Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.11.24 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
Search for more literature for 2.7.11.24

Application

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

Inhibitors

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Mammalia
-
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
MAP kinase
-
 Mammalia
mitogen-activated kinase
-
 Mammalia
p38 mitogen-activated protein kinase
-
 Mammalia

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Mammalia

IC50 Value

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