DK1-04 is a potent, selective, cell-permeable small-molecule SIRT5 inhibitor with IC50 of 0.34 uM, shows no inhibition on SIRT1-3/6 at 83 uM.

Dichloro-all-trans-retinone (DAR) is an irreversible inhibitor of retinaldehyde dehydrogenase (RALDH/ALDH1A) with IC50 of 434/55/161 nM for RALDH1/RALDH2/RALDH3.Dichloro-all-trans-retinone has no activity on human mitochondrial ALDH2.Dichloro-all-trans-retinone inhibits ATRA synthesis in a RALDH2 expressing cell line with IC50 of 3 uM.The retinaldehyde dehydrogenase (RALDH, also ALDH1A) subfamily consists of three members, RALDH1 (ALDH1A1), RALDH2 (ALDH1A2), and RALDH3 (ALDH1A3), which synthesize all-trans-retinoic acid (ATRA) from retinaldehyde.

Dichlorcyclizine (DCCZ) is a potent, small molecule HCV fusion inhibitor, also inhibits SARS-CoV and SARS-CoV-2 S-mediated infection in MA104 cells with EC50 of 9.92 and 4.53 uM, respectively.

DI-1548 (DI 1548) is a potent, selective and covalent DCN1 inhibitor with IC50 of 4.6 nM and Ki of <1 nM, does not bind to DCN3.DI-1548 could inhibit cullin 3 neddylation at concentration as low as 1 nM, which is 1000 times more potent than DI-591.DI-1548 selectively inhibit neddylation of cullin 3 in cells at low nanomolar concentrations and are 2-3 orders of magnitude more potent than our previously reported reversible DCN1 inhibitor DI-591.

DGY-09-192 is a bivalent degrader (PROTAC) that couples the pan-FGFR inhibitor BGJ398 to a CRL2VHL E3 ligase recruiting ligand,preferentially induces FGFR1/2 degradation while largely sparing FGFR3/4.DGY-09-192 exhibited two-digit nanomolar DC50s for both wildtype FGFR2 and several FGFR2-fusions, resulting in degradation-dependent antiproliferative activity in representative gastric cancer and cholangiocarcinoma cells (IC50=1 nM).DGY-09-192 induced degradation of a clinically relevant FGFR2 fusion protein in xenograft model.

DF2593A (DF 2593A) is a potent, selective, noncompetitive allosteric inhibitor of C5aR with IC50 of 5 nM (C5a-induced human PMN migration inhibition), and rat and mouse orthologs (IC50=6.0 nM and IC50=1.0 nM, respectively); dispalys >1,000-fold selective versus other chemoattractants, including CXCL8 and CXCL1 (CI50>10 uM), as well as on a panel of different GPCRs and ion channels; DF2593A demonstrated antinociceptive effects in several models of inflammatory pain and effectively inhibited articular hyperalgesia in CFA-induced mechanical and thermal hyperalgesia and arthritic nociception.

DDO-6600 (DDO 6600) is a potent, selective, covalent inhibitor of Hsp90, covalently modifies Cys598 on Hsp90 and disrupts the interaction between Hsp90 and Cdc37 (IC50=6.67 uM).DDO-6600 exhibited antiproliferative activities against multiple tumor cells without inhibiting ATPase activity.DDO-6600 induced the degradation of kinase client proteins in multiple tumor cell lines, promoted apoptosis, and inhibited cell motility.DDO-6600 exhibits antitumor activity in HCT-116 mouse models.

DDC-01-163 is an allosteric EGFR degrader that selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells while leaving wildtype EGFR Ba/F3 cells unaffected; DDC-01-163 exhibited an acceptable biochemical potency with an IC50 value of 45 nM against EGFR L858R/T790M. DDC-01-163 is also effective against osimertinib-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. The anti-proliferative activity of DDC-01-163 against L858R/T790M EGFR-Ba/F3 cells is enhanced when combined with an ATP-site EGFR inhibitor, Osimertinib.

DC-TEADin1072 is a novel TEAD1/3 covalent inhibitor with biochemical IC50 values of 0.61 and 0.58 uM against TEAD1 and TEAD3, respectively.TEADin1072 selectively inhibited TEAD1 and TEAD3 palmitoylation while sparing TEAD2 and TEAD4.TEADin1072 demonstrated selective engagement with Cys371 of TEAD3 and Cys359 of TEAD1.

DCP1-3 is a novel allosteric ligand of the angiotensin receptor AT1R, displays NAM potency on AngIV with IC50 of 0.29 uM.DCP1-3 reduces AngII-induced contraction in renal and iliac arteries in mice.DCP1-3 inhibits IgG binding to HEK-AT1R cells with IC50 of 2.9 nM.DCP1-3 reverses PAM effect of the IgG on the agonist-induced calcium response.

DC-CBi-22 is a highly potent, selective CECR2 bromodomain inhibitor with IC50 of 8.0 nM, 24.9-fold selectivity over BPTF BRD.

DCBS152A is a potent, functionally selectiver negative modulator of GABAA receptor at the modulatory PQ site in some receptor isoforms.

DC541 (DC 541) is a potent, selective peptidomimetic inhibitor of Protein N-terminal methyltransferase NTMT1 with IC50 of 0.34 uM; DC541 exhibits over 300-fold selectivity to several methyltransferases. DC541 inhibited funtions the cellular α-N-terminal methylation level of regulator of chromosome condensation 1 (RCC1, IC50 value of 30 μM) in human colorectal cancer HT29 cells.

dBRD9‐A is a chemical degrader (PROTAC) of BRD9, a highly specific binder of the BRD9 bromodomain and elicits near complete BRD9 degradation at low nanomolar concentrations.dBRD9‐A blocks synovial sarcoma tumour progression and oncogenic transcription.dBRD9‐A limited IFN‐induced expression of certain ISGs in multiple cell types, significantly reduced induction of 29 ISGs, including many ISGs known to harbor antiviral activity against the viruses, such as MX1, MX2, IFITM1, IFITM3, IDO1, and BST2.

DA-1241 (DA1241) is a novel potent, highly selective GPR119 agonist, activates human GPR119 (EC50=4.37 nM) in increasing cAMP levels in GPR119-overexpressing HEK293 cells.DA-1241 increased cAMP levels via activated mouse GPR119 (EC50, 71.5 nM) and rat GPR119 (EC50, 156 nM).DA-1241 showed no significant activity against 156 off-target proteins at 10 uM, including human GLP-1 receptor and human GPR40.DA-1241 stimulated insulin secretion in hamster insulinoma HIT-T15 cells with EC50 of 22.3 nM, association with enhanced human insulin promoter activity.DA-1241 significantly reduced postprandial glucose excursion, significantly preserved β-cell mass with reduced PDX1 levels in the islets from HFD/STZ diabetic mice.DA-1241 reduced triglyceride content in the liver thereby improved fatty liver, reduced gluconeogenic enzyme expression in HepG2 cells and mouse liver, reduced autophagic flow in HepG2 cells.

DA-0218 (DA0218) is a novel potent, selective Nav1.7 inhibitor, inhibits sodium currents in Nav1.7-expressing human embryonic kidney 293 cells with IC50 of 0.74 uM.DA-0218 has no effect on sodium currents in Nav1.5-transfected human embryonic kidney 293 cells in patch-clamp experiments.DA-0218 shows analgesic activity predominantly in phase II in formalin-induced inflammatory pain mouse model.DA-0218 produced acute reduction in paclitaxel-induced mechanical allodynia, and inhibited histamine-induced acute itch and lymphoma-induced chronic itch.

Cycloheximide (Naramycin A, Actidione) is a widely-used protein synthesis inhibitor that inhibits protein biosynthesis in eukaryotic organisms with IC50 of 532.5 nM and 2880 nM for protein synthesis and RNA synthesis in vivo, respectively; block the elongation phase of eukaryotic translation, binds the ribosome and inhibits eEF2-mediated translocation; impairs memory more as footshock intensity increases, enhances memory in an inverted-U dose-response manner at low dose; also sensitizes COLO 205 cells to TNF-alpha-induced programmed cell death.

CXF-009 is a potent, specific, dual-warhead covalent inhibitor of FGFR4 (IC50=48 nM), forms dual-warhead covalent bonds with two cysteine residues in FGFR4.CXF-009 forms covalent bonds with FGFR4(C477A) and FGFR4(C552A), respectively; display weak inhibition against FGFR1-3 with IC50 of 2579 nM, 2408 nM, and 977 nM.CXF-009 shows inhibitory effect agaginst FGFR4 muntants FGFR4(C477A), FGFR4(C552A), and FGFR4(C477A, C552A) with IC50 of 193 nM, 602 nM, and 1528 nM, respectively.CXF-009 inhibited the growth of Ba/F3 cells transformed with FGFR1-4 with IC50 values of 1562 nM, 1971 nM, 777 nM, and 38 nM, respectively.CXF-009 is slightly more reactive to GSH than PRN1371.

CXCR7 modulator 20 is a small molecule modulator of the atypical chemokine receptor CXCR7 with Ki of 52 nM.

CU7218 is a small-molecule inhibitor of 14-3-3 protein, inhibits the interaction between 9J10 and 14-3-3, displaces FOXO3a and other substrate proteins from 14-3-3 and reproduces the cellular phenotypes induced by 9J10 expression.

CU-72 is a potent, selective TLR7/8 dual inhibitor with IC50 of 5.10 and 2.87 uM, respectively.

C-type natriuretic peptide (CNP, pGC-B activator) is the native particulate guanylyl cyclase B receptor (pGC-B) activator.CNP induces anti-remodeling actions in the heart and kidney through the generation of the second messenger cGMP.CNP selectively activates pGC-B and generates cGMP in vitro.CNP is abundantly expressed in the endothelium and kidneys as well as the heart, but to lesser extent than trial natriuretic peptide (ANP) and b-type natriuretic peptide (BNP).CNP is produced as a prohormone that is cleaved intracellularly by the enzyme, furin, to yield a 53-AA intermediate form (C53).

CTN1122 (CTN-1122) is a potent, selective Leishmaniacasein kinase 1 isoform 2 (CK1.2, L-CK1.2) with IC50 of 0.72 uM (LmCK1) and 0.8 uM (amastigotes L. major), antileishmanial compound.

CTCB-405 (CTCB405) is a small molecule allosteric inhibitor of T. brucei phosphofructokinase (TbPFK) with IC50 of 0.18 uM, ITC Kd of 92 nM, no significant inhibition of human PFKs.CTCB-405 demonstrated in vitro parasite killing potency of the bloodstream form of T. brucei strain Lister 427 (EC50=0.37 uM).CTCB-405 (50, 100 mg/kg) clear parasites in a stage 1 model of HAT infection with 1-day oral dosing and show reduction of parasitaemia in the brain in a pleiomorphic model.

CS640 (CS-640) is a potent, selective CaMK1D inhibitor with nanomolar range at both the enzymatic and cellular levels.CS640 prevent Aβ induced tau hyperphosphorylation in culture, but were not able to protect cells from Aβ induced toxicity.CS640 was able to ablate Aβ induced increased tau phosphorylation at Thr181 in mouse primary neurons.

CRL inhibitor 33-11 is a small moelcule E3 CRL inhibitor, directly and selectively binds to the purified E3 ROC1-CUL4A CTD and ROC1-CUL1 CTD complex with Kd of 0.223 and 4.53 uM, respecitvely.CRL inhibitor 33-11 binds to ROC1-CUL1 more effectively than ROC1-CUL1-Nedd8.CRL inhibitor 33-11 showed the ability to inhibit ubiquitination by ROC1–CUL1 more potently than that by ROC1-CUL1-Nedd8.CRL inhibitor 33-11 inhibited the ubiquitination of CK1α by CRL4CRBN in vitro.

CRCM5484 is a potent, BET BDII-selective inhibitor with IC50 of 130/20/71 nM for BRD4-BD2/BRD3-BD2/BRD2-BD2, respectively.CRCM5484 displays 475-fold selectivity over its first bromodomain (BRD3-BD2 vs BRD3-BD1).CRCM5484 demonstrates very low activity in various cell-based assays.CRCM5484 modulates the anti-leukemic activity in combination with various FDA-approved and/or in-development drugs in a cell- and context-dependent differential manner.

CPL500036 (CPL-500036) is a highly potent, selective and orally bioavailable PDE10A inhibitor with IC50 of 35 nM.CPL500036 is highly selective for PDE10A over other PDEs and common off-targets.CPL500036 effectively penetrates the brain where increases cAMP/cGMP levels and phosphorylates effector proteins like AMPA subunits.CPL500036 reduced sensorimotor deficits in 6-OHDA-lesioned rats.Acute and chronic CPL500036 did not reduce effects of L-DOPA in sensorimotor tests.Chronic CPL500036 treatment did not decrease L-DOPA-induced contralateral rotation.

CPL302-253 is a potent, selective inhibitor of PI3Kδ with IC50 of 12.2 nM and Kd of 0.83 nM, >350-fold selectivity over PI3K isoforms α, β, and γ (IC50>4,500 nM); CPL302-253 displays no off-target interaction in KinomeScan assays. CLP302-253 blocks activation of primary lymphoid cells in vitro, blocks IL-33 cytokine production in epithelial and T cell co-cultures. CLP302-253 bocks eosinophil infiltration to the lungs and IL-33 expression in HDM induced asthma mouse model.

Cotadutide (MEDI-0382) is a dual GLP-1/glucagon receptor peptide agonist with robust anti-obesity and metabolic effects.