PSMA–DA1 may be a useful PSMA-targeting radiotheranostic agent.

Plasma kallikrein-IN-1 is a PKK inhibitor with an IC50 value of 0.5 nM.

MCA17-1 shows stronger bioactivity than the positive control obeticholic acid (OCA) against liver fibrosis.

Nln activator 1 is a first-in-class peptidomimetic neurolysin activator possessing enhanced brain penetration and stability.

RdRP-IN-3 is a promising anti-influenza drug candidate by inhibiting the activity of RNA-dependent RNA polymerase (RdRp).

Kbz probe 1 serves as a versatile probe for interrogating histone benzoylation and interactions in living cells.

Se-DMC attenuates complete Freund’s adjuvant (CFA)-induced inflammatory response, nociception, and neurobehavioral deficits in mice.

Spectinamide-1599 is a combination partner for anti-tuberculosis therapy.

Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.

P2X receptor-1 is a potential inhibitor of P2X receptor for the treatment of pain and inflammation.

TCMDC-125431 is a novel disruptor of the malaria parasite calcium dynamics but minimally inhibits heme crystallization.

TCMDC-136230 is a novel disruptor of the malaria parasite calcium dynamics but minimally inhibits heme crystallization.

TCMDC-125457 is potent in inducing calcium redistribution but minimally inhibits heme crystallization. TCMDC-125457 demonstrated high efficacy when pulsed in a single-dose combination with artesunate against tightly synchronized artemisinin-resistant ring-stage parasites.

PARP1-IN-6 is a dual tubulin/PARP-1 inhibitor with IC50 values of 0.94 and 0.48 μM, respectively.

PARP/EZH2-IN-1 is a first-in-class dual PARP (IC50 6.87 nM) and EZH2 (IC50 36.51 nM) inhibitor for triple-negative breast cancer with wild-type BRCA.

Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP), including PP1 (IC50=15-50 nM), PP2A (IC50=0.1-0.3 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), with a significantly higher affinity for PP2A. Okadaic acid increase of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter.

PTP1B-IN-14 is a selective PTP1B inhibitor (IC50 = 0.72 μM) targeting the allosteric site.

PTP1B-IN-13 is a selective PTP1B inhibitor targeting the allosteric site with an IC50 value of 1.59 μM.

PDE4-IN-3 is a novel and orally active PDE4 inhibitor with potent inhibitory affinity (IC50 = 4.2 nM).

N-Desmethyl Sildenafil (Desmethylsildenafil) is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor.

PI3K-IN-23 is an (E)-9-oxooctadec-10-en-12-ynoic acid analogue to promote glucose uptake with an EC50 value of 7.00 μM.

PI3Kγ inhibitor 5 is an inhibitor of phosphoinositide 3-kinase γ (PI3Kγ) with an IC50 value of 34 nM.

MCX 28, a triple PI3K/mTOR/PIM inhibitor, displays low nanomolar activity.

MNK/PIM-IN-1 represents an innovative dual MNK/PIM inhibitor with a good pharmacokinetic profile.

PLK1-IN-2 is a PLK1 kinase inhibitor with an IC50 value of 0.384 μM.

Propargyl-PEG2-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.

PROTAC CDK9 degrader-4 is a highly potent and efficacious CDK9 degrader for targeting transcription regulation.

MS21, a novel degrader of AKT, selectively inhibits the growth of PI3K/PTEN pathway-mutant cancers with wild-type KRAS and BRAF.

MS4322 is a first-in-class PRMT5 degrader and a valuable chemical tool for exploring the PRMT5 functions in health and disease.