p 64

CGP 64213 is a GABAb receptor agonist.

CP-642931 (Sorbitol dehydrogenase-IN-1) 是一种具有口服活性和高效性的山梨醇脱氢酶 sorbitol dehydrogenase 抑制剂，可用于研究糖尿病和心血管疾病。

ASP6432 is an antagonist of type 1 lysophosphatidic acid receptor (LPA1). For human LPA1 and rat LPA1, the IC50s are 11 nM and 30 nM , respectively.

CP-640186 是一种有效的乙酰辅酶 A 羧化酶 (ACC)抑制剂，抑制大鼠肝脏 ACC1 和大鼠骨骼肌 ACC2 的 IC50分别为 53 nM 和 61 nM。

MJP6412 作为一种高效的 p300 CBP 降解剂，具有极低的 DC50 值，分别对 p300 和 CBP 为1.6 nM 和 1.2 nM。因其显著效力，MJP6412 在癌症研究领域中扮演关键角色。

UBP646 is a GluN1/GluN2 receptors potentiator.

CGP64222, a peptoid Tat transactivation response element inhibitor, inhibits human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry.

CP-640186 hydrochloride (CP 640186 HCl) 是膜渗透性的乙酰辅酶A 羧化酶（ACC）抑制剂，抑制大鼠肝脏ACC1和大鼠骨骼肌ACC2的IC50为53 nM 和61 nM。

FPL-64170XX is a selective inhibitor of the enzyme 5-lipoxygenase.

CP-64434 hydrate is an antibiotic; anti-proliferative HDAC inhibitor.

RP-64477 是有效的胆固醇酯化酶酰基辅酶 A：胆固醇 O-酰基转移酶 (ACAT) 抑制剂。

Anti-AcmNPV Envelope glycoprotein gp64 AcmNPV-gp64 Antibody (9B642) 是一种靶向AcMNPV AcmNPV Envelope glycoprotein gp64 AcmNPV-gp64 的单克隆抗体，是一种 Mouse IgG1 抗体。

(Trp63,Trp64)-C3a(63-77) 是一种合成的 C3a 类似肽，在人中性粒细胞和表达 hC3aR 或 mC3aR 的 RBL-2H3 细胞中刺激 Ca2+通量，EC50 分别为 9.5、2.0 和 0.8 nM。

Risperidone (R 64 766) 是5-HT2受体阻断剂、P-糖蛋白抑制剂和多巴胺 D2受体的拮抗剂，对 5-HT2A 和多巴胺 D2受体的 Ki 值分别为 4.8 和 5.9 nM。

Antiangiogenic agent 8 (Compound 3m) 是一种抑菌剂，并具有抗血管生成活性。其对E. coli、P. aeruginosa、B. subtilis、S. aureus、C. glabrata的MIC分别为16、8、4、16、8 μg mL，MBC范围为32-64 μg mL。Antiangiogenic agent 8 可能在抗感染和心血管疾病研究中具有应用潜力。

AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains, Ugandan field isolates, and murine P. berghei and P. falciparum infections[1]. AN3661 is active at nanomolar (IC50=20-56 nM) concentrations against P. falciparum laboratory strains known to be sensitive (3D7) or resistant (W2, Dd2, K1, HB3, FCR3 and TM90C2B), and AN3661 is similarly active in ex vivo studies of fresh Ugandan field isolates (mean ex vivo IC50=64 nM). AN3661 shows minimal cytotoxicity against mammalian cell lines, with the CC50 60.5 μM against Jurkat cells, and all other CC50 values greater than the highest concentrations tested (25 μM or above)[1].AN3661 inhibits the stability of P. falciparum transcripts[1]. AN3661 (50-200 mg.kg; p.o.; daily for 4 days) inhibits murine P. berghei infections with ED90 (4 days) 0.34 mg kg[1].AN3661 is administered orally for 4 days, beginning on the third day of infection, the ED90 4 days after initiation of treatment is 0.57 mg kg[1]. Animal Model: P. berghei-infected mice (malaria model)[1] [1]. Sonoiki E, et al. A potent antimalarial benzoxaborole targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue. Nat Commun. 2017;8:14574. Published 2017 Mar 6.

Urotensin II is a peptide vasoconstrictor and agonist of the urotensin (UT) receptor (Ki= 2.06 nM for the human recombinant receptor expressed in HEK293 cells).1It stimulates intracellular calcium mobilization in HEK293 cells expressing human and rat UT (EC50s = 0.47 and 0.78 nM, respectively) but decreases intracellular calcium concentration in goby (G. mirabilis) enterocytes when used at a concentration of 500 nM.2Urotensin II (20 mU/ml) stimulates active sodium and chloride absorption across isolated goby posterior intestine in 5% seawater-adapted solution.3In vivo, urotensin II (1.5-150 nmol/kg) decreases diastolic blood pressure and increases heart rate in anesthetized rats.4It also reduces the pressor responses to sympathetic nerve stimulation, norepinephrine , and vasopressin in pithed rats when administered at a dose of 150 nmol/kg. 1.Ames, R.S., Sarau, H.M., Chambers, J.K., et al.Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14Nature401(6750)282-286(1999) 2.Loretz, C.A., and Assad, J.A.Urotensin II lowers cytoplasmic free calcium concentration in goby enterocytes: Measurements using quin2Gen. Comp. Endocrinol.64(3)355-361(1986) 3.Loretz, C.A., Freel, R.W., and Bern, H.A.Specificity of response of intestinal ion transport systems to a pair of natural peptide hormone analogs: Somatostatin and urotensin IIGen. Comp. Endocrinol.52(2)198-206(1983) 4.Gibson, A., Wallace, P., and Bern, H.A.Cardiovascular effects of urotensin II in anesthetized and pithed ratsGen. Comp. Endocrinol.64(3)435-439(1986)

Leoidin is a depsidone originally isolated from L. gangaleoides that has antibacterial and enzyme inhibitory activities.1,2,3 It is active against the bacteria E. faecalis, H. influenzae, M. catarrhalis, S. aureus, and S. pneumoniae (MICs = 8, 32, 1, 128, and 64 μg ml, respectively).2 Leoidin inhibits phenylalanyl-tRNA synthetase (PheRS) isolated from P. aeruginosa (IC50 = 42 μM). It also inhibits organic anion-transporting polypeptide 1B1 (OATP1B1) and OATP1B3 with Ki values of 0.08 and 1.84 μM, respectively, in CHO cells expressing the human transporters.3

ITH15004 is a non-nucleotide antagonist of the purinergic P2X7receptor (IC50= 9 μM in HEK293 cells expressing the human receptor).1It inhibits ATP-induced currents inX. laevisoocytes expressing the human P2X7receptor when used at a concentration of 100 μM. ITH15004 (1 μM) decreases IL-1β release from LPS-primed, ATP-stimulated isolated mouse peritoneal macrophages. It has high permeability in a parallel artificial membrane permeability assay (PAMPA). 1.Calzaferri, F., Narros-Fernández, P., de Pascual, R., et al.Synthesis and pharmacological evaluation of novel non-nucleotide purine derivatives as P2X7 antagonists for the treatment of neuroinflammationJ. Med. Chem.64(4)2272-2290(2021)

Phenelfamycin E is an antibiotic originally isolated from Streptomyces. It is active against β-hemolytic Streptoccus, S. pneumoniae, C. difficile, C. perfringens, and P. magnus128 μg/ml). Phenelfamycin E (4-64 mg/kg) increases survival in a mouse model of lethal S. pyogenes infection in a dose-dependent manner. Dietary administration of phenelfamycin E increases body weight in chickens.

LpxC-IN-5 is a potent, non-hydroxamate inhibitor of LpxC, which is an enzyme known as UDP-3-O-acyl-N-acetylglucosamine deacetylase. It exhibits an IC50 value of 20 nM. Furthermore, LpxC-IN-5 displays antibacterial activity against various strains including E. coli ATCC25922, P. aeruginosa ATCC27853, K. pneumoniae ATCC13883, and P. aeruginosa 5567. The minimum inhibitory concentration (MIC) values for these strains are 16 μg/mL, 4 μg/mL, 64 μg/mL, and 4 μg/mL, respectively.

Risperidone hydrochloride (R 64 766 hydrochloride) 是一种 5-HT2 受体的阻断剂，P-糖蛋白 (P-Glycoprotein) 的抑制剂和 dopamine D2 受体的拮抗剂，其能够作用于 5-HT2A (Ki: 4.8 nM) 和 dopamine D2 (Ki: 5.9 nM)受体。

Antibacterial agent 128 是一种带有可裂解接头的铁载体类似物-环丙沙星 (Ciprofloxacin (Ciprofloxacin )) 偶联物。Antibacterial agent 128 显示出针对铜绿假单胞菌 (MIC 值为 0.25-64 μg mL) 和类鼻疽伯克氏菌 (MIC 值为 1-32 μg mL) 的抗生素活性。

Antibacterialagent 135（示例7）是一种针对多种细菌具有抑制作用的有效抗菌剂，包括铜绿假单胞菌、鲍曼不动杆菌、大肠杆菌和肺炎克雷伯菌，其最小抑菌浓度（MIC）大于64 μg mL。