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Literature summary extracted from

  • Raeppel, F.; Raeppel, S.; Therrien, E.
    Design, synthesis and RON receptor tyrosine kinase inhibitory activity of new head groups analogs of LCRF-0004 (2015), Bioorg. Med. Chem. Lett., 25, 3810-3815.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.10.1 LCRF-0004 potent and selective inhibitor Homo sapiens
2.7.10.1 N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-1,3-diphenyl-1H-pyrazole-4-carboxamide
-
 Homo sapiens
2.7.10.1 N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-1,5-diphenyl-1H-pyrazole-4-carboxamide
-
 Homo sapiens
2.7.10.1 N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-1,5-diphenyl-1H-pyrrole-3-carboxamide
-
 Homo sapiens
2.7.10.1 N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-2,4-diphenyl-1,3-thiazole-5-carboxamide
-
 Homo sapiens
2.7.10.1 N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-1-phenyl-5-(pyridin-2-yl)-1H-pyrazole-4-carboxamide
-
 Homo sapiens
2.7.10.1 N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-1-phenyl-5-(pyridin-3-yl)-1H-pyrazole-4-carboxamide
-
 Homo sapiens
2.7.10.1 N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-1-phenyl-5-(pyridin-4-yl)-1H-pyrazole-4-carboxamide
-
 Homo sapiens
2.7.10.1 N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-1-phenyl-5-(thiophen-3-yl)-1H-pyrazole-4-carboxamide
-
 Homo sapiens
2.7.10.1 N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(2-fluorophenyl)-1-phenyl-1H-pyrazole-4-carboxamide
-
 Homo sapiens
2.7.10.1 N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(2-methoxyphenyl)-1-phenyl-1H-pyrazole-4-carboxamide
-
 Homo sapiens
2.7.10.1 N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(3-methoxyphenyl)-1-phenyl-1H-pyrazole-4-carboxamide
-
 Homo sapiens
2.7.10.1 N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(4-fluorophenyl)-1-phenyl-1H-pyrazole-4-carboxamide
-
 Homo sapiens
2.7.10.1 N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(4-methoxyphenyl)-1-phenyl-1H-pyrazole-4-carboxamide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.10.1 ATP + a [protein]-L-tyrosine Homo sapiens
-
 ADP + a [protein]-L-tyrosine phosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.10.1 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.10.1 ATP + a [protein]-L-tyrosine
-
 Homo sapiens ADP + a [protein]-L-tyrosine phosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.10.1 macrophage stimulating 1 receptor
-
 Homo sapiens
2.7.10.1 MST1R
-
 Homo sapiens
2.7.10.1 Ron
-
 Homo sapiens
2.7.10.1 RTK
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.10.1 0.000012
-
 pH and temperature not specified in the publication Homo sapiens LCRF-0004
2.7.10.1 0.000014
-
 pH and temperature not specified in the publication Homo sapiens N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-1-phenyl-5-(pyridin-3-yl)-1H-pyrazole-4-carboxamide
2.7.10.1 0.000023
-
 pH and temperature not specified in the publication Homo sapiens N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-1,5-diphenyl-1H-pyrazole-4-carboxamide
2.7.10.1 0.000023
-
 pH and temperature not specified in the publication Homo sapiens N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-1-phenyl-5-(pyridin-2-yl)-1H-pyrazole-4-carboxamide
2.7.10.1 0.000025
-
 pH and temperature not specified in the publication Homo sapiens N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(2-fluorophenyl)-1-phenyl-1H-pyrazole-4-carboxamide
2.7.10.1 0.000027
-
 pH and temperature not specified in the publication Homo sapiens N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl)-5-(3-methoxyphenyl)-1-phenyl-1H-pyrazole-4-carboxamide
2.7.10.1 0.000032
-
 pH and temperature not specified in the publication Homo sapiens N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-1,3-diphenyl-1H-pyrazole-4-carboxamide
2.7.10.1 0.000045
-
 pH and temperature not specified in the publication Homo sapiens N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-2,4-diphenyl-1,3-thiazole-5-carboxamide
2.7.10.1 0.000101
-
 pH and temperature not specified in the publication Homo sapiens N-(3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)-1-benzothiophen-7-yl]oxy]phenyl)-1,5-diphenyl-1H-pyrrole-3-carboxamide