9月
Antibacterial agent 141；化合物 Antibacterial agent 141Antibacterial agent 141 (2024/9/14)
簡介：compound b14 (antibacterial agent 141) exhibits antibacterial activity against the plant pathogens xoo, xac, psa, and cmm, with an ec50 value of 1.28 μm. it functions by inhibiting cell membrane formation and altering cell permeability.
IDO1-IN-22；化合物 IDO1-IN-22IDO1-IN-22 (2024/9/14)
簡介：ido1-in-22 (compound 3) is an inhibitor of ido1, demonstrating potent activity with biochemical hido1 ic50 of 67.4 nm and hela hido1 ic50 of 17.6 nm. it exhibits excellent antitumor efficacy in an llc xenograft model and possesses a desirable pharmacokinetic (pk) profile [1].
P-gp inhibitor 13；化合物 P-gp inhibitor 13P-gp inhibitor 13 (2024/9/14)
簡介：p-gp inhibitor 13, a p-glycoprotein antagonist, can counteract paclitaxel resistance in a2780/t cells, proving valuable for advanced acute myeloid leukemia research [1].
DCN-83；化合物 DCN-83DCN-83 (2024/9/14)
簡介：dcn-83, a potent anti-leishmanial compound, exhibits its highest efficacy against the amastigote form, achieving an ic50 value of 0.71 μm. it also possesses the ability to permeate the blood-brain barrier, impacting the central nervous system [1].
Anticancer agent 111；化合物 Anticancer agent 111Anticancer agent 111 (2024/9/14)
簡介：anticancer agent 111 (compound 11), exhibiting anticancer activity, serves as a potent inhibitor of cytochrome p450, particularly targeting cyp3a4 with an inhibitory concentration (ic50) of 3 μm. it is useful in cancer research [1].
AMPA receptor modulator-4；化合物 AMPA receptor modulator-4AMPA receptor modulator-4 (2024/9/14)
簡介：ampa receptor modulator-4, a 3,4-dihydro-2h-1,2,4-benzothiadiazine 1,1-dioxide (btd), serves as an orally active positive allosteric modulator of the ampa receptors (ampar pams). this compound is capable of crossing the blood-brain barrier and has been found to enhance cognitive performance and working memory in mice [1].
Antitumor agent-96；化合物 Antitumor agent-96Antitumor agent-96 (2024/9/14)
簡介："antitumor agent-96 (compound d34) is a potent mre11 inhibitor that down-regulates the homologous recombination (hr) pathway by binding to and suppressing the endonuclease functions of mre11, thereby inducing apoptosis in cm cells [1]."
PK150；化合物PK150PK150 (2024/9/14)
簡介：pk150 shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations.
PB131；化合物 PB131PB131 (2024/9/14)
簡介：pb131, a selective and brain-permeable hdac6 inhibitor, exhibits high binding affinity (ic50: 1.8 nm) and potent anti-inflammatory activity, making it suitable for inflammation research, particularly in neuroinflammation [1].
TRK-IN-23；化合物 TRK-IN-23TRK-IN-23 (2024/9/14)
簡介：trk-in-23 (compound 24b) is a potent, orally active inhibitor of trk with ic50s of 0.5 nm for trka, 9 nm for trkc, 14 nm for trka g595r, 4.4 nm for trka f589l, and 4.8 nm for trka g667c. it induces apoptosis in ba/f3-trkag595r and ba/f3-trkag667c cells [1].
Anti-inflammatory agent 40；化合物 Anti-inflammatory agent 40Anti-inflammatory agent 40 (2024/9/14)
簡介：anti-inflammatory agent 40 is a promising, orally-active compound with anti-malarial and anti-inflammatory properties. it effectively inhibits carrageenan-induced paw swelling in vivo.
Antiparasitic agent-17；化合物 Antiparasitic agent-17Antiparasitic agent-17 (2024/9/14)
簡介：antiparasitic agent-17 (compound 5u), an orally active antiparasitic, demonstrates inhibition against both chloroquine-sensitive (pf3d7) and chloroquine-resistant (pfk1) strains, with ic50 values of 0.96 μm and 1.67 μm, respectively [1].
Mps1-IN-6；化合物 Mps1-IN-6Mps1-IN-6 (2024/9/14)
簡介：mps1-in-6 is a potent mps1 inhibitor that demonstrates antiproliferative and antitumor activities, exhibiting an ic50 of 2.596 nm [1].
Antileishmanial agent-17；化合物 Antileishmanial agent-17Antileishmanial agent-17 (2024/9/14)
簡介：antileishmanial agent-17, a coumarin hybrid, exhibits potent antileishmanial activity (ic50 <0.78 μm) while proving non-toxic to normal vero cells. it specifically interacts with the folate pathway enzymes pteridine reductase and dhfr-ts. efficacy against the promastigote form is highlighted by an ic50 value of 0.40 μm, and against the amastigote form, an ic50 of 0.68 μm, respectively.
Antileishmanial agent-16；化合物 Antileishmanial agent-16Antileishmanial agent-16 (2024/9/14)
簡介：antileishmanial agent-16 (compound 14c), an anti-leishmania agent, exhibits potent activity against leishmania major promastigotes (ic50 = 0.59 μm) and amastigotes (ic50 = 0.81 μm), while maintaining a favorable safety profile in mammalian cells (vero cells) [1].
Antileishmanial agent-15；化合物 Antileishmanial agent-15Antileishmanial agent-15 (2024/9/14)
簡介：antileishmanial agent-15 (compound 13c) exhibits potent activity against l. major promastigotes and amastigotes, demonstrating ic50 values of 0.78 μm for promastigotes and 0.99 μm for amastigotes, while also showing cytotoxicity at these concentrations [1].
SARS-CoV-2-IN-38；化合物 SARS-CoV-2-IN-38SARS-CoV-2-IN-38 (2024/9/14)
簡介：sars-cov-2-in-38, also known as compound 24, is an inhibitor of sars-cov-2 that demonstrates favorable oral bioavailability in mice, with an absorption fraction of 39.75% [1].
FABP4-IN-2；化合物 FABP4-IN-2FABP4-IN-2 (2024/9/14)
簡介：fabp4-in-2 (compd 10g), a selective and orally active fabp4 inhibitor, exhibits k i values of 0.51 μm for fabp4 and 33.01 μm for fabp3, demonstrating its specificity towards fabp4. it is utilized in research investigating inflammatory diseases [1].
BYK204165；化合物BYK204165RT-017290；RT-017290 (2024/9/14)
簡介：byk204165 (rt-017290) is a potent parp inhibitor (parp1; ic50 = 44.67 nm for human recombinant parp1 in an enzyme assay)
ATR-IN-23；化合物 ATR-IN-23ATR-IN-23 (2024/9/14)
簡介：atr-in-23 (compound 34), a potent and selective atr inhibitor, exhibits an ic50 of 1.5 nm, has demonstrated antiproliferative effects on lovo cells, and induces synthetic lethality in ht-29 cells, suggesting its utility in researching dna damage response (ddr)-deficient cancers [1].
Anticancer agent 106；化合物 Anticancer agent 106Anticancer agent 106 (2024/9/14)
簡介：compound 106 (compound 10ic) induces apoptosis in b16-f10 melanoma cells and potently inhibits metastatic nodules in mouse models of lung metastatic melanoma, suggesting its utility in the study of cancer, particularly lung metastatic melanoma [1].
Anticancer agent 105；化合物 Anticancer agent 105Anticancer agent 105 (2024/9/14)
簡介：anticancer agent 105, a thienopyrimidine scaffold-based compound, exhibits selective toxicity towards melanoma and induces apoptosis. additionally, it significantly inhibits metastatic nodules, including in a pulmonary metastatic melanoma mouse model [1], while demonstrating good safety and anticancer properties.
PROTAC BRD3/BRD4-L degrader-2；化合物 PROTAC BRD3/BRD4-L degrader-2PROTAC BRD3/BRD4-L degrader-2 (2024/9/14)
簡介：protac brd3/brd4-l degrader-2, a protac molecule, selectively degrades cellular brd3 and brd4-l with k i values of 16.91 and 2.8 nm, respectively, and exhibits robust antitumor activity in mouse xenograft models, serving as a research tool for cancer [1].
Analgesic agent-2；化合物 Analgesic agent-2Analgesic agent-2 (2024/9/14)
簡介：analgesic agent-2, a selective orally active inhibitor of the nav1.8 channel, demonstrates an ic50 of 50.18 nm in hek293 cells that stably express the human nav1.8 channel, indicating its potential for analgesic activity [1].
hNTS1R agonist-1；化合物 hNTS1R agonist-1hNTS1R agonist-1 (2024/9/14)
簡介：compound 10, an hnts1r agonist-1, acts as a full agonist with a strong affinity for hnts1r (k i: 6.9 nm), showing the ability to cross the blood-brain barrier (bbb). it not only enhances motor function but also improves memory in a mouse model of parkinson´s disease (pd). additionally, this compound is an analog of neurotensin(8-13) and demonstrates neuroprotective properties [1].
SIMR3030；化合物 SIMR3030SIMR3030 (2024/9/14)
簡介：simr3030, a potent inhibitor of sars-cov-2 plpro, possesses an ic50 of 0.0399 μg/ml and demonstrates antiviral activity by diminishing the expression of sars-cov spike, orf1b, ifn-α, and il-6 mrna. additionally, simr3030 has been shown to have a satisfactory safety profile in mice [1].
Antimalarial agent 26；化合物 Antimalarial agent 26Antimalarial agent 26 (2024/9/14)
簡介：antimalarial agent 26, a derivative of 1,4-naphthoquinones, demonstrates antimalarial properties through oral administration. it exhibits cytotoxic effects on p. falciparum while maintaining selectivity against mammalian cell lines and effectively inhibits p. berghei-induced parasitemia in vivo [1].
Antimalarial agent 24；化合物 Antimalarial agent 24Antimalarial agent 24 (2024/9/14)
簡介：compound 24 (compound 7), an in vitro antimalarial agent, demonstrates inhibitory activity against the plasmodium falciparum w2 strain with an ic50 of 0.81 μm and exhibits a cytotoxicity threshold (cc50) exceeding 200 μm in hepg2 cells [1].
HIV-1 protease-IN-8；化合物 HIV-1 protease-IN-8HIV-1 protease-IN-8 (2024/9/14)
簡介：hiv-1 protease-in-8 (compound 34b) is a potent inhibitor of the hiv-1 protease enzyme, exhibiting an ic50 of 0.32 nm. it demonstrates ic50 values of 0.29 μm for the wild-type hiv-1 (hiv-1 nl4-3) and 1.90 μm against a drug-resistant variant (hiv-1 mdr), indicating strong antiviral activity against both strains [1].
Syn-Ake acetate；類蛇毒三肽Dipeptide diaminobutyroyl benzylamide；類蛇毒三肽|||Dipeptide diaminobutyroyl benzyla (2024/9/14)
簡介：syn-ake acetate (dipeptide diaminobutyroyl benzylamide) is a muscarinic acetylcholine receptor antagonist.
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