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IR-2 | IR-2 : Degrader (PROTAC) of BTK
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
BTK
  • IC50:14 nM
  • DC50:1.9 nM
  • Dmax:88%
Degrader (PROTAC)
100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Quantitative label-free proteomics
Selectivity Assessment Description:
BTK was efficiently degraded by all the PROTACs we tested. IR-2 also degraded the known ibrutinib of ...

Potency
Cellular
In Vitro

BTK

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/jacs.9b13907

Chemical Information

Molecular Formula C50H56N8O11
SMILEs Nc1ncnc2c1c(-c1ccc(Oc3ccccc3)cc1)nn2[C@@H]1CCCN(C(=O)/C=C/CCCCOCCOCCOCCOCCOc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C1
InChI InChI=1S/C50H56N8O11/c51-46-44-45(34-16-18-37(19-17-34)69-36-11-4-3-5-12-36)55-58(47(44)53-33-52-46)35-10-9-22-56(32-35)42(60)15-6-1-2-7-23-64-24-25-65-26-27-66-28-29-67-30-31-68-40-14-8-13-38-43(40)50(63)57(49(38)62)39-20-21-41(59)54-48(39)61/h3-6,8,11-19,33,35,39H,1-2,7,9-10,20-32H2,(H2,51,52,53)(H,54,59,61)/b15-6+/t35-,39?/m1/s1
Molecular weight 944.41 Da
AlogP 0.0
HBond acceptors 19
HBond donors 3
Atoms 125

Expert Reviews

by SERP
(on 23 Mar 2022 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 26 Mar 2022 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP+
(on 6 Feb 2026 )
Cellular Use Rating
This well characterised PROTAC, IR-2, demonstrated a DC50 in the low nanomolar range in two cell lines (Mino and CLL patient samples). However, off-target degradation has been seen by proteomics for CSK,...
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