CAS NO. |
Products Name |
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1257213-50-5 |
BMS-986020 |
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BMS-986020 is an LPA1 antagonist. target: LPA1 BMS-986020 is in Phase 2 clinical development for treating idiopathic pulmonary fibrosis. BMS-986020 selectively inhibits the LPA receptor, which is involved in binding of the signaling molecule lysophosphatidic acid, which in turn is involved in a host of diverse biological functions, such as cell proliferation, platelet aggregation, smooth muscle contraction and others |
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865305-30-2 |
AF-353 |
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AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0). IC50 value: pIC50 = 8.0 (pIC50, for P2X3) Target: P2X3/P2X2/3 receptor in vitro: AF-353 is a highly potent inhibitor of α,β-meATP-evoked intracellular calcium flux in cell lines expressing recombinant rat and human P2X3 and human P2X2/3 channels. AF-353 also blocks human P2X2/3 channel function with marginally reduced potency (pIC50 = 7.3). [1] in vivo: SCI rats has significantly higher frequencies for field potentials and NVC than NL rats. Intravesical ATP increases field potential frequency in control but not SCI rats, while systemic AF-353 significantly reduces this parameter in both groups. AF-353 also reduces the inter-contractile interval in control but not in SCI rats; however, the frequency of NVC in SCI rats was significantly reduced.[2 |
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1872382-47-2 |
UNC3866 |
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UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen (IC50=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel. |
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960293-88-3 |
BI605906 |
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BI605906, a novel inhibitor of IKKβ, inhibits IKKβ with an IC50 value of 380 nM when assayed at 0.1 mM ATP. IC50 value: 380 nM Target: IKKβ in vitro: BI605906 is a novel pharmacological inhibitors of the IKK family, inhibits IKKβ with an IC50 value of 380 nM when assayed at 0.1 mM ATP. The only other protein kinase that was inhibited of over 100 tested, which included IKKα and TBK1, was the IGF1 (insulin-like growth factor 1) receptor (IC50=7.6 μM). In IKKα?/? MEFs, BI605906 not only prevents the phosphorylation of physiological substrates, such as p105 and RelA, but also the phosphorylation of the serine residues in IKKβ (Ser177 and Ser181) that trigger its activation. |
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1449598-06-4 |
RO6885247 |
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RG7800 a small molecule SMN2 splicing modifier to enter human clinical trials to treat spinal muscular atrophy. |
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1191911-26-8 |
CZC25146 |
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CZC-25146 is a potent, selective and metabolically stable LRRK2 inhibitor with IC50 of 4.76 nM/6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively. IC50 value: 4.76 nM/6.87 nM(wild type/G2019S LRRK2) [1] Target: LRRK2 CZC-25146displayed a very clean profile, it inhibited only five kinases (PLK4, GAK, TNK1, CAMKK2 and PIP4K2C) with high potency, none of which have been classified as predictors of genotoxicity or hematopoietic toxicity. CZC-25146 neither caused cytotoxicity in human cortical neurons at concentrations below 5 μM over a seven-day treatment in culture nor did it block neuronal development in vitro. CZC-25146 possesses favorable pharmacokinetic properties, such as a volume of distribution of 5.4 L/kg and a clearance of 2.3 L/hr/kg that render it suitable for in-vivo studies |
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357263-13-9 |
BMS378806 |
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BMS-378806 is a potent HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions. BMS-378806 selectively inhibits the binding of HIV-1 gp120 to the CD4 receptor with EC50 of 0.85-26.5 nM in virus. |
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1346546-69-7 |
GSK872 |
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GSK'872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with high affinity (IC50=1.8 nM,), and inhibits kinase activity (IC50=1.3 nM). |
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928134-65-0 |
LCI699 |
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Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase and aldosterone synthase with IC50 values of 2.5 and 0.7 nM, respectively. |
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1262414-04-9 |
Cenerimod |
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Cenerimod (ACT-334441) is a potent and orally available sphingosine 1-phosphate 1 receptor (S1P1) agonist extracted from patent WO 2016184939 A1 and WO 2011007324 A1, example 1, with an EC50 of 2.7 nM. |
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1000025-07-9 |
Vadadustat |
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Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia. |
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