Details of the Target

General Information of Target

Target ID LDTP03329
Target Name Cathepsin S (CTSS)
Gene Name CTSS
Gene ID 1520
Synonyms
Cathepsin S; EC 3.4.22.27
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MKRLVCVLLVCSSAVAQLHKDPTLDHHWHLWKKTYGKQYKEKNEEAVRRLIWEKNLKFVM
LHNLEHSMGMHSYDLGMNHLGDMTSEEVMSLMSSLRVPSQWQRNITYKSNPNRILPDSVD
WREKGCVTEVKYQGSCGACWAFSAVGALEAQLKLKTGKLVSLSAQNLVDCSTEKYGNKGC
NGGFMTTAFQYIIDNKGIDSDASYPYKAMDQKCQYDSKYRAATCSKYTELPYGREDVLKE
AVANKGPVSVGVDARHPSFFLYRSGVYYEPSCTQNVNHGVLVVGYGDLNGKEYWLVKNSW
GHNFGEEGYIRMARNKGNHCGIASFPSYPEI
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Peptidase C1 family
Subcellular location
Lysosome
Function
Thiol protease. Key protease responsible for the removal of the invariant chain from MHC class II molecules and MHC class II antigen presentation. The bond-specificity of this proteinase is in part similar to the specificities of cathepsin L.
TTD ID
T68290
Uniprot ID
P25774
DrugMap ID
TTUMQVO
Ensemble ID
ENST00000368985.8
HGNC ID
HGNC:2545
ChEMBL ID
CHEMBL2954

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
MFE296 SNV: p.Y39Ter .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Alkylaryl probe 2
 Probe Info  		18.00  LDD0391  [1]
Alkylaryl probe 1
 Probe Info  		4.00  LDD0388  [1]
Alkylaryl probe 3
 Probe Info  		4.78  LDD0283  [2]
DBIA
 Probe Info  		C213(1.65)  LDD3312  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 KMS11 C126(0.90)  LDD2422  [3]
 LDCM0023  KB03 KMS11 C126(1.43)  LDD2839  [3]
 LDCM0024  KB05 HMCB C213(1.65)  LDD3312  [3]
 LDCM0099  Phenelzine MDA-MB-231 4.78  LDD0283  [2]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Rg7625 . D0DQ2D
Phase 1
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Sar-114137 . D08KIB
Vby- 036 . D07ODC
Vby- 891 . D01REJ
Vby-129 . D07UKF
Preclinical
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
L-006235-1 Small molecular drug D0Z0PR
Ro5461111 . DC9J1Y
Investigative
Click To Hide/Show 53 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fsn-0503 Antibody D0G3PK
2-[(2',3',4'-trifluorobiphenyl-2-yl)Oxy]Ethanol Small molecular drug D0M8WX
2-[(2'3'4'-trifluorobiphenyl-2-yl)Oxy]Ethanol Small molecular drug DB08611
4-cycloheptyl-6-propylpyrimidine-2-carbonitrile Small molecular drug D0U4TY
4-cyclooctyl-6-propylpyrimidine-2-carbonitrile Small molecular drug D01JGB
4-propyl-6-m-tolylpyrimidine-2-carbonitrile Small molecular drug D04BGT
6-(3-(Trifluoromethyl)Phenyl)Picolinonitrile Small molecular drug D01IFO
Ac-hphe-leu-ala-leuvsme Small molecular drug D05VEV
Ac-hphe-leu-gly-leuvsme Small molecular drug D09GZQ
Ac-hphe-leu-phe-leuvsme Small molecular drug D06NEB
Cbz-glu(Otbu)-ala-leuvsme Small molecular drug D0K0KT
Cbz-ile-hphe-ala-leuvsme Small molecular drug D0RL4S
Cbz-ile-leu-ala-leuvsme Small molecular drug D0I0MU
Cbz-ile-meto2-ala-leuvsme Small molecular drug D0B3US
Cbz-ile-phe-ala-leuvsme Small molecular drug D01NCW
Cbz-ile-pro-ala-leuvsme Small molecular drug D05MDE
Cbz-ile-t-butylgln-ala-leuvsme Small molecular drug D09IMK
Cbz-ile-t-butylhomoglu-ala-leuvsme Small molecular drug D0QY3R
E-64 Small molecular drug D09FGQ
Fucose Small molecular drug D0G6XS
Gnf-pf-5434 Small molecular drug D0L9VP
Jnj-10329670 Small molecular drug D0V5LJ
L-873724 Small molecular drug D0D0LD
N-(1-oxobutan-2-yl)-3-(Trifluoromethyl)Benzamide Small molecular drug D02FPU
N-(2-naphthylsulfonyl)-glycyl-glycine-nitrile Small molecular drug D07SOQ
N-(4-phenylbenzoyl)-phenylalanyl-glycine-nitrile Small molecular drug D07RSA
N-(Benzyloxycarbonyl)-leucyl-glycine-nitrile Small molecular drug D0G8OD
N-(Tert-butoxycarbonyl)-isoleucyl-glycine-nitrile Small molecular drug D01YNC
N-(Tert-butoxycarbonyl)-leucyl-glycine-nitrile Small molecular drug D09AHN
N-(Tert-butoxycarbonyl)-methionyl-glycine-nitrile Small molecular drug D0U0XG
N-(Tert-butoxycarbonyl)-norleucyl-glycine-nitrile Small molecular drug D07FLB
N-(Tert-butoxycarbonyl)-norvalyl-glycine-nitrile Small molecular drug D0A7ER
N-(Tert-butoxycarbonyl)-tyrosyl-glycine-nitrile Small molecular drug D0JF8D
N-(Tert-butoxycarbonyl)-valyl-glycine-nitrile Small molecular drug D06VIP
N-acetyl-phenylalanyl-glycine-nitrile Small molecular drug D0A8OV
N-benzoyl-phenylalanyl-glycine-nitrile Small molecular drug D0JN8Q
P2,P3 Ketoamide Derivative Small molecular drug D05WZF
Pmid22686657c(R)-26 Small molecular drug D06WQP
(1r)-2-[(Cyanomethyl)Amino]-1-({[2-(Difluoromethoxy)Benzyl]Sulfonyl}Methyl)-2-oxoethyl Morpholine-4-carboxylate . DB08195
Am-3840 . D08WDP
Bf/Pc-18 . D0P5RJ
Clik60 . D0Y8LO
Morpholine-4-carboxylic Acid (1-(3-benzenesulfonyl-1-phenethylallylcarbamoyl)-3-methylbutyl)-amide . DB03837
Morpholine-4-carboxylic Acid [1-(2-benzylsulfanyl-1-formyl-ethylcarbamoyl)-2-phenyl-ethyl]-amide . DB03984
Morpholine-4-carboxylic Acid [1s-(2-benzyloxy-1r-cyano-ethylcarbamoyl)-3-methyl-butyl]Amide . DB03767
N-(1-cyanocyclopropyl)-3-({[(2s)-5-oxopyrrolidin-2-yl]Methyl}Sulfonyl)-n~2~-[(1s)-222-trifluoro-1-(4-fluorophenyl)Ethyl]-l-alaninamide . DB07587
N-[(1s)-1-{1-[(1r3e)-1-acetylpent-3-en-1-yl]-1h-123-triazol-4-yl}-12-dimethylpropyl]Benzamide . DB07878
N-[(1s)-2-[(4-cyano-1-methylpiperidin-4-yl)Amino]-1-(Cyclohexylmethyl)-2-oxoethyl]Morpholine-4-carboxamide . DB08752
N-[(1s)-2-{[(1r)-2-(Benzyloxy)-1-cyano-1-methylethyl]Amino}-1-(Cyclohexylmethyl)-2-oxoethyl]Morpholine-4-carboxamide . DB08755
N-[1-(Aminomethyl)Cyclopropyl]-3-(Benzylsulfonyl)-n~2~-[(1s)-222-trifluoro-1-(4-hydroxyphenyl)Ethyl]-l-alaninamide . DB07589
N-[1-(Aminomethyl)Cyclopropyl]-3-(Morpholin-4-ylsulfonyl)-n~2~-[(1s)-222-trifluoro-1-(4-fluorophenyl)Ethyl]-l-alaninamide . DB07520
N~2~-13-benzoxazol-2-yl-3-cyclohexyl-n-{2-[(4-methoxyphenyl)Amino]Ethyl}-l-alaninamide . DB07839
Vby- 285 . D0J0HV
Patented
Click To Hide/Show 10 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Oxotetrahydro-2-h-furo[3.2-b]Pyrrol-4(5-h)-yl Derivative 1 Small molecular drug D0QM0D
Phenylalanine Derivative 1 Small molecular drug D01MKD
Pmid25399719-compound-17 Small molecular drug D06LLT
Pmid27998201-compound-12 Small molecular drug D06XCD
Pmid27998201-compound-15 Small molecular drug D0MR9V
Pmid27998201-compound-17 Small molecular drug D06XTA
Pmid27998201-compound-5 Small molecular drug D05OIU
Pmid27998201-compound-6 Small molecular drug D0X1AF
Pmid27998201-compound-7 Small molecular drug D0JD5W
Pmid27998201-compound-9 Small molecular drug D04VGR
Discontinued
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cra-028129 . D0K0IW
Rg-7236 . D0D3KG

References

1 Hydrazines as versatile chemical biology probes and drug-discovery tools for cofactor-dependent enzymes. bioRxiv, 2020-06.
2 Activity-Based Hydrazine Probes for Protein Profiling of Electrophilic Functionality in Therapeutic Targets. ACS Cent Sci. 2021 Sep 22;7(9):1524-1534. doi: 10.1021/acscentsci.1c00616. Epub 2021 Aug 19.
3 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