| 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. |
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| 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). |
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| DC74773 |
VU0364572 free base |
VU0364572 free base is an orally active and selective allosteric agonist of the M1 muscarinic receptor. |
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| 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. |
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| DC74775 |
VU0364572 TFA |
VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor. |
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| 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. |
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| 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. |
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| DC74778 |
LY 43578 |
LY 43578 is an aromatase inhibitor. |
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| DC74779 |
TASK-1-IN-1 |
TASK-1-IN-1 is a potent and selective TASK-1 inhibitor. |
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| 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. |
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| DC74781 |
PDCD4-IN-1 |
PDCD4-IN-1(compound 20031600) is a PDCD4 inhibitor. |
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| DC74782 |
CDK8-IN-12 |
CDK8-IN-12 is an orally active, potent CDK8 inhibitor. |
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| 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. |
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| DC74784 |
Beloxepin |
Beloxepin, also known as ADL-6906; ORG-4428, is an oral dual selective serotonin and norepinephrine uptake inhibitor. |
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| DC74785 |
PARP-1-IN-4 |
PARP-1-IN-4 is a PARP-1 inhibitor. |
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| 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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| DC74787 |
LY 235959 new |
LY 235959 is a competitive NMDA receptor antagonist. |
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| DC74788 |
PF-670462 HCl |
PF-670462 is a potent inhibitor of the CK1 isoforms CK1ε and CK1δ (IC50 = 7.7 and 14 nM, respectively), with applications towards treatment of bladder cancer. Inhibition of CKIepsilon yields a perturbation of oscillator function that forestalls light as a zeitgeber, and they demonstrate that pharmacological tools such as PF-670462 may yield valuable insight into clock function. Casein kinase Iepsilon (CKIepsilon) is an essential component of the biological clock, phosphorylating PER proteins, and in doing so regulating their turnover and nuclear entry in oscillator cells of the suprachiasmatic nucleus (SCN). |
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| DC74789 |
CAY10462 HCl |
CAY10462 is the hydrochloride salt of CAY10434 and selective inhibitor of the 20-HETE synthase CYP4A11 exhibiting an IC50 of 8.8 nM when tested in human renal microsomes.4 CAY10434 is nearly 200 times less potent as an inhibitor of 1A, 1C, and 3A CYP450. |
|
| DC74790 |
PROTAC MDM2 Degrader-2 |
PROTAC MDM2 Degrader-2 is a MDM2 degrader based on PROTAC technology. |
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| DC74791 |
Oxantel Pamoate |
Oxantel Pamoate is an anthelmintic used to treat Trichuris trichiura infection. |
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| DC74792 |
KN62 |
KN62 is a P2X7R antagonist (hP2X7 IC50 = 51 nM) and Ca2+/calmodulin-dependent protein kinase II inhibitor. KN62 inhibits the invasiveness of cancer cells in vitro and in vivo KN62 causes retrograde amnesia in the rat. KN62 attenuates glutamate release by inhibiting voltage-dependent Ca(2+)-channels. The effect of KN62 on Ca(2+)-influx appears to be specific to slowly-or non-inactivating conductances, and therefore presents KN62 as a potentially useful tool. |
|
| DC74793 |
PF-5274857 freebase |
PF-5274857 is a potent, orally active and selective hedgehog (Hh) signaling pathway inhibitor with an IC50 of 5.8 nM and a Ki of 4.6 nM. PF-5274857 was found to effectively penetrate the blood-brain barrier and inhibit Smo activity in the brain of primary medulloblastoma mice, resulting in improved animal survival rates. PF-5274857 was orally available and metabolically stable in vivo. PF-5274857 is a potentially attractive clinical candidate for the treatment of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway. |
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| DC74794 |
Otenabant free base |
Otenabant Hydrochloride is the salt of Otenabant, also known as CP-945,598, a drug which acts as a potent and highly selective CB1 antagonist. It was developed by Pfizer for the treatment of obesity, but development for this application has been discontinued following the problems seen during clinical use of the similar drug rimonabant. |
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| DC74795 |
ML-9 HCl |
ML-9 HCl a is myosin light chain kinase (MLCK) inhibitor. ML-9 enhances the anticancer activity of docetaxel, suggesting its potential application as an adjuvant to existing anticancer chemotherapy. The complex effect of ML-9 on autophagy and indentified ML-9 as an attractive tool for targeting autophagy in cancer therapy through dual inhibition of both the Akt pathway and the autophagy. |
|
| DC74796 |
AlPcS4 |
AlPcS4 , also known as aluminum phthalocyanine tetrasulfonate Chloroaluminum tetrasulfophthalocyanine; or AlS4Pc, AlPcS4(a), is a potent photosensitizer, and is potentially useful in cancer sonodynamic therapy and cancer photodynamic therapy. Aluminum phthalocyanine disulfonate is a mixture of regional isomers, in which sulfonate group can be in 3- or 4- position in phenyl ring. Aluminum phthalocyanine disulfonate is also a Coloring Agent; Dermatologic Agent; Fluorescent Dye; Indicators and Reagent; Luminescent Agent; Photosensitizing Agent; Radiation-Sensitizing Agent. |
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| DC74797 |
Etifoxine HCl |
Etifoxine, also known as HOE 36801 and etafenoxine, is an anxiolytic and anticonvulsant drug developed by Hoechst in the 1960s. Unlike benzodiazepines, etifoxine appears to produce its anxiolytic effects by binding to β2 and β3 subunits of the GABAA receptor complex, and so is acting at a different target site to benzodiazepines, although the physiological effect that is produced is similar to that of benzodiazepines. |
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| DC74798 |
JNJ-10191584 |
JNJ-10191584 is a drug which acts as a potent and selective antagonist at the histamine H4 receptor. It has antiinflammatory and analgesic effects in animal studies of acute inflammation. JNJ-10191584 binds with high affinity to the human H4 receptor (Ki = 26 nM). > 540-fold selective over the H3 receptor (Ki = 14.1 μM). |
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| DC74799 |
NSC243928 |
NSC243928 binds to LY6K in cancer cells expressing LY6K, leading to cell death. NSC243928 is an anticancer agent. |
|
| DC74800 |
PXS-5505 HCl |
PXS-5505 is a Pan-Lysyl Oxidase Inhibitor that has been found to ameliorate multiple-organ fibrosis by inhibiting collagen crosslinks in rodent models in systemic sclerosis. PXS-5505 inhibited lysyl oxidase activity in the skin and LOXL2 activity in the lung. PXS-5505 exhibited anti-fibrotic effects in the SSc skin mouse model, reducing dermal thickness and α-smooth muscle actin. Similarly, in the bleomycin-induced mouse lung model, PXS-5505 reduced pulmonary fibrosis toward normal levels, mediated by its ability to normalise collagen/elastin crosslink formation. PXS-5505 also reduced fibrotic extent in models of the ischaemia-reperfusion heart, the unilateral ureteral obstruction kidney, and the CCl4-induced fibrotic liver. |
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