General Information of Target

Target ID LDTP01991
Target Name Plasma kallikrein (KLKB1)
Gene Name KLKB1
Gene ID 3818
Synonyms
KLK3; Plasma kallikrein; EC 3.4.21.34; Fletcher factor; Kininogenin; Plasma prekallikrein; PKK) [Cleaved into: Plasma kallikrein heavy chain; Plasma kallikrein light chain]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MILFKQATYFISLFATVSCGCLTQLYENAFFRGGDVASMYTPNAQYCQMRCTFHPRCLLF
SFLPASSINDMEKRFGCFLKDSVTGTLPKVHRTGAVSGHSLKQCGHQISACHRDIYKGVD
MRGVNFNVSKVSSVEECQKRCTSNIRCQFFSYATQTFHKAEYRNNCLLKYSPGGTPTAIK
VLSNVESGFSLKPCALSEIGCHMNIFQHLAFSDVDVARVLTPDAFVCRTICTYHPNCLFF
TFYTNVWKIESQRNVCLLKTSESGTPSSSTPQENTISGYSLLTCKRTLPEPCHSKIYPGV
DFGGEELNVTFVKGVNVCQETCTKMIRCQFFTYSLLPEDCKEEKCKCFLRLSMDGSPTRI
AYGTQGSSGYSLRLCNTGDNSVCTTKTSTRIVGGTNSSWGEWPWQVSLQVKLTAQRHLCG
GSLIGHQWVLTAAHCFDGLPLQDVWRIYSGILNLSDITKDTPFSQIKEIIIHQNYKVSEG
NHDIALIKLQAPLNYTEFQKPICLPSKGDTSTIYTNCWVTGWGFSKEKGEIQNILQKVNI
PLVTNEECQKRYQDYKITQRMVCAGYKEGGKDACKGDSGGPLVCKHNGMWRLVGITSWGE
GCARREQPGVYTKVAEYMDWILEKTQSSDGKAQMQSPA
Target Type
Successful
Target Bioclass
Enzyme
Family
Peptidase S1 family, Plasma kallikrein subfamily
Subcellular location
Secreted
Function
Participates in the surface-dependent activation of blood coagulation. Activates, in a reciprocal reaction, coagulation factor XII/F12 after binding to negatively charged surfaces. Releases bradykinin from HMW kininogen and may also play a role in the renin-angiotensin system by converting prorenin into renin.
TTD ID
T82739
Uniprot ID
P03952
DrugMap ID
TTMF8H9
Ensemble ID
ENST00000264690.11
HGNC ID
HGNC:6371
ChEMBL ID
CHEMBL2000

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C781(1.75)  LDD3335  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 BRX29 C31(1.23)  LDD2270  [1]
 LDCM0023  KB03 BRX29 C31(2.00)  LDD2687  [1]
 LDCM0024  KB05 MONO-MAC-6 C781(1.75)  LDD3335  [1]

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840