PD1-PDL1-IN 1 TFA (compound 16) is a potent inhibitor of programmed cell death 1 (PD-1), functioning as an immune modulator [1].

PD1-PDL1-IN 2 (ZE132) is a potent, selective inhibitor of PD-1/PD-L1, exhibiting significant anti-tumor activity in vivo. It enhances cytotoxic T-cell tumor infiltration and stimulates IL-2 expression, while also strongly inhibiting TGF-β [1] mRNA expression, showcasing its comprehensive immunotherapeutic potential.

PD1-PDL1-IN 1 is a potent inhibitor of programmed cell death 1 (PD-1),and used as immune modulator.

BMS-1 (PD-1/PD-L1 inhibitor 1) is an inhibitor of the PD1-PD-L1 protein-protein interaction. It also acts as an immunomodulator. Programmed death ligand 1 (PD-L1) is a protein in humans that is encoded by the CD274 gene and the upregulation of PD-L1 allows Ys to evade the host immune system. High tumor expression of PD-L1 was associated with increased tumor aggressiveness and a 4.5-fold increased risk of death.

BMS-202 (PD1-PDL1 inhibitor 2) is an inhibitor of the PD-1 (Programmed death- 1) /PD-Ll (Programmed death-ligand 1) protein/protein interaction.

CU-CPD107 is a selective agonist of toll-like receptor 8 (TLR8) and also shows activation activity against ssRNA ligands. CU-CPD107 acts as an inhibitor of TLR8 signaling in the presence of R848 (IC50=13.7 μM). CU-CPD107 exhibited coagonist activity in the presence of ssRNA, while CU-CPD107 alone could not affect TLR8 signal transduction.

PD-1/PD-L1-IN-10 is an orally active PD-1/PD-L1 inhibitor (IC50 of 2.7 nM) with potent anticancer efficacy.

PD150606 is a selective nonpeptide calpain inhibitor with neuroprotective activity that inhibits μ-calpains and m-calpains. Inhibits erythrocyanine-induced Ca2+ efflux and interferes with excitotoxicity-dependent motor neuron death.

PD153035 hydrochloride (ZM 252868) is a effective and selective inhibitor of EGFR (Ki: 5.2 pM, IC50: 29 pM); few influence against FGFR, PGDFR, InsR, CSF-1, and Src.

Sex Pheromone Inhibitor iPD1 is a compound that functions as an inhibitor of the sex pheromone cPD1 [1].

CMPD167 (MRK-1) is a potent, orally active inhibitor of CCR5 with significant in vitro antiviral efficacy [1].

CMPD1 is a non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor(apparent Ki (Kiapp): 330 nM).

PD-1-IN-22 is a potent programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction inhibitor(IC50 of 92.3 nM).

BMS202 hydrochloride (1675203-84-5(free base)) (PD-1/PD-L1 inhibitor 2 hydrochloride) is a small-molecule PD-1/PD-L1 interaction inhibitor (IC50: 18 nM). Biophysical studies demonstrate that BMS202 binds directly to PD-L1. Binding of BMS202 promotes PD-L1 dimerisation and blocks the PD-L1/ PD1 interaction.

PD-1/PD-L1-IN-9, with an IC50 of 3.8 nM, is a potent and orally active inhibitor of the PD-1/PD-L1 interaction. It enhances the immune cells' ability to kill tumor cells and demonstrates significant antitumor activity in vivo in a CT26 mouse model.

PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and PKC.

PD176252 is a potent BB1 and BB2 antagonist with inhibitory effects on BB1 and BB2 receptors.PD176252 acts as a small molecule GRPR inhibitor and FPR1/FPR2 agonist to inhibit the growth and proliferation of a variety of cancer cells.

PD168,077 is an agonist of dopamine D4 receptor. It has a facilitatory effect on memory consolidation.

CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively.

PD180970 is an inhibitor of Bcr-Abl with IC50s of 5 nM, 0.8 nM and 50 nM for the autophosphorylation of p210Bcr-Abl, Src and Kit. PD180970 can be used in studies about chronic myelogenous leukemia.

PD 173212 is a blocker that blocks N-type voltage sensitive calcium channel (Cav2.2). PD173212 (0.0017-1.7 μmol/kg, Intraperitoneal Injection.) dose-dependently reduced DNBS-induced visceral hypersensitivity in mice.

PD146176 (NSC-168807) is an inhibitor of 15-Lipoxygenase (15-LO) , it inhibits rabbit reticulocyte 15-LO with Ki of 197 nM and IC50 of 0.54 μM. PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice.

PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin.

PD10 is a dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), exhibiting inhibitory potency at human AChE (hAChE IC50: 0.56 μM), electric eel AChE (eeAChE IC50: 0.59 μM), and equine serum BuChE (eqBuChE IC50: 1.06 μM). It is utilized in research pertaining to Alzheimer’s disease [1].

PD159790 is an selective inhibitor of ECE-1.

PD128907 HCl is a potent and selective dopamine D3 receptor agonist, with EC50 of 0.64 nM, exhibits 53-fold selectivity over dopamine D2 receptor.

PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for FGFR1 than PDGFR and c-Src.

PD153035 is a ATP-competitive EGFR inhibitor with an IC50 and Ki of 25 and 6 pM. PD153035 effectively blocks the enhancement of mitogenesis, induction of early gene expression, and oncogenic transformation that occur in response to EGF receptor stimulation. With human fibroblasts and epidermoid carcinoma cells, PD153035 at nanomolar concentrations rapidly inhibits EGFR autophosphorylation. With breast and ovarian cancer cells, PD153035 not only blocks cell growth via inhibition of EGFR, but also upregulates the expression of the tumor suppressor retinoic acid receptor-beta 2 (RAR-beta2).

PD173952 is an inhibitor of Src family kinase.

PD184161 is a novel, orally-active MEK inhibitor. PD184161 inhibited MEK activity (IC50 = 10-100 nM) in a time- and concentration-dependent manner[1].

PD-159206 is a nucleocapsid inhibitor. It exhibits good antiviral activity against HIV.

PD153035 (NSC-669364) hydrochloride is an effective and selective inhibitor of EGFR (Ki/IC50: 5.2/29 pM, in cell-free assays); little inhibitory against FGFR, PGDFR, InsR, CSF-1 and Src.

PD 158780 reversibly inhibits auto and transphosphorylation of all four members of the ErbB receptor superfamily: EGFR, ErbB2, ErbB3, and ErbB4 (IC50s: 8μM, 49 nM, 52 nM, and 52 nM in cell assay).

Cadonilimab (AK104) is a humanized antibody engineered from the IgG1 scaffold and targets PD1/CTLA4. It is utilized in the research of metastatic cervical cancer [1] [2].

Lipustobart is an IgG4-kappa humanized monoclonal antibody targeting PDCD1 (programmed cell death 1, PD1, PD-1, CD279), with immunostimulant and antineoplastic activity [1].

MYCi975 (NUCC-0200975) is an orally active inhibitor of MYC.

PD-1/PD-L1-IN 3 TFA inhibits the binding of human PD-1 to PD-Ll with an IC50 of 9 nM.

Evunzekibart (ATOR-1017) is an Fc-γ receptor-dependent 4-1BB agonist and an IgG4 isotype antibody. It can function as a monotherapy or synergize with anti-PD1 therapies to promote anti-tumor effects.

TNG260 is a CoREST-selective deacetylase ( CoreDAC ) inhibitor. TNG260 inhibits HDAC1 with 10-fold selectivity over HDAC3 . TNG260 leads to HDAC1 inhibition, reverses anti-PD1 resistance driven by loss of STK11. TNG260 decreases intratumoral infiltration of neutrophils. TNG260 exhibits immune-mediated cell killing .

PD-1-IN-18 is a PD1 inhibitor of signaling pathway, and acts as an immunomodulator.

HPK1-IN-7 is an orally active HPK1 inhibitor. It shows selectivity against IRAK4 (59 nM) and GLK (140 nM).

PROTAC PD-1/PD-L1 degrader-1 is a PD-L1 degrading PROTAC that inhibits PD-1/PD-L1 interaction (IC50: 39.2 nM). PROTAC PD-1/PD-L1 degrader-1 restores immunity in Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model of suppressed immunity, which reduces the protein content of PD-L1 in a lysosomal-dependent manner.

PD-1/PD-L1-IN 5 is an inhibitor of PD-1/PD-L1 protein/protein interaction (IC50 of ≤100 nM).

PD-1/PD-L1-IN-NP19, a PD-1/PD-L1 inhibitor, exhibits an IC50 of 12.5 nM against the human PD-1/PD-L1 interaction, potentially activating the tumor immune microenvironment and contributing to its antitumor effects[1].

MYCi361 (NUCC-0196361) is an inhibitor of MYC (binding to MYC with Kd of 3.2 μM).