tnk1

Mps1-IN-1 is a potent, selective and ATP-competitive inhibitor of Mps1 kinase (IC50 : 367 nM )

Rolapitant (SCH619734) hydrochloride 是一种高效选择性和具有口服活性的神经激肽 1 (NK1) 受体拮抗剂，Ki 值为 0.66 nM。Rolapitant hydrochloride (Rolapitant HCl) 不与 CYP3A4 产生互作。Rolapitant hydrochloride 在雪貂呕吐模型中显示出强效的中枢介导的止吐活性。

Mps1-IN-1 dihydrochloride 是一种有效的，ATP 竞争性 Mps1激酶抑制剂，IC50为 367 nM。Mps1-IN-1 dihydrochloride 抑制 Mps1有丝分裂激酶活性并沉默纺锤体组装检查点 (SAC) 功能。Mps1-IN-1 dihydrochloride 降低癌细胞和“正常”细胞的活力。

Rolapitant, also known as SCH-619734, is an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy.

Scyliorhinin I 是一种作用于速激肽-1 (NK-1) 及速激肽-2 (NK-2) 受体的激动剂.在大鼠颌下腺NK-1受体上的Ki值达到0.9 nM, 而在仓鼠膀胱NK-2受体上的Ki值为2 nM.此外,Scyliorhinin I 还能有效引起豚鼠回肠纵向肌肉的收缩.

XMD8-92 是 ERK5 (BMK1) BRD4的有效抑制剂，Kd 分别为80和190 nM。它抑制 DCAMKL2、PLK4 和 TNK1的 Kd 分别为190、600和890nm，具有抗癌活性。

TP-5801 是口服具有活力的非受体酪氨酸激酶 (TNK1) 抑制剂，IC50 值为 1.40 nM，具有抗肿瘤作用。

TP-5801 TFA为口服活性非受体酪氨酸激酶（TNK1）抑制剂（IC50=1.40 nM），展现抗肿瘤活性。