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SGC-iMLLT | Inhibitor of MLLT1, MLLT3
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
MLLT1
  • IC 50:260 nM
  • Kd:129 nM
  • IC 50:400 nM
MLLT3
  • IC 50:77 nM
  • IC 50:400 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Profiling of SGC-iMLLT against YEATS2 and YEATS4 revealed excellent selectivity for MLLT1/3 with no ...

Potency
Cellular
In Vitro

MLLT1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1002/anie.201810617

MLLT3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1002/anie.201810617

Negative Control Compounds

SGC‐iMLLT‐N

Orthogonal Probes def

NVS-MLLT-1, PFI-6
SR-0813

Chemical Information

Molecular Formula C22H24N6O
SMILEs C[C@H]1CCCN1Cc1nc2cc(NC(=O)c3ccc4c(cnn4C)c3)ccc2[nH]1
InChI InChI=1S/C22H24N6O/c1-14-4-3-9-28(14)13-21-25-18-7-6-17(11-19(18)26-21)24-22(29)15-5-8-20-16(10-15)12-23-27(20)2/h5-8,10-12,14H,3-4,9,13H2,1-2H3,(H,24,29)(H,25,26)/t14-/m0/s1
Molecular weight 388.20 Da
AlogP 3.686200000000002
HBond acceptors 7
HBond donors 2
Atoms 53

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 19 Apr 2021 )
Cellular Use Rating
SGC-iMLLT was developed based on a low micromolar MLLT1 YEATS domain inhibitor which was identified in a medium throughput screening campaign using AlphaScreen technology. Docking studies utilizing...
by SERP+
(on 22 Mar 2023 )
Cellular Use Rating
The compound shows potency of IC50: 300 nM in a cell free assay and should be used in cellular assays up to 1 uM. No data are available assessing its toxicity or suitability for in vivo use. No efficacy...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria