WRW4 TFA, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC50 of 0.23 μM. WRW4 TFA specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide.

SW2_110A is a selective chromobox 8 chromodomain (CBX8 ChD) inhibitor with a Kd of 800 nM. SW2_110A shows minimal 5-fold selectivity for CBX8 ChD over all other CBX paralogs in vitro.

Golotimod TFA (SCV 07 TFA), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod TFA (SCV 07 TFA) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod TFA (SCV 07 TFA) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).

Pomalidomide-PEG2-Tos is an E3 ligase ligand-linker conjugates, composed of a cereblon ligand and two-unit PEG linker.

MGS0274, an ester-based lipophilic prodrug of a metabotropic glutamate (mGlu)2 and mGlu3 receptor agonist MGS0008, shows improved oral bioavailability. MGS0274 has the potential for the research of schizophrenia.

Cariprazine D6 (RGH-188 D6) is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM).

ZEN-3411 is a BET inhibitor with IC50s of 0.05, 0.05 and 0.06 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3411 can be used to form PROTACs to induce degradation of BRD4.

CDK7-IN-2 hydrochloride hydrate (Example 6) is a potent and selective CDK7 inhibitor. CDK7-IN-2 has potent anti-cancer activity.

DMEA-PNU-159682 (molecule D12) is a ADC cytotoxin molecule including metabolites of nemorubicin (MMDX) from liver microsomes and a potent ADCs cytotoxin PNU-159682.

(S,R,S)-AHPC-PEG1-OTs is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology.

LASSBio-1632 is a new anti-asthmatic lead candidate associated with selective inhibition of PDE4A and PDE4D isoenzymes and blockade of airway hyper-reactivity (AHR) and TNF-α production in the lung tissue. LASSBio-1632 (7j) displays high experimental BBB permeability across BBB through passive diffusion.

Azonafide-PEABA is a cytotoxic drug moiety.

Azide-PEG4-VC-PAB-Doxorubicin is a drug-linker conjugate composed of a cytotoxic anthracycline antibiotic Doxorubicin and a linker Azide-PEG4-VC-PAB to make antibody drug conjugate (ADC).

FFAGLDD TFA is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release.

FFAGLDD is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release.

PUMA BH3 (TFA) is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.

TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively .

Ilexoside XLVIII is an acyl CoA cholesteryl acyl transferase (ACAT) inhibitor. Ilexoside XLVIII is a triterpene saponin isolated from an aqueous extract of the leaves of Ilex kudincha.

γ-Secretase modulator 4 is a potent γ-secretase modulator, reduces the Aβ42 level with IC50s of 0.014 μM and 0.017 μM in human and mouse, respectively.

SHP2 IN-1 (compound 13) is an allergic inhibitor of SHP2 (PTPN11), with an IC50 of 3 nM.

BMS-986299 (compound 112) is a first-in-class NLRP3 inflammasome agonist with an EC50 of 1.28 μM. (patent WO2018152396A1).

CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively.

AcLys-PABC-VC-Aur0101 is a drug-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0101 (an auristatin microtubule inhibitor), linked via the cleavable linker AcLys-PABC-VC.

MC-Val-Cit-PAB-dimethylDNA31 is a drug-linker conjugate for ADC with potent antitumor activity by using dimethylDNA31, linked via the ADC linker MC-Val-Cit-PAB. DimethylDNA31 has effective bactericidal activity against persisters and stationary-phase S. aureus.

4-Methylumbelliferyl β-D-Glucopyranoside, a β-D-glucoside, is a fluorogenic substrate for β-glucosidase, utilizes to assay β-glucosidase activity. 4-Methylumbelliferyl β-D-Glucopyranoside releases the highly fluorescent 4-methylumbelliferyl (4-MU), which has an emission maximum at 445-454 nm. The excitation maximum for 4-MU is pH-dependent: 330, 370, and 385 nm at pH 4.6, 7.4, and 10.4, respectively.

Keap1-Nrf2-IN-1 TFA (compound35) is a Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (Keap1-Nrf2) protein-protein interaction inhibitor, and with an IC50 of 43 nM for Keap1 protein. Keap1-Nrf2-IN-1 TFA activates Nrf2-regulated cytoprotective response and antagonizes acetaminophen-induced liver injury both in cellular and in vivo models.

Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.

UFP-803 TFA is a potent urotensin-II receptor (UT) ligand. UFP-803 TFA has lower residual agonist activity, so it may be an important tool for the investigations on the role played by the UT system in physiology and pathology.

[Orn5]-URP TFA is a potent and selective pure antagonist of Urotensin-II receptor (UT), with an pEC50 of 7.24. [Orn5]-URP TFA displays no agonist activity.

cIAP1 Ligand-Linker Conjugates 9 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 9 can be used to design SNIPERs.