Angiogenesis

Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1.

RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4.

PAR-2-IN-1 is a protease-activated receptor-2 (PAR2) signaling pathway inhibitor with anti-inflammatory and anticancer effects.

Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist.

Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation.

N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620. SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.

αvβ1 integrin-IN-1 (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC50 of 0.63 nM.

RO0270608, the active metabolite of R411, is a dual alpha4beta1-alpha4beta7 (α4β1/α4β7) integrin antagonist.

Protease-Activated Receptor-1, PAR-1 Agonist TFA is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist TFA corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor.

BTK inhibitor 17 is a potent and orally active irreversible BTK inhibitor with an IC50 of 2.1 nM.

Pirtobrutinib is a highly selective, non-covalent, reversible Bruton's tyrosine kinase (BTK) inhibitor, with IC 50 values of 3.2nM and 1.4nM for BTK and BTK C481S , respectively.

SJF620 hydrochloride is a PROTAC connected by ligands for Cereblon and Btk with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN.

BMS-587101 is a potent and orally active antagonist of leukocyte function associated antigen-1 (LFA-1).

TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor with an IC50 and a Ki of 1.5 nM and 11.9 nM, respectively.

Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively.

Valategrast (R-411 free base) is a potent and orally active integrin α4β1 (VLA-4) and α4β7 dual antagonist.

SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist.

Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist.

(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK.

BIIB091 is a highly selective, reversible and orally active BTK inhibitor for treating autoimmune diseases.

TAK-020 is a covalent Btk inhibitor, which becomes the clinical candidate.

Valategrast hydrochloride (R-411) is a potent integrin α4β1 (VLA-4) and α4β7 dual antagonist.

Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM).