Chemical Probes logo
NVS-MLLT-1 | Inhibitor of MLLT1, MLLT3
RATINGS:
Cellular Use: (3 reviews)

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

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MLLT1
  • IC 50:150 nM
  • Kd:109 nM
  • IC50:500 nM
MLLT3
  • IC 50:254 nM
  • IC50:500 nM
Inhibitor
up to 5µM to limit off-target activity (e.g.,TRB2)
5-10 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
The AlphaScreen assays were employed to screen NVS-MLLT-1 against a panel of bromodomains. NVS-MLLT- ...

Potency
Cellular
In Vitro

MLLT1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1101/2021.02.08.430291

MLLT3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1101/2021.02.08.430291

Negative Control Compounds

NSV-MLLT-C

Orthogonal Probes def

SGC-iMLLT, PFI-6
SR-0813

Chemical Information

Molecular Formula C23H23N5O
SMILEs C[C@H]1CCCN1Cc1nc2cc(NC(=O)c3ccc4cnccc4c3)ccc2[nH]1
InChI InChI=1S/C23H23N5O/c1-15-3-2-10-28(15)14-22-26-20-7-6-19(12-21(20)27-22)25-23(29)17-4-5-18-13-24-9-8-16(18)11-17/h4-9,11-13,15H,2-3,10,14H2,1H3,(H,25,29)(H,26,27)/t15-/m0/s1
Molecular weight 385.19 Da
AlogP 0.0
HBond acceptors 6
HBond donors 2
Atoms 52

References

Publications

Cross References

canSARChEMBLSGC Chemical Probes

Expert Reviews

by SERP
(on 29 Mar 2021 )
Cellular Use Rating
NVS-MLLT-1 was developed against the epigenetic target YEATS containing domain of MLLT1 (also called ENL, LTG19 or YEATS1) and MLLT3 (also called AF9 or YEATS3). NVS-MLLT-1 is a potent and selective...
by SERP
(on 4 May 2021 )
Cellular Use Rating
CPP2278 (NVS-MLLT-1) paired with its control compound NVS-MLLT-C can be used as a cellular probe against various human cell lines carrying both wild-type ENL/AF9 and ENL p.117_118insNHL and p.111_113NPP>...
by SERP+
(on 22 Mar 2023 )
Cellular Use Rating
This probe is a well-characterized selective inhibitor for MLLT1 and MLLT3. With in vitro potencies of 150 nM (MLLT1) and 250 nM (MLLT3), respectively, and a cellular potency of 500 nM it is comparable...
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