| DC73476 |
Naltrexone hydrochloride |
A potent, competitive antagonist for μ, κ, δ, and σ-opioid receptors with Ki of 0.0825 nM, 0.509 nM, and 8.02 nM, for MOR, KOR, and DOR, respectively. |
|
| DC73477 |
PIPE-3297 |
PIPE-3297 is a fully efficacious and selective kappa opioid receptor (KOR) agonist with functional GTPγS EC50 of 1.1 nM, Emax=91%, does not elicit β-arrestin-2 recruitment functional response. |
|
| DC73478 |
PN6047 |
PN6047 is an orally bioavailable, G protein-biased and selective δ opioid agonist with pKi of 7.25, fully engages G protein signaling but is a partial agonist in both the arrestin recruitment and internalization assays. |
|
| DC73479 |
ZYKR1 |
ZYKR1 is a potent, and peripherally restricted kappa opioid receptor (KOR)-selective agonist with EC50 of 0.061 nM in cAMP assays, highly selective over the mu and delta opioid receptors (EC50>10 μM). |
|
| DC73480 |
(R)-YNT-3708 |
(R)-YNT-3708 is a potent, selective orexin 1 receptor (OX1R) agonist with EC50 of 7.48 nM and Emax 101%, 22-fold selectivity over OX2R (IC50=168 nM). |
|
| DC73481 |
CVN45502 |
CVN45502 (CVN 45502) is a potent, orally bioavailable, highly selective orexin 1 receptor (Hcrtr1, OX1R) antagonist with binding affinity (pKi) of 7.86 (human Hcrtr1), significantly reduces feeding and body weight in diet-induced obese (DIO). |
|
| DC73482 |
CVN766
Featured
|
CVN766 (CVN 766) is a potent, exquisitely selective orexin 1 receptor (OX1R) antagonist with IC50 of 8 nM, 1000-fold selective over OX2R. |
|
| DC73483 |
OBPt-9 |
OBPt-9 is a potent, postivie allosteric potentiator of orexin receptor-mediated signaling, similarly potentiates the response of OXR1 and OXR2 to orexin A. |
|
| DC73484 |
MRS4833 |
MRS4833 is a potent, selective antagonist of Gi protein-coupled P2Y14 receptor (P2Y14R, GPR105) with IC50 of 5.9 nM, Ki of 3.44 nM (human P2Y14R). |
|
| DC73485 |
MRS4853 |
MRS4853 is a selective P2Y6 receptor (P2Y6R) antagonist with IC50 of 0.46 uM (hP2Y6R), displays weak affinity for mP2Y6R (IC50=6.15 uM). |
|
| DC73486 |
ACT-774312 |
ACT-774312 (ACT774312) is a potent and selective CRTH2 receptor antagonist with IC50 of 3 nM, 150-fold more potent than setipiprant in inhibiting PGD2-induced eosinophil cell shape change. |
|
| DC73487 |
AGN 225660 |
AGN 225660 is a second-generation prostanoid receptor antagonist acting at multiple receptor subtypes with IC50 of 220/70/2900/7100/70/180/1100/5 nM for DP1/EP1/EP2/EP3/EP4/FP/IP/TP receptors, respectively. |
|
| DC73488 |
AMX12006 |
AMX12006 (AMX-12006) is a potent, selective, orally active antagonist of prostaglandin E2 (PGE2) receptor 4 (EP4) with IC50 of 4.3 nM in cAMP assays, shows no activity against EP1, EP2, EP3 receptors. |
|
| DC73489 |
CR6086 sodium |
CR6086 sodium (CR-6086) is a potent, selective prostaglandin E2 receptor 4 (EP4) antagonist with Ki of 16.6 nM (hEP4 receptor), inhibits PGE2-stimulated cAMP production with IC50 of 22 nM. |
|
| DC73490 |
L001 |
L001 is a potent and selective EP4 antagonist with cAMP IC50 of 7.29 nM, impairs pancreatic cancer migration and invasion. |
|
| DC73491 |
LY3127760 |
LY3127760 is a potent, selective prostaglandin E4 (EP4) receptor antagonist with binding Ki of 58 nM (hEP4) and cAMP IC50 of 5.6 nM. |
|
| DC73492 |
ONO-4578 |
ONO-4578 (BMS-986310) is a potent, highly selective EP4 antagonist, potently inhibits the PGE2-induced cAMP production in CHO cells expressing mouse and human EP4 receptors with single-digit nM IC50. |
|
| DC73493 |
TG11-77 |
TG11-77 is a potent, selective, brain-permeable and orally available antagonist of the prostaglandin E2 (PGE2) receptor subtype EP2 with KB value of 9.7 nM. |
|
| DC73495 |
1-Piperidine Propionic Acid |
1-Piperidine Propionic Acid (1-PPA) is an allosteric Inhibitor of protease activated receptor-2 (PAR2) with IC50 of 2.3 uM. |
|
| DC73496 |
NRD-21 |
NRD-21 is a potent, selective, reversible, negative allosteric modulator of PAR1 with IC50 of 0.37 uM in calcium mobilization assays. |
|
| DC73497 |
TFLLRN-NH2 |
TFLLRN-NH2 is a potent, PAR1-selective agonist peptide with EC50 of 1.9 uM. |
|
| DC73498 |
Ogremorphin
Featured
|
Ogremorphin (OGM, OGM8345) represents a pioneering small-molecule inhibitor that selectively targets GPR68, demonstrating high specificity with an IC50 value of 0.71 µM. As a first-in-class compound, it offers unique therapeutic potential by precisely modulating GPR68 activity.
|
|
| DC73499 |
Ogremorphin-1 |
Ogremorphin-1 (OGM1) is a highly specific, first-in-class small-molecule inhibitor of GPR68 with IC50 of 0.16 uM. |
|
| DC73500 |
DC591053 |
DC591053 (DC 591053) is a selective small molecule agonist of relaxin family peptide receptor 4 (RXFP4) with pEC50 of 7.24 and pKi of 6.95, shows no activity against RXFP3. |
|
| DC73501 |
AZ-66 |
AZ-66 is a highly potent S1R/S2R antagonist with Ki of 0.31/1.76 nM, respectively. |
|
| DC73502 |
CM-304 |
CM-304 is a potent, selective sigma-1 receptor (S1R) antagonist with Ki of 3.41 nM, 100-fold selective over S2R. |
|
| DC73503 |
GM310 |
GM310 is a small molecule inhibitor of glycolysis, proteotoxicity, inflammation, and impairments in animal models of Alzheime's, Huntington's, and stroke by activation of the Sigma-1 receptor. |
|
| DC73504 |
JR1-157
Featured
|
JR1-157 is a potent selective sigma 2 receptor (σ2R) ligand with Ki value of 47 nM, >10-fold selectivity over σ1R. |
|
| DC73505 |
MAM03055A |
MAM03055A is a novel bivalent sigma-2 receptor/TMEM97 ligand with cytotoxic activity, exhibits high affinity and strong preference for sigma-2 receptor with Ki of 55.9 nM. |
|
| DC73506 |
RC-752 |
RC-752 is a potent, seletive sigma-1 receptor (S1R) antagonist with Ki of 6.2 nM, 50-fold selective over S2R, shows antinociceptive activity. |
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