Chemical Probes logo

BIIB129

BIIB129 : Covalent Inhibitor of BTK

Structure

Information

  • BTK
  • Covalent Inhibitor
  • up to 1 µM

In Vitro Validations

Uniprot ID: Q06187
Target Class: Kinase
Target SubClass: Tyr kinase
Potency: Kd
Potency Value: 0.63 nM
Potency Assay: KinomeSCAN
PDB ID for probe-target interaction (3D structure): 8TU4
Target aliases:
Tyrosine-protein kinase BTK, AGMX1, BTK, BTK_HUMAN ...

DOI Reference: 10.1021/acs.jmedchem.4c00220

Uniprot ID: Q06187
Target Class: Kinase
Target SubClass: Tyr kinase
Potency: Activity
Potency Value: 4.6 (log kinact/Ki)
Potency Assay: continuous-read kinetic enzyme assay using the nonphosphorylated BTK protein
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Tyrosine-protein kinase BTK, AGMX1, BTK, BTK_HUMAN ...

DOI Reference: 10.1021/acs.jmedchem.4c00220

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): KINOMEscan, Eurofins DiscoverX, for BIIB129 was performed at 1 μM concentration. Ten and 5 out of 403 kinases were inhibited with S(10) selectivity scores of 0.025. BIIB129 showed greater than 10-fold selectivity for BTK over all but one (9-fold against TEC) of the 10 kinases tested.
Potency assay, off target (cells): BIIB129 shown to bind only 4 of 190 kinases (BTK TO50 = 6.8 nM, TEC TO50 = 18 nM, ITK TO50 = 308 nM and BLK TO50 = 3.9 nM) among 3500 total proteins detected when tested in a cellular matrix comprising of human Burkitt’s lymphoma cell line (Ramos), B cell lymphoma line (TMD8), and human T cell leukemia line (Jurkat) as a 1:1:1 mixture using kinomebead competitive chemoproteomics.
I have extra information to add

SERP ratings and comments

No SERP comments found for BIIB129