| DC70677 |
PAR2 antagonist C391 |
PAR2 antagonist C391 (C391) is a selective PAR2 antagonist, potently inhibits peptidomimetic-induced PAR2 Ca2+ signalling with IC50 of 1.3 uM.C391 blocks both PAR2 Ca2+ and MAPK signalling pathways activated by peptidomimetics and/or proteinase activation.C391 effectively attenuated compound 48/80-induced thermal hyperalgesia in vivo.C391 blocked A. alternata-induced, PAR2-dependent Ca2+ and MAPK signalling in 16HBE14o- cells, as well as β-arrestin recruitment in HEK 293 cells.C391 effectively attenuated A. alternata-induced inflammation, mucus production, mucus cell hyperplasia and airway hyperresponsiveness in acute allergen-challenged murine models. |
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| DC70679 |
PBI-4547 |
PBI-4547 is an agonist of GPR40/120 and an antagonist of GPR84, also is a partial ligand and activator of PPAR.PBI-4547 dose-dependently inhibits GPR84/Gαi2 activation (reflected by an increase in BRET signal) with IC50 of 17 uM, activates GPR40 (EC50 of 102 µM for Gαq and 16 µM for Gαi2) and dose-dependently promoted β-arrestin-2 recruitment to GPR120 (EC50=148 uM).PBI-4547 prevents progression, improves glucose metabolism in a mouse model of NAFLD, restores hepatic glucose and FA metabolism. |
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| DC70686 |
PF-06669571 |
PF-06669571 (PF 6669571) is a novel dopamine D1 receptor (D1R) partial agonist with Ki of 10 nM, demonstrates efficacy in pre-clinical models of Parkinson’s disease symptoms. |
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| DC70713 |
PSB-1584 |
PSB-1584 is a potent, selective agonist of GPR84 with EC50 of 5.0 nM, β-arrestin IC50 of 3.2 nM in human GPR84-expressing cells. |
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| DC70714 |
PSB-16671
Featured
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PSB-16671 is a novel orthosteric and allosteric activator of GPR84, activates human GPR84 with EC50 of 41.3 nM in cAMP accumulation assays.
PSB-16671 is selective versus related fatty acid receptors and the arylhydrocarbon receptor.
PSB-16671 shows an EC50 of 5.47 uM in β-Arrestin assays, and allosteric KB value of 634 nM. |
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| DC70715 |
PSB-17365 |
PSB-17365 is a potent, selective, Gi-biased agonist of GPR84 with EC50 of 2.5 nM, β-arrestin IC50 of 104 nM in human GPR84-expressing cells. |
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| DC70721 |
PZ-1361 |
PZ-1361 is a potent and selective 5-HT7 receptor antagonist with Ki of 33 nM, exhibit significant in vivo antidepressant and pro-cognitive properties in rodents. |
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| DC70726 |
R995045 |
R995045 is a novel δ-opioid receptor (δOR) agonist with pKi of 5.94, cAMP pIC50 of 6.01, >10-fold selectivity over µOR and κOR.R995045 acts as a negative allosteric modulator for leu-enkephalin potency in the cAMP glosensor assay. |
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| DC70745 |
RS-1269 |
RS-1269 is a highly potent, selective CCR4 antagonist, inhibits [125I]CCL17 binding to human CCR4 with IC50 of 27.7 nM.RS-1269 also has strong affinity to displace the CCL17 binding with IC50 of 27.0 nM in CCR4-expressing CHO cells.RS-1269 displays no competitive displacement in the binding of [125I]CCL3 (MIP-1α) to CCR1 and [125I]CCL2 (MCP-1) to CCR2b.RS-1269 dose-dependently inhibited CCL17-induced migration of Th2 cells with IC50 of 5.5 nM.Orally administered RS-1269 (30 mg/kg) ameliorates ovalbumin-induced ear swelling in mice.RS-1269 also inhibited LPS-induced TNF-α production in vivo. |
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| DC70746 |
RS-1748 |
RS-1748 is a highly potent, selective, orallu active CCR4 antagonist, inhibits [125I]CCL17 binding to human CCR4 with IC50 of 59.9 nM.RS-1748 displays no competitive displacement in the binding of [125I]CCL3 (MIP-1α) to CCR1 and [125I]CCL2 (MCP-1) to CCR2b. dose-dependently inhibited 50 nM CCL22-induced [Ca2+]i mobilization with IC50 of 28.3 nM, inhibited the binding of [35S]GTPgS to human CCR4-expressing CHO cells with IC50 of 18.4 nM.Orally administered RS-1748 (30 mg/kg) significantly lowered the total cell numbers and the eosinophils numbers in ovalbumin-sensitized guinea pigs. |
|
| DC70747 |
RTI-7470-44 |
RTI-7470-44 is a potent, selective human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with IC50 of 8.4 nM in vitro cAMP functional assay.RTI-7470-44 exhibits a Ki of 0.3 nM in a radioligand binding assay, and shows species selectivity (>90-fold) for hTAAR1 over the rat and mouse orthologues.RTI-7470-44 displays good blood–brain barrier permeability, moderate metabolic stability, and a favorable preliminary off-target profile.RTI-7470-44 increased the spontaneous firing rate of mouse VTA dopaminergic neurons and blocked the effects of the known TAAR1 agonist RO5166017. |
|
| DC70748 |
RTICBM-229 |
RTICBM-229 is a potent, selective, brain-penetrant CB1 negative allosteric modulator (NAM) with IC50 of 169 nM in Ca2+ assay, 40 nM in GTPγS assay. |
|
| DC70749 |
RTICBM-74 |
RTICBM-74 is a potent, selective, brain-penetrant CB1 negative allosteric modulator (NAM) with IC50 of 23 nM in Ca2+ assays.RTICBM-74 displays excellent half-life and low clearance against rat liver microsomes and hepatocytes, and excellent brain penetrance in rats.RTICBM-74 specifically reduces alcohol intake across a range of doses in male or female Wistar or Long-Evans rats, reduces alcohol intake and does not affect locomotion or sucrose self-administration. |
|
| DC70752 |
S1P5-IN-15
Featured
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S1P5-IN-15 is a potent, selective, orally active and brain-penetrant S1P5 antagonist with IC50 of 0.1 nM, no effect on S1P1-4. |
|
| DC70817 |
SX-682
Featured
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SX-682 (SX682) is a potent, allosteric, orally bioavailable inhibitor of CXCR1 and CXCR2.SX-682 enhances tumor infiltration, activation, and the therapeutic efficacy of adoptively transferred NK cells.SX-682 significantly inhibits trafficking of PMN-MDSCs without altering CXCR2 ligand expression.SX-682 enhances T cell-based immunotherapeutic efficacy. |
|
| DC70823 |
TAK-925
Featured
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TAK-925 (Danavorexton) is a potent, selective, and brain-penetrant Orexin 2 receptor (OX2R) agonist with EC50 of 5.5 nM, no significant inhibition on OX1R (IC50>100 uM).TAK-925 also showed good selectivity against 106 off-target enzymes and receptors. |
|
| DC70825 |
TASP0410461 |
TASP0410461 is a potent, selective histamine H3 receptor antagonist/inverse agonist. |
|
| DC70837 |
TG8-260
Featured
|
TG8-260 is a second-generation, potent, selective EP2 antagonist with Schild KB of 13.2 nM.TG8-260 displays 500-fold selectivity to EP2 against other prostanoid receptors.TG8-260 has a plasma half-life of 2.14 h (PO) and excellent oral bioavailability (77.3%), TG8-260 is a potent inhibitor of CYP450 enzymes.TG8-260 displays antagonistic activity on the induction of EP2 receptor-mediated inflammatory gene expression in microglia BV2-hEP2 cells.TG8-260 reduces hippocampal neuroinflammation and gliosis after pilocarpine-induced status epilepticus in rats.TG8-260 is a tool for investigating anti-inflammatory pathways in peripheral inflammatory disease animal models. |
|
| DC70850 |
TPN672 |
TPN672 (TPN 672) a novel antipsychotic compound with high affinity for serotonin and dopamine receptors 5-HT1AR, (Ki=0.23 nM), 5-HT2AR (Ki=2.58 nM) as well as moderate affinity for D3R (Ki=11.55 nM) and D2R (Ki=17.91 nM).TPN672 acted as a potent 5-HT1AR agonist, D2R/D3R partial agonist, and 5-HT2AR antagonist in vitro functional assays.TPN672 displayed robust antipsychotic efficacy in rodent models (e.g., blocking phencyclidine-induced hyperactivity), significantly better than aripiprazole, and ameliorated negative symptoms and cognitive deficits in the sociability test, dark avoidance response, Morris water maze test, and novel object recognition test. |
|
| DC70852 |
TT-OAD2 hydrochloride |
TT-OAD2 hydrochloride is a potent, selective, non-peptide agonist of glucagon-like peptide-1 (GLP-1) receptor with EC50 of 5 nM.TT-OAD2 inhibited GLP-1- and oxyntomodulin-mediated cAMP, calcium, pERK1/2 and β-arrestin responses in a concentration-dependent manner.TT-OAD2 exhibits biased agonism, and kinetics of G-protein activation and signalling that are distinct from peptide agonists. |
|
| DC70853 |
TT-OAD2 |
TT-OAD2 is a potent, selective, non-peptide agonist of glucagon-like peptide-1 (GLP-1) receptor with EC50 of 5 nM.TT-OAD2 inhibited GLP-1- and oxyntomodulin-mediated cAMP, calcium, pERK1/2 and β-arrestin responses in a concentration-dependent manner.TT-OAD2 exhibits biased agonism, and kinetics of G-protein activation and signalling that are distinct from peptide agonists. |
|
| DC70867 |
Ulotaront |
Ulotaront (SEP-363856, SEP-856) is a novel psychotropic agent with agonism at trace amine receptor 1 (TAAR1) and 5-HT1A receptors but no appreciable action at dopamine D2 receptors.Ulotaront significantly reduced the ketamine-induced increase in dopamine synthesis capacity. |
|
| DC70880 |
V-0219 |
V-0219 is a small molecule positive allosteric modulator (PAM) of GLP-1R with Emax of 60% in the cAMP assay.V-0219 potentiated insulin secretion in INS-1 β-cells with EC50 of 0.25 nM, the best response was observed at 0.1 nM, when a fixed concentration of 0.2 nM of GLP-1 was added to the dose-response curve of 9, the maximal response observed reached a plateau at 0.1 nM, with an EC50 value of 0.008 nM.V-0219 shows a remarkable in vivo activity, reducing food intake and improving glucose handling in normal and diabetic rodents. |
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| DC70881 |
Vercirnon |
Vercirnon (GSK1605786A, CCX282-B) is a potent, selective, orally bioavailable antagonist of CCR9, inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 of 5.4 and 3.4 nM, respectively.Vercirnon (GSK1605786A, CCX282-B) displays high selectivity for CCR9 over CCR1-12 and CX3CR1-7 (IC50>10 uM).Vercirnon (GSK1605786A, CCX282-B) is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.CCX282-B also inhibited mouse and rat CCR9-mediated chemotaxis.Inhibition of CCR9 with CCX282-B results in normalization of Crohn's disease such as histopathology associated with the TNF(ΔARE) mice. |
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| DC70882 |
VISTA inhibitor M351-056 |
VISTA inhibitor M351-056 is a small molecule compound having affinity with VISTA. |
|
| DC70884 |
Vornorexant |
Vornorexant (TS-142, ORN0829) is a potent dual orexin 1 and 2 receptor antagonist with IC50 of 1.05 and 1.27 nM for hOX1R and hOX2R, resepctively.Vornorexant (TS-142, ORN0829) exhibited potent sleep-promoting effects at a po dose of 1 mg/kg in a rat polysomnogram study.Vornorexant (TS-142, ORN0829) is a viable candidate and is currently in clinical development for the treatment of insomnia. |
|
| DC70893 |
VU6007215 |
VU6007215 is a potent, selective M4 positive allosteric modulator (PAM) with EC50 of 144 nM (hM4) and 295 nM (rM4). |
|
| DC70894 |
VU6009048 |
VU6009048 is a potent, selective M4 positive allosteric modulator (PAM) with EC50 of 85 nM (hM4) and 379 nM (rM4). |
|
| DC70895 |
VU6015241 |
VU6015241 (VU 6015241) is a highly potent and selective antagonist of M4 muscarinic acetylcholine receptor (mAChR4) with IC50 of 71 nM.VU6015241 demonstrates selectivity across multiple species, excellent aqueous solubility, and moderate brain exposure in rodents after intraperitoneal administration. |
|
| DC70896 |
VU6019650 |
VU6019650 is a potent, highly selective M5 mAChR orthosteric antagonist with IC50 of 36 nM, >100-fold selectivity against human M1-4.VU6019650 blocked the nonselective muscarinic agonist oxotremorine-M-induced increases in neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area.VU6019650 also inhibited oxycodone self-administration in male Sprague-Dawley rats without impair general motor output. |
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