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PF-3166

PF-3166 : Allosteric inhibitor of PADI2

Structure

Information

  • PADI2
  • Allosteric
  • up to 10 uM

In Vitro Validations

Uniprot ID: Q9Y2J8
Target Class: Enzyme
Target SubClass: Deiminase
Potency: IC50
Potency Value: 150 nM
Potency Assay: Fluorescence Quenching (FQ) assay
PDB ID for probe-target interaction (3D structure): 9B96
Target aliases:
Protein-arginine deiminase type-2, PDI2, PAD2, KIA ...

DOI Reference: 10.1021/acschembio.4c00397

Uniprot ID: Q9Y2J8
Target Class: Enzyme
Target SubClass: Deiminase
Potency: IC50
Potency Value: 580 nM
Potency Assay: NH3-release assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Protein-arginine deiminase type-2, PDI2, PAD2, KIA ...

DOI Reference: 10.1021/acschembio.4c00397

Uniprot ID: Q9Y2J8
Target Class: Enzyme
Target SubClass: Deiminase
Potency: IC50
Potency Value: 610 nM
Potency Assay: Glutamate Dehydrogenase (GDH) coupled assay at a [Ca2+] of 0.25 mM
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Protein-arginine deiminase type-2, PDI2, PAD2, KIA ...

DOI Reference: 10.1021/acschembio.4c00397

Uniprot ID: Q9Y2J8
Target Class: Enzyme
Target SubClass: Deiminase
Potency: Kd
Potency Value: 221 nM
Potency Assay: Affinity Selection Mass Spectrometry (ASMS) assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Protein-arginine deiminase type-2, PDI2, PAD2, KIA ...

DOI Reference: 10.1021/acschembio.4c00397

Uniprot ID: Q9Y2J8
Target Class: Enzyme
Target SubClass: Deiminase
Potency: ΔTm
Potency Value: 9 degrees
Potency Assay: TSA
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Protein-arginine deiminase type-2, PDI2, PAD2, KIA ...

DOI Reference: 10.1021/acschembio.4c00397

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): No inhibition of PAD3 or PAD4 activity was observed for PF-3166 up to a high dose of 80 μM
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SERP ratings and comments

No SERP comments found for PF-3166