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T9238 |
KI-7
|
|
Adenosine Receptor
|
|
KI-7 is an adenosine A2B receptor positive allosteric modulator. |
|
T16427 |
Padsevonil
|
UCB-0942,UCB1415943-000 |
GABA Receptor
|
|
Padsevonil (UCB-0942) is a potential GABA A receptor orthosteric modulator with antiepileptic activity for the treatment of epilepsy. |
|
T15812 |
LY2979165
|
mGlu2 agonist |
GluR
|
|
LY2979165 (mGlu2 agonist) is an orthosteric agonist of mGluR2 and can be used in studies about serving as an anti-depressant. |
|
T29135 |
VU0422288
|
VU-0422288,ML-396,ML396,VU 0422288,ML 396 |
GluR
|
|
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... |
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T29541 |
AC265347
|
AC-265347 |
CaSR
|
|
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 stud... |
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T24827 |
SR 16832
|
SR-16832,SR16832 |
PPAR
|
|
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. |
|
T27405 |
GAT211
|
AZ4,GAT-211,AZ 4,GAT 211,AZ-4 |
cAMP
,
Cannabinoid Receptor
,
Arrestin
|
|
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... |
|
T20941 |
Cloransulam-methyl
|
Cloransulam methyl |
Others
|
|
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 hydrochlori... |
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T61483 |
GLP-1R modulator C5
|
|
Glucagon Receptor
|
|
GLP-1R modulator C5 is a small molecule GLP-1R orthosteric modulator that enhances GLP-1 binding to GLP-1R via transmembrane sites and can be used in the study of type II diabetes. |
|
T22638 |
CBiPES hydrochloride
|
CBiPES HCl |
GluR
|
|
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 ... |
|
T29067 |
Upacicalcet
|
PLS-240,SK-1403,AJT-240 |
Calcium Channel
|
|
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-s... |
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T50048 |
BRD4 Inhibitor 31
|
|
Others
|
|
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 h... |
|
T9180 |
LUF6096
|
CF-602 |
Adenosine Receptor
|
|
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. ... |
|
T8963 |
CYM2503
|
|
Neuropeptide Y Receptor
|
|
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 ... |
|
T35841 |
5-Benzyloxygramine
|
|
Dopamine Receptor
,
5-HT Receptor
|
|
5-Benzyloxygramine is a N protein PPI orthosteric stabilizer that exhibits both antiviral and N-NTD protein-stabilizing activities[1].
5-benzyloxygramine stabilizes the N-NTD dimers through simultaneous hydrophobic inter... |
|
T27961 |
LY593093
|
LY 593093,LY-593093 |
|
|
LY593093 is a selective partial orthosteric agonist of M1 muscarinic acetylcholine receptor. |
|
T28070 |
ML381
|
VU 0488130,ML-381,ML 381,VU-0488130,VU0488130 |
|
|
ML381 is a M5-orthosteric antagonist with a high selectivity of muscarinic subtype. |
|
T61276 |
CB1R Allosteric modulator 2
|
|
|
|
CB1R Allosteric modulator 2 (compound 18) is a potent allosteric modulator of the CB1R receptor. It exhibits negative modulation of the functional activity of orthosteric ligands (NAM) at CB1Rs, as demonstrated in previo... |
|
T12423 |
PF-06256142
|
|
Others
|
|
PF-06256142 is a potent and selective orthosteric D1 receptor agonist(D1 EC50=30 nM ). |
|
T62610 |
LY3154885
|
|
|
|
LY3154885 is an orally active dopamine D1 receptor orthosteric modulator (PAM) that reduces the risk of drug-drug interactions (DDI). |
|
T11906 |
LY 541850
|
|
GluR
|
|
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 expres... |
|
T74396 |
NAChR modulator-1
|
|
|
|
nAChR modulator-1, a insecticide, is a insect nAChR orthosteric modulator [1] . |
|
T74397 |
NAChR modulator-2
|
|
|
|
nAChR modulator-2, a insecticide, is a insect nAChR orthosteric modulator [1] . |
|
T29206 |
ZCZ011
|
ZCZ 011,ZCZ-011 |
|
|
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, includ... |
|
T38111 |
Dimethyl-W84 (dibromide)
|
Dimethyl-W84 (dibromide) |
|
|
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. |
|
T70301 |
GAT100
|
|
|
|
GAT100 is a potent and covalent negative allosteric modulator (NAM). GAT-100 behaved as a robust positive allosteric modulator of binding of orthosteric agonist CP55,940. This novel covalent probe can serve as a useful ... |
|
T28838 |
SPM-242
|
SPM 242 |
|
|
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... |
|
T69523 |
BMS-681
|
|
|
|
BMS-681 is an orthosteric antagonist of chemokine receptor 2 (CCR2) that forms a ternary complex with CCR2 and its allosteric antagonist, CCR2-RA-[R]. Together, the complex inhibits chemokine binding with BVMS-681 in the... |
|
T62016 |
CB1R Allosteric modulator 1
|
|
|
|
CB1R Allosteric modulator 1 (compound 11) is a potent allosteric modulator of CB1R. CB1R Allosteric modulator 1 negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs. |
|
T63717 |
CAM833
|
|
|
|
CAM833 is a potent orthosteric inhibitor of the interaction between BRCA2 and RAD51 and also inhibits RAD51 oligomerization and is able to act on the ChimRAD51 protein (Kd: 366 nM). |
|
T62376 |
GNE-9278
|
|
|
|
GNE-9278 is a highly selective NMDAR orthosteric modulator that acts on the GluN1 transmembrane structural domain (TMD).GNE-9278 acts on activated NMDAR and increases peak current and agonist affinity. |
|
T70326 |
Mevidalen HBA
|
|
|
|
Mevidalen, also known as LY3154207, is a novel, potent, and subtype selective human D1 positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50 = 3 nM). In contrast to orthosteric agonists, LY3... |
|
T71179 |
LON63114
|
|
|
|
LON63114, also known as FFA2-Agonist-1 is a selective orthosteric agonist of human FFA2. FFA2-Agonist-1 is potentially useful in the treatment of gastrointestinal disorders and inflammatory bowel diseases. LON63114 was ... |
|
T61180 |
GAT564
|
|
|
|
GAT564 (Compound 15d) is a highly effective allosteric modulator of cannabinoid 1 receptor (CB1R), having EC50 values of 87 nM and 320 nM for cAMP and β-arrestin2, respectively. It significantly enhances the binding of o... |
|
T72744 |
(R)-PF-06256142
|
|
|
|
(R)-PF-06256142, the R enantiomer of PF-06256142, exhibits low activity. PF-06256142 itself is distinguished as a potent and selective orthosteric D1 receptor agonist, with the capability to minimize receptor desensitiza... |
|
T37725 |
Tetrahydrodeoxycorticosterone
|
21-Hydroxypregnanolone,Tetrahydro-11-deoxycorticosterone |
GABA Receptor
|
|
Tetrahydrodeoxycorticosterone(Tetrahydro-11-deoxycorticosterone) is a potent GABAA receptor orthosteric modulator (PAM) with neuroprotective activity that selectively inhibits neurosteroid-mediated enhancement of GABA-in... |
|
T82233 |
HCAR2 agonist 1
|
|
|
|
HCAR2 agonist 1 (Compound 9n), a G i protein-biased allosteric modulator of HCAR2, activates the G i protein signaling pathway and exhibits anti-inflammatory properties by reducing mRNA levels of pro-inflammatory cytokin... |
|
T73272 |
VU6019650
|
|
|
|
VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR ( IC 50 =36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopa... |
|
T83955 |
MOMBA
|
|
|
|
MOMBA is a selective orthosteric agonist specifically targeting engineered human free fatty acid 2 (hFFA2) receptors, particularly those modified as designer receptors activated by designer drugs (DREADD). It demonstrate... |
