General Information of the Protein
Protein ID
PT03989
Protein Name
Tyrosine-protein kinase BTK
Secondarily
Protein Name
Agammaglobulinemia tyrosine kinase
B-cell progenitor kinase
Bruton tyrosine kinase
Kinase EMB
Gene Name
BTK
Secondarily
Gene Name
Bpk
Sequence
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVIPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPTAAPISTTELKKVVALYDYMPMNANDLQLRKGEEYFILEESNLPWWRARDKNGQEGYIPSNYITEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVFAKSTGEPQGVIRHYVVCSTPQSQYYLAEKHLFSTIPELINYHQHNSAGLISRLKYPVSKQNKNAPSTAGLGYGSWEIDPKDLTFLKELGTGQFGVVKYGKWRGQYDVAIKMIREGSMSEDEFIEEAKVMMNLSHEKLVQLYGVCTKQRPIFIITEYMANGCLLNYLREMRHRFQTQQLLEMCKDVCEAMEYLESKQFLHRDLAARNCLVNDQGVVKVSDFGLSRYVLDDEYTSSVGSKFPVRWSPPEVLMYSKFSSKSDIWAFGVLMWEIYSLGKMPYERFTNSETAEHIAQGLRLYRPHLASERVYTIMYSCWHEKADERPSFKILLSNILDVMDEES
    Show/Hide
Organism
Mus musculus, Mouse
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase Tec family
Function
Non-receptor tyrosine kinase indispensable for B lymphocyte development, differentiation and signaling (PubMed:7538439, PubMed:8629002, PubMed:10852954). Binding of antigen to the B-cell antigen receptor (BCR) triggers signaling that ultimately leads to B-cell activation (By similarity). After BCR engagement and activation at the plasma membrane, phosphorylates PLCG2 at several sites, igniting the downstream signaling pathway through calcium mobilization, followed by activation of the protein kinase C (PKC) family members (By similarity). PLCG2 phosphorylation is performed in close cooperation with the adapter protein B-cell linker protein BLNK (By similarity). BTK acts as a platform to bring together a diverse array of signaling proteins and is implicated in cytokine receptor signaling pathways (By similarity). Plays an important role in the function of immune cells of innate as well as adaptive immunity, as a component of the Toll-like receptors (TLR) pathway (PubMed:17725607). The TLR pathway acts as a primary surveillance system for the detection of pathogens and are crucial to the activation of host defense (By similarity). Especially, is a critical molecule in regulating TLR9 activation in splenic B-cells (By similarity). Within the TLR pathway, induces tyrosine phosphorylation of TIRAP which leads to TIRAP degradation (By similarity). BTK also plays a critical role in transcription regulation (By similarity). Induces the activity of NF-kappa-B, which is involved in regulating the expression of hundreds of genes (By similarity). BTK is involved on the signaling pathway linking TLR8 and TLR9 to NF-kappa-B (By similarity). Acts as an activator of NLRP3 inflammasome assembly by mediating phosphorylation of NLRP3 (PubMed:34554188). Transiently phosphorylates transcription factor GTF2I on tyrosine residues in response to BCR (PubMed:11120822, PubMed:16738337). GTF2I then translocates to the nucleus to bind regulatory enhancer elements to modulate gene expression (PubMed:11120822, PubMed:16738337). ARID3A and NFAT are other transcriptional target of BTK (PubMed:11120822, PubMed:16738337). BTK is required for the formation of functional ARID3A DNA-binding complexes (PubMed:11120822, PubMed:16738337). There is however no evidence that BTK itself binds directly to DNA (PubMed:11120822, PubMed:16738337). BTK has a dual role in the regulation of apoptosis (By similarity).
    Show/Hide
Uniprot ID
Primary ID:
P35991

Secondarily ID:
Q61365
    Show/Hide
Ensembl ID
ENSG00000010671
Subcellular Location
Cytoplasm
Cell membrane
Nucleus
Membrane raft
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000898 , Bone marrow macrophage immortalized BALB/c
Compound ID Compound Name Compound Formula
CP0222116
N-[2,6-difluoro-3-[5-[(5-methyl-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-2-yl)amino]-6-oxo-1H-pyridazin-3-yl]phenyl]-1-benzothiophene-2-carboxamide
   Show/Hide
C26H21F2N7O2S
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0321452
N-[2-methyl-3-[5-[(5-methyl-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-2-yl)amino]-6-oxo-1H-pyridazin-3-yl]phenyl]-1-benzothiophene-2-carboxamide
   Show/Hide
C27H25N7O2S
 1
1
IC50 = 41 nM
   TI
   LI
   LO
   TS
CP0516578
N-[2-fluoro-5-[5-[(5-methyl-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-2-yl)amino]-6-oxo-1H-pyridazin-3-yl]phenyl]-1-benzothiophene-2-carboxamide
   Show/Hide
C26H22FN7O2S
 1
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0436344
4-tert-butyl-N-[6-fluoro-2-methyl-3-[5-[(5-methyl-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-2-yl)amino]-6-oxo-1H-pyridazin-3-yl]phenyl]benzamide
   Show/Hide
C29H32FN7O2
 1
1
IC50 = 54 nM
   TI
   LI
   LO
   TS
CP0321460
5-tert-butyl-N-[6-fluoro-2-methyl-3-[5-[(5-methyl-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-2-yl)amino]-6-oxo-1H-pyridazin-3-yl]phenyl]pyrazine-2-carboxamide
   Show/Hide
C27H30FN9O2
 1
1
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0016550
N-[6-fluoro-2-methyl-3-[5-[(5-methyl-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-2-yl)amino]-6-oxo-1H-pyridazin-3-yl]phenyl]-1-benzothiophene-2-carboxamide
   Show/Hide
C27H24FN7O2S
 1
1
IC50 = 91 nM
   TI
   LI
   LO
   TS
CP0544925
N-[2-fluoro-6-methyl-3-[5-[(5-methyl-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-2-yl)amino]-6-oxo-1H-pyridazin-3-yl]phenyl]-1-benzothiophene-2-carboxamide
   Show/Hide
C27H24FN7O2S
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0559467
N-[2,6-dimethyl-3-[5-[(5-methyl-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-2-yl)amino]-6-oxo-1H-pyridazin-3-yl]phenyl]-1-benzothiophene-2-carboxamide
   Show/Hide
C28H27N7O2S
 1
1
IC50 = 387 nM
   TI
   LI
   LO
   TS
CP0197967
N-[6-fluoro-2-methyl-3-[5-[(5-methyl-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-2-yl)amino]-6-oxo-1H-pyridazin-3-yl]phenyl]thieno[3,2-b]pyridine-2-carboxamide
   Show/Hide
C26H23FN8O2S
 1
1
IC50 = 680 nM
   TI
   LI
   LO
   TS
CP0110048
N-[6-fluoro-2-methyl-3-[5-[(5-methyl-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-2-yl)amino]-6-oxo-1H-pyridazin-3-yl]phenyl]thieno[2,3-b]pyridine-2-carboxamide
   Show/Hide
C26H23FN8O2S
 1
1
IC50 = 740 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01308 Tyrosine-protein kinase BTK Homo sapiens, Human