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NVS-MALT1

NVS-MALT1 : Allosteric Inhibitor of MALT1

Structure

Information

  • MALT1
  • Allosteric Inhibitor

In Vitro Validations

Uniprot ID: Q9UDY8
Target Class: Enzyme
Target SubClass: Peptidase
Potency: IC50
Potency Value: 2.4 nM
Potency Assay: Human biochemical (TR-FRET) assay (high salt)
PDB ID for probe-target interaction (3D structure): 7A41
Target aliases:
Mucosa-associated lymphoid tissue lymphoma translo ...

DOI Reference: 10.1021/op200301h

Uniprot ID: Q9UDY8
Target Class: Enzyme
Target SubClass: Peptidase
Potency: IC50
Potency Value: 18 nM
Potency Assay: Human biochemical (TR-FRET) assay (low salt)
PDB ID for probe-target interaction (3D structure): 7A41
Target aliases:
Mucosa-associated lymphoid tissue lymphoma translo ...

DOI Reference: 10.1021/op200301h

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:
No cross-reactivity among proteases owing to allosteric mechanism. No activities across a panel of 50 kinases at 10 µM (except for FLT3 with 3.5 µM inhibition). No activities across a panel of 110 receptors, ion channels, enzymes and transporters at 10 µM (except for 52% inhibition of adenosine transporter AdT). Clean GPCR scan
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SERP ratings and comments

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