| DC48043 |
BIIB091
|
BIIB091 is a novel reversible, selective, potent BTK inhibitor with Kd of 0.07 nM. |
| DC47717 |
TAK-020
|
TAK-020 is a covalent Btk inhibitor, which becomes the clinical candidate. |
| DC42420 |
Tolebrutinib
|
Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib can be used for the research of multiple sclerosis (MS). |
| DC40447 |
N-piperidine Ibrutinib hydrochloride
|
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.
|
| DC39103 |
Remibrutinib (LOU064)
|
Remibrutinib (LOU064) is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases. |
| DC28073 |
CNX-500
|
CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn. |
| DC11914 |
Poseltinib
|
Poseltinib (HM-71224, LY-3337641) is a potent and selective, covalent inhibitor of Btk with IC50 of 1.95 nM. |
| DC8358 |
ONO-4059(Tirabrutinib)
|
ONO-4059 is a novel Small Molecule Dual Inhibitor Of Bruton’s Tyrosine Kinase (Btk) and Tec Kinase. |
| DC9942 |
GDC-0853(RG7845)
|
GDC-0853 is orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. |
| DC74379 |
DZD8586
|
DZD8586 is an oral, non-covalent, BBB penetrant LYN and BTK dual inhibitor, overcomes resistance mutations to the approved covalent and non-covalent BTK inhibitors. |
