SB02024 is a novel highly potent, selective, ATP competitive, orally active inhibitor of vacuolar protein sorting 34 (Vps34) with Kd of 1 nM, >1000 times selective towards other PI3K isoenzymes; SB02024 is also highly selective at 1 uM in the DiscoveRx ScanMax panel of 468 kinases; reduces the number of GFP-2xFYVE puncta with IC50 of 14 nM, induces a dose-dependent increase in levels of NCOA4 and p62; blocks autophagy in vitro and reduces xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7; also significantly potentiates cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro.

Cyclizine is a piperazine first-generation antagonist of histamine 1 receptor.

MRS 1845 is a potent calcium channel protein inhibitor and inhibits capacitative Ca2+ influx in HL-60 cells (IC50 = 1.7 mM).

Guanabenz (WY 8678) is an α2 adrenergic receptor agonist that is used as an antihypertensive agent, also has been proposed to exert protective effects against misfolding by interfering with eIF2α-P dephosphorylation through selective disruption of a PP1-P

PI103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (IC50= 2 nM), p110beta (IC50= 3 nM), p110delta (IC50= 3 nM), and p110gamma (IC50= 15 nM), less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.

J14 is a reversible sulfiredoxin inhibitor with an IC50 of 8.1 μM. J14 induces oxidative stress (intracellular ROS accumulation) by inhibiting sulfiredoxin, leading to cytotoxicity and cancer cell death.

The product is discontinued. DDD107498, also known as DDD 498, is a multiple-stage antimalarial agent that inhibits protein synthesis. DDD107498 demonstrates potential to address a variety of clinical needs, including single-dose treatment, transmission blocking and chemoprotection. DDD107498 was developed from a screening programme against blood-stage malaria parasites; its molecular target has been identified as translation elongation factor 2 (eEF2), which is responsible for the GTP-dependent translocation of the ribosome along messenger RNA, and is essential for protein synthesis. This discovery of eEF2 as a viable antimalarial drug target opens up new possibilities for drug discovery.

ML 204 isa blocker of TRPC4 channels (IC50 values are 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively).

ML 792 is a potent, seletive SUMO-activating enzyme (SAE) inhibitor with IC50 of 3 nM and 11 nM for SAE/SUMO1 and SAE/SUMO2, respectively.

ML092 is a covalent and reversible Cruzain inhibitor, with an IC50 of 10 nM.

ML-130 is a potent and selective inhibitor of NOD1; displays 36-fold selectivity for NOD1 over NOD2 (IC50 values are 0.56 and >20 μM for NOD1 and NOD2 respectively).

ML-213 (CID-3111211) is a selective KV7.2 (KCNQ2) and KV7.4 (KCNQ4) channel opener (EC50 values are 230 and 510 nM for KV7.2 and KV7.4 respectively).

ML216(CID-49852229) is a potent inhibitor of the DNA unwinding activity of BLM helicase; showing similar IC50s of 3.0 and 0.97 μM for full length BLM and BLM636–1298 respectively.

ML241 is a potent, selective, and reversible inhibitor of the AAA ATPase p97 (IC50=100 nM). It blocks p97-dependent proteasome substrate with an IC50 of 3500 nM.

ML281 is a potent and selective STK33 inhibitor with IC50 of 14 nM. ML281 showed a 550-fold selectivity over AurB and greater than 700-fold selectivity over PKA.

ML297 (VU0456810) is the First Potent and Selective Activator of the GIRK Potassium Channel, Displays Antiepileptic Properties in Mice.

PT2977 (MK-6482) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. PT2977, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. PT2977 is a potential treatment for clear cell renal cell carcinoma (ccRCC)[1].

ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM

ML355 is a potent and selective inhibitors of 12-Lipoxygenase(12-LOX) with IC50 of 0.34 μM, excellent selectivity over related lipoxygenases and cyclooxygenases, and possess favorable ADME properties.

ML402 is a selective TREK-1 activator.

MLN120B is a potent and effective IKKbeta inhibitor.

MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.

MN-64 is a inhibitor of tankyrases, showed 6 nM potency against tankyrase 1, isoenzyme selectivity, and Wnt signaling inhibition.

Mofezolac is a Highly Selective Cyclooxygenase-1 Inhibitors,Counteracting Inflammatory State both In Vitro and In Vivo Models of Neuroinflammation.

Mollugin is a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway.

Monomethyl auristatin D (MMAD), a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.

MPEP is a potent, highly selective non-competitive antagonist at the mGlu5a receptor subtype (IC50 = 36 nM) while having no agonist or antagonist activities at the mGlu1b receptor at concentrations up to 30 μM.

MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM.

Mps1-IN-2 is a potent Mps1 kianse inhibitor with IC50 value of 145 nM.

MS023 is a potent, selective, and cell-active inhibitor of human type I PRMTs with IC50 of 4-119 nM.