orthosteric

Calindol hydrochloride is a potent orthosteric modulator (EC50: 132 nM) of the putative calcium-calcium-sensitive receptor (CaSR), inhibits Pi-induced VC, and delays the progression of calcification in vascular smooth muscle cells.

Upacicalcet (AJT-240) is an intraventricular calcium mimetic, a SHPT available for human hemodialysis, that inhibits excessive parathyroid hormone (PTH) secretion by directly acting on parathyroid cell membrane calcium-sensitive receptors, thereby lowering blood levels of PTH.Upacicalcet is an orthosteric modulator of calcium-sensitive receptors and prevents adenine-induced secondary vascular calcification and bone disease in a rat model of adenine-induced secondary hyperparathyroidism.

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.

Cloransulam-methyl is an effective herbicide that is often applied to soybean fields to control broadleaf weeds.Cloransulam-methyl is rapidly metabolised in the soybean plant but is present in the soil.CBiPES hydrochloride (CBiPES HCl) is a potent orthosteric modulator of the mGlu2 receptor.

4,4-dimethyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-2-one is a benzodiazepine derivative. It is an orthosteric modulator of the GABAA receptor and selectively binds to the benzodiazepine site of the GABAA receptor. It has anxiolytic, anticonvulsant and sedative activity.

CYM2503 is a positive allosteric modulator (PAM) of the GAL2 receptor that potentiates galanin-induced IP1 production in vitro. It has no affinity for the orthosteric galanin binding site of the receptor (as measured by its inability to displace iodinated galanin, or to induce IP1 accumulation on its own).

KI-7 is an adenosine A2B receptor positive allosteric modulator.

LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively.LY 541850 is claimed from human ionotropic and metabotropic glutamate (mGlu) receptors expressed in non-neuronal cells.

PF-06256142 is a potent and selective orthosteric D1 receptor agonist(D1 EC50=30 nM ).

LY2979165 (mGlu2 agonist) is an orthosteric agonist of mGluR2 and can be used in studies about serving as an anti-depressant.

Padsevonil (UCB-0942) is a potential GABA A receptor orthosteric modulator with antiepileptic activity for the treatment of epilepsy.

CBiPES hydrochloride (CBiPES HCl) is a potent orthosteric modulator of the mGlu2 receptor with an EC50 value of 92.8 nM.CBiPES hydrochloride blocks the action of WT and mGlu(3) receptors.CBiPES hydrochloride can be used to study neurological disorders like epilepsy and Parkinson's syndrome. CBiPES hydrochloride can be used to study neurological disorders like epilepsy and Parkinson's syndrome.

SR 16832 is a dual-site PPARγ inhibitor. It also inhibits the binding of endogenous ligands and transcriptional activity of PPARγ, more effectively than the orthosteric covalent antagonist GW 9662 and T 0070907.

GAT211 (AZ-4) is a selective and potent cannabinoid 1 receptor (CB1R) orthosteric modulator (PAM) with high affinity for cAMP and β-arrestin2.GAT211 has IOP-lowering and antipsychotic effects and can be used in the study of epilepsy.

LY593093 is a selective partial orthosteric agonist of M1 muscarinic acetylcholine receptor.

ML381 is a M5-orthosteric antagonist with a high selectivity of muscarinic subtype.

SPM-242 is an orthosteric agonist of Sphingosine 1-phosphate (S1P) and a bitopic antagonist. S1P is a lysophospholipid signaling molecule that regulates important biological functions, including vascular development and lymphocyte trafficking, by activat

VU0422288 (ML396) is a potent orthosteric modulator of type III mGlu receptors (mGlus).VU0422288 shows inhibition of mGluR4, mGluR7, and mGluR8 in a calcium mobilization assay.VU0422288 can be used to study Rett syndrome (RTT).

ZCZ011 is a positive allosteric modulator of the cannabinoid CB1 receptor. ZCZ011 is brain penetrant, increased the potency of orthosteric agonists in mouse behavioral assays indicative of cannabimimetic activity, including antinociception, hypothermia, c

AC265347 is a potent calcium-sensitive receptor (CaSR) agonist and ago-PAM orthosteric modulator with antitumour activity that inhibits neuroblastoma tumour growth by inducing differentiation.AC265347 can be used to study neuroblastoma.

5-Benzyloxygramine is an N protein PPI orthosteric stabilizer that exhibits both antiviral and N-NTD protein-stabilizing activities. It stabilizes the N-NTD dimers through simultaneous hydrophobic interactions with both partners, resulting in abnormal N protein oligomerization, which was further confirmed in cell studies[1]. [1]. Shan-Meng Lin, et al. Structure-Based Stabilization of Non-native Protein-Protein Interactions of Coronavirus Nucleocapsid Proteins in Antiviral Drug Design. J Med Chem. 2020 Mar 26;63(6):3131-3141.

Tetrahydrodeoxycorticosterone(Tetrahydro-11-deoxycorticosterone) is a potent GABAA receptor orthosteric modulator (PAM) with neuroprotective activity that selectively inhibits neurosteroid-mediated enhancement of GABA-induced currents at the GABAA receptor, and can be used in the study of neurological disorders.

Dimethyl-W84 is a selective allosteric modulator of the M2 muscarinic acetylcholine receptor. It hinders the dissociation of the orthosteric antagonist N-methylscopolamine from the M2 receptor with an EC50 value of 3 nM.

MLS1082 is a D1-like dopamine receptor (D1R) orthosteric modulator derived from pyrimidinone that stimulates G-protein signaling upon dopamine activation. It has potential for the treatment of Parkinson's disease and other neurodegenerative disorders by enhancing D1 receptor signaling and modulating neuronal activity.