CTSG

Summary

CTSG (cathepsin G, HGNC:2532) is a protein-coding gene on chromosome 14q12, encoding Cathepsin G (P08311). Serine protease with trypsin- and chymotrypsin-like specificity.

The protein encoded by this gene, a member of the peptidase S1 protein family, is found in azurophil granules of neutrophilic polymorphonuclear leukocytes. The encoded protease has a specificity similar to that of chymotrypsin C, and may participate in the killing and digestion of engulfed pathogens, and in connective tissue remodeling at sites of inflammation. In addition, the encoded protein is antimicrobial, with bacteriocidal activity against S. aureus and N. gonorrhoeae. Transcript variants utilizing alternative polyadenylation signals exist for this gene.

Source: NCBI Gene 1511 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 37 total
• Druggable target: yes — 5 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001911

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:2532
Approved symbol	CTSG
Name	cathepsin G
Location	14q12
Locus type	gene with protein product
Status	Approved
Aliases	CG
Ensembl gene	ENSG00000100448
Ensembl biotype	protein_coding
OMIM	116830
Entrez	1511

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 2 protein_coding, 1 retained_intron

ENST00000216336, ENST00000552252, ENST00000871534

RefSeq mRNA: 1 — MANE Select: NM_001911 NM_001911

CCDS: CCDS9631

Canonical transcript exons

ENST00000216336 — 5 exons

Exon	Start	End
ENSE00000654530	24574675	24574810
ENSE00000654531	24575265	24575412
ENSE00001267767	24573518	24573810
ENSE00003587359	24574245	24574499
ENSE00003841607	24576169	24576250

Expression profiles

Bgee: expression breadth ubiquitous, 194 present calls, max score 99.71.

FANTOM5 (CAGE): breadth broad, TPM avg 170.7860 / max 93504.4473, expressed in 201 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
142633	170.7860	201

Top tissues by expression

278 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
trabecular bone tissue	UBERON:0002483	99.71	gold quality
bone marrow cell	CL:0002092	99.18	gold quality
bone marrow	UBERON:0002371	99.00	gold quality
bone element	UBERON:0001474	96.87	gold quality
triceps brachii	UBERON:0001509	89.60	silver quality
gall bladder	UBERON:0002110	89.51	gold quality
skin of hip	UBERON:0001554	88.91	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	85.66	gold quality
monocyte	CL:0000576	85.33	gold quality
gluteal muscle	UBERON:0002000	85.32	silver quality
mononuclear cell	CL:0000842	84.95	gold quality
skin of leg	UBERON:0001511	84.38	gold quality
leukocyte	CL:0000738	83.81	gold quality
zone of skin	UBERON:0000014	83.19	gold quality
skin of abdomen	UBERON:0001416	82.41	gold quality
rectum	UBERON:0001052	82.22	gold quality
subcutaneous adipose tissue	UBERON:0002190	81.22	gold quality
right coronary artery	UBERON:0001625	80.76	gold quality
lower esophagus muscularis layer	UBERON:0035833	80.55	gold quality
lower esophagus	UBERON:0013473	80.47	gold quality
upper leg skin	UBERON:0004262	80.05	gold quality
vermiform appendix	UBERON:0001154	79.73	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	79.71	gold quality
upper arm skin	UBERON:0004263	78.05	gold quality
adipose tissue	UBERON:0001013	77.94	gold quality
apex of heart	UBERON:0002098	77.82	gold quality
connective tissue	UBERON:0002384	77.69	gold quality
caecum	UBERON:0001153	77.50	gold quality
mucosa of transverse colon	UBERON:0004991	77.47	gold quality
smooth muscle tissue	UBERON:0001135	77.03	gold quality

Single-cell (SCXA)

Detected in 16 experiment(s), a significant marker in 16.

Experiment	Marker?	Max mean expression
E-GEOD-89232	yes	17101.49
E-MTAB-6505	yes	6033.03
E-MTAB-8142	yes	1986.70
E-HCAD-6	yes	1777.98
E-MTAB-9067	yes	1356.71
E-GEOD-100618	yes	995.84
E-MTAB-8884	yes	649.60
E-GEOD-76312	yes	228.35
E-CURD-112	yes	40.89
E-CURD-88	yes	27.29
E-MTAB-8410	yes	15.67
E-CURD-122	yes	13.86
E-CURD-46	yes	10.61
E-GEOD-130148	yes	7.70
E-MTAB-9801	yes	6.31

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AHR, CEBPE, HHEX, KLF6, MTA3, MYB, RUNX1, SNAI1, SP1, SPI1, SSRP1, TFAP2A

miRNA regulators (miRDB)

8 targeting CTSG, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-3915	99.45	68.49	1905
HSA-MIR-487A-5P	98.85	69.37	993
HSA-MIR-487B-5P	98.85	69.48	987
HSA-MIR-7114-5P	98.51	67.87	1349
HSA-MIR-1278	97.75	67.55	628
HSA-MIR-3664-5P	96.74	66.56	770
HSA-MIR-3657	96.33	66.29	608
HSA-MIR-4757-3P	88.86	63.55	51

Literature-anchored findings (GeneRIF, showing 40)

• high molecular mass kininogen down-regulates cathepsin G-induced platelet activation by forming a complex with cathepsin G and thus prevents binding of cathepsin G to platelets (PMID:11920276)
• UVA light stimulates the production of cathepsin G and elastase-like enzymes by dermal fibroblasts: a possible contribution to the remodeling of elastotic areas in sun-damaged skin. (PMID:11928814)
• up-regulated by the AML1-MTG8 fusion protein, suggesting a role in the granulocytic maturation characteristic of the t(8;21) acute myelogenous leukemia (PMID:11986950)
• cathepsin G enhances fibrin deposition under flow conditions by elevating the activation state of fibrinogen-adherent platelets rather than by cleaving coagulation factors (PMID:12524437)
• BPI and cathepsin G are the major antigenic targets of ANCA seen in patients with systemic sclerosis (PMID:12784398)
• Serine proteinases cathepsin G and neutrophil elastase cooperate for the proteolytic regulation of CD87/urokinase receptor on monocytic cells. (PMID:14688365)
• role in development of myelodi leukemia with promyelocytic features (PMID:14737102)
• Cathepsin G initializes and dominates the destruction of intact myelin basic protein (MBP) by B cell-derived lysosomal extracts, degrading immunodominant MBP epitope and eliminating both its binding to HLA-DRB1*1501 and MBP-specific T cell response. (PMID:15100291)
• neutrophil elastase and cathepsin G are inhibited by PAI-1 mutants (PMID:15131125)
• Release of cathepsin G from neutrophils specifically down-regulates the responsiveness of neutrophils to C5a, and this effect may play a role in the down-regulation of acute inflammation. (PMID:15140022)
• down-regulation of CatG in macrophages is advantageous to M. tuberculosis bacilli and possibly is an important mechanism by which M. tuberculosis is able to evade the host immune defenses (PMID:15385470)
• oxidants generated by myeloperoxidase regulate cathepsin G activity in vivo (PMID:15967795)
• Neutrophil cathepsin G is the principal protease to produce CCL15 proteolytic products released in the course of hemofiltration of blood from renal insufficiency patients (PMID:16034099)
• PF-4 acts as an inhibitor of the CTAP-III-processing enzymes cathepsin G and chymase without becoming cleaved itself as a competitive substrate. (PMID:16317101)
• the monocyte chemotactic activity of cathepsin G may have a role in the pathogenesis of RA synovial inflammation (PMID:16977463)
• cathepsin g may play a role in the progression to heart failure by activating angiotensin II, leading to detrimental effects on the heart (PMID:17418861)
• Substrate specificity for cathepsin G is greatly enhanced when an aromatic side chain and a strong positive charge are incorporated in residue P(1). (PMID:17653609)
• Cathepsin G from neutrophils and monocytes may provide some pro-coagulant effect by activating FVIII. (PMID:18217133)
• The cleavage of neutrophil leukosialin (CD43) by cathepsin G releases its extracellular domain and triggers its intramembrane proteolysis by presenilin/gamma-secretase (PMID:18586676)
• Cathepsin G increases MMP expression in normal human fibroblasts through fibronectin fragmentation, and induces the conversion of proMMP-1 to active MMP-1. (PMID:18835135)
• Data report that the two subsets of human dendritic cells differ in their cathepsin distribution, and suggest tha Cathepsin G may be of functional importance. (PMID:19036358)
• MC are immunoreactive to cathepsin-G in human cutaneous mastocytosis, as well as the co-localization of tryptase and cathepsin-G in MC secretory granules. (PMID:19250736)
• both Cat-G and PAR(4) play key roles in generating and/or amplifying relapses in ulcerative colitis (PMID:19528350)
• Cathepsin G is one of the mediators responsible for complement-dependent opsonophagocytic killing of Streptococcus pneumoniae by human neutrophils. (PMID:19620298)
• Historical and recent data on CatG expression, distribution, function and involvement in disease will be summarized and discussed, with a focus on its role in antigen presentation and immune-related events. (PMID:19910052)
• CatG cleaves human leukocyte antigen (HLA)-DR in vitro. Cleavage occurred on the loop between fx1 and fx2 of the membrane-proximal beta2 domain. In vivo, however, the CatG cleavage site is sterically inaccessible or masked by associated molecules. (PMID:20331476)
• Neutrophil cathepsin G can either facilitate or impede coagulation via effects on thrombin generation. (PMID:20589323)
• Cathepsin G is an antimicrobial protein with bacteriocidal activity against S. aureus and N. gonorrhoeae. (PMID:2116408)
• distinct catK/C4-S interactions are necessary for the collagenolytic activity of the enzyme. (PMID:21193413)
• potential of HNE and CatG to be used as markers for early detection of infection. Significant differences in HNE and CatG levels in infected and non-infected wound fluids were observed. (PMID:21488974)
• CatG was found to be dispensable in invariant chain conversion within intact primary human B cells and dendritic cells. (PMID:21543057)
• Data suggested the notion that CatG plays a critical role in proinsulin processing and is important in the activation process of diabetogenic T cells. (PMID:21850236)
• major binding partners of LEKTI were found to be the antimicrobial peptide dermcidin and the serine protease cathepsin G and no kallikreins. (PMID:22588119)
• the targeting and suppression of CTSG by AML1-ETO in t(8;21) AML may provide a mechanism for leukemia cells to escape from the intracellular surveillance system by preventing degradation of foreign proteins. (PMID:22641217)
• NE and CG bind to the surface of cancer cells, presumably to a cell surface receptor, and subsequently undergo clathrin pit-mediated endocytosis. (PMID:22915586)
• A novel HLA-A*0201 restricted peptide derived from cathepsin G is an effective immunotherapeutic target in acute myeloid leukemia. (PMID:23147993)
• demonstrate that cathepsin G (CG), neutrophil elastase (NE), and to a lesser extent proteinase 3 (PR3), degrade endocan (PMID:23454598)
• Increased concentrations of cathepsins B, D and G in the proliferative eutopic endometrium may play a role in the implantation of endometrial tissue outside the uterine cavity. (PMID:23466190)
• Neutrophil cathepsin G is a physiologic modulator of platelet thrombus formation in vivo and has potential as a target for novel anti-thrombotic therapies. (PMID:23940756)
• proteolytic cleavage of PLTP by cathepsin G may enhance the injurious inflammatory responses that occur in COPD (PMID:24532668)

Cross-species orthologs

2 orthologs

Organism	Symbol	Gene ID
mus_musculus	Ctsg	ENSMUSG00000040314
rattus_norvegicus	Ctsg	ENSRNOG00000020647

Paralogs (6): CMA1 (ENSG00000092009), GZMH (ENSG00000100450), GZMB (ENSG00000100453), KLK6 (ENSG00000167755), KLK13 (ENSG00000167759), AZU1 (ENSG00000172232)

Protein

Protein identifiers

Cathepsin G — P08311 (reviewed: P08311)

All UniProt accessions (1): P08311

UniProt curated annotations — full annotation on UniProt →

Function. Serine protease with trypsin- and chymotrypsin-like specificity. Also displays antibacterial activity against Gram-negative and Gram-positive bacteria independent of its protease activity. Prefers Phe and Tyr residues in the P1 position of substrates but also cleaves efficiently after Trp and Leu. Shows a preference for negatively charged amino acids in the P2’ position and for aliphatic amino acids both upstream and downstream of the cleavage site. Required for recruitment and activation of platelets which is mediated by the F2RL3/PAR4 platelet receptor. Binds reversibly to and stimulates B cells and CD4(+) and CD8(+) T cells. Also binds reversibly to natural killer (NK) cells and enhances NK cell cytotoxicity through its protease activity. Cleaves complement C3. Cleaves vimentin. Cleaves thrombin receptor F2R/PAR1 and acts as either an agonist or an inhibitor, depending on the F2R cleavage site. Cleavage of F2R at ‘41-Arg-|-Ser-42’ results in receptor activation while cleavage at ‘55-Phe-|-Trp-56’ results in inhibition of receptor activation. Cleaves the synovial mucin-type protein PRG4/lubricin. Cleaves and activates IL36G which promotes expression of chemokines CXCL1 and CXLC8 in keratinocytes. Cleaves IL33 into mature forms which have greater activity than the unprocessed form. Cleaves coagulation factor F8 to produce a partially activated form. Also cleaves and activates coagulation factor F10. Cleaves leukocyte cell surface protein SPN/CD43 to release its extracellular domain and trigger its intramembrane proteolysis by gamma-secretase, releasing the CD43 cytoplasmic tail chain (CD43-ct) which translocates to the nucleus. Cleaves CCL5/RANTES to produce RANTES(4-68) lacking the N-terminal three amino acids which exhibits reduced chemotactic and antiviral activities. During apoptosis, cleaves SMARCA2/BRM to produce a 160 kDa cleavage product which localizes to the cytosol. Cleaves myelin basic protein MBP in B cell lysosomes at ‘224-Phe-|-Lys-225’ and ‘248-Phe-|-Ser-249’, degrading the major immunogenic MBP epitope and preventing the activation of MBP-specific autoreactive T cells. Cleaves annexin ANXA1 and antimicrobial peptide CAMP to produce peptides which act on neutrophil N-formyl peptide receptors to enhance the release of CXCL2. Acts as a ligand for the N-formyl peptide receptor FPR1, enhancing phagocyte chemotaxis. Has antibacterial activity against the Gram-negative bacteria N.gonorrhoeae and P.aeruginosa. Likely to act against N.gonorrhoeae by interacting with N.gonorrhoeae penA/PBP2. Exhibits potent antimicrobial activity against the Gram-positive bacterium L.monocytogenes. Has antibacterial activity against the Gram-positive bacterium S.aureus and degrades S.aureus biofilms, allowing polymorphonuclear leukocytes to penetrate the biofilm and phagocytose bacteria. Has antibacterial activity against M.tuberculosis. Mediates CASP4 activation induced by the Td92 surface protein of the periodontal pathogen T.denticola, causing production and secretion of IL1A and leading to pyroptosis of gingival fibroblasts. Induces platelet aggregation which is strongly potentiated in the presence of ELANE.

Subunit / interactions. (Microbial infection) Interacts with CASP4; the interaction is promoted by the Td92 surface protein of the periodontal pathogen T.denticola and leads to CASP4 activation. (Microbial infection) Interacts with M.tuberculosis protein Rv3364c. (Microbial infection) Interacts with S.aureus EapH1; EapH1 acts as a reversible inhibitor of CATG activity.

Subcellular location. Cell membrane. Cytoplasmic granule. Secreted. Cytoplasm. Cytosol. Lysosome. Nucleus.

Tissue specificity. Expressed in neutrophils (at protein level). Expressed in B cells.

Post-translational modifications. Two C-terminal truncation variants have been identified, one which ends at Arg-243 and one which ends at Ser-244.

Activity regulation. Inhibited by soybean trypsin inhibitor, benzamidine, the synthetic peptide R13K, Z-Gly-Leu-Phe-CH2Cl, phenylmethylsulfonyl fluoride, 3,4-dichloroisocoumarin, DFP, SBTI and alpha-1-antitrypsin. Inhibited by LPS from P.aeruginosa but not by LPS from S.minnesota. Not inhibited by elastinal, CMK, TLCK, ETDA or leupeptin. (Microbial infection) Inhibited reversibly by S.aureus EapH1. (Microbial infection) Activity is induced by the Td92 surface protein of the periodontal pathogen T.denticola.

Induction. Induced by the Td92 surface protein of the periodontal pathogen T.denticola. Down-regulated in monocytes following M.tuberculosis infection and exposure to bacterial lipopolysaccharide which coincides with increased M.tuberculosis replication and intracellular survival.

Similarity. Belongs to the peptidase S1 family.

RefSeq proteins (1): NP_001902* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001254	Trypsin_dom	Domain
IPR001314	Peptidase_S1A	Family
IPR009003	Peptidase_S1_PA	Homologous_superfamily
IPR018114	TRYPSIN_HIS	Active_site
IPR033116	TRYPSIN_SER	Active_site
IPR043504

Pfam: PF00089

Enzyme classification (BRENDA):

• EC 3.4.21.20 — cathepsin G (BRENDA: 9 organisms, 202 substrates, 132 inhibitors, 24 Km, 22 kcat entries)

Substrate kinetics (BRENDA)

14 substrates with measured Km, best-characterized 14. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
N-SUCCINYL-L-VAL-L-PRO-L-PHE-4-NITROANILIDE	0.12–3.1	8
N-BENZOYL-L-TYROSINE ETHYL ESTER	0.42–2.6	2
SUCCINYL-ALA-ALA-PRO-LEU-P-NITROANILIDE	2.7–3.9	2
7-METHOXYCOUMARIN-4-YL-ACETYL-PHE-VAL-THR-(4-GUA	0.0097	1
7-METHOXYCOUMARIN-4-YL-ACETYL-PHE-VAL-THR-(4-GUA	0.0099	1
7-METHOXYCOUMARIN-4-YL-ACETYL-PHE-VAL-THR-(4-GUA	0.0035	1
7-METHOXYCOUMARIN-4-YL-ACETYL-PHE-VAL-THR-(4-GUA	0.0032	1
7-METHOXYCOUMARIN-4-YL-ACETYL-PHE-VAL-THR-(4-GUA	0.0021	1
ACETYL-PHE-VAL-THR-(4-GUANIDINE-L-PHENYLALANYL)-	0.203	1
METHOXYSUCCINYL-L-ALANINE-L-ALANINE-L-PROLINE-L-	1.49	1
N-ACETYL-L-PHENYLALANINE-P-NITROPHENYL ESTER	0.52	1
N-SUCCINYL-ALA-ALA-PRO-PHE-4-NITROANILIDE	0.86	1
SUCCINYL-PHE-LEU-PHE-P-NITROANILIDE	0.24	1
METHOXYSUCCINYL-L-ALANINE-L-ALANINE-L-PROLINE-L-	—	0

UniProt features (39 total): strand 15, helix 4, active site 3, disulfide bond 3, propeptide 2, glycosylation site 2, chain 2, turn 2, region of interest 2, signal peptide 1, sequence variant 1, mutagenesis site 1, domain 1

Structure

Experimental structures (PDB)

16 structures.

PDB	Method	Resolution (Å)
7H6G	X-RAY DIFFRACTION	1.21
6VTM	X-RAY DIFFRACTION	1.6
1CGH	X-RAY DIFFRACTION	1.8
8G25	X-RAY DIFFRACTION	1.8
8G24	X-RAY DIFFRACTION	1.82
1T32	X-RAY DIFFRACTION	1.85
8D4V	X-RAY DIFFRACTION	1.85
8G26	X-RAY DIFFRACTION	1.85
1AU8	X-RAY DIFFRACTION	1.9
7H6H	X-RAY DIFFRACTION	1.94
8D4S	X-RAY DIFFRACTION	1.95
9ASX	X-RAY DIFFRACTION	1.96
9ATK	X-RAY DIFFRACTION	2.11
8D7K	X-RAY DIFFRACTION	3.1
1KYN	X-RAY DIFFRACTION	3.5
8D7I	X-RAY DIFFRACTION	3.63

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P08311-F1	91.89	0.82

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (3): 201 (charge relay system); 64 (charge relay system); 108 (charge relay system)

Disulfide bonds (3): 49–65, 142–207, 172–186

Glycosylation sites (2): 71, 71

Mutagenesis-validated functional residues (1):

Position	Phenotype
71	no effect on proteolytic processing, enzyme activation or sorting to cytoplasmic granules.

Function

Pathways and Gene Ontology

Reactome pathways

25 pathways

ID	Pathway
R-HSA-1474228	Degradation of the extracellular matrix
R-HSA-1592389	Activation of Matrix Metalloproteinases
R-HSA-2022377	Metabolism of Angiotensinogen to Angiotensins
R-HSA-381426	Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)
R-HSA-448706	Interleukin-1 processing
R-HSA-6798695	Neutrophil degranulation
R-HSA-6803157	Antimicrobial peptides
R-HSA-9635465	Suppression of apoptosis
R-HSA-9660826	Purinergic signaling in leishmaniasis infection
R-HSA-1280215	Cytokine Signaling in Immune system
R-HSA-1474244	Extracellular matrix organization
R-HSA-1643685	Disease
R-HSA-168249	Innate Immune System
R-HSA-168256	Immune System
R-HSA-2980736	Peptide hormone metabolism
R-HSA-392499	Metabolism of proteins
R-HSA-446652	Interleukin-1 family signaling
R-HSA-449147	Signaling by Interleukins
R-HSA-5663205	Infectious disease
R-HSA-9635486	Infection with Mycobacterium tuberculosis
R-HSA-9637690	Response of Mtb to phagocytosis
R-HSA-9658195	Leishmania infection
R-HSA-9664424	Cell recruitment (pro-inflammatory response)
R-HSA-9824439	Bacterial Infection Pathways
R-HSA-9824443	Parasitic Infection Pathways

MSigDB gene sets: 275 (showing top): GOBP_REGULATION_OF_CELL_ACTIVATION, DAVIES_MULTIPLE_MYELOMA_VS_MGUS_DN, REACTOME_INNATE_IMMUNE_SYSTEM, GOBP_ANTIMICROBIAL_HUMORAL_RESPONSE, GOBP_REGULATION_OF_SYSTEMIC_ARTERIAL_BLOOD_PRESSURE_BY_CIRCULATORY_RENIN_ANGIOTENSIN, GOBP_REGULATION_OF_BLOOD_PRESSURE, GOBP_MYELOID_LEUKOCYTE_MIGRATION, GOBP_CIRCULATORY_SYSTEM_PROCESS, GOBP_CELL_CHEMOTAXIS, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, GOBP_RESPONSE_TO_PEPTIDE, GOBP_CELLULAR_RESPONSE_TO_LIPID, JAEGER_METASTASIS_DN, GOCC_SECRETORY_GRANULE, GCANCTGNY_MYOD_Q6

GO Biological Process (25): angiotensin maturation (GO:0002003), monocyte chemotaxis (GO:0002548), proteolysis (GO:0006508), immune response (GO:0006955), protein processing (GO:0016485), cytokine-mediated signaling pathway (GO:0019221), antibacterial humoral response (GO:0019731), extracellular matrix disassembly (GO:0022617), platelet activation (GO:0030168), purinergic nucleotide receptor signaling pathway (GO:0035590), neutrophil activation (GO:0042119), positive regulation of immune response (GO:0050778), defense response to Gram-negative bacterium (GO:0050829), defense response to Gram-positive bacterium (GO:0050830), defense response to fungus (GO:0050832), negative regulation of T cell activation (GO:0050868), protein maturation (GO:0051604), neutrophil-mediated killing of gram-positive bacterium (GO:0070946), cellular response to lipopolysaccharide (GO:0071222), biofilm matrix disassembly (GO:0098786), positive regulation of platelet aggregation (GO:1901731), protein phosphorylation (GO:0006468), chemotaxis (GO:0006935), response to lipopolysaccharide (GO:0032496), defense response to bacterium (GO:0042742)

GO Molecular Function (8): serine-type endopeptidase activity (GO:0004252), heparin binding (GO:0008201), peptidase activity (GO:0008233), serine-type peptidase activity (GO:0008236), receptor ligand activity (GO:0048018), caspase binding (GO:0089720), protein binding (GO:0005515), hydrolase activity (GO:0016787)

GO Cellular Component (13): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), nucleus (GO:0005634), lysosome (GO:0005764), cytosol (GO:0005829), plasma membrane (GO:0005886), cytoplasmic stress granule (GO:0010494), membrane (GO:0016020), secretory granule (GO:0030141), extracellular matrix (GO:0031012), azurophil granule lumen (GO:0035578), extracellular exosome (GO:0070062), cytoplasm (GO:0005737)

Reactome top-level categories

Rollup of top-13 pathways:

Category	Pathways
Metabolism of proteins	2
Innate Immune System	2
Immune System	2
Extracellular matrix organization	1
Degradation of the extracellular matrix	1
Peptide hormone metabolism	1
Interleukin-1 family signaling	1
Response of Mtb to phagocytosis	1
Cell recruitment (pro-inflammatory response)	1
Signaling by Interleukins	1
Cytokine Signaling in Immune system	1
Disease	1
Bacterial Infection Pathways	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	4
defense response to bacterium	3
protein metabolic process	2
cell surface receptor signaling pathway	2
regulation of angiotensin levels in blood	1
peptide hormone processing	1
leukocyte chemotaxis	1
mononuclear cell migration	1
myeloid leukocyte migration	1
immune system process	1
response to stimulus	1
proteolysis	1
protein maturation	1
cellular response to cytokine stimulus	1
antimicrobial humoral response	1
cellular component disassembly	1
extracellular matrix organization	1
cell activation	1
blood coagulation	1
granulocyte activation	1
positive regulation of immune system process	1
immune response	1
positive regulation of response to stimulus	1
regulation of immune response	1
defense response	1
response to fungus	1
T cell activation	1
regulation of T cell activation	1
negative regulation of lymphocyte activation	1
negative regulation of leukocyte cell-cell adhesion	1
gene expression	1
defense response to Gram-positive bacterium	1
neutrophil-mediated killing of bacterium	1
response to lipopolysaccharide	1
cellular response to molecule of bacterial origin	1
cellular response to lipid	1
cellular response to oxygen-containing compound	1
extracellular matrix disassembly	1
biofilm matrix organization	1
endopeptidase activity	1

Protein interactions and networks

STRING

2330 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CTSG	MPO	P05164	997
CTSG	LTF	P02788	996
CTSG	SERPINA3	P01011	987
CTSG	MMP9	P14780	987
CTSG	ELANE	P08246	985
CTSG	PRTN3	P15637	983
CTSG	CAMP	P49913	948
CTSG	BPI	P17213	917
CTSG	AZU1	P20160	892
CTSG	SLPI	P03973	888
CTSG	LYZL1	Q6UWQ5	826
CTSG	LYZ	P00695	817
CTSG	SERPINB1	P30740	798
CTSG	SERPINA1	P01009	791
CTSG	PADI4	Q9UM07	736

IntAct

62 interactions, top by confidence:

A	B	Type	Score
CTSG	KRT31	psi-mi:“MI:0915”(physical association)	0.560
CTSG	NOTCH2NLA	psi-mi:“MI:0915”(physical association)	0.560
NOTCH2NLA	CTSG	psi-mi:“MI:0915”(physical association)	0.560
CYSRT1	CTSG	psi-mi:“MI:0915”(physical association)	0.560
CTSG	PICK1	psi-mi:“MI:0915”(physical association)	0.560
CTSG	WIZ	psi-mi:“MI:0914”(association)	0.530
ICE2	HP	psi-mi:“MI:0914”(association)	0.530
CTSG	MANBA	psi-mi:“MI:0914”(association)	0.530
EGFL8	MPO	psi-mi:“MI:0914”(association)	0.530
PRRT2	NDUFS4	psi-mi:“MI:0914”(association)	0.530
CTSG	CFP	psi-mi:“MI:0407”(direct interaction)	0.440
CTSG	S	psi-mi:“MI:0570”(protein cleavage)	0.440
CTSG	C3	psi-mi:“MI:0915”(physical association)	0.400
APP	ESYT2	psi-mi:“MI:0914”(association)	0.350
CD177	MYO1G	psi-mi:“MI:0914”(association)	0.350
OCRL	LTF	psi-mi:“MI:0914”(association)	0.350
GSK3B	PRSS37	psi-mi:“MI:0914”(association)	0.350
IRAK2	LTF	psi-mi:“MI:0914”(association)	0.350
ULK1	HNRNPCL1	psi-mi:“MI:0914”(association)	0.350
TEX14	DNAJB6	psi-mi:“MI:0914”(association)	0.350
	ENO1	psi-mi:“MI:0914”(association)	0.350
ATG16L1	ESYT2	psi-mi:“MI:0914”(association)	0.350
ATG16L1		psi-mi:“MI:0914”(association)	0.350
GOLGA8A	ZNF320	psi-mi:“MI:0914”(association)	0.350

BioGRID (86): KRT31 (Two-hybrid), NOTCH2NL (Two-hybrid), GPRASP2 (Affinity Capture-MS), YTHDF1 (Affinity Capture-MS), RPS27A (Affinity Capture-MS), TCF25 (Affinity Capture-MS), FREM2 (Affinity Capture-MS), WIZ (Affinity Capture-MS), CTSG (Affinity Capture-MS), CTSG (Reconstituted Complex), RPS27A (Affinity Capture-MS), CTSG (Affinity Capture-MS), GPRASP2 (Affinity Capture-MS), TCF25 (Affinity Capture-MS), YTHDF1 (Affinity Capture-MS)

ESM2 similar proteins: A7WPL7, O43240, O46683, O88780, P00770, P04187, P07288, P08311, P09650, P10144, P17977, P20151, P20160, P20718, P21812, P21842, P21844, P23946, P24158, P28293, P33619, P49862, P50339, P50340, P50341, P51124, P51779, P52195, P56435, P79204, P80219, P80931, P97592, Q00356, Q03238, Q07276, Q3T0A3, Q3UP87, Q61096, Q61955

Diamond homologs: A7WPL7, O35164, O35205, O46683, O60259, O88780, P00746, P00752, P00760, P00761, P00762, P00763, P00764, P00770, P00772, P00773, P04187, P06870, P06871, P07146, P07288, P08311, P08426, P08882, P08883, P08884, P09582, P09650, P10144, P11032, P11033, P11034, P12323, P12544, P12788, P13366, P15119, P16049, P17977, P18291

SIGNOR signaling

11 interactions.

A	Effect	B	Mechanism
CTSG	“up-regulates activity”	C3	cleavage
CTSG	“up-regulates activity”	AGT	cleavage
CTSG	“down-regulates activity”	SERPIND1	cleavage
CTSG	“up-regulates activity”	F2R	cleavage
CTSG	“down-regulates activity”	F2R	cleavage
CTSG	“down-regulates activity”	F2RL1	cleavage

Disease & clinical

Clinical variants and AI predictions

ClinVar

37 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	26
Likely benign	5
Benign	4

Top pathogenic / likely-pathogenic (0)

SpliceAI

515 predictions. Top by Δscore:

Variant	Effect	Δscore
14:24573806:TCCCC:T	acceptor_gain	0.9900
14:24573807:CCCC:C	acceptor_gain	0.9900
14:24573807:CCCCC:C	acceptor_gain	0.9900
14:24573808:CCC:C	acceptor_gain	0.9900
14:24573808:CCCC:C	acceptor_gain	0.9900
14:24573809:CC:C	acceptor_gain	0.9900
14:24573809:CCCTG:C	acceptor_gain	0.9900
14:24573810:CC:C	acceptor_gain	0.9900
14:24573810:CCTGT:C	acceptor_loss	0.9900
14:24573811:C:CC	acceptor_gain	0.9900
14:24573812:T:C	acceptor_loss	0.9900
14:24574495:CTCAG:C	acceptor_gain	0.9900
14:24574808:TTG:T	acceptor_gain	0.9900
14:24574811:C:CC	acceptor_gain	0.9900
14:24573813:G:C	acceptor_gain	0.9800
14:24574239:CCTTA:C	donor_loss	0.9800
14:24574240:CTTA:C	donor_loss	0.9800
14:24574241:TTA:T	donor_loss	0.9800
14:24574242:TAC:T	donor_loss	0.9800
14:24574243:A:C	donor_loss	0.9800
14:24574497:CAG:C	acceptor_gain	0.9800
14:24574806:TATTG:T	acceptor_gain	0.9800
14:24574809:TG:T	acceptor_gain	0.9800
14:24576164:CTCA:C	donor_loss	0.9800
14:24576165:TCA:T	donor_loss	0.9800
14:24576166:CA:C	donor_loss	0.9800
14:24576167:A:T	donor_loss	0.9800
14:24576167:ACCTG:A	donor_gain	0.9800
14:24576168:CCTGC:C	donor_gain	0.9800
14:24573813:G:GC	acceptor_gain	0.9700

AlphaMissense

1637 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
14:24574398:C:A	W147C	0.998
14:24574398:C:G	W147C	0.998
14:24574691:T:A	D108V	0.996
14:24574691:T:G	D108A	0.996
14:24573694:C:A	W237C	0.994
14:24573694:C:G	W237C	0.994
14:24573721:G:C	F228L	0.994
14:24573721:G:T	F228L	0.994
14:24573723:A:G	F228L	0.994
14:24574692:C:G	D108H	0.991
14:24574682:A:G	L111S	0.989
14:24574690:G:C	D108E	0.989
14:24574690:G:T	D108E	0.989
14:24574691:T:C	D108G	0.989
14:24573806:T:A	D200V	0.988
14:24574282:C:G	C186S	0.988
14:24574283:A:T	C186S	0.988
14:24574414:C:G	C142S	0.988
14:24574415:A:T	C142S	0.988
14:24573703:G:C	F234L	0.987
14:24573703:G:T	F234L	0.987
14:24573705:A:G	F234L	0.987
14:24574397:C:A	G148C	0.987
14:24574400:A:G	W147R	0.987
14:24574400:A:T	W147R	0.987
14:24575274:C:G	C65S	0.987
14:24575275:A:T	C65S	0.987
14:24575294:A:C	F58L	0.987
14:24575294:A:T	F58L	0.987
14:24575296:A:G	F58L	0.987

dbSNP variants (sampled 300 via entrez): RS1000333362 (14:24575228 T>C), RS1001851042 (14:24573244 C>A), RS1002706454 (14:24576915 C>A,T), RS1003238583 (14:24577830 G>A), RS1003921584 (14:24574806 T>G), RS1004020393 (14:24574583 C>A,T), RS1004519210 (14:24574854 C>T), RS1006289714 (14:24576731 G>A), RS1006453148 (14:24576384 G>C,T), RS1007365788 (14:24577370 T>A), RS1007779377 (14:24577715 G>A), RS1007871490 (14:24577725 A>G), RS1008158146 (14:24573787 C>G), RS1008876405 (14:24574090 A>T), RS1009540595 (14:24577033 C>T)

Disease associations

OMIM: gene MIM:116830 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST004721_13	Congenital heart disease (maternal effect)	8.000000e-06
GCST004723_11	Conotruncal heart defects (maternal effects)	8.000000e-06

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4071 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

5 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 37,471 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL325041	BORTEZOMIB	4	13,120
CHEMBL585	TRIAMTERENE	4	21,663
CHEMBL270515	DELANZOMIB	2	1,883
CHEMBL4297596	FULACIMSTAT	2	82
CHEMBL63440	ALOXISTATIN	2	723

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: enzyme — S1: Chymotrypsin

Most potent curated ligand interactions (3 total), top 3:

Ligand	Action	Affinity	Parameter
compound 1 [PMID: 11425539]	Inhibition	9.4	pIC50
aloxistatin	Inhibition	5.96	pIC50
compound 4g [PMID: 22595175]	Inhibition	4.85	pIC50

Binding affinities (BindingDB)

86 measured of 111 human assays (111 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
2-(2,4-dimethoxyphenyl)-6,7-dimethoxy-3,1-benzoxazin-4-one	KI	100 nM	US-9695194: Benzoxazinone derivatives for treatment of skin diseases
2-(2-methylsulfonylphenyl)-7,8-dihydro-[1,4]dioxino[2,3-g][3,1]benzoxazin-4-one	KI	200 nM	US-9695194: Benzoxazinone derivatives for treatment of skin diseases
2-thiophenecarboxylic acid [5-amino-1-(benzenesulfonyl)-3-pyrazolyl] ester	IC50	247 nM
2-(2-chlorophenyl)-7,8-dihydro-[1,4]dioxino[2,3-g][3,1]benzoxazin-4-one	KI	400 nM	US-9695194: Benzoxazinone derivatives for treatment of skin diseases
2-(2-methylsulfonylphenyl)-8,9-dihydro-7H-[1,4]dioxepino[2,3-g][3,1]benzoxazin-4-one	KI	500 nM	US-9695194: Benzoxazinone derivatives for treatment of skin diseases
2-(4,6-dimethoxycyclohexa-1,3-dien-1-yl)-7,8-dihydro-[1,4]dioxino[2,3-g][3,1]benzoxazin-4-one	KI	500 nM	US-9695194: Benzoxazinone derivatives for treatment of skin diseases
2-(2,4-dimethoxyphenyl)-8,9-dihydro-7H-[1,4]dioxepino[2,3-g][3,1]benzoxazin-4-one	KI	600 nM	US-9695194: Benzoxazinone derivatives for treatment of skin diseases
MLS000087437	IC50	631 nM
2-(2-methoxyphenyl)-8,9-dihydro-7H-[1,4]dioxepino[2,3-g][3,1]benzoxazin-4-one	KI	700 nM	US-9695194: Benzoxazinone derivatives for treatment of skin diseases
6,7-dimethoxy-2-(2-methylsulfanylphenyl)-3,1-benzoxazin-4-one	KI	700 nM	US-9695194: Benzoxazinone derivatives for treatment of skin diseases
2-(2-methoxyphenyl)-7,8-dihydro-[1,4]dioxino[2,3-g][3,1]benzoxazin-4-one	KI	700 nM	US-9695194: Benzoxazinone derivatives for treatment of skin diseases
2-Furan-2-yl-benzo[d][1,3]oxazin-4-one	IC50	793 nM
MLS000097371	IC50	923 nM
1,3-benzodioxol-5-yl(1-benzotriazolyl)methanone	IC50	957 nM
MLS000115326	IC50	1020 nM
2-(2,4-dimethoxyphenyl)-6-ethoxy-7-methoxy-3,1-benzoxazin-4-one	KI	1100 nM	US-9695194: Benzoxazinone derivatives for treatment of skin diseases
2-thiophenecarboxylic acid [5-amino-1-(4-methoxyphenyl)sulfonyl-3-pyrazolyl] ester	IC50	1160 nM
6-ethoxy-7-methoxy-2-(2-methoxyphenyl)-3,1-benzoxazin-4-one	KI	1200 nM	US-9695194: Benzoxazinone derivatives for treatment of skin diseases
2-(2-methylsulfanylphenyl)-8,9-dihydro-7H-[1,4]dioxepino[2,3-g][3,1]benzoxazin-4-one	KI	1300 nM	US-9695194: Benzoxazinone derivatives for treatment of skin diseases
(3-amino-1,2,4-triazol-1-yl)-(4-methoxyphenyl)methanone	IC50	1310 nM
7-methoxy-N-(3-pyridinylmethyl)-4,5-dihydrobenzo[g][1,2]benzoxazole-3-carboxamide	IC50	1390 nM
MLS000087458	IC50	1470 nM
MLS000087436	IC50	1580 nM
(3-amino-1,2,4-triazol-4-yl)-(3,4-dimethylphenyl)methanone	IC50	1580 nM
3-(2-furyl)-5-(methylthio)-1-(2-thienylcarbonyl)-1H-1,2,4-triazole	IC50	1780 nM
2-(2-chlorophenyl)-8,9-dihydro-7H-[1,4]dioxepino[2,3-g][3,1]benzoxazin-4-one	KI	1900 nM	US-9695194: Benzoxazinone derivatives for treatment of skin diseases
2-(2-Iodo-phenyl)-6,7-dimethoxy-benzo[d][1,3]oxazin-4-one	KI	1900 nM	US-9695194: Benzoxazinone derivatives for treatment of skin diseases
MLS000083777	IC50	1950 nM
2-thiophenecarboxylic acid [5-amino-1-(4-methylphenyl)sulfonyl-3-pyrazolyl] ester	IC50	1990 nM
MLS000061720	IC50	2170 nM
MLS000081703	IC50	2260 nM
MLS000087424	IC50	2480 nM
MLS000116425	IC50	2520 nM
MLS000116420	IC50	2550 nM
MLS000041934	IC50	2670 nM
2-(3-pyridinyl)-3,1-benzoxazin-4-one	IC50	2770 nM
6-ethoxy-7-methoxy-2-(2-methylsulfonylphenyl)-3,1-benzoxazin-4-one	KI	2800 nM	US-9695194: Benzoxazinone derivatives for treatment of skin diseases
7-methoxy-N-[1-(4-methylbenzyl)-1H-pyrazol-3-yl]-4,5-dihydronaphtho[2,1-d]isoxazole-3-carboxamide	IC50	2910 nM
MLS000090237	IC50	3430 nM
1-(4,5,6,7-tetrahydro-1-benzothien-3-ylcarbonyl)-1H-pyrazole	IC50	3610 nM
MLS000087425	IC50	3730 nM
5-amino-1-[4-[(4-methyl-1,2,4-triazol-3-yl)sulfanylmethyl]benzoyl]pyrazole-4-carbonitrile	IC50	3860 nM
(3-amino-1,2,4-triazol-4-yl)-(3,5-dimethylphenyl)methanone	IC50	3880 nM
2-(benzotriazole-1-carbonyl)benzoic acid propargyl ester	IC50	3970 nM
2-(3-morpholin-4-ylsulfonylphenyl)-3,1-benzoxazin-4-one	IC50	4050 nM
MLS000087439	IC50	4130 nM
MLS000116422	IC50	4250 nM
1-(1-benzothien-3-ylcarbonyl)-1H-pyrazole	IC50	4330 nM
7-methoxy-N-(2-methoxyethyl)-4,5-dihydrobenz[g]indoxazene-3-carboxamide	IC50	4360 nM
(5-amino-3-phenyl-1,2,4-triazol-1-yl)-(3,4-dimethoxyphenyl)methanone	IC50	4430 nM

ChEMBL bioactivities

189 potent at pChembl≥5 of 243 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.82	Ki	0.15	nM	CHEMBL453539
9.76	Ki	0.174	nM	CHEMBL418050
9.73	Ki	0.187	nM	CHEMBL285285
9.59	Ki	0.26	nM	CHEMBL4592765
9.41	IC50	0.39	nM	CHEMBL47394
9.36	Ki	0.437	nM	CHEMBL2448441
9.05	Ki	0.89	nM	CHEMBL4061897
9.04	Ki	0.916	nM	CHEMBL290577
8.96	Ki	1.1	nM	CHEMBL4077874
8.85	IC50	1.4	nM	CHEMBL108540
8.80	Ki	1.6	nM	CHEMBL4092637
8.77	Ki	1.7	nM	CHEMBL4081142
8.68	IC50	2.1	nM	CHEMBL1807526
8.64	IC50	2.3	nM	CHEMBL296771
8.54	Ki	2.9	nM	CHEMBL4097952
8.47	Ki	3.4	nM	CHEMBL4069983
8.43	Ki	3.74	nM	CHEMBL291026
8.41	Ki	3.9	nM	CHEMBL3349045
8.41	Ki	3.85	nM	CHEMBL288176
8.32	Ki	4.8	nM	CHEMBL4070520
8.32	IC50	4.8	nM	CHEMBL1807531
8.31	Ki	4.9	nM	CHEMBL4097688
8.19	IC50	6.4	nM	CHEMBL335675
8.15	IC50	7	nM	CHEMBL1807638
8.14	Ki	7.3	nM	CHEMBL4088524
8.13	Ki	7.4	nM	CHEMBL4469390
8.09	Ki	8.2	nM	CHEMBL4586444
8.08	IC50	8.4	nM	CHEMBL108294
8.06	IC50	8.7	nM	CHEMBL108294
8.06	IC50	8.8	nM	CHEMBL1807538
8.02	IC50	9.5	nM	CHEMBL1807535
8.00	IC50	10	nM	CHEMBL108294
7.92	Ki	12	nM	CHEMBL4105401
7.92	Ki	12	nM	CHEMBL3623771
7.87	EC50	13.5	nM	DELANZOMIB
7.86	IC50	13.7	nM	DELANZOMIB
7.85	Ki	14	nM	CHEMBL4590739
7.84	Ki	14.3	nM	CHEMBL287918
7.82	IC50	15	nM	CHEMBL134816
7.68	IC50	21	nM	CHEMBL436591
7.66	IC50	22	nM	CHEMBL1807640
7.60	Ki	25.3	nM	CHEMBL36744
7.42	Ki	38	nM	CHEMBL374027
7.42	Ki	38	nM	CHEMBL4472052
7.36	Ki	44.1	nM	CHEMBL291261
7.32	IC50	48	nM	CHEMBL424453
7.28	IC50	52	nM	CHEMBL1807642
7.27	Ki	54	nM	CHEMBL4457132
7.21	Ki	62	nM	CHEMBL4089025
7.19	IC50	64	nM	CHEMBL134821

PubChem BioAssay actives

171 with measured affinity, of 558 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
3-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,40S,43S,49S)-34,49-dibenzyl-4-[(2S)-butan-2-yl]-40-(carboxymethyl)-22-(hydroxymethyl)-25-[(4-hydroxyphenyl)methyl]-28-methyl-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-19-yl]propanoic acid	1582055: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate at pH 7.2 and 298 K measured every 60 secs for 600 secs	ki	0.0001	uM
2-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,40S,43S,49S)-25-(4-aminobutyl)-49-benzyl-4,19-bis[(2S)-butan-2-yl]-34-[3-(diaminomethylideneamino)propyl]-28-[(1R)-1-hydroxyethyl]-22-(hydroxymethyl)-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-40-yl]acetic acid	350910: Inhibition of cathepsin G	ki	0.0001	uM
benzyl N-[(2S)-1-oxo-3-phenyl-1-[(2S)-2-[[2-phenyl-1-[(2S,6R)-2,9,9-trimethyl-3,5-dioxa-4-boratricyclo[6.1.1.02,6]decan-4-yl]ethyl]carbamoyl]pyrrolidin-1-yl]propan-2-yl]carbamate	48215: Binding affinity against cathepsin G	ki	0.0002	uM
benzyl N-[(2S)-1-oxo-3,3-diphenyl-1-[(2S)-2-[[2-phenyl-1-[(2S,6R)-2,9,9-trimethyl-3,5-dioxa-4-boratricyclo[6.1.1.02,6]decan-4-yl]ethyl]carbamoyl]pyrrolidin-1-yl]propan-2-yl]carbamate	48215: Binding affinity against cathepsin G	ki	0.0002	uM
3-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,40S,43S,49S)-28-(3-amino-3-oxopropyl)-49-benzyl-4-[(2S)-butan-2-yl]-40-(carboxymethyl)-34-[3-(diaminomethylideneamino)propyl]-22-(hydroxymethyl)-25-[(4-hydroxyphenyl)methyl]-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-19-yl]propanoic acid	1582055: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate at pH 7.2 and 298 K measured every 60 secs for 600 secs	ki	0.0003	uM
1,3-dibenzyl-1,3-diazetidine-2,4-dione	48195: Compound was evaluated for its inhibitory activity against human cathepsin G	ic50	0.0004	uM
benzyl N-[(2S)-1-[(2S)-2-[[5-hydrazinyl-5-sulfanylidene-1-[(2S,6R)-2,9,9-trimethyl-3,5-dioxa-4-boratricyclo[6.1.1.02,6]decan-4-yl]pentyl]carbamoyl]pyrrolidin-1-yl]-1-oxo-3-phenylpropan-2-yl]carbamate;hydrobromide	48215: Binding affinity against cathepsin G	ki	0.0004	uM
2-[(1R,4S,7S,13S,19S,22S,25S,31R,34S,40S,43S,49S)-25,49-dibenzyl-4,19-bis[(2S)-butan-2-yl]-28-butyl-34-[(1R)-1-hydroxyethyl]-22-(hydroxymethyl)-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-40-yl]acetamide	1483616: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate after 30 mins	ki	0.0009	uM
benzyl N-[(2S)-1-[(2S)-2-[[2,2-dimethyl-1-[(2S,6R)-2,9,9-trimethyl-3,5-dioxa-4-boratricyclo[6.1.1.02,6]decan-4-yl]butyl]carbamoyl]pyrrolidin-1-yl]-1-oxo-3-phenylpropan-2-yl]carbamate	48215: Binding affinity against cathepsin G	ki	0.0009	uM
3-[(1R,4S,7S,13S,19S,22S,25S,31R,34S,40S,43S,49S)-40-(2-amino-2-oxoethyl)-25,49-dibenzyl-4-[(2S)-butan-2-yl]-28-butyl-34-[(1R)-1-hydroxyethyl]-22-(hydroxymethyl)-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-19-yl]propanoic acid	1483616: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate after 30 mins	ki	0.0011	uM
[3-[(4-cyanobenzoyl)amino]-2,2-dimethyl-5-phenylpentanoyl] 3-[(4-cyanobenzoyl)amino]-2,2-dimethyl-5-phenylpentanoate	48207: Inhibitory activity against human leukocyte cathepsin G (h-CG)	ic50	0.0014	uM
2-[(1R,4S,7S,13S,19S,22S,25S,31R,34S,40S,43S,49S)-40-(2-amino-2-oxoethyl)-49-benzyl-4-[(2S)-butan-2-yl]-28-butyl-25-[[4-(diaminomethylideneamino)phenyl]methyl]-34-[(1R)-1-hydroxyethyl]-22-(hydroxymethyl)-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-19-yl]acetic acid	1483616: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate after 30 mins	ki	0.0016	uM
2-[(1R,4S,7S,13S,19S,22S,25S,31R,34S,40S,43S,49S)-40-(2-amino-2-oxoethyl)-25,49-dibenzyl-4-[(2S)-butan-2-yl]-28-butyl-34-[(1R)-1-hydroxyethyl]-22-(hydroxymethyl)-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-19-yl]acetic acid	1483616: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate after 30 mins	ki	0.0017	uM
3-[3-[(4-methyl-1-benzothiophen-3-yl)methyl]-2-oxobenzimidazol-1-yl]propanoic acid	609664: Inhibition of human cathepsin G after 1 hr by fluorometric assay	ic50	0.0021	uM
1,3-bis(4-methylphenyl)-1,3-diazetidine-2,4-dione	48195: Compound was evaluated for its inhibitory activity against human cathepsin G	ic50	0.0023	uM
2-[(1R,4S,7S,13S,22S,25S,31R,34S,40S,43S,49S)-25,49-dibenzyl-4-[(2S)-butan-2-yl]-28-butyl-34-[(1R)-1-hydroxyethyl]-22-(hydroxymethyl)-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-19-[(4-phenylphenyl)methyl]-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-40-yl]acetamide	1483616: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate after 30 mins	ki	0.0029	uM
2-[(1R,4S,7S,13S,19S,22S,25S,31R,34S,40S,43S,49S)-25,49-dibenzyl-4,19,34-tris[(2S)-butan-2-yl]-28-butyl-22-(hydroxymethyl)-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-40-yl]acetic acid	1483616: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate after 30 mins	ki	0.0034	uM
benzyl N-[(2S)-1-oxo-3-phenyl-1-[(2S)-2-[1-[(2S,6R)-2,9,9-trimethyl-3,5-dioxa-4-boratricyclo[6.1.1.02,6]decan-4-yl]hexylcarbamoyl]pyrrolidin-1-yl]propan-2-yl]carbamate	48215: Binding affinity against cathepsin G	ki	0.0037	uM
benzyl N-[(2R)-1-[(2S)-2-[[(1S)-4-methoxy-1-[(2S,6R)-2,9,9-trimethyl-3,5-dioxa-4-boratricyclo[6.1.1.02,6]decan-4-yl]butyl]carbamoyl]pyrrolidin-1-yl]-1-oxo-3-phenylpropan-2-yl]carbamate	48215: Binding affinity against cathepsin G	ki	0.0039	uM
benzyl N-[(2S)-1-[(2S)-2-[[2,2-dimethyl-1-[(2S,6R)-2,9,9-trimethyl-3,5-dioxa-4-boratricyclo[6.1.1.02,6]decan-4-yl]butyl]carbamoyl]pyrrolidin-1-yl]-3-naphthalen-2-yl-1-oxopropan-2-yl]carbamate	48215: Binding affinity against cathepsin G	ki	0.0039	uM
2-[(1R,4S,7S,13S,19S,25S,31R,34S,40S,43S,49S)-25,49-dibenzyl-4,19-bis[(2S)-butan-2-yl]-22,28-dibutyl-34-[(1R)-1-hydroxyethyl]-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-40-yl]acetic acid	1483616: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate after 30 mins	ki	0.0048	uM
3-[3-[(1,4-dimethylindol-3-yl)methyl]-2-oxobenzimidazol-1-yl]propanoic acid	609664: Inhibition of human cathepsin G after 1 hr by fluorometric assay	ic50	0.0048	uM
2-[(1R,4S,7S,13S,19S,22S,25S,31R,34S,40S,43S,49S)-25,49-dibenzyl-4,19,34-tris[(2S)-butan-2-yl]-28-butyl-22-(hydroxymethyl)-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-40-yl]acetamide	1483616: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate after 30 mins	ki	0.0049	uM
(3-benzamido-2,2-dimethylheptanoyl) 3-benzamido-2,2-dimethylheptanoate	48207: Inhibitory activity against human leukocyte cathepsin G (h-CG)	ic50	0.0064	uM
3-[2-oxo-3-[(1,2,3,5-tetramethylindol-7-yl)methyl]benzimidazol-1-yl]propanoic acid	609664: Inhibition of human cathepsin G after 1 hr by fluorometric assay	ic50	0.0070	uM
2-[(1R,4S,7S,13S,19S,22S,25S,31R,34S,40S,43S,49S)-25,49-dibenzyl-4,19-bis[(2S)-butan-2-yl]-28-butyl-34-[(1R)-1-hydroxyethyl]-22-(hydroxymethyl)-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-40-yl]acetic acid	1483616: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate after 30 mins	ki	0.0073	uM
2-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,40S,43S,49S)-34,49-dibenzyl-4-[(2S)-butan-2-yl]-22-(hydroxymethyl)-25-[(4-hydroxyphenyl)methyl]-28-methyl-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-19-[(4-phenylphenyl)methyl]-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-40-yl]acetic acid	1582055: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate at pH 7.2 and 298 K measured every 60 secs for 600 secs	ki	0.0074	uM
3-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,40S,43S,49S)-49-benzyl-4-[(2S)-butan-2-yl]-40-(carboxymethyl)-34-[3-(diaminomethylideneamino)propyl]-28-[(1R)-1-hydroxyethyl]-22-(hydroxymethyl)-25-[(4-hydroxyphenyl)methyl]-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-19-yl]propanoic acid	1582055: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate at pH 7.2 and 298 K measured every 60 secs for 600 secs	ki	0.0082	uM
ethyl (2S)-2-[[3-[(4-cyanobenzoyl)amino]-2,2-dimethylnonanoyl]amino]-3-phenylpropanoate	48196: Compound was tested by chromogenic assay for the inhibition of serine proteases like Human cathepsin G	ic50	0.0084	uM
3-[3-[(1,3-dimethylindol-7-yl)methyl]-2-oxobenzimidazol-1-yl]propanoic acid	609664: Inhibition of human cathepsin G after 1 hr by fluorometric assay	ic50	0.0088	uM
3-[3-[(4,6-dimethyl-1,2-benzothiazol-3-yl)methyl]-2-oxobenzimidazol-1-yl]propanoic acid	609664: Inhibition of human cathepsin G after 1 hr by fluorometric assay	ic50	0.0095	uM
2-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,40S,43S,49S)-40,49-bis(2-amino-2-oxoethyl)-4-[(2S)-butan-2-yl]-25-[3-(diaminomethylideneamino)propyl]-28,34-bis[(1R)-1-hydroxyethyl]-22-(hydroxymethyl)-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-19-yl]acetic acid	1483616: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate after 30 mins	ki	0.0120	uM
2-[(1R,4S,7S,13S,19S,25S,31R,34S,40S,43S,49S)-25,49-dibenzyl-4,19-bis[(2S)-butan-2-yl]-22,28-dibutyl-34-[(1R)-1-hydroxyethyl]-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-40-yl]acetamide	1483616: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate after 30 mins	ki	0.0120	uM
[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(6-phenylpyridine-2-carbonyl)amino]butanoyl]amino]-3-methylbutyl]boronic acid	526655: Inhibition of cathepsin G in human MOLT4 cells	ec50	0.0135	uM
3-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,40S,43S,49S)-49-benzyl-19-(2-carboxyethyl)-40-(carboxymethyl)-34-[3-(diaminomethylideneamino)propyl]-28-[(1R)-1-hydroxyethyl]-22-(hydroxymethyl)-25-[(4-hydroxyphenyl)methyl]-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-4-yl]propanoic acid	1582055: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate at pH 7.2 and 298 K measured every 60 secs for 600 secs	ki	0.0140	uM
benzyl N-[(2S)-1-oxo-3,3-diphenyl-1-[(2S)-2-[1-[(2S,6R)-2,9,9-trimethyl-3,5-dioxa-4-boratricyclo[6.1.1.02,6]decan-4-yl]hexylcarbamoyl]pyrrolidin-1-yl]propan-2-yl]carbamate	48215: Binding affinity against cathepsin G	ki	0.0143	uM
[3-[(4-cyanobenzoyl)amino]-2,2-dimethyl-3-phenylpropanoyl] 3-[(4-cyanobenzoyl)amino]-2,2-dimethyl-3-phenylpropanoate	48207: Inhibitory activity against human leukocyte cathepsin G (h-CG)	ic50	0.0150	uM
[3-(butanoylamino)-2,2-dimethyl-5-phenylpentanoyl] 3-(butanoylamino)-2,2-dimethyl-5-phenylpentanoate	48207: Inhibitory activity against human leukocyte cathepsin G (h-CG)	ic50	0.0210	uM
3-[3-[(5-chloro-1,2,3-trimethylindol-7-yl)methyl]-2-oxobenzimidazol-1-yl]propanoic acid	609664: Inhibition of human cathepsin G after 1 hr by fluorometric assay	ic50	0.0220	uM
benzyl N-[(2S)-1-[(2S)-2-[[4-methoxy-1-[(2S,6R)-2,9,9-trimethyl-3,5-dioxa-4-boratricyclo[6.1.1.02,6]decan-4-yl]butyl]carbamoyl]pyrrolidin-1-yl]-1-oxo-3,3-diphenylpropan-2-yl]carbamate	48215: Binding affinity against cathepsin G	ki	0.0253	uM
[2-[3-[methyl-[1-(naphthalene-2-carbonyl)piperidin-4-yl]carbamoyl]naphthalen-2-yl]-1-naphthalen-1-yl-2-oxoethyl]phosphonic acid	281267: Inhibition of human neutrophil Cat G	ki	0.0380	uM
[2-[1-[methyl-[1-(naphthalene-2-carbonyl)piperidin-4-yl]carbamoyl]naphthalen-2-yl]-1-naphthalen-1-yl-2-oxoethyl]phosphonic acid	1530544: Inhibition of cathepsin G in human neutrophils using Suc-Ala-Ala-Pro-Phe-(p-nitroanilide) as substrate for 15 mins by spectrophotometric method	ki	0.0380	uM
benzyl N-[(2S)-1-[(2S)-2-[[2,2-dimethyl-1-[(2S,6R)-2,9,9-trimethyl-3,5-dioxa-4-boratricyclo[6.1.1.02,6]decan-4-yl]butyl]carbamoyl]pyrrolidin-1-yl]-1-oxo-3,3-diphenylpropan-2-yl]carbamate	48215: Binding affinity against cathepsin G	ki	0.0441	uM
(3-benzamido-2,2-dimethyloctanoyl) 3-benzamido-2,2-dimethyloctanoate	48207: Inhibitory activity against human leukocyte cathepsin G (h-CG)	ic50	0.0480	uM
4-[1-[(4-methyl-1-benzothiophen-3-yl)methyl]benzimidazol-2-yl]sulfanylbutanoic acid	748039: Inhibition of human cathepsin G using bis(succinoyl-L-alanyl-L-prolyl-L-phenylalanylamide) as substrate after 1 hr by fluorescence assay	ic50	0.0520	uM
3-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,40S,43S,49S)-28-(3-amino-3-oxopropyl)-49-benzyl-34-(3-carbamimidamidopropyl)-19-(2-carboxyethyl)-40-(carboxymethyl)-22-(hydroxymethyl)-25-[(4-hydroxyphenyl)methyl]-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-4-yl]propanoic acid	1582055: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate at pH 7.2 and 298 K measured every 60 secs for 600 secs	ki	0.0540	uM
2-[(1R,4S,7S,13S,19S,22S,25S,31R,34S,40S,43S,49S)-49-(2-amino-2-oxoethyl)-25-benzyl-4,19-bis[(2S)-butan-2-yl]-28-butyl-34-[(1R)-1-hydroxyethyl]-22-(hydroxymethyl)-3,6,12,18,21,24,27,30,33,36,39,42,48,51-tetradecaoxo-53,54-dithia-2,5,11,17,20,23,26,29,32,35,38,41,47,50-tetradecazapentacyclo[29.20.4.07,11.013,17.043,47]pentapentacontan-40-yl]acetamide	1483616: Inhibition of human cathepsin G using Suc-AAPF-MCA as substrate after 30 mins	ki	0.0620	uM
(3-benzamido-2,2-dimethyl-5-phenylpentanoyl) 3-benzamido-2,2-dimethyl-5-phenylpentanoate	48207: Inhibitory activity against human leukocyte cathepsin G (h-CG)	ic50	0.0640	uM
[3-[(4-cyanobenzoyl)amino]-3-cyclohex-3-en-1-yl-2,2-dimethylpropanoyl] 3-[(4-cyanobenzoyl)amino]-3-cyclohex-3-en-1-yl-2,2-dimethylpropanoate	48207: Inhibitory activity against human leukocyte cathepsin G (h-CG)	ic50	0.0690	uM
(3-benzamido-2,2-dimethylhexanoyl) 3-benzamido-2,2-dimethylhexanoate	48207: Inhibitory activity against human leukocyte cathepsin G (h-CG)	ic50	0.0750	uM

CTD chemical–gene interactions

29 total (human), top 29 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Methotrexate	decreases expression, increases expression	2
N-Formylmethionine Leucyl-Phenylalanine	decreases reaction, increases secretion	2
Tetradecanoylphorbol Acetate	affects localization, increases secretion	2
Tretinoin	affects cotreatment, decreases expression	2
2,4,6-tribromophenol	decreases expression	1
alpha phellandrene	decreases expression	1
honokiol	decreases reaction, increases secretion	1
bisphenol A	decreases expression	1
decabromobiphenyl ether	decreases expression	1
sulforaphane	decreases expression	1
tetrabromobisphenol A	decreases expression	1
vanadyl sulfate	increases expression	1
cyclosporin H	decreases reaction, increases secretion	1
epsilon-viniferin	decreases reaction, increases secretion	1
(2-(5-amino-2-(4-fluorophenyl)-1,6-dihydro-6-oxo-1-pyrimidinyl)-N-(1-((5-methoxycarbonyl-2-benzoxazolyl)carbonyl)-2-phenylethyl)acetamide)	decreases activity	1
2,2’,4,4’-tetrabromodiphenyl ether	decreases expression	1
pentabrominated diphenyl ether 100	decreases expression	1
hexabrominated diphenyl ether 153	decreases expression	1
2,6-dichloro-(1,4)benzoquinone	decreases expression	1
Arsenic Trioxide	decreases expression, affects cotreatment	1
Acetaminophen	decreases expression	1
Air Pollutants	decreases expression, increases abundance	1
Aniline Compounds	increases hydrolysis	1
Arsenic	affects expression, increases abundance	1
Benzo(a)pyrene	increases methylation	1
Cacodylic Acid	increases abundance, affects expression	1
Doxorubicin	affects response to substance	1
Smoke	increases expression	1
Particulate Matter	decreases expression, increases abundance	1

ChEMBL screening assays

160 unique, capped per target: 155 binding, 4 admet, 1 toxicity

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1004878	Binding	Inhibition of cathepsin G in human U937 cells	Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing. — J Biol Chem
CHEMBL4047160	ADMET	Drug metabolism assessed as cathepsin G (unknown origin)-mediated compound hydrolysis after 4 hrs by RP-HPLC analysis	d-Amino acid mutation of PMI as potent dual peptide inhibitors of p53-MDM2/MDMX interactions. — Bioorg Med Chem Lett
CHEMBL5326794	Toxicity	Inhibition of human Cathepsin G	Structure-guided design of direct-acting antivirals that exploit the gem-dimethyl effect and potently inhibit 3CL proteases of severe acute respiratory syndrome Coronavirus-2 (SARS-CoV-2) and middle east respiratory syndrome coronavirus (MERS-CoV). — Eur J Med Chem

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_D1VZ	Abcam A-549 CTSG KO	Cancer cell line	Male
CVCL_D2N9	Abcam THP-1 CTSG KO	Cancer cell line	Male

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.