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Literature summary for 2.7.11.24 extracted from

  • Wurz, R.P.; Pettus, L.H.; Henkle, B.; Sherman, L.; Plant, M.; Miner, K.; McBride, H.J.; Wong, L.M.; Saris, C.J.; Lee, M.R.; Chmait, S.; Mohr, C.; Hsieh, F.; Tasker, A.S.
    Part 2: Structure-activity relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase (2010), Bioorg. Med. Chem. Lett., 20, 1680-1684.
    View publication on PubMed
Search for more literature for 2.7.11.24

Application

Application Comment Organism
medicine p38alpha is an attractive target for small molecule drug discovery Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
 Homo sapiens
4-chloro-3-[[1-(2-chlorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-N-cyclopropylbenzamide
-
 Homo sapiens
4-chloro-N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
 Homo sapiens
4-chloro-N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]benzamide
-
 Homo sapiens
4-chloro-N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
 Homo sapiens
4-chloro-N-cyclopropyl-3-[[1-(2,5-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
 Homo sapiens
4-chloro-N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
 Homo sapiens
4-chloro-N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
 Homo sapiens
4-chloro-N-cyclopropyl-3-[[1-(3-fluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
 Homo sapiens
4-chloro-N-cyclopropyl-3-[[1-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
 Homo sapiens
4-chloro-N-cyclopropyl-3-[[1-(4-fluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
 Homo sapiens
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-fluorobenzamide
-
 Homo sapiens
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
 Homo sapiens
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]-4-methylbenzamide
-
 Homo sapiens
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
 Homo sapiens
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-5-fluoro-4-methylbenzamide
-
 Homo sapiens
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]-4-methylbenzamide
-
 Homo sapiens
N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
 Homo sapiens
N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]-4-methylbenzamide
-
 Homo sapiens
N-cyclopropyl-3-[[1-(3-fluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
 Homo sapiens
N-cyclopropyl-3-[[1-(4-fluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
 Homo sapiens
N-cyclopropyl-3-[[1-(4-fluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]-4-methylbenzamide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens Q16539
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + a protein
-
 Homo sapiens ADP + a phosphoprotein
-
 ?

Synonyms

Synonyms Comment Organism
MAP kinase
-
 Homo sapiens
MAPK
-
 Homo sapiens
mitogen-activated kinase
-
 Homo sapiens
p38alpha mitogen-activated protein kinase
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000014
-
 4-chloro-N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
 Homo sapiens
0.0000016
-
 4-chloro-3-[[1-(2-chlorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-N-cyclopropylbenzamide
-
 Homo sapiens
0.0000016
-
 4-chloro-N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
 Homo sapiens
0.0000017
-
 4-chloro-N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
 Homo sapiens
0.0000017
-
 N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
 Homo sapiens
0.0000021
-
 4-chloro-N-cyclopropyl-3-[[1-(2,5-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
 Homo sapiens
0.0000023
-
 4-chloro-N-cyclopropyl-3-[[1-(4-fluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
 Homo sapiens
0.0000027
-
 N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
 Homo sapiens
0.000003
-
 N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
 Homo sapiens
0.000003
-
 N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]-4-methylbenzamide
-
 Homo sapiens
0.0000033
-
 4-chloro-N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
 Homo sapiens
0.0000041
-
 N-cyclopropyl-3-[[1-(4-fluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
 Homo sapiens
0.0000046
-
 N-cyclopropyl-3-[[1-(3-fluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
 Homo sapiens
0.000005
-
 4-chloro-N-cyclopropyl-3-[[1-(3-fluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
 Homo sapiens
0.0000063
-
 N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]-4-methylbenzamide
-
 Homo sapiens
0.0000077
-
 N-cyclopropyl-3-[[1-(4-fluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]-4-methylbenzamide
-
 Homo sapiens
0.0000085
-
 4-chloro-N-cyclopropyl-3-[[1-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
 Homo sapiens
0.00001
-
 N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]-4-methylbenzamide
-
 Homo sapiens
0.00001
-
 N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-5-fluoro-4-methylbenzamide
-
 Homo sapiens
0.000012
-
 3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
 Homo sapiens
0.000036
-
 4-chloro-N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]benzamide
-
 Homo sapiens
0.000043
-
 N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-fluorobenzamide
-
 Homo sapiens

General Information

General Information Comment Organism
physiological function p38alpha mitogen-activated protein kinase is involved in the signaling cascade responsible for the development of inflammation, increased activity of the p38 enzyme results in cytokine overproduction Homo sapiens