DC73449 |
RTI-122 |
RTI-122 (RTI 122) is a highly potent, selective and brain permeable GPR88 agonist with cAMP EC50 of 11 nM (hGPR88 CHO). |
|
DC73450 |
RGH-235 |
RGH-235 is a potent, selective, and orally active H3 receptor antagonist/inverse agonist with high affinity (Ki=3.0-9.2 nM, depending on species), without affinity to H1, H2 or H4 receptors. |
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DC73451 |
UR-MB-69 |
UR-MB-69 is a potent agonist of histamine H2 receptor (H2R) dopamine receptor D3R with pKi of 8.69 and 8.06, respectively. |
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DC73452 |
LY290154 |
LY290154 is a leukotriene LTD4/E4 antagonist. |
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DC73453 |
ACT-1016-0707
Featured
|
ACT-1016-0707 is a potent, selective, and orally active lysophosphatidic acid receptor subtype 1 receptor (LPA1 receptor, LPAR1) antagonist with IC50 of 3.1 nM, highly selective over LPAR2 or LPAR3. |
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DC73454 |
ASP1126 |
ASP1126 is a potent, selective and orally active sphingosine-1-phosphate (S1P) agonist with EC50 of 7.12 and 517 nM for hS1P1 and hS1P3 in GTPgS-binding assays, respectively. |
|
DC73455 |
IMMH002 |
IMMH002 is a potent, selective and orally active S1P1 agonist, IMMH002 can be transformed to IMMH002-P in vivo, IMMH002-P activates S1P1, S1P4, and S1P5 with 12.4, 19.8 and 29.4 nM respectively. |
|
DC73457 |
NXC736 hydrochloride |
NXC736 hydrochloride (SLB736) is a selective functional antagonist for type 4 sphingosine-1-phosphate receptor (S1PR4), has immunomodulatory and anti-fibrotic effects. |
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DC73458 |
SLB1122168 |
SLB1122168 is a potent, specific inhibitor of S1P transporter spinster homologue 2 (Spns2), inhibits Spns2-mediated S1P release with IC50 of 94 nM. |
|
DC73459 |
SLB1122168 hydrochloride |
SLB1122168 hydrochloride is a potent, specific inhibitor of S1P transporter spinster homologue 2 (Spns2), inhibits Spns2-mediated S1P release with IC50 of 94 nM. |
|
DC73460 |
TP0541640 |
TP0541640 (TP 0541640) is a novel potent LPA1 antagonist with IC50 of 1.6 nM, shows potential for the treatment of lung and skin fibrosis. |
|
DC73461 |
UCM-14216 |
UCM-14216 (UCM14216) is a potent and selective antagonist of type 2 lysophosphatidic acid receptor (LPA2) with KD value of 1.3 nM and IC50 of 1.9 uM. |
|
DC73462 |
VU0405645 |
VU0405645 is a potent, biased M1 receptor-positive allosteric modulator, potentiates Ca2+ mobilization in CHO cells stably expressing the M1 receptor with EC50 of 340 nM. |
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DC73463 |
CRN04894
Featured
|
CRN04894 is a highly potent, selective, orally available melanocortin 2 receptor (MC2R antagonist) antagonist with Ki of 2.1 nM. |
|
DC73464 |
SNT-207707 |
SNT-207707 (SNT207707) is a potent, selective, BBB-penetrating, and orally active melanocortin-4 (MC-4) receptor antagonist with binding/fuaction IC50 of 8/5 nM, respectively. |
|
DC73465 |
SNT-207858 |
SNT-207858 (SNT207858) is a potent, selective, BBB-penetrating, and orally active melanocortin-4 (MC-4) receptor antagonist with binding/fuaction IC50 of 22/11 nM, respectively. |
|
DC73466 |
TCMCB07 |
TCMCB07 is a synthetic, cyclic nonapeptide peptide antagonist of the melanocortin-4 receptor (MC4R), ameliorates cancer- and chronic kidney disease-associated cachexia. |
|
DC73467 |
CVN636 |
CVN636 is a potent, selective, CNS penetrant and allosteric agonist of mGluR7 with EC50 of 7 and 2 nM for human and mouse mGluR7, respectively. |
|
DC73468 |
MK-8768 |
MK-8768 (MK8768) is a potent, selective mGluR2 negative allosteric modulator (NAM) with IC50 of 9.6 nM, shows no activity against mGluR 1,3,4,5,6,8. |
|
DC73469 |
ML353
Featured
|
ML353 (VU0478006) is a highly potent, selective, MPEP-site silent allosteric modulator of mGlu5 receptor with with sub-100 nM affinity. |
|
DC73470 |
VU6046980 |
VU6046980 is a potent, selective and in vivo active mGlu7 positive allosteric modulator (PAM) with EC50 of 0.15 uM (rat mGlu7). |
|
DC73471 |
VU0506013 |
VU0506013 is a high-affinity, selective positive allosteric modulator (PAM) of neuropeptide Y4 receptor (Y4R) with EC50 of 125 nM. |
|
DC73472 |
ML301 |
ML301 is a selective full (79-93%) neurotensin-1 (NTR1) receptor agonist with EC50 of 2.0-4.1 uM, good selectivity relative to NTR2 and GPR35. |
|
DC73473 |
AT-039 |
AT-039 is a potent, selective agonist of nociceptin opioid peptide (NOP) receptor, AT-039 is useful for treatment of hypertension and/or volume overload/hyponatraemic states. |
|
DC73474 |
LY2817412 |
LY2817412 is a potent, selective andorally active nociceptin/orphanin FQ (NOP) receptor antagonist with Ki of 0.176 nM, Kb of 0.273 nM in functional assay of receptor-mediated G-protein activation using [35S]-GTPγS binding. |
|
DC73475 |
MP135 |
MP135 is a potent, μ-δ opioid receptor heteromer-selective agonist with EC50 of 0.8 nM in GTPγS assays, shows functional selectivity for μ-δ heteromers over homomeric μOR and δOR and low β-arrestin2 recruitment activity. |
|
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). |
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