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.

LIT-001 improves social interaction in a mouse model of autism.It is the first nonpeptide oxytocin receptor agonist with EC50 of 55 nM and Ki of 226 nM.

CMF019 (CMF-019) is a potent, G-protein-biased small-molecule agonist of the Apelin receptor (APJ/APLNR). CMF019 exhibits pKi values of 8.58, 8.49, and 8.71 for binding to APJ in humans, rats, and mice, respectively. CMF-019 exhibits cardioprotective effects in rodents. CMF019 can be utilized in mechanism and drug development for heart failure and pulmonary arterial hypertension.

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.

CCKBR agonist-2 (Compound z-44) is a CCKBR-Gi-biased agonist that activates the Gi signaling pathway (EC50 = 0.27 nM) with negligible activity on Gq and Gs pathways. It exhibits no significant protective effect in mouse models of Alzheimer's disease.

S1P1 agonist 7 is a potent and orally active β-arrestin-biased S1P1 agonist [EC50 (G-protein) = 12.7 nM, EC50 (β-arrestin) = 3.23 nM], exhibiting strong immunomodulatory activity and favorable safety. It has excellent metabolic stability, shows weak to moderate CYP inhibition, and demonstrates high selectivity without affecting the S1P3 receptor. In a mouse model of experimental autoimmune encephalomyelitis, S1P1 agonist 7 shows favorable pharmacokinetic properties, effectively reduces circulating lymphocyte counts, and significantly alleviates disease severity. This compound is applicable for research in multiple sclerosis.

EP2 receptor agonist 2 (compound 18a) is a potent and selective G protein-biased EP2 receptor agonist with an efficacy of hEP2G protein EC50= 13 nM and hEP2βarrestin EC50 > 10000 nM. It shows exceptional selectivity over hEP1/3/4, hIP, and hFP, with EC50 values exceeding 10000 nM.

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.