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LH168 | LH168 : Inhibitor of WDR5
RATINGS:
Cellular Use: (1 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:13 nM
  • Kd:38 nM
  • ΔTm:19.8 K
  • EC50:10 nM
Inhibitor
Up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
LH168 was tested against 13 histone/arginine methyltransferases by radioactivity-based assay, none o ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Proteomic analysis of a sample enriched by pull down experiment A cell lysate was subjected to pull ...

Potency
Cellular
In Vitro

WDR5

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

Other Reference: Peer reviewed at SGC

Negative Control Compounds

LH222
Notes: Negative control LH222 showed no tracer displacement in target engagement assay
SMILES: O=C([C@@H](CCC)NC(C1=CC(CN2C(C)=C(C)N=C2)=CC(C3=CN(CC)N=C3C(F)(F) F)=C1)=O)N4CCC(SC=C5)=C5C4

Orthogonal Probes def

Homer

Chemical Information

Molecular Formula C29H31F3N6O2S
SMILEs CCC[C@H](NC(=O)c1cc(Cn2ccnc2)cc(-c2cn(CC)nc2C(F)(F)F)c1)C(=O)N1CCc2sccc2C1
InChI InChI=1S/C29H31F3N6O2S/c1-3-5-24(28(40)37-9-6-25-20(16-37)7-11-41-25)34-27(39)22-13-19(15-36-10-8-33-18-36)12-21(14-22)23-17-38(4-2)35-26(23)29(30,31)32/h7-8,10-14,17-18,24H,3-6,9,15-16H2,1-2H3,(H,34,39)/t24-/m0/s1
Molecular weight 584.22 Da
AlogP 5.378500000000005
HBond acceptors 8
HBond donors 1
Atoms 72

Expert Reviews

by SERP
(on 7 Feb 2025 )
Cellular Use Rating
( The reviewer did not leave any comments )
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