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Literature summary for 2.7.11.30 extracted from

  • Sawyer, J.S.; Beight, D.W.; Britt, K.S.; Anderson, B.D.; Campbell, R.M.; Goodson, T.Jr.; Herron, D.K.; Li, H.Y.; McMillen, W.T.; Mort, N.; Parsons, S.; Smith, E.C.; Wagner, J.R.; Yan, L.; Zhang, F.; Yingling, J.M.
    Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain (2004), Bioorg. Med. Chem. Lett., 14, 3581-3584.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
TGF-beta
-
Mus musculus
TGF-beta
-
Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression of His-tagged transforming growth factor-beta type I receptor kinase domain mutant T204D in Spodoptera frugiperda Sf9 cells using the baculovirus infection system Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4(quinolin-4-yl)-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole derivatives IC50 of 0.00005-0.0013 mM Homo sapiens
4(quinolin-4-yl)-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole derivatives IC50 of 0.00015-0.0051 mM, overview Mus musculus
4-phenyl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole derivatives IC50 of 0.000005-0.0195 mM Homo sapiens
4-phenyl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole derivatives IC50 of 0.00011-0.020 mM, overview Mus musculus
LY364947 IC50 is 51 nM Homo sapiens
LY364947 IC50 is 31 nM Mus musculus

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
Mus musculus 16020
-
membrane
-
Homo sapiens 16020
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Mus musculus the enzyme is involved in p38 MAPK activation ?
-
?
additional information Homo sapiens the enzyme is involved in p38 MAPK activation ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant His-tagged transforming growth factor-beta type I receptor kinase domain mutant T204D from insect Sf9 cells by nickel affinity chromatography Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
fibroblast
-
Mus musculus
-
NIH-3T3 cell fibroblast cell line Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information the enzyme is involved in p38 MAPK activation Mus musculus ?
-
?
additional information the enzyme is involved in p38 MAPK activation Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
TbetaR-I
-
Mus musculus
TbetaR-I
-
Homo sapiens
TGF-beta type I receptor kinase
-
Mus musculus
TGF-beta type I receptor kinase
-
Homo sapiens
transforming growth factor-beta type I receptor kinase
-
Mus musculus
transforming growth factor-beta type I receptor kinase
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at Mus musculus
30
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Mus musculus
7.5
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Mus musculus
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000005 0.0195 IC50 of 0.000005-0.0195 mM Homo sapiens 4-phenyl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole derivatives
0.000031
-
IC50 is 31 nM Mus musculus LY364947
0.00005 0.0013 IC50 of 0.00005-0.0013 mM Homo sapiens 4(quinolin-4-yl)-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole derivatives
0.000051
-
IC50 is 51 nM Homo sapiens LY364947
0.00011 0.02 IC50 of 0.00011-0.020 mM, overview Mus musculus 4-phenyl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole derivatives
0.00015 0.0051 IC50 of 0.00015-0.0051 mM, overview Mus musculus 4(quinolin-4-yl)-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole derivatives