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Takinib

Takinib : Inhibitor of MAP3K7

Structure

Information

  • MAP3K7
  • Inhibitor
  • up to 5 µM

In Vitro Validations

Uniprot ID: O43318
Target Class: Kinase
Target SubClass: TKL
Potency: IC50
Potency Value: 5.46 nM
Potency Assay: Radiometric assay (Activity of purified TAK1-TAB1 protein using 5 µM ATP)
PDB ID for probe-target interaction (3D structure): 5V5N
Target aliases:
Mitogen-activated protein kinase kinase kinase 7, ...

DOI Reference: 10.1016/j.chembiol.2017.07.011

Uniprot ID: O43318
Target Class: Kinase
Target SubClass: TKL
Potency: Kd
Potency Value: 200 nM
Potency Assay: Fluorescence-linked enzyme assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Mitogen-activated protein kinase kinase kinase 7, ...

DOI Reference: 10.1016/j.chembiol.2017.07.011

Uniprot ID: O43318
Target Class: Kinase
Target SubClass: TKL
Potency: IC50
Potency Value: 9.5 nM
Potency Assay: Enzymatic assay (MRC Dundee)
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Mitogen-activated protein kinase kinase kinase 7, ...

DOI Reference: 10.1016/j.chembiol.2017.07.011

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Off Target: IRAK4
Potency end-point : IC50 120 nM
Probe Selectivity in Vitro:
Screened at 10 µM against 140 kinases, Dundee Selectivity Profiling. Closest targets >90% of control: CLK2 (4%), MINK1 (9%), GCK (9%), IRAK1 (4%), IRAK4 (7%). In-vitro potency of closest targets (enzymatic assay, MRC Dundee): IC50(IRAK4) = 120 nM, IC50(IRAK1) = 390 nM, IC50(GCK) = 430 nM, IC50(CLK2) = 430 nM, IC50(MINK1) = 1900 nM. Kinase proteome profiling in RA-FLS cells, against 45 kinases, closest targets as % of activity: LCK (42.6%), full screening data available as supporting info, PMID: 31847895. No cross reactivity in in a purine-wide selectivity assay based on γ-linked ATP Sepharose.
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SERP ratings and comments

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