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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 public comments)
by SERP
(on 26 Mar 2022)
Cellular Use Rating
(The reviewer did not leave any public 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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