ZINC 17988990 is a potent, selective inhibitor of TRPV5 mediated currents, inhibits rbTRPV5/hTRPV5 with IC50 of 106/177 nM, showing marked selectivity for TRPV5 over TRPV6.ZINC 17988990 shows no activity on other TRP channels (TRPV1, TRPV3, TRPV4 and TRPM8) at 1-3 uM, and moderate inhibition on TRPV3 and TRPM8 at >10 uM.ZINC17988990 (10 uM) fully inhibited Ca2+ signals elicited by application of external Ca2+ in HEK293 cells transfected with TRPV5, but had no effect in cells expressing TRPV6.

Maleimide-DOTA is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

a KRASG12D degrader for the treatment of solid tumors.

INT-777 is a semisynthetic bile acid that acts as an agonist of TGR5 (EC50 = 0.82 μM). INT-777 mitigates inflammatory response in human endometriotic stromal cells: A therapeutic implication for endometriosis.

ABT-702 is a potent non-nucleoside adenosine kinase inhibitor (IC50 = 1.7 nM), selective over other sites of adenosine interaction (A1, A2A and A3 receptors, adenosine transporter and adenosine deaminase).

F17464 is a dopamine D3 receptor preferential antagonist exhibiting high affinity for human dopamine receptor subtype 3 (hD3) (Ki=0.17 nM) and 5-HT1a (Ki=0.16 nM) and a >50 fold lower affinity for the human dopamine receptor subtype 2 short and long form (hD2s/l) (Ki=8.9 and 12.1 nM, respectively). F17464 is a D3 receptor antagonist, 5-HT1a receptor partial agonist. F17464 blocks ketamine induced morphological changes, an effect D3 receptor mediated, in human dopaminergic neurons. F17464 increases dopamine release in the rat prefrontal cortex and mouse lateral forebrain-dorsal striatum and seems to reduce the effect of MK801 on % c-fos mRNA medium expressing neurons in cortical and subcortical regions. F17464 also rescues valproate induced impairment in a rat social interaction model of autism, with dose range 0.32-2.5 mg/kg i.p. in both rats and mice

NCP26 is a potent, ATP-competitive prolyl-tRNA synthetase (ProRS, PRS) inhibitor, inhibits recombinant human ProRS in the presence of 100 μM proline with KD of 0.35 nM in TR-FRET assays.

Solriamfetol (JZP-110) is a selective dopamine and norepinephrine reuptake inhibitor with robust wake-promoting effects. Solriamfetol binds to dopamine and norepinephrine transporters, so it can inhibit reuptake of dopamine and norepinephrine. Solriamfetol treatment significantly improves the ability to stay awake and subjective symptoms of excessive sleepiness in adults with narcolepsy.

Solriamfetol hydrochloride (JZP-110, R-228060, ADX-N05, YKP-10A) is a norepinephrine-dopamine reuptake inhibitor that inhibits dopamine and norepinephrine transporter with IC50 of 2.9 and 4.4 uM, respectively.

BB-83698 is a peptide deformylase inhibitor and potent antimicrobial with excellent activity against streptococci and Moraxella catarrhalis strains.

Q308 is a small molecule that silences the latent HIV-1 provirus by inhibiting Tat-mediated gene transcription and selectively downregulates the expression levels of the facilitated chromatin transcription (FACT) complex.Q308 induced the preferential apoptosis in HIV-1 latently infected cells, Q308 may reduce the size of the viral reservoir.

Seladelpar is a selective peroxisome proliferator-activated receptor (SPPAR) -δ receptor agonist.

BI-9774 (BI 9774) is a potent pan-AMPK activator with EC50 of 64 nM in an ADP-Glo kinase assay with human AMPK (α1β1γ1) and EC50 of 8 nM in a cellular GLUT4 translocation assay.

PXS-4748 (PXS4748) is a potent, selective and irreversible pan-lysyl oxidase (pan-LOX) inhibitor with IC50 of 2.0 uM and 3.2/0.6/1.4/0.2 uM for bovine (aorta) LOX and rh LOXL1/2/3/4, respectively.

AD-9308 is a water-soluble, orally bioavailable, potent, and highly selective ALDH2 activator, AD-9308 is a valine ester prodrug of a potent and selective small molecule ALDH2 activator AD-5591.

Lu AA41178 is a potent, pan-selective Kv7.2-7.5 opener with EC50 of 1.5, 0.6 20.5, and 37.0 uM for Kv7.2, Kv7.2/7.3, Kv7.4 and Kv7.5, respectively.Lu AA41178 displays no activity at Kv7.1 channels, has no potentiating impact on currents through GABAA ion channels, and a clean off-target profile against common cardiac ion channels.Lu AA41178 significantly increased the seizure thresholds in mice, demonstrating anticonvulsant efficacy in the maximum electroshock seizure threshold test and PTZ seizure threshold test.Lu AA41178 demonstrated antipsychotic-like activity by reducing amphetamine-induced hyperlocomotion in mice as well as lowering conditioned avoidance responses in rats, significantly reduced immobility in mouse model with antidepressant predictivity.

KT-413 (example I-3) is a potent IRAK degrader.

NX-1607 (Compound 23) is an inhibitor of Cbl-b, an E3 enzyme in the ubiquitin-proteasome pathway, with an IC50 value of less than 1 nM. NX-1607 can be used in cancer research.

NX-5948,be also known as BTK-IN-24,is an oral BTK degrader.

CFT8634 is an oral activity degrader targeting BRD9 extracted from patent WO2021178920A1 compound 174. CFT8634 can be used for the research of synovial sarcoma and SMARCB1-deleted solid tumors.

CFT1946 is an orally active and selective target ligand for BRAF kinase.

Alprostadil(Caverject) is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation. Prostaglandin E1 can be used as a vasodilator for the research of peripheral vascular diseases.

CPAG-1 (PGRMC2 activator CPAG-1) is a small-molecule activator of PGRMC2. CPAG-1 treatment had no effect on weight or food intake but treated mice had reduced fasting glycemia and insulin levels. CPAG-1 decreased Rev-Erbα protein in BAT of CPAG-1-treated mice. CPAG-1 also significantly increased labile heme in the nucleus of brown adipocytes from CPAG-1-treated mice within 4 days of treatment.

Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%).

Enfumafungin, a triterpene glycoside, is isolated from extracts derived from an endophytic species of Hormonema. Enfumafungin is an antifungal compound that is acting on the fungal cell wall, as the (1,3)-beta-D-glucan synthase inhibitor. Enfumafungin is specific for yeasts and fungi (excluding Cryptococcus) and does not inhibit the growth of Bacillus subtilis[1][2].

BRD5814 is a potent, selective, highly brain penetrant β-arrestin biased dopamine D2 receptor (D2R) antagonist with Ki of 0.27 uM.

ZINC 39395747 is a novel potent derivative of propylthiouracil that functions as a cell-active inhibitor of cytochrome b5 reductase 3 (CYB5R3) with IC50 of 9.14 uM.

Diarylpropionitrile (DPN) is a non-steroidal estrogen receptor β(ERβ) selective ligand, demonstrates the neuroprotective effects against 10 0M Aβ1-42-induced oxidative stress and inflammation in primary rat cortical cell culture.

A potent and selective GPER/GPR30 agonist with Ki of 11 nM, EC50 of 2 nM.