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JNK2_3 COV56d

JNK2/3 COV56d : Covalent Inhibitor of MAPK9, MAPK10

Structure

Information

  • MAPK9
  • MAPK10
  • Covalent Inhibitor
  • up to 5 uM

In Vitro Validations

Uniprot ID: P45984
Target Class: Kinase
Target SubClass: CMGC
Potency: IC50
Potency Value: 25 nM
Potency Assay: PhosphoSens assay @ 60 min
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Mitogen-activated protein kinase 9, SAPK1A, PRKM9, ...

DOI Reference: 10.1021/acs.jmedchem.5c00884

Uniprot ID: P45984
Target Class: Kinase
Target SubClass: CMGC
Potency Value: kinact/KI 38,200 M–1·s–1
Potency Assay: Binding kinetics assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Mitogen-activated protein kinase 9, SAPK1A, PRKM9, ...

DOI Reference: 10.1021/acs.jmedchem.5c00884

Uniprot ID: P45984
Target Class: Kinase
Target SubClass: CMGC
Potency: Kd
Potency Value: 15 nM
Potency Assay: KINOMEscan
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Mitogen-activated protein kinase 9, SAPK1A, PRKM9, ...

DOI Reference: 10.1021/acs.jmedchem.5c00884

Uniprot ID: P45984
Target Class: Kinase
Target SubClass: CMGC
Potency: IC50
Potency Value: 830 nM
Potency Assay: 33PanQuinase assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Mitogen-activated protein kinase 9, SAPK1A, PRKM9, ...

DOI Reference: 10.1021/acs.jmedchem.5c00884

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay, off target (cells): Selective 11x over JNK1 as confirmed by NanoBRET
Potency assay (off target): Kinome screening was carried out in a representative panel consisting of 97 kinases (scanEDGE─KINOMEscan) showing a clean kinome profile at a compound concentration of 500 nM, showing a percentage of control (POC) of 1.4% for JNK2 and 0.3% for JNK3 respectively. All other kinases tested showed a POC > 35%
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SERP ratings and comments

No SERP comments found for JNK2_3 COV56d