DC46844 |
Emraclidine
Featured
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Emraclidine is a muscarinic M4 receptor positive allosteric modulator (WO2018002760, compound 11). Emraclidine can be used for the research of neurological diseases. |
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DC46845 |
MCL0020 |
MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC50 of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake. |
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DC46846 |
UCM 608 |
UCM 608 is a high affinity melatonin (MT) membrane receptor agonist. The pKi values for MT1 and MT2 are 10.7 and 10.4. |
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DC46847 |
DH97 |
DH97 is a potent and selective antagonist of MT2 melatonin receptor, with a pKi of 8.03 for human MT2. DH97 shows 89- and 229-fold selectivity for human MT2 over human mt1 and Xenopus mel1c receptor subtypes. DH97 can inhibit melatonin-induced enhancement of electrically-evoked responses. |
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DC46848 |
UPF-523 |
UPF-523 (AIDA), a rigid (carboxyphenyl) glycine derivative, is a relatively potent and selective antagonist of group I metabotropic glutamate receptors (mGlu1a) with an IC50 of 214 μM. But UPF-523 has no effect on group II (mGlu2), group III (mGlu4) receptors or ionotropic glutamate receptors. UPF-523 has the potential for the research of the acute arthritis. |
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DC46849 |
L-AP3 |
L-AP3, metabotropic glutamate receptor (mGluR) antagonist, inhibits D-phosphoserine and L-phosphoserine with IC50s of 368 μM and 2087 μM, respectively. |
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DC46850 |
SB 218795
Featured
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SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit. |
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DC46851 |
Imnopitant |
Imnopitant is a NK1 receptor antagonist (WO2020132716, compound 1) . |
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DC46852 |
2-Methylthio-AMP diTEA |
2-Methylthio-AMP (2-MeSAMP) diTEA is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP diTEA is an inhibitor of ADP-dependent platelet aggregation. |
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DC46853 |
BGC-20-1531 free base |
BGC-20-1531 (PGN 1531) free base is a potent and selective prostanoid EP4 receptor antagonist, with a pKb of 7.6. BGC-20-1531 free base has the potential for the research of migraine headache. |
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DC46854 |
BMY-14802 hydrochloride
Featured
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BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects. |
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DC46942 |
CCR4 antagonist 3 hydrochloride |
CCR4 antagonist 3 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity. |
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DC46970 |
L-372662 |
L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR. |
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DC46979 |
Angiopeptin TFA |
Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibit adenylate cyclase or stimulate extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research. |
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DC46980 |
Litorin |
Litorin, an amphibian bombesin peptide derivative, is an bombesin receptor agonist. Litorin stimulates the contraction of smooth muscle, stimulates gastrin, gastric acid, and pancreatic secretion, and suppresses the nutriment in vivo. |
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DC46982 |
Setmelanotide acetate
Featured
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Setmelanotide (RM-493, BIM-22493, CAM 4072) is a cyclic peptide full agonist of melanocortin-4 receptor (MC4R) with an EC50 of 0.27 nM and a Ki of 2.1 nM. |
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DC46996 |
[Leu31,Pro34]-Neuropeptide Y (porcine) |
[Leu31,Pro34]- Neuropeptide Y (porcine), a Neuropeptide Y (NPY) analog, is a selective NPY Y1 receptor agonist. [Leu31,Pro34]- Neuropeptide Y (porcine) exhibits anxiolytic effects. |
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DC47006 |
A2B receptor antagonist 2 |
A2B receptor antagonist 2 (compound 18) is an adenosine receptor A2B antagonist, with Ki values of 2.30 μM, 6.8 μM and 3.44 μM for rA1, rA2A and hA2B, respectively. |
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DC47011 |
Elinzanetant |
Elinzanetant is a neurokinin receptors antagonist used for the research of Schizophrenia. |
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DC47014 |
Medifoxamine |
Medifoxamine is a monoamine re-uptake inhibiting antidepressive drug which preferentially inhibits dopamine reuptake. |
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DC47017 |
Vibozilimod
Featured
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Vibozilimod (example 33) is a S1p1 receptor agonist (extracted from patent WO2012140020A1). |
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DC47044 |
Onzigolide |
Onzigolide (BIM-23A760), a chimeric dopamine-somatostatin compound, shows potent agonist activity at both DA type 2 (D2R) and SST type 2 (SSTR2) receptors. |
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DC47054 |
Trazpiroben |
Trazpiroben (TAK-906) is a dopamine D2/D3 receptor antagonist used for chronic research of moderate-to-severe gastroparesis. |
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DC47056 |
Usmarapride |
Usmarapride (SUVN-D4010) is a selective 5-HT4 receptor ligand with EC50 value 27.5nM, intended for the symptomatic research of Alzheimer's disease and other disorders of memory and cognition like attention deficient hyperactivity, Parkinson's and schizophrenia. |
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DC47057 |
Vazegepant
Featured
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Vazegepant is the first intranasal CGRP receptor antagonist for the study the acute research of migraine. |
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DC47063 |
Enuvaptan |
Enuvaptan is a vasopressin receptor antagonist and has the potential for research into renal and cardiovascular diseases. |
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DC47074 |
Sunobinop |
Sunobinop (S 117957) is a modulator of the opioid receptor-like orphan receptor (ORL1). |
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DC47080 |
Velufenacin
Featured
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Velufenacin is a muscarinic receptor antagonist. |
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DC47089 |
Treprostinil palmitil |
Treprostinil palmitil (TP) is the prodrug of DP1 and EP2 agonist, Treprostinil (UT-15), whose EC50 values were 0.6 and 6.2 nM, respectively. Treprostinil palmitil is a pure prodrug and possesses no inherent binding to G-protein coupled receptors including prostanoid receptors. |
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DC47092 |
Lazuvapagon |
Lazuvapagon is a vasopressin V2 receptor agonist for the research of nocturia. |
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