BTK

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Catalog No. Information Product Use Citations Product Validations
S2680

Ibrutinib (PCI-32765)

Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.

S7173

CC-292 (AVL-292)

CC-292 (AVL-292) is a covalent, orally active, and highly selective BTK inhibitor with IC50 of <0.5 nM, displaying at least 1400-fold selectivity over the other kinases assayed. Phase 1.

S7257

CNX-774

CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM.

S7080

RN486

RN486 is a potent and selective BTK inhibitor with IC50 of 4 nM.

S7734

LFM-A13

LFM-A13 is a specific Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 2.5 μM, >100-fold selectivity over other protein kinases including JAK1, JAK2, HCK, EGFR,and IRK.

S8116New

ACP-196

Acalabrutinib(ACP-196) is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. ACP-196 has improved target specificity over ibrutinib with 323-, 94-, 19- and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC, respectively) and no activity against EGFR.

S7877

ONO-4059 analogue

ONO-4059 analogue is an analogue of ONO-4059, which is a highly potent and selective oral BTK inhibitor with IC50 of 23.9 nM. Phase 1.

S7051

CGI1746

CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM.

Catalog No. Information Product Use Citations Product Validations
S2680

Ibrutinib (PCI-32765)

Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.

S7173

CC-292 (AVL-292)

CC-292 (AVL-292) is a covalent, orally active, and highly selective BTK inhibitor with IC50 of <0.5 nM, displaying at least 1400-fold selectivity over the other kinases assayed. Phase 1.

S7257

CNX-774

CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM.

S7080

RN486

RN486 is a potent and selective BTK inhibitor with IC50 of 4 nM.

S7734

LFM-A13

LFM-A13 is a specific Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 2.5 μM, >100-fold selectivity over other protein kinases including JAK1, JAK2, HCK, EGFR,and IRK.

S8116New

ACP-196

Acalabrutinib(ACP-196) is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. ACP-196 has improved target specificity over ibrutinib with 323-, 94-, 19- and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC, respectively) and no activity against EGFR.

S7877

ONO-4059 analogue

ONO-4059 analogue is an analogue of ONO-4059, which is a highly potent and selective oral BTK inhibitor with IC50 of 23.9 nM. Phase 1.

S7051

CGI1746

CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM.