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BSJ-05-37 | BSJ-05-37 : Degrader (PROTAC) of ITK
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
ITK
  • Inhibition:97%
  • DC50:17.6 – 41.8 nM
Degrader (PROTAC)
250 nM, up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Biochemical selectivity of BSJ-05-037 was assessed against a panel of 468 kinases with a treatment c ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Protein abundance measurements were made using tandem mass tag quantitative mass spectrometry on MOL ...
Selectivity Assessment Description:
These data identified significant downregulation of ITK, as well as RNF166, ZNF653, and ZNF692.

Potency
Cellular
In Vitro

ITK

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.chembiol.2023.03.007

In Vivo Validations

Mouse
Dose: 2 mg/Kg
Route of delivery: Intravenous
Plasma half life: 2.18 h
Systemic clearance: 25.20 mL/min/Kg
Cmax: 1707 ng/mL
Tmax: 0.08 h
Area Under the Curve:: 82031 min*ng/mL
Volume of Distribution at Steady-State: 2.94 L/Kg

DOI Reference: 10.1016/j.chembiol.2023.03.007

Dose: 10 mg/Kg
Route of delivery: Intraperitoneal
Plasma half life: 1.90 h
Systemic clearance: 40.69 mL/min/Kg
Cmax: 3372 ng/mL
Tmax: 0.22 h
Area Under the Curve:: 266810 min*ng/mL

DOI Reference: 10.1016/j.chembiol.2023.03.007

Negative Control Compounds

canSAR7437545
Notes: BSJ-Bump was not able to degrade ITK even after 16h.

Chemical Information

Molecular Formula C51H59N9O10S2
SMILEs COc1cc(C)c(Sc2cnc(NC(=O)c3ccc(N4CCN(CCCCCCCNC(=O)COc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cc3)s2)cc1C(=O)N1CCN(C(C)=O)CC1
InChI InChI=1S/C51H59N9O10S2/c1-32-28-40(69-3)37(48(66)59-26-24-57(25-27-59)33(2)61)29-41(32)71-44-30-53-51(72-44)55-46(64)34-12-14-35(15-13-34)58-22-20-56(21-23-58)19-8-6-4-5-7-18-52-43(63)31-70-39-11-9-10-36-45(39)50(68)60(49(36)67)38-16-17-42(62)54-47(38)65/h9-15,28-30,38H,4-8,16-27,31H2,1-3H3,(H,52,63)(H,53,55,64)(H,54,62,65)
Molecular weight 1021.38 Da
AlogP 4.836820000000004
HBond acceptors 19
HBond donors 3
Atoms 131

Expert Reviews

by SERP+
(on 6 Feb 2026 )
Cellular Use Rating
In Model Organisms
We recommend this probe for use in cells, as long as the reported off-targets are considered during experimental design. The concentration at which the probe is used should be considered, as inhibition...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria