Activity (binding)
|
= 14 %
|
Agonist activity at REV-ERBalpha in human U2OS cells assessed as suppression of BMAL1 expression at 20 uM after 40 hrs by luciferase reporter gene assay relative to DMSO-treated control
|
ChEMBL.
|
23656296
|
Activity (binding)
|
= 30 %
|
Agonist activity at biotinylated REV-ERBalpha (unknown origin) assessed as increase in biotinylated NCOR peptide recruitment at 10 mM after 1 hr by FRET assay relative to control
|
ChEMBL.
|
23656296
|
EC50 (binding)
|
> 50 uM
|
Agonist activity at biotinylated REV-ERBalpha (unknown origin) assessed as increase in biotinylated NCOR peptide recruitment after 1 hr by FRET assay
|
ChEMBL.
|
23656296
|
IC50 (binding)
|
= 560 nM
|
Increased REV-ERB-beta LBD dependent repressor activity in HEK293 cell reporter assay
|
ChEMBL.
|
22460951
|
IC50 (functional)
|
= 620 nM
|
REV-ERB-alpha mediated transcriptional suppression at Bmal1 promoter in HEK293 cell reporter assay
|
ChEMBL.
|
22460951
|
IC50 (binding)
|
= 790 nM
|
Increased REV-ERB-alpha LBD dependent repressor activity in HEK293 cell reporter assay
|
ChEMBL.
|
22460951
|
IC50 (binding)
|
= 13 uM
|
Binding affinity to LXRalpha (unknown origin) by radioligand displacement assay
|
ChEMBL.
|
23656296
|
Inhibition (binding)
|
|
Effect on PGR(NR3C3) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on SHP(NR0B2) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on TFCOUP1(NR2F1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on PPARA(NR1C1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on NURR1(NR4A2) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on NOR1(NR4A3) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on ERR2(NR3B2) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on GFRP1(NR4A1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on HNF4A(NR2A1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on ESR2(NR3A2) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on RORA(NR1F1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on PPARG(NR1C3) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on PXR(NR1I2) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on RORB(NR1F2) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on THRA(NR1A1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on THRB(NR1A2) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on ERR1(NR3B1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on ERR3(NR3B3) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on CAR(NR1I3) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on RARB(NR1B2) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on BAR(NR1H4) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on TR4(NR2C2) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on TR2(NR2C1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on TLX(NR2E1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on PNR(NR2E3) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on EAR2(NR2F6) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on DAX1(NR0B1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on AR(NR3C4) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on GCNF(NR6A1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on TFCOUP2(NR2F2) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on GCR(NR3C1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on RARG(NR1B3) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on RXRG(NR2B3) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on CPF(NR5A2) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on RXRB(NR2B2) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on MCR(NR3C2) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on RARA(NR1B1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on LXRB(NR1H2) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on SF1(NR5A1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on RORG(NR1F3) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on PPARD(NR1C2) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on HNF4G(NR2A2) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on VDR(NR1I1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on RXRA(NR2B1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
Inhibition (binding)
|
|
Effect on ESR1(NR3A1) dependent reporter activity in HEK293 cells at 20 uM
|
ChEMBL.
|
22460951
|
NcoR1_recruitment (functional)
|
|
Recruitment of co-repressor NcoR1 to REV-ERB-alpha
|
ChEMBL.
|
22460951
|
Time (binding)
|
= 1.3 hr
|
Agonist activity at REV-ERBalpha in human U2OS cells assessed as delay of peak of second cycle at 20 uM by luciferase reporter gene assay relative to DMSO-treated control
|
ChEMBL.
|
23656296
|