allosteric agonist

BMT-145027 is a positive allosteric modulator of mGluR5 without inherent agonist activity (EC50 = 47 nM).

LUF6096 (CF-602) is a potent allosteric enhancer of the adenosine A3 receptor, exhibiting the capability to enhance agonist binding allosterically while demonstrating low orthosteric affinity across adenosine receptors. It displays protective effects in myocardial ischemia reperfusion injury.

Cinacalcet (AMG 073) is an orally active, allosteric Ca receptor (CaR) agonist used in the treatment of cardiovascular disease.

4-CMTB is a selective agonist of FFA2 and GPR43.It also is a positive allosteric modulator (pEC50=6.38).

L-838417 D9 (C-21191) is a novel deuterated subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].

ATI-2341 acetate is an effective allosteric agonist of CXCR4, it activates Gα1 instead of Gα13. ATI-2341 acetate activates inhibitory heterotrimeric G protein (GI) to promote the inhibition of cAMP production and induce calcium mobilization.

VU0119498 is a M1 muscarinic receptor agonist (EC50 = 3.1 μM) and pan mAChR M3, M5 positive allosteric modulator (PAM),and is a neuroprotective agent.

4BP-TQS is an allosteric agonist of α7 nAChRs.

Cinacalcet metabolite M4 (Rarechem AL BW 1078) is a metabolite of Cinacalcet. Cinacalcet is an allosteric agonist of Ca receptor.

GPR40 FFAR1 modulator 1 is a Gq-coupled free fatty acid receptor 1 (GPR40 FFAR1) agonist and allosteric modulator.

LY3154207 is a subtype selective, potent, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM).

MRK-016 is a selective GABAA α5 receptor inverse agonist negative allosteric modulator, (IC50=3 nM) with the advantages of being orally available and penetrating the blood-brain barrier.MRK-016 increases long time period potentiation (LTP) in mouse hippocampal slices, with memory-improvement, antidepressant, and pain-treating effects.

nAChR agonist 1 (DUN71755) is a brain-permeable and orally efficacious positive allosteric α7 nicotinic acetylcholine receptor (α7 nAChR)modulator.

NCGC00229600 is an allosteric inverse thyrotropin receptor (TSHR) agonist. NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously and can be used in Graves' disease studies.

(Z)-Leukadherin-1 (ADH-503 free base) is an allosteric agonist of CD11b.

AP5 is a potent and selective agonist for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49 nM against the GPR40 receptor.

AC260584 is an allosteric agonist of the M1 muscarinic receptor with a pEC50 of 7.6.

Fenobam shows inverse agonist activity which blocks the mGlu5 receptor basal activity(IC50: 84 nM). Fenobam has anxiolytic activity. Fenobam is a selective and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively).

FzM1.8 is an allosteric FZD4 agonist with a pEC50 of 6.4. FzM1.8 binds to FZD4, promotes TCF LEF transcriptional activity in the absence of any WNT ligand, and activates the WNT β-catenin pathway.

Ogerin is a selective GPR68 positive allosteric modulator (pEC50: 6.83) that blocks recall in fear conditioning in mice. It exhibits inverse agonist and antagonist activity (Ki, 220 nM) at the A2A receptor and weak antagonist activity (Ki, 736 nM) at the 5-HT2B receptor.

(-)-(S)-B-973B is an effective allosteric agonist and positive allosteric modulator of α7 nAChR.

TBPB, an allosteric M1 mAChR agonist, is an [iso]propyl (2-{4-methoxy-3-[3-(4-methylpiperidin-1-yl)propoxy]phenyl}ethyl)carbamate exhibiting a molar mass of 430.6 g mol.

VU0029767 is an allosteric enhancer of the M1 muscarinic receptor, capable of modulating the receptor's activity. This compound enhances M1 receptor activity by increasing agonist affinity. However, VU0029767 demonstrates distinct characteristics from other compounds, particularly under varying experimental conditions such as its interaction with mutated M1 receptors and its effects on downstream signaling pathways.

24(S)-hydroxy Cholesterol (24S-OHC) is the terminal product of the cholesterol elimination pathway in neural tissues. It is an LXR agonist and a selective positive allosteric modulator of NMDARs. It can serve as a biomarker for NPD, induce cognitive decline in mice, and is useful for studying neurological diseases.