TAK-659 hydrochloride is a potent, selective and orally available spleen tyrosine kinase (Syk) inhibitor with an IC50 of 3.2 nM.

TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.

TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc.

TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.

TAK-875 is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 0.072 μM.

TAK-901 is a non-selective Aurora kinase inhibitor (IC50s = 3.1, 10, and 4.2 nM for Aurora A, B, and C, respectively).

Talabostat mesilate(PT-100; Val-boroPro) is an orally active, specific inhibitor of dipeptidyl peptidases(IC50=1 nM for DPP4), including tumor-associated fibroblast activation protein.

Tamoxifen(ICI-46474) is an antagonist of the estrogen receptor in breast tissue via its active metabolite, hydroxytamoxifen,showed potent activity against COVID-19(SARS-COV-2) with EC50 MERS-COV(10.117), SARS-COV(11.696).

Tandutinib (MLN518, CT53518) is a potent FLT3 antagonist with IC50 of 0.22 μM, also inhibits PDGFR and c-Kit, 15 to 20-fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR and KDR. Phase 2.

Tanomastat is an angiogenesis and Matrix Metalloproteinase inhibitor

Taranabant is a highly selective cannabinoid-1 (CB1) receptor inverse agonist.

Tariquidar (XR9576) is a potent and selective noncompetitive inhibitor of P-glycoprotein with Kd of 5.1 nM.

Tasisulam sodium is The sodium salt of an acyl-sulfonamide with potential antineoplastic activity.

Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling.

TBA-354 is a potent anti-tuberculosis compound; maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates.

TD139 is a novel high-affinity inhibitor of the galectin-3 carbohydrate binding domain with a Kd of 14 nM.

TD-4208 is a potent and selective inhaled muscarinic antagonist with functional lung selectivity and long duration of action in preclinical models of bronchoconstriction.

TDZD-8 is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM.

Tecovirimat (ST-246, Tpoxx) is a potent, orally bioavailable, first-in-class inhibitor of orthopoxvirus egress with EC50 of 0.01-0.6 uM against a panel of Orthopoxviruses; ST-246 is active against multiple orthopoxviruses, including vaccinia, monkeypox, c

Tegafur (also known as Ftorafur) is a chemotherapeutic 5-FU prodrug used in the treatment of cancers; is a component of tegafur-uracil.

Teglicar, in vitro and in animal models, reduces gluconeogenesis and improves glucose homeostasis, refreshing the interest in selective and reversible L-CPT1 inhibition as a potential antihyperglycemic approach.

Telaprevir (VX-950) is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM.