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Literature summary for 2.7.11.24 extracted from

  • Hynes, J.; Wu, H.; Pitt, S.; Shen, D.R.; Zhang, R.; Schieven, G.L.; Gillooly, K.M.; Shuster, D.J.; Taylor, T.L.; Yang, X.; McIntyre, K.W.; McKinnon, M.; Zhang, H.; Marathe, P.H.; Doweyko, A.M.; Kish, K.; Kiefer, S.E.; Sack, J.S.; Newitt, J.A.; Barrish, J.C.; Dodd, J.; Leftheris, K.
    The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor (2008), Bioorg. Med. Chem. Lett., 18, 1762-1767.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide i.e. BMS-640994, a potent and efficacious p38alpha MAP kinase inhibitor; inhibition of p38alpha MAP kinase Homo sapiens
2-(ethylamino)-N-[5-(ethylcarbamoyl)-2-methylphenyl]-4-methyl-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
2-bromothiazole-5-carboxylic acid inhibition of p38alpha MAP kinase Homo sapiens
2-[(1-methylethyl)amino]-N-[2-methyl-5-(1H-pyrazol-5-ylcarbamoyl)phenyl]-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
2-[(1-methylethyl)amino]-N-[2-methyl-5-(methylcarbamoyl)phenyl]-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
2-[(1-methylethyl)amino]-N-[2-methyl-5-[(1-methyl-1H-pyrazol-5-yl)carbamoyl]phenyl]-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
2-[(2-methoxyethyl)amino]-N-[2-methyl-5-(methylcarbamoyl)phenyl]-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
3-[2-(cyclopropylamino)-6-oxo-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]-N,4-dimethylbenzamide inhibition of p38alpha MAP kinase Homo sapiens
3-[2-(cyclopropylamino)-6-oxo-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]-N-ethyl-4-methylbenzamide inhibition of p38alpha MAP kinase Homo sapiens
C2-alkylaminothiazole
-
Homo sapiens
N,4-dimethyl-3-[2-[(1-methylethyl)amino]-6-oxo-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]benzamide inhibition of p38alpha MAP kinase Homo sapiens
N,4-dimethyl-3-[6-oxo-2-(propylamino)-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]benzamide inhibition of p38alpha MAP kinase Homo sapiens
N-(2-chloro-6-methylphenyl)-2-(cyclobutylamino)-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
N-(2-chloro-6-methylphenyl)-2-(ethylamino)-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
N-(2-chloro-6-methylphenyl)-2-(phenylamino)-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
N-(2-chloro-6-methylphenyl)-2-(propylamino)-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
N-(2-chloro-6-methylphenyl)-2-[(1-methylethyl)amino]-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
N-(5-carbamoyl-2-methylphenyl)-2-(propylamino)-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
N-(5-carbamoyl-2-methylphenyl)-2-[(1-methylethyl)amino]-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
N-ethyl-4-methyl-3-[2-[(1-methylethyl)amino]-6-oxo-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]benzamide inhibition of p38alpha MAP kinase Homo sapiens
N-ethyl-4-methyl-3-[6-oxo-2-(propylamino)-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]benzamide inhibition of p38alpha MAP kinase Homo sapiens
N-[2-methyl-5-(methylcarbamoyl)phenyl]-2-(propylamino)-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
N-[2-methyl-5-(methylcarbamoyl)phenyl]-2-[[(1S)-1-methylpropyl]amino]-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
N-[5-(ethylcarbamoyl)-2-methylphenyl]-2-(propylamino)-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
N-[5-(ethylcarbamoyl)-2-methylphenyl]-2-[(1-methylethyl)amino]-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
N-[5-(ethylcarbamoyl)-2-methylphenyl]-4-methyl-2-(propylamino)-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens
N-[5-(isoxazol-3-ylcarbamoyl)-2-methylphenyl]-2-[(1-methylethyl)amino]-1,3-thiazole-5-carboxamide inhibition of p38alpha MAP kinase Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
p38alpha MAP kinase
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000002
-
-
Homo sapiens N-[5-(ethylcarbamoyl)-2-methylphenyl]-2-(propylamino)-1,3-thiazole-5-carboxamide
0.0000023
-
-
Homo sapiens N-[2-methyl-5-(methylcarbamoyl)phenyl]-2-[[(1S)-1-methylpropyl]amino]-1,3-thiazole-5-carboxamide
0.0000032
-
-
Homo sapiens N-(5-carbamoyl-2-methylphenyl)-2-[(1-methylethyl)amino]-1,3-thiazole-5-carboxamide
0.0000034
-
-
Homo sapiens N-[5-(ethylcarbamoyl)-2-methylphenyl]-2-[(1-methylethyl)amino]-1,3-thiazole-5-carboxamide
0.0000035
-
-
Homo sapiens (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide
0.0000035
-
-
Homo sapiens 2-[(1-methylethyl)amino]-N-[2-methyl-5-(methylcarbamoyl)phenyl]-1,3-thiazole-5-carboxamide
0.0000038
-
-
Homo sapiens N-[5-(isoxazol-3-ylcarbamoyl)-2-methylphenyl]-2-[(1-methylethyl)amino]-1,3-thiazole-5-carboxamide
0.0000041
-
-
Homo sapiens N-(5-carbamoyl-2-methylphenyl)-2-(propylamino)-1,3-thiazole-5-carboxamide
0.0000042
-
-
Homo sapiens 2-[(1-methylethyl)amino]-N-[2-methyl-5-(1H-pyrazol-5-ylcarbamoyl)phenyl]-1,3-thiazole-5-carboxamide
0.0000045
-
-
Homo sapiens N-[2-methyl-5-(methylcarbamoyl)phenyl]-2-(propylamino)-1,3-thiazole-5-carboxamide
0.0000054
-
-
Homo sapiens 2-[(1-methylethyl)amino]-N-[2-methyl-5-[(1-methyl-1H-pyrazol-5-yl)carbamoyl]phenyl]-1,3-thiazole-5-carboxamide
0.000013
-
-
Homo sapiens N-(2-chloro-6-methylphenyl)-2-[(1-methylethyl)amino]-1,3-thiazole-5-carboxamide
0.000022
-
-
Homo sapiens 2-[(2-methoxyethyl)amino]-N-[2-methyl-5-(methylcarbamoyl)phenyl]-1,3-thiazole-5-carboxamide
0.000028
-
-
Homo sapiens N-(2-chloro-6-methylphenyl)-2-(propylamino)-1,3-thiazole-5-carboxamide
0.000034
-
-
Homo sapiens N-ethyl-4-methyl-3-[2-[(1-methylethyl)amino]-6-oxo-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]benzamide
0.000036
-
-
Homo sapiens N-(2-chloro-6-methylphenyl)-2-(cyclobutylamino)-1,3-thiazole-5-carboxamide
0.000039
-
inhibition of isozyme p38 MAPK alpha Homo sapiens C2-alkylaminothiazole
0.000053
-
-
Homo sapiens 3-[2-(cyclopropylamino)-6-oxo-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]-N-ethyl-4-methylbenzamide
0.000062
-
-
Homo sapiens N-(2-chloro-6-methylphenyl)-2-(phenylamino)-1,3-thiazole-5-carboxamide
0.00011
-
-
Homo sapiens N,4-dimethyl-3-[2-[(1-methylethyl)amino]-6-oxo-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]benzamide
0.00011
-
-
Homo sapiens 3-[2-(cyclopropylamino)-6-oxo-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]-N,4-dimethylbenzamide
0.00013
-
-
Homo sapiens N-[5-(ethylcarbamoyl)-2-methylphenyl]-4-methyl-2-(propylamino)-1,3-thiazole-5-carboxamide
0.00014
-
-
Homo sapiens N-(2-chloro-6-methylphenyl)-2-(ethylamino)-1,3-thiazole-5-carboxamide
0.00016
-
-
Homo sapiens N-ethyl-4-methyl-3-[6-oxo-2-(propylamino)-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]benzamide
0.00027
-
-
Homo sapiens N,4-dimethyl-3-[6-oxo-2-(propylamino)-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]benzamide
0.00033
-
-
Homo sapiens 2-(ethylamino)-N-[5-(ethylcarbamoyl)-2-methylphenyl]-4-methyl-1,3-thiazole-5-carboxamide