MBX-4055 is a potent and specific antimalarial compound with IC50 of 42 nM (P. falciparum growth inhibition), acts directly on plasmodial surface anion channel (PSAC, Target K0.5=21 nM) to quantitatively abolish parasite-induced permeability changes.

ML276 (ML 276) is a potent, selective inhibitor of Plasmodium falciparum glucose-6-phosphate dehydrogenase (PfG6PDH) with IC50 of 889 nM, with no activity against human G6PD.

ML304 (ML 304) is a potent, selective inhibitor of Plasmodium falciparum glucose-6-phosphate dehydrogenase (PfG6PDH) with IC50 of 190 nM, with no activity against human G6PD (IC50=80 uM).

MMV019266 is a potent antibabesial inhibitor with IC50 of 0.278 uM and 0.909 uM for Babesia spp. (B. bovis and B. divergens), respectively.

MMV396797 is a small molecule inhibitor of the parasite's phosphatidylinositol kinase PfPI4KIIIB, block parasite protein secretion and export.

Nemacol-1 is a small molecule inhibitor of C. elegans vesicular acetylcholine transporter (VAChT), demonstrates nematode-selective activity (C. elegans, EC50=7.1 uM).

OJT008 is a small molecule Mtb. MetAP inhibitor against M. tuberculosis, has MIC50 of 0.063 µg/mL against both active and MDR Mtb.

OSM-S-106 is a reaction hijacking inhibitor of Plasmodium falciparum asparagine tRNA synthetase (PfAsnRS), inhibits the 3D7 line of P. falciparum with IC50 of 58 nM.

P4Q-391 is an antimalarial agent with selective inhibition of the parasite's coenzyme Q cycle, inhibits mitochondrial cytochrome bc1 complex (Cyt bc1).

SCR0911 is a potent malarial cytochrome bc1 inhibitor, inhibits cell growth and ATP synthesis in both the fast- and slow-growing M. smegmatis and M. bovis bacillus Calmette-Guérin, respectively.

T-3767758 is a potent, proline-uncompetitive inhibitor of prolyl-tRNA synthetase (ProRS), displays good activity with EC50 of 595 nM against P. falciparum Dd2-2D4 wild-type parasites.

TCMDC-136879 is a cyclic acyl guanidine compound with antimalarial activity.

TDI-8304 is a highly selective, macrocyclic peptide inhibitor of malaria parasite Plasmodium falciparum proteasome (Pf20S) with IC50 of 0.06 uM, shows high potency against P. falciparum strain Pf 3D7 (EC50=0.009 uM).

UBMC-4 is a potential Trypanosoma cruzi AKT-like pleckstrin homology (PH) domain, exhibits trypanocidal effect on T. cruzi amastigotes with EC50 of 1.85 uM (0.774 ug/mL).

WEHI-518 is a small molecule inhibitor of the parasite's phosphatidylinositol kinase PfPI4KIIIB, shows EC50 of 22 nM against blood-stage P. falciparum parasites.

WEHI-600 is a potent, small molecule inhibitor of the aspartic proteases Plasmepsin X (PMX) with IC50 of 3 nM, possess potent anti-parasitic activity (P. falciparum parasite, IC50=7 nM).

WEHI-601 is a potent, small molecule inhibitor of the aspartic proteases Plasmepsin X (PMX) with IC50 of 5 nM, possess potent anti-parasitic activity (P. falciparum parasite, IC50=9 nM).

WJM228 (WJM-228) is a potent selective inhibitor of P. falciparum cytochrome bc1, targets the Qo site of cytochrome b (cyt b), shows potent parasite activity against P. falciparum 3D7 with EC50 of 19 nM.

ARN1468 is an anti-prion, cellular active small molecule targeting SERPINA3 (ITC KD=26 uM), decreases prion accumulation and reduces PrPSc in the ScGT1 RML cell line with EC50 of 8.64 uM.

OBR-5-340 is a potent, orally bioavailable inhibitor targeting capsid of Rhino- and Enteroviruses,exhibits broad-spectrum antiviral activity against of enteroviruses and rhinoviruses.

AVG-388 is a potent, allosteric, orally efficacious inhibitor of respiratory syncytial virus (RSV) RNA synthesis, potently blocks RSV RNA-dependent RNA polymerase (RdRP) bioactivity, exhibits strong antiviral efficacy in vivo.

JNJ-8003 is a highly potent, selective, non-nucleoside inhibitor of respiratory syncytial virus (RSV) polymerase with IC50 of 0.67 nM, shows EC50 of 0.15 nM in RSV subgenomic replicon assays.

(S)-chlorcyclizine ((S)-CCZ) is an approved antihistamine drug that is related to dichlorcyclizine (DCCZ), inhibits SARS-CoV and SARS-CoV-2 S-mediated infection in MA104 cells with EC50 of 6.91 and 4.09 uM.

AB-00011778 is a small molecule inhibitor of SARS-CoV-2 entry and the Spike/ACE2 interaction, inhibits viral replication with EC50 of 250 nM in A549-ACE2 cells, AB-00011778 is equally effective in impairing the S/ACE2 association in the different mutants.

AC1115 is a potent, selective, next-generation antiviral targeting SARS-CoV-2 Mpro and host lysosomal cysteine protease cathepsin L (CTSL) with high antiviral activity, AC1115 is the active form of Olgotrelvir.

Acriflavine (Acriflavin) is a topical antiseptic that found to be a potent papain-like protease (PLpro) inhibitor, inhibits SARS-CoV-2 and other betacoronaviruses.

ALG-097111 is a potent and selective SARS-CoV-2 3-chymotrypsin-like cysteine protease (3CLpro) with IC50 of 7 nM, without effect against human cathepsin L (IC50>10 uM).

Cyanorona-20 is a potent and specific SARS-CoV-2 inhibitor with very high selectivity (209- and 45-fold more potent than favipiravir and remdesivir, respectively), effectively binds to and inhibits the SARS-CoV-2 RdRp.

D-4-77 is a potent, covalent peptidyl inhibitor of SARS-CoV-2 main protease (Mpro) with IC50 of 0.95 uM and antiviral EC50 of 0.49 uM.

Difluorobenztropine (AHN 1-055) is a direct-acting SARS-CoV-2 entry inhibitor that targets the SARS-CoV-2 spike fusion peptide domain.

DMGA is an allosteric and covalent inhibitor of SARS-CoV-2 papain-like protease (SARS-CoV-2 PLpro) with IC50 of 9.4 uM, covalently binds with C270 of the SARS-CoV-2 PLpro.

DS0464 is a selective, bisubstrate competitive inhibitor SARS-CoV-2 nonstructural protein 14 (nsp14) with IC50 of 1.1 uM, also selective against 28 out of 33 RNA, DNA, and protein MTases.

EIDD-2801 (MK-4482, Molnupiravir) is a highly potent ribonucleoside analog, and prodrug of EIDD-1931, exhibits broad-spectrum antiviral inhibitor of multiple RNA viruses including SARS-CoV-2.

GC-14 is a potent, selective and non-covalent non-peptide SARS-CoV-2 main protease (Mpro) inhibitor with IC50 of 0.4 uM, displays excellent selectivity over cathepsins B, F, K, L, and caspase 3 (IC50>50 uM).

GC373 is a potent, covalent inhibitor of SARS CoV-2 main protease (MPro) with Kd of 0.15 uM, the reactive aldehyde form of GC376.

GC-78-HCl is a potent nonpeptide SARS-CoV-2 main protease (Mpro) inhibitor with IC50 of 0.19 uM, exhibits excellent antiviral activity (EC50=0.4 uM).

JC19 is a a cysteine-reactive small molecule degrader of SARS-CoV-2 nsp14 with DC50 of 8.7 uM in HEK293T cells.

JMX0286 is a potent, specific and allosteric inhibitor against SARS-CoV-2 3CLpro with IC50 of 4.8 uM in FRET based screening assays, shows strong inhibition of SARS-CoV-2 virus with EC50 of 2.25 uM in A549-hACE2 cells.

Jun9-57-3R is a potent, selective, covalent SARS-CoV-2 Mpro inhibitor with IC50 of 0.05 uM.

Jun9-62-2R is a potent, selective, covalent SARS-CoV-2 Mpro inhibitor with IC50 of 0.43 uM.

Jun9-88-6R is a potent, selective, covalent SARS-CoV-2 Mpro inhibitor with IC50 of 0.08 uM.

KSL-128114 (KLS 128114) is a highly potent and metabolically stable peptide inhibitor that binds to the PDZ1 domain of syntenin (KD=0.3 uM), inhibits SARS-CoV-2 infection by blocking the endosomal entry of the virus.

MAC-5576 (MAC5576) is a small molecule, covalent inhibitor of coronavirus SARS-CoV 3CLpro with IC50 of 0.5 uM, inhibits SARS-CoV-2 3CL protease with IC50 of 0.093 uM.

MAT-POS-e194df51-1 is potent, selective and noncovalent SARS-CoV-2 main protease (SARS-CoV-2 Mpro) inhibitor with IC50 of 36.8 nM, shows antiviral activity with EC50 of 64 nM in A549-ACE2-TMPRSS2 cells.

MDOLL-0229 is a selective small molecule inhibitor for SARS-CoV-2 Mac1 with IC50 of 2.1 uM, inhibits coronavirus replication.

MI-30 (SARS-CoV-2 Mpro inhibitor MI-30) is a potent, selective SARS-CoV-2 Mpro inhibitor with IC50 of 17.2 nM.

MK-7845 is a potent, reversible covalent SARS-CoV-2 3CLPro inhibitor with IC50 of 8.7 nM, inhibits wild-type SARS-CoV-2 3CLPro in SARS-CoV-2 reporter replicon assay in A549 cells with IC50 of 15 nM.

ML300 (ML 300) is a potent, selective, noncovalent inhibitor of the SARS-CoV 3CL protease (3CLpro) with IC50 of 4.11 uM, inhibits SARS-CoV-2 3CLpro with IC50 of 4.99 uM.

Molnupiravir N-1 is an impurity chemical of Molnupiravir (EIDD-2801, MK4482), which is anti-SARS-CoV-2 for treatment of COVID-19.

MPI8 is a highly potent SARS-CoV-2 main protease (MPro) inhibitor with IC50 of 8.5 nM.

MPI8 is a highly potent SARS-CoV-2 main protease (MPro) inhibitor with IC50 of 33 nM, completely prevented the SARS-CoV-2-induced cytopathogenic effect in Vero E6 cells at 2.5-5 uM and A549 cells at 0.16-0.31 uM.

MU-UNMC-1 is a potential small-molecule inhibitor of S-RBD and ACE-2 interaction, shows antiviral activity against SARS-CoV-2 with IC50 of 0.67 uM in human bronchial epithelial cells.

MU-UNMC-2 is a potential small-molecule inhibitor of S-RBD and ACE-2 interaction, shows antiviral activity against SARS-CoV-2 with IC50 of 1.72 uM in human bronchial epithelial cells.

NACE2i is a cell permeable, specific and selective peptide inhibitor of nuclear ACE2, inhibits binding between IMP1α and ACE2 and SARS-CoV-2 viral replication. NACE2i specifically targets nuclear ACE2 and not other nuclear proteins targeted by the importin pathway. NACE2i has no impact on ACE2 enzymatic activity. NACE2i prevents inflammation and macrophage infiltration, and increases NK cell infiltration in bronchioles. NACE2i treatment increases the levels of the active histone mark, H3K27ac, restores host translation in infected hamster bronchiolar cells, and leads to an enrichment in methylated ACE2 in hamster bronchioles and lung macrophages. NACE2i has a dual mode of action: suppressing the lethal inflammation in severe COVID-19 and inhibiting viral replication by restoring host translation of anti-viral cytokines.

NBCoV1 is a highly potent small molecule viral fusion inhibitor with potential pan-Coronavirus activity (SARS-CoV IC50=17 nM, SARS-CoV-2 IC50=51 nM, MERS-CoV IC50=75 nM, cell-based single-cycle assays).

NBCoV2 is a highly potent small molecule viral fusion inhibitor with potential pan-Coronavirus activity (SARS-CoV IC50=13.8 nM, SARS-CoV-2 IC50=22.8 nM, MERS-CoV IC50=77 nM, cell-based single-cycle assays). NBCoV2 also has potent antiviral activity against all mutant pseudoviruses carrying single-, double-, or triple-mutations featured in the B.1.1.7 UK, B.1.351 RSA, and B.1.617.2 Delta variants (IC50=30-80 nM). NBCoV2 completely preventing the induction of any virus-induced CPE (IC100=1.25 uM, SARS-CoV-2 (US_WA-1/2020)). NBCoV2 bind to the S2 subdomain of the SARS-CoV-2 trimer, thus, inhibits the fusion of CoVs with the cell membran, and is specific for the SARS-CoV-2 S protein.

NSC 621601 (Compound Q34) is a potent, specific inhibitor of SARS-CoV-2 cellular entry with IC50 of 15 uM.

Olgotrelvir (STI-1558) is a next-generation antiviral targeting SARS-CoV-2 Mpro and host lysosomal cysteine protease cathepsin L (CTSL) with high antiviral activity, Olgotrelvir is the prodrug of AC1115.

P2119 (P-2119) is an anticoronaviruse chemical probe that inhibit SARS-CoV-2 Spike binding to human ACE2 receptor.

P2165 (P-2165) is a anticoronaviruse chemical probe that inhibit SARS-CoV-2 Spike binding to human ACE2 receptor.

PAV-104 (PAV104) is a novel viral assembly inhibitor, shows potent anti-SARS-CoV-2 activity in Calu-3 cells with EC50 of 1.7 nM and EC90 of 23.5 nM, inhibits the oligomerization of the SARS-CoV-2 nucleocapsid.

Pomotrelvir (PBI-0451) is a potent competitive inhibitor of SARS-CoV-2 Mpro (Ki=2.7 nM) with high selectivity against human proteases, inhibits wild-type SARS-CoV-2 Mpro with IC50 of 24 nM.

SB27012 (SB 27012) is a small molecule PPI inhibitor of the Spike RBD-ACE2 interaction (IC50=7.7 uM in ELISA assays), binds ACE2 (Kd=210 nM) without affecting ACE2 enzymatic activity.

SCoV2 Plpro-Probe-7 is a peptidomimetic activity probe and substrate for SCoV2 PLpro, exhibits excellent sensitivity to wild-type (WT) SCoV2 PLpro, but not to the catalytically inactive mutant, SCoV2 PLproC112S, consists of a fluorogenic HCC conjugated to

Simnotrelvir (SSD8432, SIM0417) is a potent, selective, covalent and orally bioavailable SARS-CoV-2 3C-like protease (3CLpro) inhibitor with IC50 of 9 nM in enzymatic inhibition assays.

Titanocene dichloride (Cp2 TiCl 2) is an active inhibitor of interaction between SARS-CoV-2 spike (S) protein with the ACE2 receptor (IC50=3.9 uM)

TKB245 (TKB-245) is a potent, specific SARS-CoV-2 Mpro inhibitor with IC50 of 7 nM, exhibits highly potent anti-SARS-CoV-2 activity with EC50 and EC95 values of 0.03 and 0.53 µM, respectively.

TKB248 (TKB-248) is a potent, specific SARS-CoV-2 Mpro inhibitor with IC50 of 74 nM, exhibits highly potent anti-SARS-CoV-2 activity with EC50 and EC95 values of 0.22 and 0.87 µM, respectively.

VE607 is a specific small molecule inhibitor that block S protein-ACE2-mediated cellular entry of the SARS-CoV, inhibits pseudovirus entry with EC50 of 3 μM and inhibited SARS-CoV plaque formation with EC50 of 1.6 μM.

WNN2048-F004 (Compound 4a) is a potent, covalent, nonpeptidomimetic SARS-CoV-2 main protease (Mpro) inhibitor with biochemical IC50 of 103 nM, covalently binds to the substrate-binding pocket (Cys145) of SARS-CoV-2 Mpro.

WU-04 is a highly potent, non-covalent, orally active inhibitor of SARS-CoV-2 3C-like protease (3CLpro) with IC50 of 72 nM, binding Kd of 37 nM.

Y180 is a highly potent, selective, covalent, and orally active SARS-CoV-2 main protease (Mpro) inhibitor with IC50 of 8.1 nM in enzymatic assays, binding Ki value of 1 nM.

Z222979552 is a small molecule non-covalent SARS-CoV-2 Mpro inhibitor with IC50 of 1.0 uM.

Z8539_0072 is a potent SARS-CoV-2 macrodomain inhibitor that binds to the NSP3 macrodomain of SARS-CoV-2 (Mac1) with IC50 of 460 nM.

ANP0903 is an analog of HIV-1 protease inhibitor darunavir, induces cytotoxicity in hepatocellular carcinoma cell lines, triggers apoptosis by enhancing ER stress.

Tpz-1 is a unique cytotoxic compound that elicits potent and selective programmed cell death in human blood, breast, colon, and cervical cancer cell lines, interferes with components of signaling pathways and the cytoskeleton that are important to cell sh

WZY-321 a small molecule glioma cell apoptosis inducer, binds to XAF1 3-UTR and decreases XAF1 (X-linked inhibitor of apoptosis-associated factor 1) mRNA levels.

BAU-243 (BAU243) is a novel BH3 mimetic Bcl-2 inhibitor with a high affinity, effectively reduces overall GBM cell proliferation including a subpopulation of cancer-initiating cells.

BDM44898 is a small molecule inhibitor of anti-apoptotic protein BCL2A1/Bfl-1 with IC50 of 1.6 uM.

BDM44931 is a small molecule inhibitor of anti-apoptotic protein BCL2A1/Bfl-1 with IC50 of 1.3 uM.

BDM49234 is a selective small molecule inhibitor of anti-apoptotic protein BCL2A1/Bfl-1 with IC50 of 6.3 uM (inhibition FITC–Bim BH3 binding to Bfl-1).

BDM53787 is a selective small molecule inhibitor of anti-apoptotic protein BCL2A1/Bfl-1 with IC50 of 0.8 uM (inhibition FITC–Bim BH3 binding to Bfl-1).

BI-5273 is a negative control compound of BI-3802 and BI-3812, which are potent and efficacious BCL6 degrader and inhibitor, respectively.

CCT372064 is a potent, ligand-efficient inhibitor of BCL6 with IC50 of 3.9 nM and 12 nM in TR-FRET and cellular NanoBRET assays, respectively.

CCT373566 is a highly potent, in vivo active BCL6 degarder with IC50 of 2.2 nM and DC50 of 0.7 nM in TR-FRET and cellular BCL6 degradation assays, respectively.

CCT373567 is a potent, selective and cell-active BCL6 inhibitor with IC50 of 2.9 nM in TR-FRET assays, and 25.9 nM in NanoBRET cellular inhibition assays.

CCT374705 is a potent, selective, in-vivo active BCL6 inhibitor with TR-FRET IC50 of 6 nM.

CGDF-183-20 is a selective small molecule inhibitor of anti-apoptotic protein BCL2A1/Bfl-1 with IC50 of 264 nM in FP assays.

CGDF-190-20 is a selective small molecule inhibitor of anti-apoptotic protein BCL2A1/Bfl-1 with IC50 of 365 nM in FP assays.

DC-B01 is a novel small molecule BCL-2 inhibitor that binds to the BH4 domain with KD of 2.16 uM, disrupts the BCL-2/c-Myc interaction and consequently suppresses the transcriptional activity of c-Myc.

GSK137 is a potent, small-molecule BCL6 inhibitor binding to BCL6 BTB-POZ domain, displaces peptides derived from the human SMRT co-repressor from the BCL6 BTB-POZ domain in a TR-FRET assay with a pIC50 of 8.0.

M109S is a small molecule protecting cells from mitochondria-dependent apoptosis wtih EC50 of 23.4 nM in iBax cells, directly interacts with Bax (Kd=153 nM, MST assay) and inhibits Bax activation.

MI-238 (MI 238) is a potent and specific Mcl-1 inhibitor with Ki of 0.45 uM to human Mcl-1 protein in FP assays, disrupts the association of Mcl-1 with BH3-only proteins.

A potent inhibitor of Bcl-2 family with IC50s of 1-7 uM for Bcl-2, Bcl-XL, Bcl-w, Bcl-B, Mcl-1 and Bfl-1.

OICR12694 (OICR 12694, JNJ-65234637) is a potent, selective, and orally bioavailable BCL6-BTB inhibitor with SPR KD value of 5 nM.

Sonrotoclax (BGB-11417) is a potent, selective and second-generation BCL2 inhibitor with IC50 of 0.014 nM and SPR KD value of 0.046 nM, overcomes BCL2 G101V mutation-induced venetoclax resistance.

WK369 (WK-369) is a specific small molecule inhibitor of BCL6, directly binds to the BCL6-BTB domain (SPR KD=2.24 uM) and blocks the interaction between BCL6 and SMRT with IC50 of 0.32 uM in HTRF assays.

WK499 (WK-499) is a small molecule inhibitor of BCL6 with IC50 of 11.7 nM in HTRF assay, directly binds to BCL6 BTB (SPR KD=148 nM), inhibits the BCL6-mediated transcriptional repression activity.

WK500B is an orally available small molecule BCL6 inhibitor with IC50 of 1.39 uM (HTFR), exhibits potent efficacy against DLBCL in vitro and in vivo.

AKI-02 is a hydroxypyridinone-based iron chelator, potently inhibits labile iron-mediated ferroptosis.

FSEN1 (Ferroptosis Sensitizer 1) is a specific small molecule, uncompetitive inhibitor of ferroptosis suppressor protein 1 (FSP1) with IC50 of 133 nM, sensitizes cancer cells to ferroptosis.

LOC1886 is a small molecule allosteric inhibitor of GPX4, inhibits enzymatic activity of GPX4 in HT1080 cell lysates with Ki of 102 uM, degrades GPX4 to induce ferroptosis, binds covalently to C66 of GPX4.

142D6 is a potent, Lys-covalent pan-IAP inhibitor, targets the BIR3 domain of the inhibitor of the apoptosis protein (IAP) family with IC50 of 43/21/21 nM for XIAP/cIAP1/cIAP2, respectively.

ARTS mimetic A4 is a small molecule that mimics the function of the pro-apoptotic ARTS (Sept4_i2) protein, binds the ARTS pocket in XIAP-BIR3, but not cIAP1, specifically promotes degradation of XIAP and induces caspase-mediated cell death.

DEBIO 1143 (Xevinapant, AT-406, SM406, ARRY-334543, D1143) is a potent, orally active Smac mimetic that antagonizes cIAP1, cIAP2 and XIAP with Ki of 66.4, 1.9 and 5.1 nM, respectively.

RMT 5265 (RMT5265) is a potent, small molecule bivalent mimic of Smac, inhibits XIAP and cIAP1/2 through the BIR3 domain.

BAY 1892005 is a small molecule that modulate mutant p53 condensation and nuclear accumulation, binds covalently to mutant p53R175H and p53Y220C and shows stabilization of p53WT and p53Y220C, exhibits anti-proliferative activity in a set of cell lines wit

BAY 249716 is a small molecule that modulate mutant p53 condensation, showed significant stabilization of all three p53 protein variants, p53WT p53R175H and p53Y220C.

GY1-22 is a small molecule inhibitor against DNAJA1-mutP53R175H interacting pocket, reduces mutp53 protein expression in colon cancer cell line with p53R175H mutation.

RPL11-MDM2 inhibitor S9 (J012-3168) is a small-molecule RPL11 mimetic and potential inhibitor of RPL11-MDM2 interaction, directly binds MDM2 and induces p53 stabilization and activation.

K-181 is a specific small-molecule Protein-Protein Interaction (PPI) inhibitor of Mdmx-p53 interaction, exhibits neuroprotective effects on ischemic stroke by disrupting Mdmx-p53 interaction and inhibiting HDAC6 activity.

MMRi67 is a potent E3 ligase inhibitor of the MDM2-MDM4 E3 complex, inhibits RING-RING interaction of MDM4 and MDM2B with Kd of 896 nM.

MMRi71 is a small molecule inhibitor of the E3 ligase activity of MDM2-MDM4, and an inducer of MDM4 and FTH1 dual protein degradation and p53-independent apoptosis in leukemia cells.

Morncide (Morn3 (222-237)) is a cell-penetrating, 16-AA Morn3-targeting peptide that disrupts the interaction between p53 and Morn3-mediated complex, Morncide peptide stabilizes and reactivates p53 in cancer cells.

NSC146109 (XI-011) is a small-molecule p53 activator, induces apoptosis of breast cancer cells through inhibiting MDMX (MDM4) expression.

ReACp53 is a cell-penetrating 17-residue peptide designed to inhibit p53 amyloid formation, rescues p53 function in cancer cell lines.

UC2288 is a small molecule p21 inhibitor, attenuates p21 protein abundance at 10 µM, independently of p53 activity and at the level of transcription or post-transcription.

UCI-LC0019 is a specific small molecule that restores mutant p53 activity by targeting the cryptic L1/S3 pocket of p53, directly binds to mutant p53 and restores wild-type-like conformation of mutant p53R175H.

UCI-LC0023 is a small molecule that restores mutant p53 activity by targeting the cryptic L1/S3 pocket of p53, directly binds to mutant p53 and restores wild-type-like conformation of mutant p53R175H.

AC-003 is a novel oral small-molecule inhibitor of receptor interacting protein kinase 1(RIPK1) and has the potential for treating idiopathic pulmonary fibrosis.

aYM155 is a brain-penetrating prodrug form of YM155 (Cat. PC-42439, potent survivin inhibitor), displays potent cell killing activity against a broad panel of patient-derived GBM cancer stem-like cells (IC50=0.7-10 nM).

cRIPGBM (RIPGBM derivative cRIPGBM, RIPGBM-18) is a metabolite of RIPGBM induces apoptosis in GBM CSCs (EC50=68 nM in GBM 1 cells) by interacting with RIPK2 (Kd=2.3 uM).

Flizasertib is a potent, selective RIP1 kinase (RIPK1) inhibitor with potential for treating prophylaxis.

GNE-684 is a potent, cross-species, specific RIP1 kinase (RIPK1) inhibitor with IC50 of 21, 189 and 691 nM for human, mouse and rat RIP1, respectively.

GSK2593074A (GSK'074, GSK-2593074A) is novel potent, selective RIP1/RIP3 kinase dual inhibitor, directly binds to RIP1 and RIP3 with Kd of 130 and 12 nM, respectively.

Oditrasertib is a potent, selective RIPK1 inhibitor.

Zharp1-211 is a potent, selective, type II inhibitor of RIPK1 kinase with IC50 of 53 nM and binding Kd of 8.7 nM.

Zharp2-1 is a novel potent, selective RIPK2 inhibitor with IC50 of 38.5 nM in ADP-Glo kinase assay, effectively blocks RIPK2 kinase function and NOD-mediated NF-κB/MAPK activation.

JS-017 (JS017) is a small molecule degrader of N-retinylidene-N-retinylethanolamine (A2E), one of the components of lipofuscin, degrades A2E-BDP from ARPE-19 cells with IC50 of 3.239 uM.

RH1115 is a small molecule activator and inducer of autophagy targeting Lamin A/C and LAMP1, induces changes to LAMP1 vesicle properties and alters lysosome positioning.

YTK-2205 (YTK2205) is a small molecule p62 agonist targeting ZZ domain, induces selective autophagy activation, YTK-2205 augments the translocation of p62 to mitochondria, targeting their lysosomal degradation.

DC-ATG4in is a small molecule autophagy related 4B (ATG4B) inhibitor, directly binds to ATG4B and inhibits its enzyme activity with IC50 of 3.08 uM, DC-ATG4in is an autophagy inhibitor.

EB-42168 is a potent, selective G2019S-LRRK2 kinase inhibitor with IC50 of 1.1 nM (pS935-LRRK2) in FRET-based assay, >100-fold selective over WT-LRRR2.

FX2149 (FX 2149) is a potent, BBB permeable inhibitor of LRRK2 GTP binding activity with IC90 of 10 nM, reduces PD-linked mutant LRRK2 variants (G2019S and R1441C) that bound with GTP.

MK-1468 is a potent, selective, brain-penetrant LRRK2 inhibitor with IC50 of 0.4 nM (G2019S LRRK2), potently inhibits the phosphorylation of LRRK2 serine 935 (pSer935) in hPBMCs with IC50 of 2.8 nM.

GLPG3312 is a potent and selective pan-SIK inhibitor with IC50 of 2.0/0.7/0.6 nM for SIK1/SIK2/SIK3, respectively.

JRD-SIK1/2i-4 is a potent, highly selective SIK1/2 inhibitor, modulates innate immune activation and suppress intestinal inflammation.

SK-124 (SK124) is a potent, selective, orally active SIK2/SIK3 inhibitor with IC50 of 8.8/11.3 nM in cell-based NanoBRET assays, 15-fold selectivity versus SIK1.

MR-2088 is a potent and selective ULK1/2 inhibitor with IC50 of 2.0 nM and MST Kd value of 1.5-4.4 nM (ULK1), efficiently inhibits autophagy.

SW118150 is a selective small molecule inhibitor of WNK3 kinase with IC50 of 3.0 uM, 5-fold selectivity over WNK1.

SW120619 is a specific small molecule inhibitor of WNK3 kinase with IC50 of 0.7 uM, weakly inhibits WNK1 and WNK2 with IC50 of 2.3 and 16.8 uM, respectively.

TH7299 is a potent mitochondrial inhibitor of mitochondrial MTHFD2L with IC50 of 274 nM.

ART0380 (ART-0380) is a potent, selective and ATP-competitive ATR kinase inhibitor, inhibits ATR-ATRIP complex enzyme activity with IC50 of 51.7 nM, and phospho-Chk1 IC50 of 22 nM in cell western assay.

LXY18 is a potent orally available blocker of AURKB relocation in mitosis with minimum effective concentration (MEC) of 3.5 nM for inducing polyploidy, shows broad-spectrum growth inhibitory and apoptosis-inducing activities with low nanomolar potencies.

GPS192 (GPS 167) is a specific small molecule splicing regulator SRSF10 inhibitor, modulates BCLAF1 splicing with IC50 of 2 uM in human colorectal HCT116 cells, directly inhibits CLK1, CLK2 and CLK4, but not SRPK1 and DYRK1A.

Leucettinib-92 is a potent DYRK/CLK inhibitor, inhibits CLK1, CLK2, CLK4, DYRK1A and DYRK1B with IC50 of 9.2, 6, 6, 1.2 and 1.8 nM, respectively.

ML315 is a small molecule inhibitor of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases with IC50 of 68, 231, >10,000, 68, 282 and 1156 nM for CLK1/2/3/4 and DYRK1/2, respectively.

MW01 is a specific inhibitor for DNA damage-induced NF-κB activity, inhibits CLK2 and CLK4 with IC50 of 360 and 14.1 nM, does not inhibit CLK3.

MW05 is a specific inhibitor for DNA damage-induced NF-κB activity, inhibits CLK2 and CLK4 with IC50 of 1400 and 307 nM, does not inhibit CLK3.

BMS-357075 is a potent pan inhibitor of cyclin-dependent kinases (CDKs) with IC50 of 18, 3 and 26 nM for CDK1, CDK2, and CDK4, respectively, also inhibits CDK20 with Kd of 56 nM.

CAF-382 (CDKL5 inhibitor B1) is a potent, specific inhibitor of serine-threonine kinase cyclin dependent kinase-like 5 (CDKL5) with IC50 of 11 nM in NanoBRET assays, shows no activity against GSK3β.

Cdk5i peptide is a Cdk5-derived 12-amino acid long Cdk5-derived peptide that interferes with the Cdk5/p25 complex with Kd of 0.17 uM, 40-fold more strongly to either Cdk5 or Cdk2 alone.

Crozbaciclib is a highly potent, selective, blood-brain barrier (BBB) permeable CDK4/6 inhibitor with IC50 values of 3 nM and 1 nM against CDK4/cyclin D1 and CDK6/cyclin D3, respectively.

Cyclin K degrader DS17 is a selective cyclin K molecular glue degrader with TR-FRET EC50 of 19 nM.

EF-4-177 is a potent, selective, allosteric and orally active CDK2 inhibitor with ITC KD of 7.4 nM. EF-4-177 binds CDK2 in a manner that is negatively cooperative with cyclin binding.

ERP1.14a is a selective, small molecule inhibitor of cell division cell cycle kinase 7 (CDC-7) with IC50 of 125 nM, decreases the enhanced TDP-43 phosphorylation in cells derived from TDP-43-related pathogenesis such as FTLD and ALS.

ERP1.28a is a selective, small molecule inhibitor of cell division cell cycle kinase 7 (CDC-7) with IC50 of 140 nM, decreases the enhanced TDP-43 phosphorylation in cells derived from TDP-43-related pathogenesis such as FTLD and ALS.

GFH009 is a potent, selective CDK9 inhibitor, inhibits the activity of the CDK9/cyclin T1 regulatory complex of P-TEFb.

ISM042-2-048 is a potent, selective inhibitor of cyclin-dependent kinase 20 (CDK20, cell cycle-related kinase/CCRK) with IC50 of 33.4 nM (CDK20/CycT1), Kd value of 566 nM.

LGR6768 is a potent, selective CDK7 inhibitor with IC50 of 20 nM, >12-fold selectivity over other CDKs.

MER-128 is a potent, selective CDK20 inhibitor with IC50 of 2 nM.

MK256 (MK-256) is a potent, selective CDK8 inhibitor with IC50 of 2.5 nM and 3.3 nM against CDK8/cyclin C and CDK19/cyclin C, respectively.

NCGC00131308 is a small molecule inhibitor that effectively disrupts IQGAP1-Cdc42 interaction in breast cancer cells, shows EC50 of 4.47 uM in biochemical HTRF assays.

NCT02 is a small moelcule that induces ubiquitination of cyclin K (CCNK) and proteasomal degradation of CCNK and its complex partner CDK12.

RGB-286199 (GPC-286199) is a potent broad spectrum CDKs (cyclin dependent kinases) inhibitor with IC50 of 5-100 nM against CDKs 1-6, shows antiproliferative activity in vitro and in vivo.

SNX631 (SNX-631) is a potent, selective inhibitor of CDK8/19 Mediator kinase with IC50 of 10.3 nM in the NF κB-dependent cell-based assays.

SW394703 is a novel DDB1-dependent molecular glue degrader for cyclin K, SW394703 is toxic to HCT116 cells (IC50=1.2 uM).

TMX-2039 is a pan-CDK inhibitor with low nanomolar enzymatic IC50s (0.5-50 nM) for both cell cycle CDKs (CDK1, CDK2, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9).

XPW1 is a potent and selective CDK9 inhibitor with excellent anti-ccRCC activity and low toxicity.

YPN-005 (YPN005) is a highly potent, selective inhibitor of cyclin-dependent kinase 7 (CDK7) with IC50 of 31 nM, with low inhibition for CDK2 and CDK5.

ZNL-05-044 is a potent, selective CDK11 inhibitor with Kd of 69 nM (CDK11A), shows significantly kinome-wide selectivity. ZNL-05-044 treatment leads to G2/M cell cycle arrest, impacts CDK11-dependent mRNA splicing in cells.

ZSQ836 (ZSQ 836) is a potent, selective and orally bioavailable CDK12/CDK13 covalent inhibitor with IC50 of 32 nM (CDK12), covalently interacts with Cys1039 of CDK12.

OBI-3424 S-isomer (TH-3424, OBI 3424) is a highly potent DNA alkylating prodrug that is converted by AKR1C3 to a potent DNA-alkylating agent.

CDEAH is a monofunctional alkylating agent that selectively kills PARP1- and xeroderma pigmentosum A-deficient cells.

NSC373981 (NSC 373981) is a CARD11 G-quadruplex (G4) stabilizing small molecule that downregulates CARD11 gene expression in DLBCL cells.

QBS10072S is a novel dual-function, BBB permeable chemotherapeutic agent with alkylating moiety and a selective large neutral amino acid transporter 1 (LAT1, SLC7A5) substrate, shows excellent BBB penetration and promising efficacy in vitro (U251 cell IC5

H3B-960 is a potent, selective and covalent inhibitor of Werner syndrome protein (WRN) helicase activity with IC50 of 60 nM.

H3B-968 is a potent, selective and covalent inhibitor of Werner syndrome protein (WRN) helicase activity with IC50 of 41 and 13 nM in ADP-Glo assay DNA unwinding assay, respectively.

HRO761 is a potent, selective, allosteric WRN inhibitor with IC50 of 100 nM (ATPase assay) and GI50 of 40 nM (SW48 cells), respectively. HRO761 binds at the interface of the D1 and D2 helicase domains, locking WRN in an inactive conformation.

KY386 is a potent, selective inhibitor of RNA helicase DHX33 with IC50 of 19 nM.

SU0448 is a specific, cell-permeable small molecule activator of the DNA repair enzyme Human MutT Homolog 1 (MTH1) with AC50 value of 5.5 uM, inhibits cell viability of HCC1806 cells with IC50 of 36.1 uM.

Fraisinib is a specific and effective inhibitor of glycyl-tRNA synthetase 1 (GARS1), suppresses the synthesis of Ap4A by GARS1 and displays strong anti-tumoral potential.

RBI2 (Ribosome biogenesis inhibitor 2) is a small molecule inhibitor of ribosome biogenesis inhibitor, potently inhibits pre-rRNA levels in A375 with IC50 of 169 nM.

Ku-DBi 245 is a novel DNA-PK inhibitor with a unique mechanism of action, blocking the Ku 70/80 heterodimer interaction with DNA.

SN38023 is a bioreductive prodrug of DNA-dependent protein kinase inhibitor IC87361 (Cat# PC-62995), SN38023 is metabolised to a potent DNA-PKi (IC87361) selectively in radioresistant hypoxic cells.

ZL-2201 mesylate (ZL2201) is a highly potent, selective and orally bioavailable inhibitor of DNA-dependent protein kinase (DNA-PK) with IC50 of 1.1 nM.

CCT241950 (CCT 241950) is a small molecule NEK2 inhibitor, induces Tyr70Nek2 to jut into the ADP-binding pocket.

T-1101 tosylate (TAI-95 tosylate) is a potent, orally abioavailable Hec1 inhibitor that disrupts Hec1-Nek2 protein interaction wide anti-cancer spectrum (GI50=14.29-73.65 nM, breast cancer cell lines).

SYL1073 is a potent, selective and covalent Threonine tyrosine kinase (TTK) inhibitor with IC50 of of 16 nM.

DI-87 ((R)-DI-87) is a highly potent, specific, orally bioavailable deoxycytidine kinase (dCK) inhibitor with IC50 of 3.15 nM.

F-aza-T-dCyd (NSC801845) is a novel cytidine analog and is more efficacious than aza-T-dCyd in cell culture and mouse xenograft studies in HCT-116 human colon carcinoma.

JLT048 is a small molecule inhibitor of tyrosyl-DNA-phosphodiesterases 1 and 2 (TDP1 and TDP2) with IC50 of 7.7 and 32 uM, respectively.

PSB-071 (PSB071) is a small molecule inhibitor of nucleoside triphosphate diphosphohydrolases (NTPDase).

PSB-0952 (PSB0952) is a potent, selective ecto-5'-Nucleotidase (eN, CD73) inhibitor with Ki of 260 nM, >150-fold selectivity over NTPDases and P2Y receptor subtypes P2Y2, P2Y4, P2Y6, and P2Y12.

PSB-0963 (PSB0963) is a potent, selective ecto-5'-Nucleotidase (eN, CD73) inhibitor with Ki of 150 nM, >100-fold selectivity over NTPDases.

TH6342 (TH-6342) is a specific small-molecule inhibitor against the dNTP triphosphohydrolase (dNTPase) SAMHD1, inhibits the enzymatic activities of SAMHD1 against dGTP, Cl-F-ara-ATP, and ara-CTP with IC50 of 9.6, 11.0 and 5.8 uM, respectively.

TH7528 (TH-7528) is a specific small-molecule inhibitor against the dNTP triphosphohydrolase (dNTPase) SAMHD1, inhibits the enzymatic activities of SAMHD1 against dGTP, Cl-F-ara-ATP, and ara-CTP with IC50 of 4.5, 2.8 and 2.6 uM, respectively.

AMXI-5001 (AMXI 5001) is a novel, highly potent, orally active dual PARP1/2 (IC50 5/0.05 nM) and microtubule polymerization inhibitor, inhibits intracellular PAR formation with IC50 of 7 nM.

G-631 is a potent and selective TNKS1/2 inhibitor with IC50 of 7 nM in biochemical assays of tankyrase auto-PARsylation activity, and cellular potency of 8 nM (HEK293).

KMR-206 (KMR206) is a potent, selective PARP7 inhibitor with IC50 of 13.7 nM, displays 75-fold selectivity for PARP7 over PARP2 and does not inhibit PARP1 up to 3 uM.