biased

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.

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.

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.

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.

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.

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

NI-42 is a structurally orthogonal chemical probe for the BRPFs and is biased. It effective inhibitor of the BRD of the BRPFs (IC50s of BRPF1/2/3=7.9/48/260 nM; Kds of BRPF1/2/3=40/210/940 nM). It also has excellent selectivity over nonclass IV BRD protei

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.

SBI-810 hydrochloride is a β-arrestin-2 (βarr2)-biased allosteric modulator of NTSR1 (neurotensin receptor 1), exerting analgesic effects through peripheral and central mechanisms by inhibiting excitatory synaptic transmission, suppressing NMDA receptor and ERK signalling in spinal nociceptive neurons, and reducing Nav1.7 expression and action potential discharge in primary sensory neurons.

5-HT2A receptor agonist-9 is a β-arrestin-biased agonist of the 5-HT2A receptor. It may be utilized in research related to neurological conditions such as depression and psychedelia.

NLX-266 is an orally active ERK1/2-biased 5-HT1A receptor agonist [NLX-266]. This compound is utilized in research related to Parkinson's disease.

JR-6 is a Gi/o pathway-biased muscarinic M2-selective partial agonist.

KRN7000 analog 1 stimulates a strong Th1-biased immune response by inducing interferon-γ (IFN-γ) and reducing interleukin-4 (IL-4). This compound shows potential as an antitumor agent and vaccine adjuvant.

LM-189 is a G protein α subunit I (Gαi)-biased agonist and serves as a Gαi-biased ligand for the β2-adrenergic receptor (β2AR). It stabilizes a specific conformation in TM6 and enhances the dynamics of ICL2. LM-189 is useful for developing Gαi-biased β2AR agonists.

ATR-258 is a GRK2-biased partial agonist of β2AR. It acts as a competitive antagonist of β1AR and exhibits weak partial agonist activity on β3AR at a concentration of 10 μM. ATR-258 enhances glycemic control and reduces lipid accumulation in obese mice with minimal side effects. It is applicable in research on type 2 diabetes (T2DM).

DW34 is an orally bioactive pan-BRD4-D1-biased inhibitor that also exhibits BRD4-D2 activity. It demonstrates a low nanomolar inhibitory effect comparable to I-BET151 (EC50 value of 0.16 μM), with an EC50 value of 0.14 μM. DW34 significantly alleviates lipopolysaccharide (LPS)-induced liver inflammation and acetaminophen (APAP)-induced toxicity by reducing chemokine expression and cell necrosis.

LM-189 free base is a G protein α subunit I (Gαi)-biased agonist and acts as a Gαi-biased ligand for the β2-adrenergic receptor (β2AR). It stabilizes a particular conformation in TM6 and enhances the dynamics of ICL2. LM-189 free base is useful for the development of Gαi-biased β2AR agonists.

RS130-180 is a β-arrestin-biased agonist that selectively targets the 5-hydroxytryptamine 2A receptor (5-HT2aR). It shows promise for research in neuropsychiatric disorders such as depression.

UNC9994 is a β-arrestin-biased dopamine D₂ receptor agonist (β-arrestin EC50 = 50 nM; Emax = 97%) with robust in vivo antipsychotic drug-like activities.

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

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.

Bilaid C is a tetrapeptide μ-opioid receptor agonist (Ki= 210 nM in HEK293 cell membranes expressing the human receptor) that has been found inPenicillium.1It inhibits forskolin-induced cAMP accumulation by 77% in HEK293 cells expressing the human μ-opioid receptor when used at a concentration of 10 μM. Bilaid C induces inward rectifying potassium channel (Kir) currents in rat locus coeruleus slices that endogenously express high levels of the μ-opioid receptor (EC50= 4.2 μM). 1.Dekan, Z., Sianati, S., Yousuf, A., et al.A tetrapeptide class of biased analgesics from an Australian fungus targets the μ-opioid receptorProc. Natl. Acad. Sci. USA116(44)22353-22358(2019)

Potent and selective GPR84 biased agonist (EC50 = 33 nM). Exhibits no significant activity in a panel of 168 other GPCRs. Exhibits bias for G protein signaling pathways. Induces morphological changes in primary murine bone marrow-derived macrophages (BMDMs) in a cellular impedance assay, and promotes phagocytosis by M1 polarized U937 cells. Induces migration of primary human monocytes, but has no effect on macrophage chemotaxis.

SAR247799 (S1P1 agonist 3) is a selective and G-protein-biased S1P1 agonist that activates downstream G-protein signaling pathways more preferentially than β-blocker proteins and internalized signaling pathways, activates S1P 1 on endothelial cells without causing receptor desensitization, and protects the endothelium without affecting lymphocyte populations, and can be used to study type 2 diabetes, endothelial dysfunction and vascular hyperpermeability.