U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Approval Year

Unknown
139594
Substance Class Protein
Created
by admin
on Sat Dec 16 12:12:27 GMT 2023
Edited
by admin
on Sat Dec 16 12:12:27 GMT 2023
Protein Sub Type
Sequence Type COMPLETE
Record UNII
SBH6S6T2J2
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TYROSINE-PROTEIN KINASE BTK
Common Name English
BRUTON TYROSINE KINASE
Common Name English
BPK
Common Name English
AGMX1
Common Name English
BRUTON'S TYROSINE KINASE
Common Name English
B-CELL PROGENITOR KINASE
Common Name English
AGAMMAGLOBULINEMIA TYROSINE KINASE
Common Name English
ATK
Common Name English
Classification Tree Code System Code
EU-Orphan Drug EU/3/17/1951
Created by admin on Sat Dec 16 12:12:28 GMT 2023 , Edited by admin on Sat Dec 16 12:12:28 GMT 2023
Code System Code Type Description
UNIPROT
Q06187
Created by admin on Sat Dec 16 12:12:28 GMT 2023 , Edited by admin on Sat Dec 16 12:12:28 GMT 2023
PRIMARY
PHAROS
Q06187
Created by admin on Sat Dec 16 12:12:28 GMT 2023 , Edited by admin on Sat Dec 16 12:12:28 GMT 2023
PRIMARY
FDA UNII
SBH6S6T2J2
Created by admin on Sat Dec 16 12:12:28 GMT 2023 , Edited by admin on Sat Dec 16 12:12:28 GMT 2023
PRIMARY
Related Record Type Details
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DEGRADER->TARGET
Structure of JNJ-64264681
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k(inactivation)
Structure of ACALABRUTINIB
INHIBITOR -> TARGET
Acalabrutinib forms a covalent bond with Cys481 in the BTK adenosine triphosphate (ATP).
IRREVERSIBLE INHIBITOR
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INHIBITOR -> TARGET
INHIBITOR
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INHIBITOR -> TARGET
Structure of FENEBRUTINIB
INHIBITOR -> TARGET
Structure of TAK-020
INHIBITOR -> TARGET
IRREVERSIBLE INHIBITOR
Structure of ORELABRUTINIB
INHIBITOR -> TARGET
Structure of BRANEBRUTINIB
INHIBITOR -> TARGET
IRREVERSIBLE INHIBITOR
IC50
NX-5948 free base
DEGRADER->TARGET
NX-5948 is a chimeric targeting molecule (CTM) that induces the degradation of BTK in cells through recruitment of cereblon (CRBN), an adaptor protein of the E3 ubiquitin ligase complex, and promotes the formation of a ternary complex of CRBN, NX-5948, and BTK. Within this complex, ubiquitin is transferred to BTK directing it for degradation by the proteasome
PRECLINICAL
Structure of Rocbrutinib
INHIBITOR -> TARGET
IN-VITRO
Structure of Tirabrutinib
INHIBITOR -> TARGET
IRREVERSIBLE INHIBITOR
IC50
Structure of BMS-986142
INHIBITOR -> TARGET
human whole blood assay (hWB) measuring BCR stimulated CD69 expression on B cells
COMPETITIVE INHIBITOR
IC50
Structure of ELSUBRUTINIB
INHIBITOR -> TARGET
IRREVERSIBLE INHIBITOR
Structure of Milrebrutinib
INHIBITOR -> TARGET
IN-VITRO
IC50
Structure of ZANUBRUTINIB
INHIBITOR -> TARGET
IRREVERSIBLE INHIBITOR
Structure of Cinsebrutinib
INHIBITOR -> TARGET
PRECLINICAL
Structure of POSELTINIB
INHIBITOR -> TARGET
Structure of IBRUTINIB
INHIBITOR -> TARGET
Binds to a cysteine residue (Cys-481) in the BTK active site
IRREVERSIBLE INHIBITOR
IC50
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT CHEMICAL
NIH
NCATS
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