Compound name
BAY-876
Protein family
SLC
Target name
SLC2A1
Affinity on-target cellular (nM)
2
CG-Set
Ion Channel
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000307b
SMILES
Cc1c(NC(=O)c2cc(C(N)=O)nc3cc(F)ccc23)c(C(F)(F)F)nn1Cc1ccc(C#N)cc1
InChIKey
BKLJDIJJOOQUFG-UHFFFAOYSA-N
NCBI gene ID
6513
UniProt ID
P11166
Synonyms
CSE DYT17 DYT18 DYT9 EIG12 GLUT GLUT-1 GLUT1 GLUT1DS HTLVR PED SDCHCN
Mode of action
Inhibitor
Negative control
BAY-588
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
CellTiter-Glo® Luminescent Cell Viability Assay (DLD1 cells; Promega)
Affinity on-target cellular relation
=
Selectivity platform
Glucose transporter panel, literature
Selectivity platform number of targets
4
Selectivity remarks
Selectivity against other glucose transporters (CellTiter-Glo® Luminescent Cell Viability Assay, Promega): IC50(SLC2A4) = 270 nM, IC50(SLC2A3) = 1.6 µM, IC50(SLC2A2) = 9.4 µM, >100-fold selective; Screened against 468 targets in KinomeScan (DiscoverX) at 1 µM, closest targets as % of contr.: WNK4 (0%), DDR1 (1.5%); Screened against 45 GPCRs (PDSP screen) at 10 µM, closest target: Ki(HRH2) = 8078 nM; Screened in Eurofins-Panlabs radioligand binding assay against 68 enzymes, closest targets: IC50(ADORA3) =1.14 µM, IC50(PTGER4) = 1.12 µM;
Selectivity Source Knowledge
https://doi.org/10.1002/cmdc.201600276
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/BAY-876
Selectivity Number of Off-targets
0