9月
Syk-IN-8；化合物 Syk-IN-8Syk-IN-8 (2024/9/14)
簡(jiǎn)介：syk-in-8 (compound 19q) functions as a syk inhibitor with demonstrated antiproliferative effects on a variety of hematological tumor cells. it specifically inhibits plcγ2 phosphorylation and is applicable for blood cancer research [1].
DprE1-IN-7；化合物 DprE1-IN-7DprE1-IN-7 (2024/9/14)
簡(jiǎn)介：dpre1-in-7 (compound 64) is a dpre1 inhibitor with potent anti-tuberculosis (tb) activity, demonstrating a minimum inhibitory concentration (mic) of 1 μm against the mtb h37rv strain. it exhibits antimycobacterial effects on drug-resistant strains. additionally, dpre1-in-7 shows high microsomal stability and exhibits medium clearance [1].
DprE1-IN-6；化合物 DprE1-IN-6DprE1-IN-6 (2024/9/14)
簡(jiǎn)介：dpre1-in-6 (compound 56) is a dpre1 inhibitor with demonstrated anti-tb activity, exhibiting a minimum inhibitory concentration (mic) of 1 μm against the mtb h37rv strain, along with efficacy against drug-resistant mycobacterial strains. moreover, it possesses high microsomal stability and medium clearance [1].
DprE1-IN-5；化合物 DprE1-IN-5DprE1-IN-5 (2024/9/14)
簡(jiǎn)介：dpre1-in-5 (compound 10), a potent dpre1 inhibitor, exhibits anti-tb activity with an mic of 4 μm against the mtb h37rv strain and demonstrates antimycobacterial efficacy against drug-resistant strains. additionally, it possesses high microsomal stability [1].
VPS34 inhibitor 1 (Compound 19, PIK-III analogue)；化合物VPS34PIK-III analogue；PIK-III analogue (2024/9/14)
簡(jiǎn)介：vps34 inhibitor 1 (compound 19, pik-iii analogue) (pik-iii analogue) is a potent and selective inhibitor of vps34( ic50 : 15 nm)
c-Myc inhibitor 12；化合物 c-Myc inhibitor 12c-Myc inhibitor 12 (2024/9/14)
簡(jiǎn)介：compound 67h, also known as c-myc inhibitor 12, is a potent inhibitor of c-myc, exhibiting a pec50 value of 6.4 [1].
c-Myc inhibitor 11；化合物 c-Myc inhibitor 11c-Myc inhibitor 11 (2024/9/14)
簡(jiǎn)介：c-myc inhibitor 11 (compound 67e), a c-myc inhibitor (p ec 50 : 6.4), exhibits high clearance, a moderate volume of distribution, and a short half-life in rat pharmacokinetic assays, making it suitable for cancer research [1].
NAMPT degrader-3；化合物 NAMPT degrader-3NAMPT degrader-3 (2024/9/14)
簡(jiǎn)介：nampt degrader-3 (compound c5) is a nampt degrader that functions through a vhl- and proteasome-dependent mechanism. it exhibits cytotoxic properties and inhibits the proliferation of a2780 cells [1].
AHR agonist 4；化合物 AHR agonist 4AHR agonist 4 (2024/9/14)
簡(jiǎn)介：ahr agonist 4 (compound 24e), as an aryl hydrocarbon receptor (ahr) agonist, modulates the immune equilibrium between th17/22 and treg cells. it is a lead compound under investigation for anti-psoriasis drugs and demonstrates efficacy in mitigating imiquimod (imq)-induced psoriasis-like skin lesions [1].
Metallo-β-lactamase-IN-11；化合物 Metallo-β-lactamase-IN-11Metallo-β-lactamase-IN-11 (2024/9/14)
簡(jiǎn)介：metallo-β-lactamase-in-11 (compound 5f), a potent inhibitor of metallo-β-lactamases (mbls), demonstrates efficacy against the bacterial metallophyllactamase cpha with an ic50 value of 45 ?m. at a concentration of 10 ?m, metallo-β-lactamase-in-11 inhibits ndm-1 by 49% and aim-1 by 61%, indicating its potential application in research focused on countering antibiotic resistance [1].
Antitumor agent-103；化合物 Antitumor agent-103Antitumor agent-103 (2024/9/14)
簡(jiǎn)介：antitumor agent-103 (compound 24l) induces apoptosis and possesses antiproliferative and anti-colony formation properties. this compound halts the cell cycle at the g0/g1 phase, augments nitric oxide (no) production, and demonstrates anti-tumor efficacy [1].
AKR1C3-IN-10；化合物 AKR1C3-IN-10AKR1C3-IN-10 (2024/9/14)
簡(jiǎn)介：akr1c3-in-10 (compound 5r), a selective inhibitor of akr1c3 with an ic50 of 51 nm, demonstrates efficacy in a prostate cancer xenograft model [1].
NXT-10796；化合物 NXT-10796NXT-10796 (2024/9/14)
簡(jiǎn)介：nxt-10796 is an orally active, intestinally restricted agonist of the ep4 receptor [1].
Mu opioid receptor antagonist 7；化合物 Mu opioid receptor antagonist 7Mu opioid receptor antagonist 7 (2024/9/14)
簡(jiǎn)介：compound 24, also known as mu opioid receptor antagonist 7, is a potent, centrally-acting ?-opioid receptor (?or) antagonist with an inhibitory concentration (ic50) of 29 ± 3.0 nm. it is valuable for pain and opioid use disorder research [1].
μ opioid receptor agonist 3；化合物 μ opioid receptor agonist 3μ opioid receptor agonist 3 (2024/9/14)
簡(jiǎn)介：compound 20, identified as μ opioid receptor agonist 3, is a potent ?or agonist that exhibits an ec50 value of 0.87 nm. it holds promise for research into pain management and neuropsychiatric disorders [1].
Fluphenazine decanoate；癸氟奮乃靜Fluphenazine decanoate (2024/9/14)
簡(jiǎn)介：fluphenazine decanoate is dopamine d2 receptor blocke,and is a long-acting phenothiazine neuroleptic that used to treat schizophrenia.
Tubulin polymerization-IN-50；化合物 Tubulin polymerization-IN-50Tubulin polymerization-IN-50 (2024/9/14)
簡(jiǎn)介：tubulin polymerization-in-50 (compound 7n) serves as an inhibitor of tubulin polymerization, exhibiting an ic50 of 5.05 μm in sk-mel-28 cells and inducing cell cycle arrest at the g2/m phase [1].
AF-2112；化合物 AF-2112AF-2112 (2024/9/14)
簡(jiǎn)介：af-2112, a tead inhibitor derived from flufenamic acid, significantly diminishes the expression of ctgf, cyr61, axl, and nf2.
LM-41；化合物 LM-41LM-41 (2024/9/14)
簡(jiǎn)介：lm-41, a flufenamic acid-derived tead inhibitor, significantly reduces the expression of ctgf, cyr61, axl, and nf2, and inhibits the migration of human mda-mb-231 breast cancer cells [1].
SARS-CoV-2-IN-61；化合物 SARS-CoV-2-IN-61SARS-CoV-2-IN-61 (2024/9/14)
簡(jiǎn)介：sars-cov-2-in-61 (compound 8i) is a potent inhibitor of the sars-cov-2 plpro, exhibiting an ic50 of 16 ?m and demonstrating antiviral activities [1].
TGR5 agonist 4；化合物 TGR5 agonist 4TGR5 agonist 4 (2024/9/14)
簡(jiǎn)介：tgr5 agonist 4 (compound 19), a derivative of cholic acid, selectively activates the tgr5 receptor with an effective concentration (ec50) of 4 μm [1].
TGR5 agonist 3；化合物 TGR5 agonist 3TGR5 agonist 3 (2024/9/14)
簡(jiǎn)介：compound 8, a cholic acid derivative, functions as a selective tgr5 agonist and exhibits an ec50 value of 5 μm [1].
BuChE-IN-9；化合物 BuChE-IN-9BuChE-IN-9 (2024/9/14)
簡(jiǎn)介：buche-in-9 (compound 22a), an eqbuche (equine serum-derived butyrylcholinesterase) inhibitor, exhibits potent activity with an ic50 of 173 nm. in addition to eqbuche, it also inhibits human bace1, aβ aggregation, and mouse gaba transporters 1 and 4 (mgat1 and mgat4). notably, buche-in-9 demonstrates significant antiamnesic properties [1].
BuChE-IN-8；化合物 BuChE-IN-8BuChE-IN-8 (2024/9/14)
簡(jiǎn)介：buche-in-8 (compound 19c), a butyrylcholinesterase (buche) inhibitor, exhibits an ic50 value of 559 nm and concurrently inhibits human β-secretase (bace1) and aβ40 aggregation. it also demonstrates notable antiamnesic properties [1].
DCLK1-IN-2；化合物 DCLK1-IN-2DCLK1-IN-2 (2024/9/14)
簡(jiǎn)介：dclk1-in-2 (compound i-5) is a potent inhibitor of dclk1, exhibiting an ic50 of 171.3 nm, and demonstrates significant antiproliferative effects on sw1990 cell lines with an ic50 of 0.6 μm, as well as in vivo antitumor potency [1].
FLT3-IN-22；化合物 FLT3-IN-22FLT3-IN-22 (2024/9/14)
簡(jiǎn)介：flt3-in-22 (compound 22f) is a potent inhibitor of flt3, demonstrating ic50 values of 0.941 nm for flt3 and 0.199 nm for the flt3/d835y mutant. this compound displays significant antiproliferative effects against mv4-11 cells and ba/f3 cell lines expressing mutant flt kinase variants, such as flt-d835y and flt3-f691l [1].
Tranylcypromine hemisulfate；反苯環(huán)丙胺半硫酸鹽Tranylcypromine Sulfate|||Tranylcypromine (hemisulfate)；Tranylc (2024/9/14)
簡(jiǎn)介：tranylcypromine hemisulfate (tranylcypromine sulfate) is an inhibitor of monoamine oxidase (mao) and lysine-specific demethylase 1 (lsd1) with a rapid onset of activity.
Antileishmanial agent-24；化合物 Antileishmanial agent-24Antileishmanial agent-24 (2024/9/14)
簡(jiǎn)介：antileishmanial agent-24 (compound 33) exhibits antileishmanial activity, demonstrating an inhibitory concentration 50 (ic50) value of 5.39 μm against amastigotes [1].
BLT2 antagonist-1；化合物 BLT2 antagonist-1BLT2 antagonist-1 (2024/9/14)
簡(jiǎn)介：blt2 antagonist-1 (compound 15b) is a selective inhibitor of the blt2 receptor, impeding the chemotaxis of cho-blt2 cells at an ic50 of 224 nm, while not affecting cho-blt1 cell chemotaxis. it blocks the interaction between ltb4 and the blt2 receptor with a k_i of 132 nm and may serve as a research tool for inflammatory airway diseases, including asthma and chronic obstructive pulmonary disease [1].
PITB；化合物 PITBPITB (2024/9/14)
簡(jiǎn)介：pitb, a selective and orally active transthyretin (ttr) aggregation inhibitor, is utilized in transthyretin amyloidosis (attr) disease research [1].
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