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Homer | Homer : Degrader (PROTAC) of WDR5
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
WDR5
  • Kd:18 nM
  • DC50:53 nM
  • Dmax:DCmax: 58% at 1 µM
Degrader (PROTAC)
Dependent on the cell line of interest, higher concentrations might be required
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Quantitative Proteomics revealed that only WDR5 is significantly and substantially depleted by Homer ...

Potency
Cellular
In Vitro

WDR5

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.1c00146

Negative Control Compounds

CANSAR3550550
CANSAR3550551

Chemical Information

Molecular Formula C52H60F3N9O7S
SMILEs Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCNC(=O)c2ccc(-c3ccc(N4CCN(C)CC4)c(NC(=O)c4c[nH]c(=O)cc4C(F)(F)F)c3)cc2)C(C)(C)C)cc1
InChI InChI=1S/C52H60F3N9O7S/c1-31-45(72-30-59-31)34-11-9-32(10-12-34)27-58-49(70)42-25-37(65)29-64(42)50(71)46(51(2,3)4)61-43(66)8-6-7-19-56-47(68)35-15-13-33(14-16-35)36-17-18-41(63-22-20-62(5)21-23-63)40(24-36)60-48(69)38-28-57-44(67)26-39(38)52(53,54)55/h9-18,24,26,28,30,37,42,46,65H,6-8,19-23,25,27,29H2,1-5H3,(H,56,68)(H,57,67)(H,58,70)(H,60,69)(H,61,66)/t37-,42+,46-/m1/s1
Molecular weight 1011.43 Da
AlogP 0.0
HBond acceptors 16
HBond donors 6
Atoms 132

Expert Reviews

by SERP
(on 14 Apr 2022 )
Cellular Use Rating
I strongly encourage the usage of the available negative control compound (nc_VHL) that are incapable of binding VHL. This compound has near-identical physicochemical properties and retains any residual...
by SERP
(on 21 Apr 2022 )
Cellular Use Rating
Recommended to use with both provided negative controls.
by SERP
(on 20 Feb 2025 )
Cellular Use Rating
We recommend using this compound with its two negative controls, however, if a complete knockout is required, it will only result in a Dmax of 58%. In VHL-overexpressing cells, it was shown that the Dmax...
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