Compound name
Tropifexor
Protein family
NR
Target name
NR1H4
Affinity on-target cellular (nM)
0.3
CG-Set
NR
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001169a
SMILES
FC1=C2C(SC(N3[C@H]4CC[C@@H]3C[C@H](OCC5=C(C6CC6)ON=C5C7=CC=CC=C7OC(F)(F)F)C4)=N2)=CC(C(O)=O)=C1
InChIKey
VYLOOGHLKSNNEK-PIIMJCKOSA-N
NCBI gene ID
9971
UniProt ID
Q96RI1
Synonyms
FXR, RIP14, HRR1, HRR-1
Mode of action
Agonist
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
cell-based
Affinity on-target cellular source knowledge
https://doi.org/10.1021/acs.jmedchem.7b00907
Affinity on-target cellular relation
=
Selectivity platform
Reportergenassay
Selectivity platform number of targets
26
Selectivity remarks
rem. activity(NR5A1) = 0.47, inactive at 1 µM for NR1H2, NR1H3, UL48, RXRA, HNF4A, NR2C1, NR2E1, NR4A1
Selectivity Source Knowledge
https://zenodo.org/records/10474037