subnanomolar

Copanlisib (BAY 80-6946) is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. By inhibiting the PI3K signaling pathway, Copanlisib may impede tumor cell growth and survival in certain tumor populations. Dysregulated PI3K signaling, often linked to tumorigenesis, may also contribute to tumor resistance to various antineoplastic agents.

TPN171 is potent PDE5 inhibitor with subnanomolar potency for PDE5 and good selectivity over PDE6, which has the potential for the treatment of pulmonary arterial hypertension (PAH). TPN171 was proven to exert a longer lasting effect than sildenafil in animal models, providing a foundation for a once-daily oral administration for its clinical use.

WR99210 hydrochloride is a potent inhibitor of Plasmodium falciparum dihydrofolate reductase (pfDHFR), which is a major malarial drug target. It has subnanomolar potency for the wild type, double mutant and quadruple mutant dihydrofolate reductases.

ACHN-975 TFA is a selective LpxC inhibitor with subnanomolar inhibitory activity against a wide range of gram-negative bacteria, exhibiting low MIC values (≤1 μg mL).

ACHN-975 is a highly potent and selective LpxC inhibitor, demonstrating subnanomolar inhibitory activity. It effectively targets a broad spectrum of gram-negative bacteria, with low minimum inhibitory concentration (MIC) values (≤1 μg mL)[1].

Maytansine (NSC-153858), an ansamycin antibiotic originally isolated from the Ethiopian shrub Maytenus serrata, inhibits the assembly of microtubules by binding to tubulin at the rhizoxin binding site.

Stampidine can prevent the sexual transmission of HIV-1. It exhibited remarkable subnanomolar to low nanomolar in vitro antiretroviral potency against nucleoside reverse transcriptase inhibitor-resistant primary clinical HIV isolates, non-nucleoside RT-re

85548e is used as an inhibitor that exhibiting subnanomolar affinity towards HIV type-1 aspartic proteinase (HIV-1 PR).

Aplaviroc is a human cellular CC chemokine receptor 5 (CCR5) entry inhibitor. Aplaviroc binds specifically to CCR5 and demonstrates potent anti-human immunodeficiency virus activity in vitro in the subnanomolar range. In vitro studies show that aplaviroc

REDX05358 is a highly selective and potent pan RAF inhibitor with a potential therapeutic for BRAF and RAS mutant tumors. REDX05358 has improved therapeutic potential and predicted safety profile. REDX05358 demonstrates subnanomolar binding affinity for B

Potent and selective CLK inhibitor (IC50 values are 28, 88 and 510 nM for CLK4, 1 and 2, respectively). Exhibits no significant activity at CLK3, DYRK, CDK or GSK3 at a concentration of 10 μM. Inhibits growth of a range of cancer cell lines in vitro at subnanomolar concentrations. Walter et al (2018) Molecular structures of cdc2-like kinases in complex with a new inhibitor chemotype. PLoS One 13 e0196761 PMID:29723265

RJ-34, an aristolactam analogue, demonstrates strong antitumor effects across a wide range of cancer cell lines, with subnanomolar GI 50 values (GI 50 <0.1 nM) observed for A431, MES-SA, MES-SA DX5, HCT-15, and HCT-15 CLO2 cells [1].

MRT-92 is a potent and selective Smoothened (Smo) receptor inhibitor. MRT-92 displays subnanomolar antagonist activity against Smo in various Hh cell-based assays. MRT-92 inhibits rodent cerebellar granule cell proliferation induced by Hh pathway activation through pharmacologic (half maximal inhibitory concentration [IC50] = 0.4 nM) or genetic manipulation. Smo is the target of anticancer drugs that bind to a long and narrow cavity in the 7-transmembrane (7TM) domain.

Oxocarbazate, also known as CID23631927, is an inhibitor of human cathepsin L. In the cathepsin L inhibition assay, The oxocarbazate caused a time-dependent 17-fold drop in IC50 from 6.9 nM (no preincubation) to 0.4 nM (4-h preincubation). Slowly reversible inhibition was demonstrated in a dilution assay. CID23631927 demonstrate activity in blocking both SARS-CoV (IC50 = 273 nM) and Ebola virus (IC50 = 193 nM) entry into human embryonic. CID 23631927 was a subnanomolar, slow-binding, reversible inhibitor of human cathepsin L that blocked SARS-CoV and Ebola pseudotype virus entry in human cells. Inhibition of cathepsin L thus holds promise for therapeutic intervention for both SARS-CoV and Ebola virus infection.

OM137 is an inhibitor of Aurora kinases. which is growth inhibitory to cultured cells when applied at high concentration and potentiates the growth inhibitory effects of subnanomolar concentrations of paclitaxel.

CC-90002, a humanized anti-CD47 monoclonal antibody (mAb), demonstrates high affinity for CD47, characterized by a subnanomolar dissociation constant (K d). It is utilized in the research of hematologic malignancies and solid tumors [1] [2].