biased

UNC9975 is a beta-inhibitory protein-biased dopamine D(2) receptor agonist with antipsychotic activity and can be used to study neurologic disorders such as schizophrenia.

UNC0006 is a beta-inhibitory protein biased D(2)R ligand, and is also an antagonist of G(i)-regulated cAMP production and a partial agonist of D(2)R beta-arrestin-2 interaction. It has antipsychotic activity and is used in the study of neurological disorders.

F13714 fumarate is a selective 5-HT1A receptor-biased agonist with antidepressant-like properties after a single dose in a mouse model of chronic mild stress.

AP1189 acetate is a biased agonist at melanocortin 1 and melanocortin 3 receptors.

TRV120056 acetate is a Gq-biased agonist with 10-fold greater molecular efficiency on AT1R-Gq fusion proteins than AT1R-βarr2 fusion proteins.

MLS1547 (MLS000051547) is a highly efficacious agonist of G protein-biased dopamine D2 receptor with a Ki of 1.2 μM. MLS1547 stimulates D2R G protein-mediated signaling with EC50 of 0.37 μM in a calcium mobilization assay.

TRV120027 TFA is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R) and engages ß-arrestins while blocking G-protein signaling.

ML-335 is a μ-δ isomer-targeted agonist, a μOR-δOR-biased ligand that can serve as a scaffold for the development of unique types of (isomer-biased) drugs.ML-335 is a MOR (μ-opioid receptor) DOR (δ-opioid receptor) heterodimer, with anti-injury sensory activity and pain inhibitory activity.

TRV056 is a Gq-biased agonist of the angiotensin II type 1 receptor (AT1R), demonstrating efficacy in stimulating Gq-mediated cellular signaling. It can serve as a foundation for the development of Gq-biased AT1R agonists.

TRV120055, a Gq-biased agonist, demonstrates a 10-fold higher molecular efficacy when tested against the AT1R-Gq fusion protein in comparison to the AT1R-βarr2 fusion protein.

TRV055 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 is efficacious in stimulating cellular Gq-mediated signaling. TRV055 can be used to develop the Gq-biased AT1R agonists.

ATI-2341 is an effective functionally selective allosteric agonist for the c-x-c chemokine receptor type 4 (CXCR4), which ACTS as a biased ligand in favor of G G G G G 1 activation instead of G G G G G 13.ATI-2341 activates the inhibitory heterotrimer G p

5-HT7R antagonist 1 (free base) is a G protein-biased antagonist for the 5-HT7R receptor, with a dissociation constant (K_i) of 6.5 nM.

DFPQ is a powerful and selective β-arrestin-biased negative allosteric modulator(NAM) targeting the β2-adrenergic receptor. It specifically inhibits the interaction of β-arrestin with β2AR without altering β-agonist-induced cAMP production. Additionally, DFPQ reduces functional desensitization of the β2AR in airway smooth muscle, enhancing β-agonists' capacity to maintain bronchorelaxation and curbing cell migration during prolonged β-agonist treatment.

TRV-120027 acetate is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1 receptor) and engages -arrestins while blocking G-protein signaling.

ML314 is a brain-permeable nonpeptide β-inhibin-biased neurotensin NTR1 receptor agonist (EC50: 1.9 μM), a biased neurotensin receptor ligand for methamphetamine abuse that inhibits NTR2 and GPR35.

UCSF678 is a 42 nM arrestin-biased partial agonist at the 5-HT5AR with a more restricted off-target profile and decreased assay liabilities compared to the commercial antagonist SB-699551. UCSF678 is a selective probe for studying the function of the 5-HT5AR [1].

AY 254 is a potent PAR2 biased agonist. Selectively activates ERK1 2 signaling (EC50= 2 nM for ERK1 2 phosphorylation versus 80 nM for Ca2+release). Reduces cytoKi ne-induced caspase 3 8 activation, promotes scratch-wound healing, and induces IL-8 secretion, in human colorectal cancer (HT29) cellsin vitro.

SBI-810 is a functional selective β-arrestin-biased allosteric modulator of the neurotensin receptor 1 (NTSR1). In the presence of the endogenous ligand neurotensin (NT), SBI-810 regulates NTSR1 signaling through a G protein-specific mechanism. It fully antagonizes NT-induced Gq activation and partially antagonizes NT-induced Gi1 activation, allowing NTSR1 to activate GoA and G12.

PW0464 ((Rac)-Razpipadon) is a non-catechol D1R agonist and potent omplete G protein biased ligand with an EC50 (Gs-cAMP)=5.8 nM for the study of neurological disorders.

SAR247799 (S1P1 agonist 3) is an orally-active, selective G-protein-biased agonist for the sphingosine-1 phosphate receptor-1 (S1P1). It demonstrates EC50 values ranging from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 holds promise as a valuable tool for investigating endothelial protection, particularly in the context of type-2 diabetes and metabolic syndrome [4].

TRV120056 is a Gq-biased agonist that demonstrates a molecular efficacy ten times greater at the AT1R-Gq fusion protein than at the AT1R-βarr2 fusion protein.

MOR agonist-4 (2d), having an EC50 of 11 nM, is a G protein-biased agonist of the Kappa opioid receptor (KOR). This compound features a triazole-based, electron-withdrawing CF3 group and a bias factor of 38. MOR agonist-4 is utilized for antipruritic and analgesic applications.

UNC9995 is a β-Arrestin-Biased Dopamine D2 Receptor agonist (β-Arrestin, EC50 = 120 nM; Emax = 88%).