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Approval Year

Unknown
149,124
Substance Class Protein
Protein Sub Type
Sequence Type COMPLETE
Record UNII
SBH6S6T2J2
Record Status Validated (UNII)
Record Version
Subunit 0

Related Record Type Details
Structure of Zelebrudomide
DEGRADER->TARGET
Kd
18 NANOMOLAR [15 to 21] (average)
Structure of JNJ-64264681
INHIBITOR -> TARGET
k(inactivation)
0.0003 sec-1 [0.0003 to 0.0004] (average)
Structure of Catadegbrutinib
DEGRADER->TARGET
PRECLINICAL
Structure of Acalabrutinib
INHIBITOR -> TARGET
Structure of Civorebrutinib
INHIBITOR -> TARGET
Structure of FENEBRUTINIB
INHIBITOR -> TARGET
Structure of ORELABRUTINIB
INHIBITOR -> TARGET
Structure of NX-5948
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 BMS-986142
INHIBITOR -> TARGET
Structure of Zanubrutinib
INHIBITOR -> TARGET
IRREVERSIBLE INHIBITOR
Structure of ELSUBRUTINIB
INHIBITOR -> TARGET
IRREVERSIBLE INHIBITOR
Structure of Docirbrutinib
INHIBITOR -> TARGET
IN-VITRO
IC50
Structure of IBRUTINIB
INHIBITOR -> TARGET
Structure of Cinsebrutinib
INHIBITOR -> TARGET
PRECLINICAL
Structure of 5-[4-[4-[[1-[4-(2,4-dioxo-1,3-diazinan-1-yl)-3-methylphenyl]piperidin-4-yl]methyl]piperazin-1-yl]-3-fluoroanilino]-3-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]-1,2,4-triazine-6-carboxamide
DEGRADER->TARGET
Structure of TAK-020
INHIBITOR -> TARGET
Structure of Nemtabrutinib
INHIBITOR -> TARGET
Structure of POSELTINIB
INHIBITOR -> TARGET
Structure of BRANEBRUTINIB
INHIBITOR -> TARGET
Structure of Tirabrutinib
INHIBITOR -> TARGET

Structural Modifications

Modification Type Location Site Location Type Residue Modified Extent Fragment Name Fragment Approval
AMINO_ACID_SUBSTITUTION [1_142] [1_153] [1_154] [1_164] SITE_SPECIFIC C3H1-TYPE ZINC FINGER JKX41V9FYM
AMINO ACID SUBSTITUTION [1_20] [1_54] [1_114] [1_622] [1_658] DEXFOSFOSERINE VI4F0K069V
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT CHEMICAL
NIH
NCATS
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