one
2.7.11.24 0.00005
-
-
 Mammalia SB203580
2.7.11.24 0.0001
-
-
 Mammalia 2-[(2-aminophenyl)amino]-10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-one
2.7.11.24 0.00013
-
-
 Mammalia 2-[(2-amino-4-fluorophenyl)amino]-10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-one
2.7.11.24 0.00013
-
-
 Mammalia 2-[(2,4-difluorophenyl)amino]-10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-one
2.7.11.24 0.00018
-
-
 Mammalia 8-[(2,4-difluorophenyl)amino][1]benzoxepino[3,4-b]pyridin-5(11H)-one
2.7.11.24 0.00024
-
-
 Mammalia 8-[(2,4-difluorophenyl)amino]-10,11-dihydro-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one
2.7.11.24 0.00024
-
-
 Mammalia 3-[(2,4-difluorophenyl)amino]dibenzo[b,e]oxepin-11(6H)-one
2.7.11.24 0.0003
-
-
 Mammalia 3-[(2-aminophenyl)amino]dibenzo[b,e]oxepin-11(6H)-one
2.7.11.24 0.00031
-
-
 Mammalia 8-[(2-aminophenyl)amino]-10,11-dihydro-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one
2.7.11.24 0.00033
-
-
 Mammalia 8-[(2,4-difluorophenyl)amino]-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one
2.7.11.24 0.00044
-
-
 Mammalia 8-[(2-aminophenyl)amino]-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-one
2.7.11.24 0.00106
-
-
 Mammalia 2-[(2-aminophenyl)amino]-5H-dibenzo[a,d][7]annulen-5-one
2.7.11.24 0.00108
-
-
 Mammalia 8-[(2-aminophenyl)amino]-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one
2.7.11.24 0.00119
-
-
 Mammalia 8-[(2-amino-4-fluorophenyl)amino]-10,11-dihydro-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one
2.7.11.24 0.00195
-
-
 Mammalia 8-[(2-aminophenyl)amino]-11H-benzo[5,6]cyclohepta[1,2-c]pyridin-11-one
2.7.11.24 0.00253
-
-
 Mammalia 2-[(2,4-difluorophenyl)amino]-5H-dibenzo[a,d][7]annulen-5-one
2.7.11.24 0.00268
-
-
 Mammalia 8-[(2-aminophenyl)amino][1]benzoxepino[3,4-b]pyridin-5(11H)-one
2.7.11.24 0.00273
-
-
 Mammalia 8-[(2-amino-4-fluorophenyl)amino][1]benzoxepino[3,4-b]pyridin-5(11H)-one