Angiogenesis

Vorapaxar是一种具有口服活性、选择性和竞争性的凝血酶受体蛋白酶激活受体 (PAR-1) 拮抗剂，K d 值为1.27±0.3nM，K i 值随血浆浓度升高而升高，100%血浆时达到39.2nM。

A potent inhibitor of tubulin polymerization

TCS 2314 (compound 3) 是具有口服活性和选择性的甚晚期抗原 4 (VLA-4, α4β1, CD49d/CD29) 拮抗剂，IC50 为 4.4 nM。

A PAR2 antagonist

An inhibitor of HIF-1-mediated gene transcription

A dual inhibitor of MMP-2 and MMP-9

MMP-8 Inhibitor I是一种强效的基质金属蛋白酶-8（MMP-8）抑制剂，但口服生物利用度较低。

BMS 986120是一种专门针对蛋白酶激活受体4（PAR4）的化合物，在体外实验中，其对人和猴的血液中由PAR4选择性激活肽（PAR4-AP）诱导的血小板聚集（PA）具有相当的抑制作用（人和猴的半数抑制浓度IC 50 分别为9.5±2.7和2.1±0.4nM）。

An angiogenesis inhibitor with anticancer activity

A BTK inhibitor

GLPG0187是一种广谱整合素（integrin）受体拮抗剂，对多种整合素受体表现出选择性，其IC 50 值如下：α V β 1 为1.3nM，α V β 3 为3.7nM，α V β 5 为2.0nM，α V β 6 为1.4nM，α V β 8 为1.2nM，α 5 β 1 为7.7nM。

An inhibitor of the LFA-1/ICAM-1 interaction

A HIF-PH1, -2, and -3 inhibitor

A BTK inhibitor

Cyclo(RADfK)是选择性α(v)β(3)整合素配体,广泛用于新血管生成的研究,治疗和诊断。

PCI-33380是布鲁顿酪氨酸激酶(BTK)的不可逆抑制剂(荧光探针)。

Gly-Arg-Gly-Asp-Ser是一种五肽，构成了糖蛋白，骨桥蛋白与细胞的结合域。

Glucosamine (2-amino-2-deoxy-D-glucose) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids. It is commonly used as a treatment for osteoarthritis. Glucosamine（GS） treatment selectively downregulates HIF-1α at the protein level in YD-8 cells via interference of production of the citric acid cycle metabolites.

Dencichin是一种最初从三七中提取的非蛋白质氨基酸，可以抑制HIF-脯氨酰羟化酶2（PHD-2）的活性。

PRN1008 (Rilzabrutinib) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.

HIF-2α-IN-1是一种HIF-2α抑制剂,IC50值小于500nM。

A pan HIF-PH inhibitor

Nemtabrutinib (ARQ 531, MK-1026) is an ATP-competitive tyrosine kinase inhibitor designed to target BTK with an IC50 of 0.85 nM. It also has a distinct kinase selectivity profile with strong inhibitory activity against several key oncogenic drivers from TEC, Trk and Src family kinases.

A BTK inhibitor