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Literature summary for 2.7.11.24 extracted from

  • Aronov, A.M.; Tang, Q.; Martinez-Botella, G.; Bemis, G.W.; Cao, J.; Chen, G.; Ewing, N.P.; Ford, P.J.; Germann, U.A.; Green, J.; Hale, M.R.; Jacobs, M.; Janetka, J.W.; Maltais, F.; Markland, W.; Namchuk, M.N.; Nanthakumar, S.; Poondru, S.; Straub, J.; ter Haar, E.; Xie, X.
    Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control (2009), J. Med. Chem., 52, 6362-6368.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(R)-N-(2-hydroxyl-1-phenylethyl)-4-[5-methyl-2-(phenylamino)-pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-4-[2-(2,3-dimethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-4-[2-(2-chlorophenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-4-[2-(2-ethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-4-[2-(2-ethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-4-[2-(2-fluorophenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-4-[2-(2-hydroxyphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-4-[2-(2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-4-[2-(2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-4-[2-(2-trifluoromethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-4-[2-(3-fluoro-2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-4-[2-(4-chloro-2-fluorophenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-4-[2-(4-chloro-2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-4-[2-(benzo[d]1,3-dioxolylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-N-(2-hydroxyl-1-phenylethyl)-4-[5-methyl-2-(phenylamino)-pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[-2-(2,2-difluorobenzo[d][1,3]dioxol-4-ylamino)-5-methylpyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[-2-(2,3-dihydro-1H-inden-4-ylamino)-5-methylpyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[-2-(2,3-dihydrobenzo[b][1,4]dioxin-5-ylamino)-5-methylpyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[5-methyl-2(5,6,7,8-tetrahydronaphthalen-1-ylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[5-methyl-2-(phenylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-N-[1-(3-fluorophenyl)-2-hydroxyethyl]-4-[5-methyl-2-(phenylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
(S)-N-[1-(3-methylphenyl)-2-hydroxyethyl]-4-[5-methyl-2-(phenylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
N-[(1S)-1-(3-chloro-4-fluorophenyl)-2-hydroxyethyl]-4-[4-(3-chlorophenyl)-1H-pyrazol-3-yl]-1H-pyrrole-3-carboxamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P28482
-
-

Synonyms

Synonyms Comment Organism
ERK2
-
Homo sapiens
extracellular signal-regulated kinase 2
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000002
-
(S)-4-[2-(2,3-dimethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide Ki below 0.000002 mM Homo sapiens
0.000002
-
(S)-N-(2-hydroxyl-1-phenylethyl)-4-[5-methyl-2-(phenylamino)-pyrimidin-4-yl]-1H-pyrrole-2-carboxamide Ki below 0.000002 mM Homo sapiens
0.000002
-
(S)-4-[2-(2-chlorophenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide Ki below 0.000002 mM Homo sapiens
0.000002
-
(S)-4-[2-(2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide Ki below 0.000002 mM Homo sapiens
0.000002
-
(S)-4-[2-(2-fluorophenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide Ki below 0.000002 mM Homo sapiens
0.000002
-
(S)-N-[1-(3-fluorophenyl)-2-hydroxyethyl]-4-[5-methyl-2-(phenylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide Ki below 0.000002 mM Homo sapiens
0.000002
-
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[5-methyl-2-(phenylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide Ki below 0.000002 mM Homo sapiens
0.000002
-
(S)-N-[1-(3-methylphenyl)-2-hydroxyethyl]-4-[5-methyl-2-(phenylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide Ki below 0.000002 mM Homo sapiens
0.000002
-
(S)-4-[2-(2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide Ki below 0.000002 mM Homo sapiens
0.000002
-
(S)-4-[2-(2-ethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide Ki below 0.000002 mM Homo sapiens
0.000002
-
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[-2-(2,3-dihydro-1H-inden-4-ylamino)-5-methylpyrimidin-4-yl]-1H-pyrrole-2-carboxamide Ki below 0.000002 mM Homo sapiens
0.000002
-
(S)-4-[2-(benzo[d]1,3-dioxolylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide Ki below 0.000002 mM Homo sapiens
0.000002
-
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[-2-(2,2-difluorobenzo[d][1,3]dioxol-4-ylamino)-5-methylpyrimidin-4-yl]-1H-pyrrole-2-carboxamide Ki below 0.000002 mM Homo sapiens
0.000002
-
(S)-4-[2-(2-chloro-4-fluorophenylamino)-5-methylpyrimidin-4-yl]- N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide Ki below 0.000002 mM, potent, selective, and orally bioavailable inhibitor of ERK Homo sapiens
0.000003
-
(S)-4-[2-(2,3-dimethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
0.000003
-
(S)-4-[2-(2-ethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
0.000004
-
(S)-4-[2-(2-trifluoromethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
0.000004
-
(S)-4-[2-(2-hydroxyphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
0.000005
-
(S)-4-[2-(4-chloro-2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
0.000005
-
(S)-4-[2-(4-chloro-2-fluorophenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
0.000013
-
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[5-methyl-2(5,6,7,8-tetrahydronaphthalen-1-ylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
0.000015
-
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[-2-(2,3-dihydrobenzo[b][1,4]dioxin-5-ylamino)-5-methylpyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
0.000034
-
(S)-4-[2-(3-fluoro-2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
0.00067
-
(R)-N-(2-hydroxyl-1-phenylethyl)-4-[5-methyl-2-(phenylamino)-pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
Homo sapiens