​​X-376​​ is a highly selective and potent inhibitor of ​​ALK (anaplastic lymphoma kinase) tyrosine kinase​​, demonstrating strong activity with an ​​IC50 of 0.61 nM​​. While it primarily targets ALK, it also exhibits inhibitory effects on ​​MET kinase​​, though with slightly reduced potency (IC50 = 0.69 nM). Due to its robust kinase-blocking properties, X-376 shows significant ​​anti-tumor efficacy​​, making it a promising candidate for cancer research and therapeutic development.

Zilurgisertib fumarate(INCB-000928 fumarate, NBU-928 fumarate) is a selective ALK 2 inhibitor.It is under development for the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.

Ficonalkib is a potent, selective anaplastic lymphoma kinase (ALK) inhibitor for treating an ALK-mediated disease.

Ensartinib (X-396) dihydrochloride is a potent, selective and second-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) with biochemical IC50 of <0.4 nM, inhibits MET with IC50 of 0.74 nM.

Repotrectinib(TPX-005) is a multi-target macrocycle inhibitor of anaplastic lymphoma kinase (ALK), c-ros proto-oncogene 1 receptor tyrosine kinase (ROS1), and neurotrophic tyrosine kinase receptor (TRK)

ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM.

TL13-22 is a negative control for TL13-12 and a potent ALK inhibitor with an IC50 of 0.54 nM. TL13-22 does not degrade ALK in cells.

LDN193189 HCl is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.

J-1048 is an activin receptor-like kinase 5 (ALK5) inhibitor. J-1048 can inhibit TAA-induced liver fibrosis in mice by explicitly blocking the TGF-β/Smad signaling pathway.

TPX-0131 is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). TPX-0131 has strong antitumor activities.

PF-2341066 (Crizotinib) is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nnM, respectivley.

PF06463922 is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.

NVP-TAE684(TAE684) is a highly potent and selective small-molecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM.

CH5424802(AF 802; Alectinib) is a potent ALK inhibitor with IC50 of 1.9 nM, sensitive to L1196M mutation.

TL13-110 is a negative control for TL13-112 and a potent ALK inhibitor with an IC50 of 0.34 nM. TL13-110 does not degrade ALK in cells.

Envonalkib citrate is a potent and orally active inhibitor of ALK, with IC50s of 1.96 nM, 35.1 nM, and 61.3 nM for WT and mutated L1196M and G1269S-ALK. Envonalkib citrate can be used for the research of non-small cell lung cancer.

J-1063 is a potent, selective and orally active ALK5 inhibitor with an IC50 of 0.039 µM. J-1063 shows anti-fibrotic effect by the inhibition of inflammatory infiltration, collagen deposition, and hepatocytes necrosis. J-1063 has the potential for the research of liver fibrosis.

XMU-MP-5 is a new-generation potent and selective ALK inhibitor (IC50=4.15 nM) to overcome crizotinib resistance mutations, including L1196M and G1202R; XMU-MP-5 significantly induced apoptosis in EML4-ALK Ba/F3 cells did not affect apoptosis in wild-type Ba/F3 cells. XMU-MP-5 shows highest binding affinities for ALK and its mutants ALK(C1156Y) and ALK(L1196M), with K d values of 0.57, 0.4, and 0.77 nM, respectively. XMU-MP-5 blocks ALK signaling pathways and inhibits the proliferation of cells harboring either wild-type or mutant EML4-ALK in vitro and suppresses tumor growth in xenograft mouse models in vivo. XMU-MP-5 induces significant regression of lung tumors in two genetically engineered mouse (GEM) models.

THRX-144644 (THRX144644) is a potent, lung-selective ALK5 inhibitor with IC50 of 0.14 nM, inhibits p-SMAD3 in a BEAS2B cell line with IC50 of 23 nM; THRX-144644 displays high selectivity in a broad secondary pharmacology panel with exception of e Lymphocyte CellSpecific Protein-Tyrosine Kinase (LCK, IC50=140 nM). THRX-144644 demonstrated favorable TGFβ pathway pharmacodynamic inhibition in lung while minimizing key systemic toxicities.

MU1700 is a potent, selective ALK1 (ACVRL1) and ALK2 (ACVR1) protein kinase inhibitor with IC50 of 13 and 6 nM, respectively.MU1700 inhibits only ALK1/2/6 and no additional off targets by kinome-wide screening against 369 protein kinases at 1 uM.MU1700 affects phosphorylation of SMAD1/5/8 that corresponds to BMP branch of signalling wchich is mediated also by ALK1/2 kinases.MU1700 is suitable chemical probe for in vivo disease models, and has remarkably high brain penetrance (mice, PO, 1 g/kg).

M4K2234 is a potent, selective ALK1 (ACVRL1) and ALK2 (ACVR1) protein kinase inhibitor with IC50 of 7 and 14 nM, respectively.M4K2234 inhibits only ALK1/2 and one additional off target (TNIK) by kinome-wide screening against 375 protein kinases at 1 uM.M4K2234 demonstrated in cell based target engagement assays with an IC50 of 83nM for ALK1 and 13 nM for ALK2.M4K2234 exhibits only very weak potency against ALK4/5.M4K2234 affects phosphorylation of SMAD1/5/8 that corresponds to BMP branch of signalling which is mediated, besides others, also by ALK1/2 kinases.M4K2234 has only a very weak effect on SMAD2/3 phosphorylation that corresponds to TGF beta branch of signalling which is mediated mostly via ALK4/5/7.

ALK2 R206H inhibitor 23 is a potent and selective inhibitor of Activin Receptor-Like Kinase-2 (ALK2/ACVR1) with IC50 of 8 nM for mutant ALK2 R206H.ALK2 R206H inhibitor 23 displays >15-fold selectivity over ALK1/ALK3, and >100-fold over ALK5/ALK6.

ConB-1 is a potent and selective ALK inhibitor with low toxicity to normal cells.

Iruplinalkib (WX-0593) is a potent, selective, and orally active inhibitor of ALK and ROS1 tyrosine kinase. Iruplinalkib (WX-0593) shows favorable safety and promising antitumor activity in advanced NSCLC with ALK or ROS1 rearrangement.

Zilurgisertib is a selective ALK 2 inhibitor for treating diseases such as cancer.

CEP-28122 is a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers.

CH5424802(AF 802; Alectinib) is a potent ALK inhibitor with IC50 of 1.9 nM, sensitive to L1196M mutation.

KRCA-0008 is a potent Ack1 and anaplastic lymphoma kinase (ALK) dual inhibitor (IC50 values are 4 and 12 nM respectively).

LDN193189 is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively.

ALK-IN-13 is an ALK inhibitor, extracted from patent US20130225528A1, example 19.