Compound name
Meclizine dihydrochloride
Protein family
Nuclear Receptors
Target name
NR1I3
Affinity on-target cellular (nM)
60
CG-Set
Nuclear Receptor set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000551aCl
SMILES
CC1=CC(=CC=C1)CN2CCN(CC2)C(C3=CC=CC=C3)C4=CC=C(C=C4)Cl.Cl.Cl
InChIKey
VCTHNOIYJIXQLV-UHFFFAOYSA-N
NCBI gene ID
9970
UniProt ID
Q14994
Synonyms
MB67, CAR1, CAR
Mode of action
Inverse Agonist
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Gal4 hybrid reporter gene assay (HepG2 cells were cotansfected with pG5E1b-Luciferase reporter, pSV2-?-galactosidase control reporter and Gal4-hCAR-LBD)
Affinity on-target cellular source knowledge
https://doi.org/10.1210/me.2004-0046
Affinity on-target cellular relation
0
Selectivity platform
Nuclear receptor panel, bromodomain and kinase panel
Selectivity platform number of targets
20
Selectivity remarks
Screened at 1 µM against NR1I1, NR1I2, 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)