A peptide, non-selective melanocortin receptor agonist for treatment for female sexual dysfunction; selectively stimulates solicitational behaviors in the female rat, without affecting lordosis, pacing, or other sexual behaviors, does not cause generalized motor activation; a peptide analogue of α-MSH.

AC1-IN-38 is a potent, selective inhibitor of adenylyl cyclase type 1 (AC1) with IC50 of 0.54 uM.AC1-IN-38 shows selectivity over a closely related isoform AC8, and no activity against AC2/5 and other common neurological targets.AC1-IN-38 displayed modest antiallodynic effects in a mouse model of inflammatory pain.

AEP07 (AEP 07) is a selective small molecule inhibitor of PARP4 (vPARP) inhibitor with IC50 of 0.8 uM, >12-fold selective over other PARP family members.

AGH-107 is a potent, selective 5-HT7 receptor agonist with Ki of 6 nM and EC50 of 19 nM, 176-fold selectivity over 5-HT1AR.AGH-107 exhibited high selectivity over related CNS targets, high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures.

ARN 23746 (ARN-23746) is a potent, selective inhibitor of Na+-K+-Cl- importer NKCC1, shows NKCC1 inhibition 31.8% at 10 uM, and 95.2% at 100 uM in the Cl− influx assay on NKCC1-transfected HEK293 cells.ARN23746 did not show significant NKCC2 inhibition and KCC2 inhibition at 10 uM.ARN23746 selectively blocks NKCC1 in a human cell line and restore the physiological [Cl−]i in murine DS neurons in culture, has excellent solubility and metabolic stability, and displays no issues with off-target activity in vitro.ARN23746 demonstrated in vivo efficacy in rescuing cognitive impairment in a DS mouse model and social deficits and repetitive behaviors in an autism mouse model.

AS105 (AS-105) is a highly potent, ATP-competitive CaMKII inhibitor, inhibits CaMKIIδ with IC50 of 8 nM, Ki of 3 nM. AS105 is also effective against autophosphorylated CaMKII (in contrast to the commonly used allosteric CaMKII-inhibitor KN-93). In isolated atrial cardiomyocytes from human donors and ventricular myocytes from CaMKIIδC-overexpressing mice with heart failure, AS105 effectively reduced diastolic SR Ca2+ leak by 38% to 65% as measured by Ca2+-sparks or tetracaine-sensitive shift in [Ca2+]i. AS105 effectively reduced SR Ca2+-leak, thus improving SR Ca2+-accumulation and reducing cellular arrhythmogenic correlates, without negatively influencing excitation-contraction coupling.

ASP8302 (ASP 8302) is a potent, selective, positive allosteric modulator (PAM) of muscarinic M3 receptor.Threonine 230 (Thr 230) is the amino acid essential for the PAM effect of ASP8302.

Asundexian, also known as BAY2433334 and BI1265162, is a blood coagulation factor XIa inhibitor. Asundexian binds directly to the active site of FXIa and thereby inhibits its activity.

AZ13102909 (AZ909) is a potent and selrctive TBK1 inhibitor with IC50 of 5 nM, 100-1000 fold greater for other related kinases.AZ909 combines with AZD6244 to enhance apoptosis in AZD6244-resistant lines in 3D culture.

AZ5576 (AZ-5576) is a potent, selective CDK9 inhibitor with an IC 50 <5 nM, decreases phosphorlyation of Ser2-RNAPII in cells with an IC 50 of 96 nM.AZ5576 downregulated Mcl-1 and MYC protein abundance across multiple tested DLBCL cell lines and in primary DLBCL cells.MYC sensitizes DLBCL cells to AZ5576, genetic downregulation of MYC in U-2932 and OCI-LY19 cells resulted in diminished susceptibility to AZ5576.AZ5576 dose-dependently downregulated MYC transcription of a luciferase reporter containing multiple canonical MYC-MAX-binding sites, an effect more pronounced compared with multi-CDK inhibitor dinaciclib.AZ5576 restricts growth of xenografted DLBCL tumors in vivo.

AZD4604 (AZD-4604) is a potent, selective Janus-associated kinase 1 (JAK1) inhibitor with anti-inflammatory effect.

AZD4625 is a potent, selective, covalent allosteric inhibitor of mutant GTPase KRAS G12C with IC50 of 3 nM, inhibitor H358 cell proliferation with GI50 of 4 nM.AZD4625 is a clinical development candidate for the treatment of KRASG12C positive tumors.

BAY2666605 is a potent, small molecule PDE3A-SLFN12 complex inducer with EC50 of 7 nM.BAY2666605 triggers the formation of a complex of two proteins called SLFN12 and PDE3A. This complex drive cancer cells into cell death by a mechanism called apoptosis.

BAY-747 (BAY747) is a novel potent, selective, brain-penetrant soluble guanylate cyclase (sGC) stimulator.

BFL-1 inhibitor 4E14 (4E14) is a potent, selective, covalent BFL-1 inhibitor that disrupt BH3-binding activity with IC50 of 1.3 uM, targets a unique C55 residue in the BFL-1 groove.4E14 blocks BFL-1 suppression of BAX-mediated mitochondrial apoptosis.

BI 1265162 is a potent ENaC inhibitor, inhibits Na+ transport with IC50 3 nM and 8 nM in M1 and NCI-H441 cells, respectively.BI 1265162 dose-dependently inhibited Na+ transport and decreased water resorption in cell line models.BI 1265162 reduced liquid absorption in rat lungs and increased MCC in sheep, with no effects on renal function in the animal models.BI 1265162 alone and in combination with CF transmembrane conductance regulator (CFTR) modulators decreased water transport and increased MCC in both normal and CF airway human epithelial models.

BI-4924 (BI 4924) is a potent, selective NADH/NAD+-competitive PHGDH inhibitor with IC50 of 2 nM.BI-4924 splays high selectivity against the majority of other dehydrogenase targets.

BMS-986202 (BMS 986202) is potent, selective Tyk2 inhibitor that binds to Tyk2 JH2 domain with IC50 of 0.19 nM, Ki of 0.02 nM, >10,000-fold over 273 kinases and pseudokinases; BMS-986202 demonstrated cellular activity (IL-23 IC50=12 nM) in IL-23 stimulated reporter assay (in Kit225 T cells). BMS-986202 also binds Jak1 JH2 with an IC50 of 7.8 nM, but this enzymatic binding did not lead to any functional activities, as BMS-986202 displayed an activity (IC50) of greater than 12.5 μM in the IL-2 stimulated Jak1/3-dependent cellular assay. BMS-986202 showed in vivo efficacy in mouse models of IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus.

BMS-986313 is a potent, selective, orally active RORγt inverse agonist with EC50 of 3.6 nM in GAL-4 reporter assay in Jurkat cell line, and 50 nM in IL-17 human whole blood assay.BMS-986313 demonstrated robust efficacy in preclinical models of psoriasis (the IMQ-induced skin lesion model and the IL-23-induced acanthosis model).

BT173 is a small molecule allosteric inhibitor of HIPK2-Smad3 interaction, specifically inhibits the TGF-β1/Smad3 pathway.BT173 disrupts HIPK2-Smad3 protein-protein interaction (PPI) without significant inhibition of HIPK2 kinase activity or inhibition of p53 activation.BT173 inhibits Smad3 phosphorylation in human kidney cells in vitro.BT173 significantly attenuated renal fibrosis development in the UUO mice, significantly decreased Smad3 phosphorylation and α-SMA expression in the UUO kidneys.Treatment of BT173 ameliorated kidney fibrosis in Tg26 mice.

CCR4-IN-38 (CCR4-351) is a potent, selective, orally bioavailable CCR4 antagonist with IC50 of 50 nM (Chemotaxis inhibition).CCR4-IN-38 inhibits the recruitment of Treg into the tumor microenvironment (TME).CCR4-IN-38 elicits antitumor responses as a single agent or in combination with an immune checkpoint blockade.

CDDD11-8 is a potent CDK9 inhibitor co-targeting FLT3-ITD with Ki values of 8 and 13 nM, respectively.CDDD11-8 displays excellent kinome selectivity in a panel of 369 human kinases.CDDD11-8 displays antiproliferative activity against leukemia cell lines, and particularly potent effects against MV4-11 and MOLM-13 cells, which are known to harbor the FLT3-ITD mutation and mixed lineage leukemia (MLL) fusion proteins.CDDD11-8 causes a robust tumor growth inhibition by oral administration in animal xenografts, induces tumor regression at dose of 125 mg/kg.