| DC74756 |
(-)-GSK598809 HCl |
(-)-GSK598809 is an isomer of GSK598809. GSK598809 is a selective D(3)R antagonist recently progressed in Phase I trials. GSK-598809 may decrease the rewarding effects of contextual cues associated with drug intake preclinically, which may reduce drug craving in humans. |
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| DC74757 |
Tirabrutinib free base |
Tirabrutinib, also known as ONO-4059 and GS-4059, is a potent and orally active Bruton agammaglobulinemia tyrosine kinase (BTK) in hibitor. Upon administration, ONO-4059 covalently binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development. As a result, this agent may inhibit the proliferation of B-cell malignancies. BTK, a cytoplasmic tyrosine kinase and member of the Tec family of kinases, plays an important role in B lymphocyte development, activation, signaling, proliferation and survival. |
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| DC74758 |
Rupatadine Fumarate |
Rupatadine Fumarate, also known as Rupatadine, is a second-generation H1-antihistamine with dual affinity for histamine H1 and PAF receptors. Rupatadine is indicated for the treatment of allergic rhinitis and urticaria. |
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| DC74759 |
GSK-1034702 |
GSK-1034702 is a potent M1 receptor allosteric agonist. GSK-1034702, a selective M(1) receptor allosteric agonist, may have therapeutic benefits in disorders of impaired learning including Alzheimer's disease. |
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| DC74760 |
Sonidegib phosphate |
Sonidegib (also known as erismodegib, LDE225, and NVP-LDE225) is an orally bioavailable small-molecule Smoothened (Smo) antagonist with potential antineoplastic activity. Erismodegib selectively binds to the Hedgehog (Hh)-ligand cell surface receptor Smo, which may result in the suppression of the Hh signaling pathway and, so, the inhibition of tumor cells in which this pathway is abnormally activated. It was approved by the FDA for treating basal cell carcinoma in July 2015. |
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| DC74761 |
MPEP HCl |
MPEP is a selective mGluR5 antagonist. MPEP reverses maze learning and PSD-95 deficits in Fmr1 knock-out mice. MPEP elevates accumbal dopamine and glycine levels; interaction with strychnine-sensitive glycine receptors. MPEP activates specific stress-related brain regions and lacks neurotoxic effects of the NMDA receptor antagonist MK-801: significance for the use as anxiolytic/antidepressant drug. |
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| DC74762 |
S1R agonist 2 |
S1R agonist 2 (Compound 8b) is a selective S1R agonist. |
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| DC74763 |
CpCDPK1/TgCDPK1-IN-3 |
CpCDPK1/TgCDPK1-IN-3 (Compound 20) is a CpCDPK1 and TgCDPK1 inhibitor |
|
| DC74765 |
Manidipine HCl |
Manidipine, also known as CV-4093, is a calcium channel blocker (dihydropyridine type) that is used clinically as an antihypertensive. Manidipine is a lipophilic, third-generation dihydropyridine calcium channel antagonist with a high degree of selectivity for the vasculature, thereby inducing marked peripheral vasodilation with negligible cardiodepression. In addition, manidipine does not significantly affect norepinephrine levels, suggesting a lack of sympathetic activation. Manidipine has shown antihypertensive efficacy and appears to be well tolerated in adult and elderly patients with mild or moderate essential hypertension. |
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| DC74766 |
ARTD3/PARP3-IN-1 |
ARTD3/PARP3-IN-1 is an unselective inhibitor of diphtheria toxin-like ADP-ribosyltransferase 3 (ARTD3)/PARP3. |
|
| DC74767 |
NDM-1 inhibitor-3 |
NDM-1 inhibitor-3 (Compound 89) is a New Delhi Metallo-β-lactamase-1 (NDM-1) inhibitor |
|
| DC74768 |
Tosufloxacin tosylate |
Tosufloxacin, also known as T-3262, is a fluoroquinolone antibiotic used to treat susceptible infections. It has a controversial safety profile in relation to other fluoroquinolones. It is associated with severe thrombocytopenia and nephritis, and hepatotoxicity. It is sold in Japan under the brand name Ozex. |
|
| DC74769 |
NSC-87877 free acid |
NSC-87877 is a cell-permeable, inhibitor of both SHP-1 and SHP-2 (IC50 = 355 and 318 nM, respectively). NSC-87877 shows effective growth inhibition and induction of apoptosis in NB cell lines. In an intrarenal mouse model of NB, NSC-87877 treatment results in decreased tumor growth and increased p53 and p38 activity. DUSP26 inhibition with NSC-87877 is an effective strategy to induce NB cell cytotoxicity in vitro and in vivo through activation of the p53 and p38 mitogen-activated protein kinase (MAPK) tumor-suppressor pathways. |
|
| DC74770 |
Tubulin inhibitor 32 |
Tubulin inhibitor 32 is a potent and orally active tubulin inhibitor. |
|
| DC74771 |
Ulipristal acetate |
Ulipristal acetate, also known as CDB-2914, is a selective progesterone receptor modulator (SPRM) approved for contraception, and for uterine fibroid. As a SPRM, ulipristal acetate has partial agonistic as well as antagonistic effects on the progesterone receptor. It also binds to the glucocorticoid receptor, but is only a weak antiglucocorticoid relative to mifepristone, and has no relevant affinity to the estrogen, androgen and mineralocorticoid receptors. |
|
| DC74772 |
SLx-2119 |
SLx-2119, also known as KD-025 and Belumosudil, is an orally bioavailable inhibitor of ROCK-II that is greater than 200-fold selective over ROCK-I (IC50s = 105 nM and 24 µM, respectively). |
|
| DC74773 |
VU0364572 free base |
VU0364572 free base is an orally active and selective allosteric agonist of the M1 muscarinic receptor. |
|
| DC74774 |
SHP099 HCl |
SHP099 is a potent, selective, orally bioavailable, and efficacious SHP2 inhibitor with IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM. SHP099 exhibits dose-dependent pathway inhibition and antitumor activity in xenograft models. SHP2 is a nonreceptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene involved in cell growth and differentiation via the MAPK signaling pathway. SHP2 also purportedly plays an important role in the programmed cell death pathway (PD-1/PD-L1). Because it is an oncoprotein associated with multiple cancer-related diseases, as well as a potential immunomodulator, controlling SHP2 activity is of significant therapeutic interest. |
|
| DC74775 |
VU0364572 TFA |
VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor. |
|
| DC74776 |
HT-61 |
HT-61, also known as HY-50A, is a pyrroloquinolone antibiotic potentially for the treatment of staphylococcal infections. HT61 was effective at reducing biofilm viability and was associated with increased expression of cell wall stress and division proteins, confirming its potential as a treatment for S. aureus biofilm infections. HT61 enhances the effect of tobramycin against Pseudomonas aeruginosa in vitro and in vivo. |
|
| DC74777 |
Ivermectin |
Ivermectin is a medication that is effective against many types of parasites. It is used to treat head lice, scabies, river blindness, strongyloidiasis, and lymphatic filariasis, among others. Ivermectin and other avermectins (insecticides most frequently used in home-use ant baits) are macrocyclic lactones derived from the bacterium Streptomyces avermitilis. Ivermectin kills by interfering with nervous system and muscle function, in particular by enhancing inhibitory neurotransmission. Ivermectin is a mixture of mostly avermectin H2B1a (CAS# 71827-03-7) with some avermectin H2B1b (CAS# 70209-81-3), which are macrolides from STREPTOMYCES avermitilis. |
|
| DC74778 |
LY 43578 |
LY 43578 is an aromatase inhibitor. |
|
| DC74779 |
TASK-1-IN-1 |
TASK-1-IN-1 is a potent and selective TASK-1 inhibitor. |
|
| DC74780 |
Lefamulin free base |
Lefamulin is an antibiotic medication used it to treat adults with community-acquired bacterial pneumonia. It is a pleuromutilin antibiotic that inhibits the large subunit of bacterial ribosomes Lefamulin is used to treat adults with community-acquired bacterial pneumonia. It was also investigated for treatment of acute bacterial skin and skin-structure infections (ABSSSI). Lefamulin has in vitro activity against Streptococcus viridans, Moraxella catarrhalis, Enterococcus faecium, methicillin-resistant Staphylococcus aureus (MRSA), among other bacteria. . Lefamulin was approved in 2019. |
|
| DC74781 |
PDCD4-IN-1 |
PDCD4-IN-1(compound 20031600) is a PDCD4 inhibitor. |
|
| DC74782 |
CDK8-IN-12 |
CDK8-IN-12 is an orally active, potent CDK8 inhibitor. |
|
| DC74783 |
Raxatrigine HCl |
Raxatrigine, also known as vixotrigine, GSK1014802, and CNV1014802, is a small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor. |
|
| DC74784 |
Beloxepin |
Beloxepin, also known as ADL-6906; ORG-4428, is an oral dual selective serotonin and norepinephrine uptake inhibitor. |
|
| DC74785 |
PARP-1-IN-4 |
PARP-1-IN-4 is a PARP-1 inhibitor. |
|
| DC74786 |
Physostigmine salicylate |
Physostigmine salicylate is a reversible cholinesterase inhibitor, a parasympathomimetic alkaloid. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity. |
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