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Literature summary for 2.7.11.24 extracted from

  • Liu, C.; Lin, J.; Pitt, S.; Zhang, R.F.; Sack, J.S.; Kiefer, S.E.; Kish, K.; Doweyko, A.M.; Zhang, H.; Marathe, P.H.; Trzaskos, J.; Mckinnon, M.; Dodd, J.H.; Barrish, J.C.; Schieven, G.L.; Leftheris, K.
    Benzothiazole based inhibitors of p38alpha MAP kinase (2008), Bioorg. Med. Chem. Lett., 18, 1874-1879.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
6-[1-(2-chlorophenyl)-1H-pyrazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[1-(2-fluorophenyl)-1H-pyrazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[1-(3-chlorophenyl)-1H-pyrazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[1-(3-fluorophenyl)-1H-pyrazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[1-(4-chlorophenyl)-1H-pyrazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[1-(4-fluorophenyl)-1H-pyrazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[4-(2-fluorophenyl)-1,3-oxazol-5-yl]-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[4-(2-fluorophenyl)-1,3-oxazol-5-yl]-1,3-benzothiazole
-
Rattus norvegicus
6-[4-(2-fluorophenyl)-1,3-oxazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[4-(2-fluorophenyl)-1,3-oxazol-5-yl]-N-[(1R)-1-methylpropyl]-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[4-(2-fluorophenyl)-1,3-oxazol-5-yl]-N-[(1S)-1-methylpropyl]-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[4-(2-fluorophenyl)-1H-imidazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[4-(2-fluorophenyl)-1H-imidazol-5-yl]-N-[(1R)-1-methylpropyl]-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[4-(2-fluorophenyl)-1H-imidazol-5-yl]-N-[(1S)-1-methylpropyl]-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[5-amino-1-ethyl-3-(2-fluorophenyl)-1H-pyrazol-4-yl]-N-[(1R)-1-methylpropyl]-2,3-dihydro-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[5-amino-3-(2-fluorophenyl)-1-methyl-1H-pyrazol-4-yl]-N-[(1R)-1-methylpropyl]-2,3-dihydro-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[5-amino-3-(2-fluorophenyl)-1H-pyrazol-4-yl]-N-(1-methylethyl)-2,3-dihydro-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[5-amino-3-(2-fluorophenyl)-1H-pyrazol-4-yl]-N-[(1R)-1-methylpropyl]-2,3-dihydro-1,3-benzothiazol-2-amine
-
Rattus norvegicus
6-[5-amino-3-(2-fluorophenyl)-1H-pyrazol-4-yl]-N-[(1S)-1-methylpropyl]-2,3-dihydro-1,3-benzothiazol-2-amine
-
Rattus norvegicus
additional information synthesis of benzothiazole based inhibitors of p38alpha MAP kinase Rattus norvegicus
N-(1-methylethyl)-6-(1-phenyl-1H-pyrazol-5-yl)-1,3-benzothiazol-2-amine
-
Rattus norvegicus
N-(1-methylethyl)-6-(4-phenyl-1,3-oxazol-5-yl)-1,3-benzothiazol-2-amine
-
Rattus norvegicus
N-(1-methylethyl)-6-(4-phenyl-1H-imidazol-5-yl)-1,3-benzothiazol-2-amine
-
Rattus norvegicus
N-(1-methylethyl)-6-[1-(2-methylphenyl)-1H-pyrazol-5-yl]-1,3-benzothiazol-2-amine
-
Rattus norvegicus
N-(1-methylethyl)-6-[1-(3-methylphenyl)-1H-pyrazol-5-yl]-1,3-benzothiazol-2-amine
-
Rattus norvegicus
N-(1-methylethyl)-6-[1-(4-methylphenyl)-1H-pyrazol-5-yl]-1,3-benzothiazol-2-amine
-
Rattus norvegicus
N-ethyl-6-[4-(2-fluorophenyl)-1,3-oxazol-5-yl]-1,3-benzothiazol-2-amine
-
Rattus norvegicus
SB203580
-
Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus P70618
-
-

Synonyms

Synonyms Comment Organism
p38alpha MAP kinase
-
Rattus norvegicus
p38alpha mitogen-activated protein kinase
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000016
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[4-(2-fluorophenyl)-1H-imidazol-5-yl]-N-[(1S)-1-methylpropyl]-1,3-benzothiazol-2-amine
0.0000027
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[4-(2-fluorophenyl)-1H-imidazol-5-yl]-N-[(1R)-1-methylpropyl]-1,3-benzothiazol-2-amine
0.0000032
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[5-amino-3-(2-fluorophenyl)-1H-pyrazol-4-yl]-N-[(1R)-1-methylpropyl]-2,3-dihydro-1,3-benzothiazol-2-amine
0.0000033
-
inhibition of p38alpha MAP kinase Rattus norvegicus N-(1-methylethyl)-6-(4-phenyl-1H-imidazol-5-yl)-1,3-benzothiazol-2-amine
0.0000033
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[4-(2-fluorophenyl)-1H-imidazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amine
0.0000037
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[5-amino-3-(2-fluorophenyl)-1H-pyrazol-4-yl]-N-(1-methylethyl)-2,3-dihydro-1,3-benzothiazol-2-amine
0.0000055
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[5-amino-3-(2-fluorophenyl)-1H-pyrazol-4-yl]-N-[(1S)-1-methylpropyl]-2,3-dihydro-1,3-benzothiazol-2-amine
0.0000064
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[4-(2-fluorophenyl)-1,3-oxazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amine
0.0000065
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[4-(2-fluorophenyl)-1,3-oxazol-5-yl]-N-[(1S)-1-methylpropyl]-1,3-benzothiazol-2-amine
0.00001
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[4-(2-fluorophenyl)-1,3-oxazol-5-yl]-N-[(1R)-1-methylpropyl]-1,3-benzothiazol-2-amine
0.000011
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[5-amino-3-(2-fluorophenyl)-1-methyl-1H-pyrazol-4-yl]-N-[(1R)-1-methylpropyl]-2,3-dihydro-1,3-benzothiazol-2-amine
0.000012
-
inhibition of p38alpha MAP kinase Rattus norvegicus N-ethyl-6-[4-(2-fluorophenyl)-1,3-oxazol-5-yl]-1,3-benzothiazol-2-amine
0.000016
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[4-(2-fluorophenyl)-1,3-oxazol-5-yl]-1,3-benzothiazol-2-amine
0.000017
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[5-amino-1-ethyl-3-(2-fluorophenyl)-1H-pyrazol-4-yl]-N-[(1R)-1-methylpropyl]-2,3-dihydro-1,3-benzothiazol-2-amine
0.00002
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[1-(2-fluorophenyl)-1H-pyrazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amine
0.000021
-
inhibition of p38alpha MAP kinase Rattus norvegicus N-(1-methylethyl)-6-(1-phenyl-1H-pyrazol-5-yl)-1,3-benzothiazol-2-amine
0.000021
-
inhibition of p38alpha MAP kinase Rattus norvegicus N-(1-methylethyl)-6-(4-phenyl-1,3-oxazol-5-yl)-1,3-benzothiazol-2-amine
0.000033
-
inhibition of p38alpha MAP kinase Rattus norvegicus N-(1-methylethyl)-6-[1-(3-methylphenyl)-1H-pyrazol-5-yl]-1,3-benzothiazol-2-amine
0.000033
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[1-(3-fluorophenyl)-1H-pyrazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amine
0.000047
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[4-(2-fluorophenyl)-1,3-oxazol-5-yl]-1,3-benzothiazole
0.000048
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[1-(4-fluorophenyl)-1H-pyrazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amine
0.000072
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[1-(3-chlorophenyl)-1H-pyrazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amine
0.000146
-
inhibition of p38alpha MAP kinase Rattus norvegicus N-(1-methylethyl)-6-[1-(2-methylphenyl)-1H-pyrazol-5-yl]-1,3-benzothiazol-2-amine
0.000175
-
inhibition of p38alpha MAP kinase Rattus norvegicus 6-[1-(2-chlorophenyl)-1H-pyrazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amine
0.001
-
above, inhibition of p38alpha MAP kinase Rattus norvegicus N-(1-methylethyl)-6-[1-(4-methylphenyl)-1H-pyrazol-5-yl]-1,3-benzothiazol-2-amine
0.001
-
above, inhibition of p38alpha MAP kinase Rattus norvegicus 6-[1-(4-chlorophenyl)-1H-pyrazol-5-yl]-N-(1-methylethyl)-1,3-benzothiazol-2-amine