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PPM-3 | PPM-3 : Degrader (PROTAC) of MAPK7
RATINGS:
Cellular Use: (2 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
MAPK7
  • IC50:62.4 ± 18.6 nM
  • DC50:17 nM
  • DC50:<45 nM
Degrader (PROTAC)
up to 500 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
PPM-3 demonstrated outstanding kinase selectivity among more than 300 kinases at 500 nM in terms of ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
The ligand component of PPM-3 may also target bromodomain-containing protein 4 (BRD4), doublecortin- ...

Potency
Cellular
In Vitro

MAPK7

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.3c00864

Chemical Information

Molecular Formula C54H69N11O6S
SMILEs COc1cc(N2CCN(CCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1Nc1ncc2c(n1)N(C)c1ccccc1C(=O)N2C
InChI InChI=1S/C54H69N11O6S/c1-34(36-18-20-37(21-19-36)47-35(2)56-33-72-47)57-50(68)43-30-39(66)32-65(43)52(70)48(54(3,4)5)59-46(67)17-11-9-10-14-24-63-25-27-64(28-26-63)38-22-23-41(45(29-38)71-8)58-53-55-31-44-49(60-53)61(6)42-16-13-12-15-40(42)51(69)62(44)7/h12-13,15-16,18-23,29,31,33-34,39,43,48,66H,9-11,14,17,24-28,30,32H2,1-8H3,(H,57,68)(H,59,67)(H,55,58,60)/t34-,39+,43-,48+/m0/s1
Molecular weight 999.52 Da
AlogP 0.0
HBond acceptors 17
HBond donors 4
Atoms 141

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Expert Reviews

by SERP+
(on 20 Feb 2025 )
Cellular Use Rating
Degradation of ERK5 by PPM-3 begins within 2-4 hours and peaks at 12 hours. Proteomics analysis was performed at a late time point (48 h) which therefore may include secondary effects. The selectivity...
by SERP+
(on 6 Feb 2026 )
Cellular Use Rating
A potent degrader of ERK5 with DC50 and Dmax values of 80% respectively across a panel of five cell lines. Degradation was observed between 2-4h, reaching a maximum at 12 h and lasting >72 h. The mechanism...
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