at 1001

AT-1001 is an α3β4 nAChR partial agonist. AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats. AT-1001 also potently and reversibly blocks epibatidine-induced inward currents in HEK cells transfected with α3β4 nAChR. Importantly, AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding. When tested in a nucleus accumbens (NAcs) synaptosomal preparation, AT-1001 inhibits nicotine-induced [³H]dopamine release poorly and at significantly higher concentrations compared with mecamylamine and conotoxin MII.

BMS-1001 is a potent inhibitor of PD-1 PD-L1 interaction(IC50 : 2.25 nM, in a homogenous time-resolved fluorescence binding assay).

ORY-1001 is a KDM1A inhibitor (IC50 <20nM) with high selectivity against related FAD dependent aminoxidases (MAO-A/B, IL4I1, KDM1B >100uM, SMOX 7uM). Treatment of THP-1 (MLL-AF9) cells with ORY-1001, results in a time/dose dependent me2H3K4 accumulation a

GL-1001 disodium tetrahydrate is an ACE2 inhibitor.

DPM-1001 is an orally bioavailable and non-competitive protein-tyrosine phosphatase (PTP1B) inhibitor (IC50: 100 nM) with the anti-diabetic property.

(S)-BI-1001 is an active S-enantiomer of BI-1001. (S)-BI-1001 has antiviral potency against HIV-1 integrase (IC50: 28 nM, and EC50: 450 nM and a Kd: 4.7 μM).

INO-1001 is a potent, selective poly(ADP-ribose) polymerase (PARP) inhibitor with antitumor activity.INO-1001 is a potent radiosensitization enhancer that uses interference with DNA repair mechanisms to enhance radiation-induced cell killing and necrotic cell death.

ATM-1001 is an inhibitor of the cancer-associated tropomyosin 3.1 (Tpm3.1), suppressing glucose-stimulated insulin secretion (GSIS) from the pancreatic islets.

GL-1001 sodium salt is an ACE2 inhibitor.

DPM-1001 trihydrochloride, an analog of the specific protein-tyrosine phosphatase (PTP1B) inhibitor MSI-1436, is a potent, specific, non-competitive, orally active inhibitor of PTP1B with an IC50 of 100 nM, exhibiting anti-diabetic properties.

INO-1001 methanesulfonate is an isoindolinone derivative and potent inhibitor of the nuclear enzyme poly (ADP-ribose) polymerase (PARP) with chemosensitization and radiosensitization properties.

BMS-1001 hydrochloride is an orally active inhibitor of human PD-1/PD-L1 immune checkpoint with low-toxicity in cells.BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. BMS-1001 is capable of alleviating the PD-1/PD-L1 immune checkpoint-mediated exhaustion of Jurkat T-lymphocytes.

3-Aminobenzamide (PARP-IN-1) is a potent PARP inhibitor (IC50 < 50 nM in CHO cells) and mediates oxidant-induced myocyte dysfunction during reperfusion.

ORY1001 (ORY 1001) is an orally active and selective lysine-specific demethylase LSD1 KDM1A inhibitor, with high selectivity against related FAD dependent aminoxidases with IC50 of <20 nM.

DS-1001b is an inhibitor of mutant IDH-1 (Isocitrate Dehydrogenase-1)

M1001 is a HIF-2α agonist.

JAMI1001A is a positive allosteric modulator of the AMPA receptor, effectively modulating the deactivation and desensitization of both [flip] and [flop] receptor isoforms.

SR 1001 is an inverse agonist for RORα/RORγ (Kis: 172/111 nM).

T1001 is an antagonist of hypoxia-inducible factor-2α subunit (HIF-2α) which displaces residue M252 from inside the HIF-2α PAS-B pocket toward the ARNT subunit to weaken heterodimerization.

Iadademstat dihydrochloride (ORY-1001(trans)) , a Potent and Selective Covalent KDM1A/LSD1 Inhibitor, for the Treatment of Acute Leukemia.

Kahweol oleate is emi-syntetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1 induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.

Kahweol linoleate is a semi-syntetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1 induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.

Kahweol stearate is a semi-synthetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1-induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.

Kahweol Acetate is a semi-synthetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1 induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.

Kahweol has anticarcinogenic, anti-angiogenic,and anti-inflammatory activities, it can block the LPS-induced activation of NF-kappaB by preventing IkappaB degradation and inhibiting IkappaB kinase activity.