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Literature summary for 2.7.11.30 extracted from
- Kinetic characterization of novel pyrazole TGF-beta receptor I kinase inhibitors and their blockade of the epithelial-mesenchymal transition (2005), Biochemistry, 44, 2293-2304.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression of His-tagged wild-type and mutant ALK5 in Spodoptera frugiperda Sf9 cells using the baculovirus infection system | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| T204D | constitutively active ALK5 mutant | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 4-phenyl substituted pyrazole inhibitors | inhibitory potency of 4-phenyl substituted pyrazole derivatives, IC50 of 30-555 nM, overview | Homo sapiens | |
| LY364947 | competitive to ATP, noncompetitive to the peptide substrate, IC50 is 175 nM, mechanism | Homo sapiens |  |
| LY566578 | competitive to ATP, noncompetitive to the peptide substrate, IC50 is 70 nM, mechanism | Homo sapiens | |
| LY580276 | competitive to ATP, noncompetitive to the peptide substrate, IC50 is 580 nM, mechanism | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0057 | - |
ATP | pH 7.5, 30°C, recombinant mutant T204D ALK5 | Homo sapiens | |
| 0.0088 | - |
ATP | pH 7.5, 30°C, recombinant wild-type ALK5 | Homo sapiens | |
| 0.26 | - |
KKVLTQMGSPSIRCS(P)SVS | pH 7.5, 30°C, recombinant wild-type ALK5 | Homo sapiens | |
| 0.331 | - |
KVLTQMGSPSVRCS(P)SMS | pH 7.5, 30°C, recombinant wild-type ALK5 | Homo sapiens | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | - |
Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| phosphoprotein | ALK5 performs autophosphorylation, wild-type and mutant T204D enzymes | Homo sapiens |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant His-tagged wild-type and mutant ALK5 from Spodoptera frugiperda Sf9 cells by nickel affinity chromatography | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + KKVLTQMGSPSIRCS(P)SV(P)S | Smad3-derived peptide substrate | Homo sapiens | ADP + ? | - |
? | |
| ATP + KKVLTQMGSPSIRCS(P)SVA | Smad3-derived peptide substrate | Homo sapiens | ADP + ? | - |
? | |
| ATP + KKVLTQMGSPSIRCS(P)SVS | Smad3-derived peptide substrate | Homo sapiens | ADP + ? | - |
? | |
| ATP + KVLTQMGSPSIRCS(P)SVS | Smad3-derived peptide substrate | Homo sapiens | ADP + ? | - |
? | |
| ATP + KVLTQMGSPSIRCSSV(P)S | Smad3-derived peptide substrate | Homo sapiens | ADP + ? | - |
? | |
| ATP + KVLTQMGSPSVRCS(P)SMS | Smad2-derived peptide substrate | Homo sapiens | ADP + ? | - |
? | |
| ATP + KVLTQMGSPSVRCSSMS | Smad2-derived peptide substrate | Homo sapiens | ADP + ? | - |
? | |
| ATP + KVLTQMGSPSVRCSSMS(P)S | Smad2-derived peptide substrate | Homo sapiens | ADP + ? | - |
? | |
| additional information | ALK5 performs autophosphorylation, substrate specificities of recombinant wild-type and mutant T204D ALK5, ALK5 is the intracellular domain of the transforming growth factor beta type-I receptor | Homo sapiens | ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| More | ALK5 is the intracellular domain of the transforming growth factor beta type-I receptor | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| ALK5 | - |
Homo sapiens |
| TbetaRI | - |
Homo sapiens |
| TGF-beta receptor I kinase | - |
Homo sapiens |
| TGF-beta type-I receptor | - |
Homo sapiens |
| transforming growth factor beta type-I receptor | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 30 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.5 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.000028 | - |
LY364947 | pH 7.5, 30°C, recombinant mutant T204D ALK5, inhibition of autophosphorylation | Homo sapiens | |
| 0.000037 | - |
LY580276 | pH 7.5, 30°C, recombinant mutant T204D ALK5, inhibition of autophosphorylation | Homo sapiens | |
| 0.000038 | - |
LY566578 | pH 7.5, 30°C, recombinant mutant T204D ALK5, inhibition of autophosphorylation | Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00003 | 0.000555 | inhibitory potency of 4-phenyl substituted pyrazole derivatives, IC50 of 30-555 nM, overview | Homo sapiens | 4-phenyl substituted pyrazole inhibitors | |
| 0.00007 | - |
competitive to ATP, noncompetitive to the peptide substrate, IC50 is 70 nM, mechanism | Homo sapiens | LY566578 | |
| 0.000175 | - |
competitive to ATP, noncompetitive to the peptide substrate, IC50 is 175 nM, mechanism | Homo sapiens | LY364947 | |
| 0.00058 | - |
competitive to ATP, noncompetitive to the peptide substrate, IC50 is 580 nM, mechanism | Homo sapiens | LY580276 | |
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