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RILZABRUTINIB

RILZABRUTINIB : Covalent Inhibitor of BTK

Structure

Information

  • BTK
  • Covalent Inhibitor
  • up to 1 uM

In Vitro Validations

Uniprot ID: Q06187
Target Class: Kinase
Target SubClass: Tyrosin Kinase
Potency: IC50
Potency Value: 1.3 nM
Potency Assay: Biochemical assay using the Caliper electrophoresis method
PDB ID for probe-target interaction (3D structure): 7L5P
Target aliases:
Tyrosine-protein kinase BTK, AGMX1, BTK, BTK_HUMAN ...

DOI Reference: 10.1021/acs.jmedchem.1c01170

Uniprot ID: Q06187
Target Class: Kinase
Target SubClass: Tyrosin Kinase
Potency Value: 84%
Potency Assay: Biochemical occupancy was determined at room temperature by a FRET-based fluorescence competition assay where 1.5 μM compound was preincubated with BTK for 15 min
PDB ID for probe-target interaction (3D structure): 7L5P
Target aliases:
Tyrosine-protein kinase BTK, AGMX1, BTK, BTK_HUMAN ...

DOI Reference: 10.1021/acs.jmedchem.1c01170

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:
The selectivity of PRN1008 was evaluated in a panel of 251 kinases. The highest levels of inhibition were seen against 4 kinases that share a homologous cysteine residue (RLK 1.2 nM, TEC 0.8 nM, BMX 1.0 nM, and BLK 6.3 nM). A biochemical off-rate assay similar to that employed for BTK demonstrated that PRN1008 dissociated more rapidly from these kinases than was seen for BTK. Outside target family: PRN1008 did not inhibit T-cell receptor, IL-4, or EGFR signalling up to 5 μM (Cerep).
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