ChEMBL logo


ChEMBL Statistics
  Loading Statistics...

Target Report Card

Target Name and Classification

Target ID CHEMBL5251
Preferred Name Tyrosine-protein kinase BTK
Synonyms AGMX1 | ATK | ATK | Agammaglobulinemia tyrosine kinase | B-cell progenitor kinase | BPK | BPK | BTK | Bruton tyrosine kinase | Tyrosine-protein kinase BTK
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > tk protein kinase group > tyrosine protein kinase tec family

Target Components

Component Description Relationship Accession
Tyrosine-protein kinase BTK SINGLE PROTEIN Q06187

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1873475 IBRUTINIB Tyrosine-protein kinase BTK inhibitor 4 FDA
CHEMBL3301600 SPEBRUTINIB BESYLATE Tyrosine-protein kinase BTK inhibitor 2 PubMed
CHEMBL3544928 ONO-4059 Tyrosine-protein kinase BTK inhibitor 1 Other PubMed
CHEMBL3544969 HM-71224 Tyrosine-protein kinase BTK inhibitor 1 ClinicalTrials PubMed
CHEMBL3545193 MSC-2364447 Tyrosine-protein kinase BTK inhibitor 1 Other

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000010671
Ensembl ENSG00000010671
GO Cellular Component GO:0005634 (nucleus)
GO:0005737 (cytoplasm)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0016020 (membrane)
GO:0031234 (extrinsic component of cytoplasmic side of plasma membrane)
GO:0031410 (cytoplasmic vesicle)
GO:0043231 (intracellular membrane-bounded organelle)
GO:0045121 (membrane raft)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0004672 (protein kinase activity)
GO:0004713 (protein tyrosine kinase activity)
GO:0004715 (non-membrane spanning protein tyrosine kinase activity)
GO:0005102 (receptor binding)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0005547 (phosphatidylinositol-3,4,5-trisphosphate binding)
GO:0008289 (lipid binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0042802 (identical protein binding)
GO:0046872 (metal ion binding)
GO Biological Process GO:0001818 (negative regulation of cytokine production)
GO:0002250 (adaptive immune response)
GO:0002376 (immune system process)
GO:0002721 (regulation of B cell cytokine production)
GO:0002755 (MyD88-dependent toll-like receptor signaling pathway)
GO:0002902 (regulation of B cell apoptotic process)
GO:0006351 (transcription, DNA-templated)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006468 (protein phosphorylation)
GO:0006915 (apoptotic process)
GO:0007169 (transmembrane receptor protein tyrosine kinase signaling pathway)
GO:0007249 (I-kappaB kinase/NF-kappaB signaling)
GO:0007498 (mesoderm development)
GO:0016310 (phosphorylation)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0019722 (calcium-mediated signaling)
GO:0035556 (intracellular signal transduction)
GO:0038083 (peptidyl-tyrosine autophosphorylation)
GO:0038095 (Fc-epsilon receptor signaling pathway)
GO:0042113 (B cell activation)
GO:0042127 (regulation of cell proliferation)
GO:0045087 (innate immune response)
GO:0045579 (positive regulation of B cell differentiation)
GO:0048469 (cell maturation)
GO:0050853 (B cell receptor signaling pathway)
GO:0051092 (positive regulation of NF-kappaB transcription factor activity)
GO:0097190 (apoptotic signaling pathway)
Wikipedia Bruton%27s_tyrosine_kinase

Target Cross References - Protein

canSAR Q06187
CGD Agammaglobulinemia, X-linked; Agammaglobulinemia and isolated hormone deficiency; Hypogammaglobulinemia, X-linked
Human Protein Atlas ENSG00000010671
IntAct Q06187
Guide to Pharmacology 1948
Open Targets ENSG00000010671
PharmGKB PA25454
Pharos Q06187 (Tclin)
Reactome R-HSA-1236974 (ER-Phagosome pathway.)
R-HSA-166058 (MyD88:Mal cascade initiated on plasma membrane.)
R-HSA-2029482 (Regulation of actin dynamics for phagocytic cup formation.)
R-HSA-2424491 (DAP12 signaling.)
R-HSA-2871809 (FCERI mediated Ca+2 mobilization.)
R-HSA-5602498 (MyD88 deficiency (TLR2/4).)
R-HSA-5603041 (IRAK4 deficiency (TLR2/4).)
R-HSA-5663213 (RHO GTPases Activate WASPs and WAVEs.)
R-HSA-983695 (Antigen activates B Cell Receptor (BCR) leading to generation of second messengers.)
UniProt B2RAW1 Q06187 Q32ML5

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR000980 (SH2.)
IPR001245 (Ser-Thr/Tyr_kinase_cat_dom.)
IPR001452 (SH3_domain.)
IPR001562 (Znf_Btk_motif.)
IPR001849 (PH_domain.)
IPR008266 (Tyr_kinase_AS.)
IPR011009 (Kinase-like_dom.)
IPR011993 (PH_dom-like.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR020635 (Tyr_kinase_cat_dom.)
Pfam PF00017 (SH2)
PF00018 (SH3_1)
PF00169 (PH)
PF00779 (BTK)
PF07714 (Pkinase_Tyr)

Target Cross References - Structure

PDBe 1B55 1BTK 1BWN 1K2P 2Z0P 3GEN 3K54 3OCS 3OCT 3P08 3PIX 3PIY 3PIZ 3PJ1 3PJ2 3PJ3 4NWM 4OT5 4OT6 4OTF 4OTQ 4OTR 4RFY 4RFZ More...
CREDO 1B55 1BTK 1BWN 1K2P 2Z0P 3GEN 3K54 3OCS 3OCT 3P08 3PIX 3PIY 3PIZ 3PJ1 3PJ2 3PJ3 4NWM 4OT5 4OT6 4OTF 4OTQ 4OTR 4RFY 4RFZ More...