T1467

Acemetacin (TVX 1322) is a carboxymethyl ester of indometacin and a potent non-steroidal anti-inflammatory drug derived from indol-3-acetic acid, with its activity primarily attributed to its active metabolite, indomethacin. In clinical trials, acemetacin shows better gastric tolerability compared to indomethacin.

BMS-688521 BMS-688521 is an orally active and potent inhibitor of LFA-1/ICAM interaction, a small molecule antagonist of leukocyte function-associated antigen-1 (LFA-1), with potential anti-inflammatory activity.

Motixafortide (BKT140 4-fluorobenzoyl) is an antagonist of CXCR4 (IC50: 1 nM). BMS-1166 hydrochloride is an inhibitor of PD-1/PD-L1 interaction (IC50: 1.4 nM). BMS-1166 rivalries the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.

BMS-193885 is a selective, brain-penetrant, and competitive antagonist of the neuropeptide Y1 receptor with a Ki of 3.3 nM, and an IC50 of 5.9 nM for hY1.

BMS-248360 is a potent, orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ETA) receptor, with Kis of 10 nM and 1.9 nM for hAT1 and hETA receptors, respectively. BMS-248360 demonstrates hypertensive effects[1].

BMS 299897 is a sulfonamide γ-secretase inhibitor with an IC50 of 7 nM for inhibiting Aβ production in HEK293 cells stably overexpressing amyloid precursor protein (APP).

BMS-509744 is a selective, ATP-competitive Itk inhibitor with an IC50 of 19 nM. It inhibits IL-8 expression and HIV infection, ameliorates pulmonary inflammation in allergic asthma mouse models, and reduces Imiquimod-induced skin inflammation in mice.

BMS-564929 is a highly effective androgen receptor (AR) agonist that upregulates the expression and activity of lipogenic enzymes, reduces VAT content and lipid content, and downregulates the expression of acetyl-CoA carboxylase, FASN, and SCD.

BMS-690514 is a potent, orally active inhibitor of EGFR and VEGFR, with IC50 values of 5 nM for EGFR, 20 nM for HER 2, and 60 nM for HER 4.

BMS-819881, a melanin-concentrating hormone receptor 1 (MCHR1) antagonist, binds rat MCHR1 with a Ki of 7 nM, and is selective and potent for CYP3A4 activity with an EC50 of 13 μM.

XL041 (BMS-852927) is an agonist selective for LXRβ.