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Search Results for " lbd "

17

Compounds

Cat No. Product Name Synonyms Targets
T8779 HBT1 GluR
HBT1 is an AMPA receptor potentiator that induces production of brain-derived neurotrophic factor (BDNF) and exhibits little agonistic effect in primary neurons. HBT1 binds to ligand-binding domain of AMPA-R in glutamate...
T7904 SR 19881 Estrogen/progestogen Receptor
SR 19881 is a full agonist of ERRγ(EC50 value of 0.39 μM in a binding assay and an EC50 value of 4.7 μM in a cell-based assay).
T13272 UT-155 Androgen Receptor
UT-155 is a selective and potent antagonist of the androgen receptor (AR) (Ki: 267 nM for UT-155 binding to AR-LBD).
T77549 Nurr1 agonist 2 Others
Nurr1 agonist 2 is a Nurr1 agonist with an EC50 value of 0.07 μM. Nurr1 agonist 2 increases the mRNA expression of the Nurr1-regulated genes tyrosine hydroxylase (TH) and vesicular amino acid transporter 2 (VMAT2). Nurr1...
T75129 Luxdegalutamide ARV-766 Androgen Receptor , PROTACs
Luxdegalutamide (ARV-766) is an orally available and effective protein degrader of protein hydrolysis-targeted chimeras (PROTAC).Luxdegalutamide degrades the wild-type androgen receptor AR, as well as AR LBD mutants incl...
T12406 PEPA iGluR
PEPA is an allosteric AMPA receptors modulator; binds to the GluA2o and GluA3o LBDs and can be utilized as an indicator of AMPA receptor heterogeneity.
T8381 Amodiaquine Others , Histone Methyltransferase , Parasite
Amodiaquine is a synthetic aminoquinoline, used to treat malaria.
T12754 RORγt Inverse agonist 8 ROR
RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist(human RORγt-LBD with an IC50 of 19 nM).
T69982 VPC-16606
VPC-16606 is a potent and selective inhibitor of ERα-dependent cell growth and gene expression. VPC-16606 prevents the interaction between ERα-LBD and SRC-3 fusion proteins in a dose-dependent manner.
T40349 DS45500853
DS45500853, an estrogen-related receptor α (ERRα) agonist, acts as an inhibitor of the binding interaction between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain ...
T76375 Targefrin
Targefrin is a potent antagonist targeting EphA2, exhibiting a dissociation constant of 21 nM and an IC50 value of 10.8 nM for the EphA2-LBD. It promotes receptor internalization and degradation across multiple pancreati...
T39916 GNE-274
GNE-274, a non-degrader compound structurally similar to GDC-0927 (an ER degrader), serves as a partial ER agonist in breast cancer cell lines without triggering ER turnover. Notably, GNE-274 enhances chromatin accessibi...
T73842 Leriglitazone hydrochloride
Leriglitazone (Hydroxypioglitazone) hydrochloride, a pioglitazone metabolite, acts as a PPARγ agonist, effectively stabilizing the PPARγ activation function-2 (AF-2) co-activator binding surface to enhance co-activator b...
T60759 DS20362725
DS20362725 is an agonist of estrogen-related receptor α (ERRα) that is able to be used for the metabolic disorders research, for example, type 2 diabetes mellitus (T2DM). The IC 50 value of DS20362725 inhibiting the bind...
T83894 4A7C-301-Nurr1 Agonist 4A7C-301-Nuclear Receptor-Related 1
The compound 4A7C-301-Nurr1 agonist is a specific agonist for the nuclear receptor-related 1 (Nurr1). By binding to the Nurr1 ligand-binding domain with an IC50 value of 48.22 nM, it enhances the transcriptional activity...
T22242 Amodiaquine hydrochloride
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a member of the 4-aminoquinoline class, serves as an antimalarial agent and exhibits potent oral activity as a histamine N-methyltransferase inhibitor, displaying...
T15736 Leriglitazone Hydroxypioglitazone Others
Leriglitazone, a metabolite of pioglitazone, binds to the PPARγ C-terminal ligand-binding domain (Ki: 1.2 μM) and induces transcriptional efficacy of the PPARγ (EC50: 680 nM). Leriglitazone PioOH is a PPARγ agonist, stab...
TargetMol