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Search Results for " allosteric "

20

Compounds

Cat No. Product Name Synonyms Targets
T61562 CB1R Allosteric modulator 3 cAMP , Cannabinoid Receptor
CB1R Allosteric modulator 3 is a potent CB1R modulator.CB1R Allosteric modulator 3 inhibits cAMP and β-Arrestin, and can be used for the study of obesity and nicotine addiction.
T5456 WNK-IN-11 Allosteric WNK Kinase Inhibitor Serine/threonin kinase
WNK-IN-11 (Allosteric WNK Kinase Inhibitor) is an allosteric With-No-Lysine (WNK) kinase inhibitor,WNK1(IC50 : 4 nM)
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.
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...
T61371 CB1R Allosteric modulator 4
CB1R Allosteric modulator 4 is an effective and positive modulator of cannabinoid type-1 (CB1R), exhibiting significant biological activity. This compound inhibits the production of cAMP and demonstrates strong β-arresti...
T64096 Integrase-LEDGF/p75 allosteric inhibitor 1
Integrase-LEDGF/p75 allosteric inhibitor 1 is an orally active integrase-LEDGF/p75 (IN-LEDGF/p75) allosteric inhibitor. It inhibits HIV-1 DNA integration and exhibits antiviral effects, acting on the HIV-1 recombinant mo...
T22641 CDPPB GluR
CDPPB is a modulator of mGluR5 positive allosteric(with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5).
T21781 A-286982 Integrin
A 286982 is an inhibitor that blocks the integrin-ligand interaction between leukocyte function-associated antigen-1 (LFA-1) and intercellular adhesion molecule-1.
T3464 PHCCC (-) PHCCC GluR
PHCCC ((-) PHCCC) is a Group I metabotropic glutamate receptor antagonist and a positive allosteric modulator of mGluR4. It also is a potent to antagonism for mGluR2 and mGluR8.
T22703 CYM-5520 CYM 5520 S1P Receptor , LPL Receptor
CYM-5520 is a noncompetitive allosteric agonist of S1P2
T8868 4BP-TQS AChR
4BP-TQS is an allosteric agonist of α7 nAChRs.
T9884 EN523 Others
EN523 targets non-catalytic allosteric cysteine C23 in K48 ubiquitin-specific deuquitinase OTUB1.
T4573 Cyclothiazide GluR
Cyclothiazide is a benzothiadiazide that acts as a potentiator of AMPA receptorsthat potently inhibits AMPA receptor desensitization, positively modulating its response to glutamic acid (EC50 = 3.8 M).
T23515 VU-29 VU 29 GluR
VU-29 is a positive allosteric mGlu5 receptor modulator with EC50=9 nM and Ki=244 nM for rmGluR5. It is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM).
T21747 VU0483605 GluR
VU0483605 is an effective and selective positive allosteric modulator of mGluR1 with EC50s of 390 and 356 nM for human and rat, respectively.
T22027 AH-7614 AH 7614 GPR
AH-7614 (AH 7614) is a selective and potent free fatty acid receptor 4 (FFA4/GPR120) antagonist.
T9238 KI-7 Adenosine Receptor
KI-7 is an adenosine A2B receptor positive allosteric modulator.
T8642 4-CMTB GPR
4-CMTB is a selective agonist of FFA2 and GPR43.It also is a positive allosteric modulator (pEC50=6.38).
T22711 DCB 3,3'-dichlorobenzaldazine Others , GluR
DCB (3,3'-dichlorobenzaldazine) is an allosteric ligand for mGluR5 and shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB). DCB blocks the positive allosteric regulation of mGluRs with the help of ...
T9466 RTICBM-189 Others
RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectivel...
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