Compound name
T3
Protein family
Nuclear Receptors
Target name
NR1A2
Affinity on-target cellular (nM)
2.4
CG-Set
Nuclear Receptor set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000555a
SMILES
N[C@@H](Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1)C(O)=O
InChIKey
AUYYCJSJGJYCDS-LBPRGKRZSA-N
Mode of action
Agonist
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Reporter gene assay (HeLa cells were cotransfected with a repoter plasmid containing a synthetic THR response element, pRL-TK control plasmid and full-length hTHR?- or hTHR?-CMV expression plasmid)
Affinity on-target cellular source knowledge
https://doi.org/10.1016/j.bmc.2007.10.040
https://doi.org/10.1021/jm0201013
Affinity on-target cellular relation
0
Selectivity platform
Nuclear receptor panel, bromodomain and kinase panel
Selectivity platform number of targets
19
Selectivity remarks
Screened at 1 µM against NR2A1, NR2B1, NR2C1, NR2E1, NR4A1, NR5A1 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV containing the Gal4-DBD fused with human NR-LBD of interest or pECE-SV40-Gal4-VP16): clean selectivty profile with no significant agonism/antagonism detected; Screened at 20 µM in a bromodomain and kinase panel against ABL1, AURKA, BRD4, BRPF1, CDK2, CSNK1D, FGFR3, GSK3B, MAPK1, TRIM24 in DSF assays: clean selectivity profile with no significant binding (?Tm < 2 K)