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BI01383298 | BI01383298 : an irreversible inhibitor of SLC13A5
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
SLC13A5
  • ΔTm:> 10 K @ 10 uM
  • IC50:56 nM
  • IC50:24 nM
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
BI01383298 is more than 1000-fold selective (table 1) over the closest family members: human SLC13A ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Citrate uptake inhibition was measured for all citrate transporters and glycine uptake measured to G ...

Potency
Cellular
In Vitro

SLC13A5

Mode of Action: irreversible

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1042/BCJ20200592

Negative Control Compounds

BI01372674
SMILES: CP(C)(C1=CC=C(C=C1)CNC(C2CCN(S(=O)(C3=CC(Cl)=CC(Cl)=C3)=O)CC2)=O)=O

Orthogonal Probes def

PF-06649298

Chemical Information

Molecular Formula C19H19Cl2FN2O3S
SMILEs O=C(NCc1ccc(F)cc1)C1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1
InChI InChI=1S/C19H19Cl2FN2O3S/c20-15-9-16(21)11-18(10-15)28(26,27)24-7-5-14(6-8-24)19(25)23-12-13-1-3-17(22)4-2-13/h1-4,9-11,14H,5-8,12H2,(H,23,25)
Molecular weight 444.05 Da
AlogP 3.8496000000000032
HBond acceptors 5
HBond donors 1
Atoms 47

Vendors

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Expert Reviews

by SERP
(on 5 Feb 2023)
Cellular Use Rating
Due to the non-reversible mechanism of action of BI01383298, a pre-incubation of 30 minutes is required to achieve maximal inhibition of cellular uptake of citrate. Of note, using kinetic analysis of citrate...
by SERP
(on 9 Feb 2023)
Cellular Use Rating
Available data for this probe consists exclusively of cellular inhibition experiments. No direct binding has been demonstrated via biochemical or biophysical approaches.
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