Selitrectinib (LOXO-195) is a potent and selective inhibitor of the receptor tyrosine kinases(TRK)( TrkA and TrkC with IC50s of 0.6 and <2.5 nM, respectively)

Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 of 1.01 nM, 5.3 nM, 1.08 nM and 1.26 nM for WT ALK, SRC, ALK L1196M and ALK G1202R, respectively.

Entrectinib (RXDX-101) is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectinib blocks proliferation of ALK-dependent cell lines, including those with C1156Y or L1196M resistance mutations, and inhibits ALK‐dependent signaling. It has been shown to inhibit the growth of a non-small cell lung Y cell line bearing an EML4-ALK rearrangement. In mice bearing various ROS1, Trk, or ALK-driven xenografts, Entrectinib has been shown to induce tumor regression.

CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases. With a cellular IC50s of 4.7 and 1 nM.

ONO-7475 is an inhibitor with high specificity for anexelekto and MER tyrosine kinase

GNF-5837 is a specific, and orally bioavailable pan-TRK inhibitor for TrkA/TrkB (IC50: 8/12 nM).

PF-06273340 is an effective, Selective, and Peripherally Restricted Pan-Trk inhibitor (IC50: Trk-A = 6 nM; Trk-B = 4 nM; Trk-C = 3 nM). PF-06273340 has low metabolic turnover in HLM and hHep is a good substrate for efflux transporters P-gp (ER = 35.7) and BCRP (ER = 4.0) and has moderate passive permeability (RRCK Papp = 5.4 × 10 6 cm s 1).

LM22A-4 is a brain-derived neurotrophic factor (BDNF) mimetic and agonist of the receptor tropomyosin-related kinase B (TrkB; IC50 : 47 nM in a fluorescence anisotropy assay)

GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM.

Altiratinib (DCC-2701)(DCC-2701) is a novel c-MET/TIE-2/VEGFR inhibitor; effectively reduce tumor burden in vivo and block c-MET pTyr(1349)-mediated signaling, cell growth and migration as compared with an HGF antagonist in vitro.

ANA-12 is a potent and selective TrkB antagonist with anxiolytic and antidepressant activity in mice.

LM22B-10 is an activator of TrkB/TrkC neurotrophin receptor and can induce TrkB, TrkC, ERK and AKT activation in vitro and in vivo.

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl.

N-Acetyl-5-hydroxytryptamine (O-Demethylmelatonin) , also known as Normelatonin, is the immediate precursor of melatonin. It is produced from serotonin by the enzyme aralkylamine N-acetyltransferase and is converted to melatonin by acetylserotonin O-methyltransferase. It can potently activate TrkB receptor.

AZ-23 is an inhibitor of ATP-competitive and Trk kinase A/B/C. For TrkA, TrkB, FGFR1, Flt3, Ret, MuSk, Lck, the IC50s values are 2 nM, 8 nM, 24 nM, 52 nM, 55 nM, 84 nM, 99 nM, respectively.

7,8-Dihydroxyflavone (7,8-DHF) is a naturally-occurring flavone and exist in Tridax procumbens, Godmania aesculifolia, and primula tree leaves.

CH7057288 is an effective and selective TRK inhibitor with an IC50 value of 1.1 nM, 7.8 nM and 5.1 nM for TRKA, TRKB and TRKC, respectively.

Belizatinib (TSR-011) is an effective, oral and dual inhibitor of ALK (IC50: 0.7 nM, wild-type recombinant ALK) and TRKA, TRKB, and TRKC.

Larotrectinib sulfate (LOXO-101 sulfate) is an oral active and specific ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).

Tyrphostin AG 879 (AG 879) effectively inhibits HER2/ErbB2 (IC50: 1 μM), 100- and 500-fold higher selective to ErbB2 than EGFR and PDGFR.

DS-1205 is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205 also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205 can inhibit cell migration in vitro and tumor growth in vivo[1].

Amitriptyline hydrochloride (Annoyltin) is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities.

Larotrectinib (LOXO-101) is an orally administered inhibitor of the TRK kinase and is highly selective only for the TRK family of receptors(IC50s = 2-20 nM).