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T2086 |
ELN-441958
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ELN 441958 |
Bradykinin Receptor
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ELN-441958 is a potent, neutral antagonist of B1 receptor, inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM. ELN-441958(ELN 441958) is highly selective for B1 over B2 receptors. |
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T39442 |
AM-8123
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AM-8123 is an APJ agonist with high oral bioavailability and potency. It effectively inhibits Forskolin-stimulated cAMP production and activates Gα proteins. This compound is valuable for cardiovascular disease research. |
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T26863 |
BMS-929075
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BMS 929075,BMS929075 |
HCV Protease
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BMS-929075 is an orally active HCV NS5B replicase (HCV NS5B replicase) palm site variant inhibitor with potency, high oral bioavailability and pharmacokinetic parameters.BMS-929075 shows cytotoxicity. |
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T9692 |
Paltusotine
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Somatostatin
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Paltusotine is a nonpeptide, small molecule somatostatin type 2 (SST2) receptor agonist with high oral bioavailability. Paltusotine maintains GH and IGF-1 levels in acromegaly patients |
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T26690 |
AVN-101
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5-HT Receptor
,
Adrenergic Receptor
,
Histamine Receptor
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AVN-101 is a potent 5-HT7 receptor antagonist. |
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T27374 |
FR-181877
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FR181877,FR 181877 |
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FR-181877, a nonprostanoid PGI2 agonist, inhibits ADP-induced aggregation of human platelets with an IC50 value of 0.081 microM and has high oral bioavailability (56%) with a long half-life (4.3 h) in rats. |
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T74167 |
PCSK9-IN-3
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PCSK9-IN-3 is a next-generation tricyclic peptide inhibitor of PCSK9, characterized by its novel structure, high potency, and oral bioavailability. |
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T70420 |
PHA 543613 hydrochloride
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PHA-543613 hydrochloride acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. It is under developmen... |
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T39787 |
KRH-3955 hydrochloride
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KRH-3955 hydrochloride is a CXCR4 antagonist with oral bioavailability. It effectively inhibits the binding of SDF-1α to CXCR4, exhibiting an IC 50 of 0.61 nM. Additionally, KRH-3955 hydrochloride displays high potency a... |
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T38910 |
MGluR2 antagonist 1
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mGluR2 antagonist 1 is a potent and selective class of negative allosteric modulator targeting the metabotropic glutamate receptor 2 (mGluR2) with high oral bioavailability. It displays a remarkable affinity for mGluR2, ... |
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T78744 |
IRAK4-IN-24
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IRAK
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IRAK4-IN-24 (compound 16), a potent IRAK4 inhibitor, exhibits high clearance (Cl) and low oral bioavailability. It is utilized in research pertaining to inflammatory and autoimmune disorders. |
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T70951 |
ELND006
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ELND006 is a novel gamma secretase inhibitor previously under investigation for the oral treatment of Alzheimer's disease. ELND006 shows poor solubility and has moderate to high permeability. The in vivo performance of t... |
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T14191 |
Alpelisib hydrochloride
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BYL-719 hydrochloride |
Others
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Alpelisib hydrochloride (BYL-719 hydrochloride) exhibits anticancer properties[1][2]. As a potent, selective PI3Kα inhibitor with high oral bioavailability, it demonstrates IC50 values of 5 nM for p110α, 250 nM for p110γ... |
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T61797 |
HIV-1 inhibitor-15
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HIV-1 inhibitor-15 (compound 9d) is a potent and broad-spectrum inhibitor targeting HIV-1. It exhibits inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, and E138K with respective EC50 values of 1.7 nM, 4 nM, 2 n... |
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T71088 |
AM-211 sodium
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AM-211 sodium is a novel and potent antagonist of the prostaglandin D2 receptor type 2. AM-211 is active in animal models of allergic inflammation. AM211 has high affinity for human, mouse, rat, and guinea pig DP2 and it... |
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T69133 |
Etozolin HCl
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Etozolin HCl is a safe and effective diuretic agent in the treatment of acute cardiac failure. In isolated rings of guinea-pig aorta not responding to acetylcholine, the diuretic dexetozoline did not influence basal vasc... |
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T61693 |
AAK1-IN-5
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AAK1-IN-5 is a potent and specific inhibitor of adaptor protein-2-associated kinase 1 (AAK1), characterized by its ability to penetrate the central nervous system and its oral bioavailability. It displays high selectivit... |
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T61753 |
MPT0G211 mesylate
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MPT0G211 mesylate is a powerful and selective HDAC6 inhibitor (IC50 = 0.291 nM), with high oral bioavailability. It exhibits remarkable selectivity for HDAC6 over other HDAC isoforms (>1000-fold selectivity). Additionall... |
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T68547 |
SNJ-1945
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SNJ-1945 is a calpain inhibitor with more favorable retinal penetration, high oral bioavailability, and long half-life. SNJ1945 rescued defective function in lissencephaly. SNJ-1945 protects SH-SY5Y cells against MPP(+) ... |
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T61814 |
JAK3-IN-9
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JAK3-IN-9 is a potent and orally active inhibitor of the Janus kinase 3 (JAK3) enzyme, displaying an impressive IC50 value of 1.7 nM. It exhibits high selectivity towards the JAK3 signaling pathway, making it a valuable ... |
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T39035 |
FXIa-IN-6
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FXIa-IN-6 is a potent FXIa inhibitor with selectivity against most of the relevant serine proteases ( K i = 0.3 nM). FXIa-IN-6 also demonstrated excellent pharmacokinetics (PK) profile (high oral bioavailability and low ... |
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T79833 |
ROCK-IN-9
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ROCK
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ROCK-IN-9 (Compound T345), a ROCK inhibitor, exhibits cytotoxicity in HepG2 cells with an IC50 of 40.8 μM. It demonstrates favorable pharmacokinetic properties in mice, achieving high in vivo exposure and oral bioavailab... |
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T77630 |
EP3 antagonist 4
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Prostaglandin Receptor
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EP3 antagonist 4 is an EP3 antagonist that inhibits hEP with a Ki of 2 nM. EP3 antagonist 4 showed low in vivo clearance, high oral AUC and good bioavailability in complete PK studies in rats. EP3 antagonist 4 can be use... |
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T80787 |
WAY-649123
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WAY-649123 is an active molecule that exhibits (in vitro) antagonistic properties against (alpha-1A adrenergic receptors), with a (pKi) of 8.9. It also demonstrates a 70-fold selectivity over (alpha-1B) and 100-fold sele... |
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T69603 |
BR103354
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BR103354 is a novel fibroblast activation protein (FAP) inhibitor with anti-diabetic and anti-steatotic effects. BR103354 inhibited FAP with an IC50 value of 14 nM, showing high selectivity against dipeptidyl peptidase (... |
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T80789 |
WAY-639872
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WAY-639872 is an active molecule exhibiting (in vivo) efficacy. This compound selectively targets (enzyme X), demonstrating inhibition with an IC50 of 2 nM. Importantly, it possesses a (high level) of specificity, showin... |
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T71252 |
PC-046
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PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4/SMAD4) deficient tumors. PC-046 has growth inhibitory acti... |
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T36308 |
PF-06843195
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PF-06843195 is a selective PI3Kα inhibitor, demonstrating potent activity with an IC50 of 18 nM in Rat1 fibroblasts and Kis for PI3Kα and PI3Kδ less than 0.018 nM and 0.28 nM, respectively, in biochemical kinase assays. ... |
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T35527 |
PI3Kα-IN-4
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PI3Kα-IN-4 |
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PI3Kα-IN-4 is a potent, selective, and orally active PI3Kα inhibitor, demonstrating an IC50 of 1.8 nM and exhibiting antitumor activity[1]. |
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T36084 |
PKI-179
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PKI-179 is a potent, orally active compound that functions as a dual PI3K/mTOR inhibitor. It demonstrates IC50 values of 8 nM for PI3K-α, 24 nM for PI3K-β, 74 nM for PI3K-γ, 77 nM for PI3K-δ, and 0.42 nM for mTOR. Additi... |
