KLK5

Summary

KLK5 (kallikrein related peptidase 5, HGNC:6366) is a protein-coding gene on chromosome 19q13.41, encoding Kallikrein-5 (Q9Y337). May be involved in desquamation.

Kallikreins are a subgroup of serine proteases having diverse physiological functions. Growing evidence suggests that many kallikreins are implicated in carcinogenesis and some have potential as novel cancer and other disease biomarkers. This gene is one of the fifteen kallikrein subfamily members located in a cluster on chromosome 19. Its expression is up-regulated by estrogens and progestins. The encoded protein is secreted and may be involved in desquamation in the epidermis. Alternative splicing results in multiple transcript variants encoding the same protein.

Source: NCBI Gene 25818 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 53 total
• Druggable target: yes
• MANE Select transcript: NM_012427

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:6366
Approved symbol	KLK5
Name	kallikrein related peptidase 5
Location	19q13.41
Locus type	gene with protein product
Status	Approved
Aliases	SCTE, KLK-L2
Ensembl gene	ENSG00000167754
Ensembl biotype	protein_coding
OMIM	605643
Entrez	25818

Gene structure

Transcript identifiers

Ensembl transcripts: 11 — 10 protein_coding, 1 retained_intron

ENST00000336334, ENST00000391809, ENST00000593428, ENST00000594846, ENST00000595585, ENST00000860844, ENST00000860845, ENST00000860846, ENST00000860847, ENST00000860848, ENST00000860849

RefSeq mRNA: 3 — MANE Select: NM_012427 NM_001077491, NM_001077492, NM_012427

CCDS: CCDS12810

Canonical transcript exons

ENST00000336334 — 6 exons

Exon	Start	End
ENSE00001116575	50948640	50948773
ENSE00001188457	50948859	50949115
ENSE00001377703	50952747	50953038
ENSE00003135228	50943303	50943786
ENSE00003477440	50952585	50952668
ENSE00003560105	50949855	50950116

Expression profiles

Bgee: expression breadth ubiquitous, 152 present calls, max score 98.28.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 4.8863 / max 699.3924, expressed in 162 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
182294	4.6708	158
182296	0.1269	38
182295	0.0487	23
208908	0.0400	22

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
upper arm skin	UBERON:0004263	98.28	gold quality
skin of leg	UBERON:0001511	96.97	gold quality
skin of abdomen	UBERON:0001416	96.94	gold quality
upper leg skin	UBERON:0004262	96.63	gold quality
zone of skin	UBERON:0000014	96.22	gold quality
tongue squamous epithelium	UBERON:0006919	94.36	silver quality
penis	UBERON:0000989	93.78	gold quality
skin of hip	UBERON:0001554	90.21	gold quality
mammalian vulva	UBERON:0000997	89.64	gold quality
gingiva	UBERON:0001828	88.37	gold quality
gingival epithelium	UBERON:0001949	86.60	gold quality
sperm	CL:0000019	83.99	silver quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	82.98	gold quality
mouth mucosa	UBERON:0003729	82.98	gold quality
nipple	UBERON:0002030	82.86	gold quality
minor salivary gland	UBERON:0001830	82.11	gold quality
male germ cell	CL:0000015	81.88	silver quality
epithelium of esophagus	UBERON:0001976	80.96	gold quality
esophagus mucosa	UBERON:0002469	80.58	gold quality
epithelium of mammary gland	UBERON:0003244	79.46	gold quality
esophagus squamous epithelium	UBERON:0006920	79.38	gold quality
oral cavity	UBERON:0000167	79.17	gold quality
mammary duct	UBERON:0001765	79.02	gold quality
squamous epithelium	UBERON:0006914	77.86	gold quality
hair follicle	UBERON:0002073	77.76	silver quality
left testis	UBERON:0004533	77.53	gold quality
saliva-secreting gland	UBERON:0001044	77.29	gold quality
right testis	UBERON:0004534	76.94	gold quality
buccal mucosa cell	CL:0002336	75.19	silver quality
testis	UBERON:0000473	74.38	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 3.

Experiment	Marker?	Max mean expression
E-GEOD-75688	yes	443.35
E-MTAB-10885	yes	267.30
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

31 targeting KLK5, 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-5196-5P	100.00	67.98	2761
HSA-MIR-4747-5P	100.00	67.90	2681
HSA-MIR-4533	100.00	69.48	2758
HSA-MIR-3605-5P	99.96	67.12	932
HSA-MIR-4492	99.87	68.25	3611
HSA-MIR-4447	99.85	67.81	2900
HSA-MIR-4319	99.76	69.83	2586
HSA-MIR-6764-5P	99.75	67.89	2304
HSA-MIR-4766-5P	99.75	69.23	2662
HSA-MIR-4306	99.72	70.50	3630
HSA-MIR-1915-3P	99.58	66.79	1988
HSA-MIR-4472	99.56	66.08	1478
HSA-MIR-4441	99.49	66.56	3216
HSA-MIR-4498	99.47	67.42	2360
HSA-MIR-125A-5P	99.36	70.59	1640
HSA-MIR-125B-5P	99.36	70.36	1662
HSA-MIR-185-5P	99.35	68.60	2497
HSA-MIR-4644	99.35	69.12	2514
HSA-MIR-5001-5P	99.05	66.76	1972
HSA-MIR-6506-5P	99.04	65.66	1386
HSA-MIR-330-5P	98.73	67.63	1788
HSA-MIR-619-5P	98.57	64.97	1988
HSA-MIR-326	98.25	66.44	1565
HSA-MIR-204-3P	97.80	66.84	1656
HSA-MIR-4646-5P	97.70	66.84	1692
HSA-MIR-665	97.60	65.64	1781
HSA-MIR-4314	97.50	67.30	1369
HSA-MIR-558	97.50	67.16	977
HSA-MIR-4690-3P	97.02	64.72	981
HSA-MIR-5685	97.02	64.34	1004

Literature-anchored findings (GeneRIF, showing 40)

• expression in prostate cancer negatively correlated with cancer aggressiveness (PMID:11948967)
• We found significantly lower expression of KLK5 in testicular tumors than in normal testicular tissue. (PMID:12385949)
• High expression of KLK5 transcript with a short 5’-untranslated region is associated with ovarian cancer (PMID:12738725)
• has trypsin-like substrate specificity and forms complexes with protease inhibitors in serum and ascites fluid from ovarian cancer patients (PMID:12890555)
• scte induced degradation of three corneodesmosomal components: corneodesmosin, desmocollin 1 and desmoglein 1 (PMID:15140227)
• may be part of a protease cascade in the stratum corneum, and that the observed pH effects may have physiological relevance (PMID:15654974)
• in normal skin the LG system transports and secretes LEKTI earlier than KLK7 and KLK5 preventing premature loss of stratum corneum integrity/cohesion. (PMID:15675955)
• hK5 may be implicated in tumor progression, particularly in invasion and angiogenesis (PMID:15713679)
• variability in KLK5 and KLK7 gene expression might be involved in lung tumorigenesis (PMID:15766562)
• hK5 is able to internally cleave insulin-like growth factor-binding proteins 1, 2, 3, 4, and 5, but not 6, suggesting that it might be involved in prostate cancer progression through growth factor regulation (PMID:16517595)
• in majority of patients with Netherton syndrome, Dsg1 & Dsc1 were reduced in living layers of epidermis; SCTE-like & SCCE-like activities were increased, suggesting these proteases participate in premature degradation of corneodesmosomal cadherins (PMID:16628198)
• KLK5 and KLK7 were shown to control activation of CAP18 and also influence further processing to smaller peptides with alternate biological activity; the balance of proteolytic activity at an epithelial interface will control innate immune defense (PMID:17012259)
• KLK5 may participate in epidermal desquamation through cleavage of desmoglein 1 and regulation by lympho-epithelial Kazal-type-related inhibitor (LEKTI). (PMID:17158887)
• A target of gene amplification, which may play a crucial role in promoting cancer-cell invasion in bladder tumor. (PMID:17459052)
• KLK5 and KLK14, but neither KLK7 nor KLK8, induced PAR2 signalling. (PMID:17625593)
• Dada shoe that the His96-99-57 triad is responsible for the Zn2+-mediated inhibition of hK5 catalysis. (PMID:17881000)
• predominant localisation of KLK5 and KLK7 in acinar cells of the exocrine pancreas; KLK5 and KLK7 generate transcripts in pancreas variant from those in skin or ovary (PMID:18163887)
• KLK4 and KLK5 activate pro-HGFA. (PMID:18221492)
• kallikreins 5, 7, 8, and 10 are abundantly expressed in human OSCC and may be implicated in malignant progression (PMID:19085836)
• reduced expression of LEKTI and increased expression of SCCE and SCTE in human epidermal keratinocytes after UVB irradiation may contribute to desquamation of the stratum corneum. (PMID:19118981)
• Treatment of PC3 prostate cancer cells with mitoxantrone, etoposide, doxorubicin and carboplatin induces distinct alterations in the expression of kallikreins 5 and 11. (PMID:19190824)
• the KLK region was subject to copy number imbalances or involved in unbalanced translocations and were associated with increased protein expression of KLKs 5, 6, 7, 8, 9, 10 and 11 in ovarian cancer cells (PMID:19383346)
• Parallel underexpression of KLK5 and KLK7 mRNA in breast malignancies is reported. (PMID:19453546)
• Combination of KLK2, 3, 13, and 14 and KLK1, 2, 5, 6, 7, 8, 10, 13, and 14 showed very strong discriminatory potential for semen liquefaction and viscosity, respectively. (PMID:19558318)
• Data show that it was unable to distinguish men with and without prostate cancer using multiple kallikreins as urinary biomarkers. (PMID:19560453)
• KLK5 is a potential new biomarker to be used in combination with other biomarkers for ovarian cancer detection. (PMID:19820362)
• expression and activity of KLK are under fine control and can be distinctly influenced by variables such as differentiation, calcium, vitamin D, and retinoic acid (PMID:20090765)
• KLK5 may promote metastatic dissemination of OSCC by promoting loss of junctional integrity through cleavage of desmoglein 1. (PMID:21163944)
• Increased serum and ascitic fluid KLK5 levels are associated with poor patient outcome, thus underlining the importance of KLK5 as a biomarker for early detection as well as for disease management in ovarian cancer. (PMID:21273346)
• Data indicate that the KLK5 SNP rs268908 was associated with an increased risk of prostate cancer. (PMID:21741862)
• Significant co-expression of KLKs 5 and 7 was observed in the same cancer samples. Increased KLK5 expression was a statistically significant independent prognostic factor for DFS and OS of patients (PMID:21868565)
• Loss of KLK5 is associated with ovarian cancer. (PMID:22102857)
• the inhibition and binding of different SPINK9 variants towards KLK5, KLK7, KLK8 and KLK14 (PMID:22505519)
• Kallikrein 5 and kallikrein 12 cleave human influenza hemagglutinins and activate thrombolytic zymogens. (PMID:23612974)
• KLK5 is required for biochemical processing of profilaggrin in human skin. (PMID:23629652)
• Low KLK5 expression is associated with breast cancer. (PMID:24158494)
• KLK5 is an important contributor to the Netherton syndrome proteolytic cascade. (PMID:24534191)
• This report demonstrates that concurrent loss of KLK5 and KLK7 associates with a poor clinical outcome in Oral Squamous-Cell Carcinoma and could therefore serve as prognostic marker in this disease. (PMID:26022646)
• the expression level of hK5 in tumor stromal cells is a promising biomarker for poor prognosis in TNBC. (PMID:26345898)
• The results of the present study indicated that the mRNA and protein expression levels of KLK5 were significantly upregulated in CRC tissues and sera, and were associated with an advanced tumor stage. (PMID:27430713)

Cross-species orthologs

13 orthologs

Organism	Symbol	Gene ID
mus_musculus	Klk5	ENSMUSG00000074155
rattus_norvegicus	Klk5	ENSRNOG00000018831
drosophila_melanogaster	CG9673	FBGN0030775
drosophila_melanogaster	CG4477	FBGN0035971
drosophila_melanogaster	CG17404	FBGN0038001
drosophila_melanogaster	CG12256	FBGN0038002
drosophila_melanogaster	CG3916	FBGN0038003
drosophila_melanogaster	CG17477	FBGN0038479
drosophila_melanogaster	CG4053	FBGN0038482
drosophila_melanogaster	CG31269	FBGN0051269
drosophila_melanogaster	CG32808	FBGN0052808
drosophila_melanogaster	Phae2	FBGN0263235
drosophila_melanogaster	Send2	FBGN0264253

Paralogs (12): PRSS54 (ENSG00000103023), KLK14 (ENSG00000129437), KLK8 (ENSG00000129455), TMPRSS4 (ENSG00000137648), KLK3 (ENSG00000142515), KLK1 (ENSG00000167748), KLK4 (ENSG00000167749), KLK2 (ENSG00000167751), KLK11 (ENSG00000167757), KLK7 (ENSG00000169035), KLK12 (ENSG00000186474), PRSS58 (ENSG00000258223)

Protein

Protein identifiers

Kallikrein-5 — Q9Y337 (reviewed: Q9Y337)

Alternative names: Kallikrein-like protein 2, Stratum corneum tryptic enzyme

All UniProt accessions (2): Q9Y337, M0QXX2

UniProt curated annotations — full annotation on UniProt →

Function. May be involved in desquamation.

Subunit / interactions. Interacts with SPINK9.

Subcellular location. Secreted.

Tissue specificity. Expressed in skin, breast, brain and testis. Expressed at the stratum granulosum of palmar skin.

Activity regulation. Inhibited by Zn2+.

Similarity. Belongs to the peptidase S1 family. Kallikrein subfamily.

RefSeq proteins (3): NP_001070959, NP_001070960, NP_036559* (*=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.B39 — (BRENDA: organisms, substrates, inhibitors, Km, kcat entries)

UniProt features (44 total): strand 17, disulfide bond 6, glycosylation site 4, helix 4, active site 3, sequence variant 2, turn 2, signal peptide 1, chain 1, domain 1, region of interest 1, compositionally biased region 1, site 1

Structure

Experimental structures (PDB)

4 structures.

PDB	Method	Resolution (Å)
6QFE	X-RAY DIFFRACTION	1.67
2PSX	X-RAY DIFFRACTION	2.3
2PSY	X-RAY DIFFRACTION	2.3
7U5B	X-RAY DIFFRACTION	2.37

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9Y337-F1	83.80	0.69

Antibody-complex structures (SAbDab): 1 — 7U5B

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 (4): 108 (charge relay system); 153 (charge relay system); 245 (charge relay system); 150 (major binding site for inhibitory zinc)

Disulfide bonds (6): 73–206, 93–109, 178–279, 185–251, 217–231, 241–266

Glycosylation sites (4): 173, 208, 252, 69

Function

Pathways and Gene Ontology

Reactome pathways

5 pathways

ID	Pathway
R-HSA-6809371	Formation of the cornified envelope
R-HSA-9725554	Differentiation of Keratinocytes in Interfollicular Epidermis in Mammalian Skin
R-HSA-1266738	Developmental Biology
R-HSA-6805567	Keratinization
R-HSA-9734767	Developmental Cell Lineages

MSigDB gene sets: 109 (showing top): GOBP_EPITHELIUM_DEVELOPMENT, GOBP_ANTIMICROBIAL_HUMORAL_RESPONSE, GOCC_SECRETORY_GRANULE, GOBP_PEPTIDE_METABOLIC_PROCESS, GOBP_EPIDERMAL_CELL_DIFFERENTIATION, GOBP_ANIMAL_ORGAN_MORPHOGENESIS, GOBP_PROTEIN_MATURATION, GOBP_DEFENSE_RESPONSE_TO_OTHER_ORGANISM, CHARAFE_BREAST_CANCER_BASAL_VS_MESENCHYMAL_UP, GOBP_HUMORAL_IMMUNE_RESPONSE, GOBP_EPIDERMIS_DEVELOPMENT, GOBP_AMELOGENESIS, CHARAFE_BREAST_CANCER_LUMINAL_VS_BASAL_DN, GOBP_EXTRACELLULAR_MATRIX_DISASSEMBLY, GOBP_ODONTOGENESIS_OF_DENTIN_CONTAINING_TOOTH

GO Biological Process (9): antibacterial peptide biosynthetic process (GO:0002780), proteolysis (GO:0006508), epidermis development (GO:0008544), extracellular matrix disassembly (GO:0022617), positive regulation of G protein-coupled receptor signaling pathway (GO:0045745), protein maturation (GO:0051604), cornification (GO:0070268), amelogenesis (GO:0097186), positive regulation of antibacterial peptide production (GO:0002803)

GO Molecular Function (5): serine-type endopeptidase activity (GO:0004252), peptidase activity (GO:0008233), serine-type peptidase activity (GO:0008236), protein binding (GO:0005515), hydrolase activity (GO:0016787)

GO Cellular Component (5): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), cytosol (GO:0005829), secretory granule (GO:0030141), epidermal lamellar body (GO:0097209)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
Developmental Biology	2
Keratinization	1
Developmental Cell Lineages of the Integumentary System	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
antibacterial peptide production	2
protein metabolic process	2
cellular anatomical structure	2
antimicrobial peptide biosynthetic process	1
tissue development	1
cellular component disassembly	1
extracellular matrix organization	1
G protein-coupled receptor signaling pathway	1
regulation of G protein-coupled receptor signaling pathway	1
positive regulation of signal transduction	1
gene expression	1
programmed cell death	1
keratinization	1
cornified envelope assembly	1
odontogenesis of dentin-containing tooth	1
anatomical structure formation involved in morphogenesis	1
positive regulation of antimicrobial peptide production	1
regulation of antibacterial peptide production	1
positive regulation of defense response to bacterium	1
endopeptidase activity	1
serine-type peptidase activity	1
hydrolase activity	1
catalytic activity, acting on a protein	1
peptidase activity	1
serine hydrolase activity	1
binding	1
catalytic activity	1
cytoplasm	1
endomembrane system	1
secretory vesicle	1
lamellar body	1

Protein interactions and networks

STRING

0 interactions, top by confidence (×1000):

IntAct

36 interactions, top by confidence:

A	B	Type	Score
KLK5	DENND11	psi-mi:“MI:0914”(association)	0.640
CCND3	CDK1	psi-mi:“MI:0914”(association)	0.640
ALDH3A1	RCCD1	psi-mi:“MI:0914”(association)	0.640
CFAP298	PEX7	psi-mi:“MI:0914”(association)	0.620
KLK5	FLG	psi-mi:“MI:0194”(cleavage reaction)	0.570
FLG	KLK5	psi-mi:“MI:0403”(colocalization)	0.570
FLG	KLK5	psi-mi:“MI:2364”(proximity)	0.570
MANBAL	KLK5	psi-mi:“MI:0915”(physical association)	0.560
FTH1	A2ML1	psi-mi:“MI:0914”(association)	0.530
NAT2	STARD7	psi-mi:“MI:0914”(association)	0.530
KLK5	AURKA	psi-mi:“MI:0915”(physical association)	0.370
BAG4	KLK5	psi-mi:“MI:0915”(physical association)	0.370
KLK5	CASP8	psi-mi:“MI:0915”(physical association)	0.370
ERBB2	KLK5	psi-mi:“MI:0915”(physical association)	0.370
KLK5	ESR1	psi-mi:“MI:0915”(physical association)	0.370
IGF1R	KLK5	psi-mi:“MI:0915”(physical association)	0.370
NOTCH2	KLK5	psi-mi:“MI:0915”(physical association)	0.370
KLK5	TGFB1	psi-mi:“MI:0915”(physical association)	0.370
KLK5	TSG101	psi-mi:“MI:0915”(physical association)	0.370
PI4KAP1	A2ML1	psi-mi:“MI:0914”(association)	0.350
TEFM	A2ML1	psi-mi:“MI:0914”(association)	0.350
PRSS16	KLK10	psi-mi:“MI:0914”(association)	0.350
ZDHHC19	QSOX1	psi-mi:“MI:0914”(association)	0.350

BioGRID (158): KLK5 (Affinity Capture-MS), TUBB4A (Affinity Capture-MS), TUBB3 (Affinity Capture-MS), TUBB8 (Affinity Capture-MS), VWA9 (Affinity Capture-MS), FREM2 (Affinity Capture-MS), METTL13 (Affinity Capture-MS), TUBA4A (Affinity Capture-MS), TUBA1A (Affinity Capture-MS), ITGB5 (Affinity Capture-MS), NEU3 (Affinity Capture-MS), OS9 (Affinity Capture-MS), CBWD1 (Affinity Capture-MS), FRAS1 (Affinity Capture-MS), PASK (Affinity Capture-MS)

ESM2 similar proteins: A7WPL7, O35164, O35205, O46683, O88780, P00770, P04187, P07288, P08883, P08884, P09582, P09650, P10144, P11032, P11034, P13366, P15119, P17977, P20151, P20718, P21812, P21842, P21844, P23946, P28293, P33619, P36368, P36369, P43430, P49862, P50339, P50340, P50341, P52195, P56435, P79204, P80219, P80931, P85202, P97592

Diamond homologs: O18783, O35164, O35205, O46683, O60259, O88780, P00746, P00747, P00752, P00756, P00758, P00759, P00760, P00761, P00762, P00763, P00764, P00770, P03953, P04187, P07146, P07288, P08311, P08426, P08882, P08883, P09582, P09650, P10144, P11032, P11034, P12323, P12544, P12545, P15119, P15946, P15949, P18291, P19799, P20151

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	42
Likely benign	5
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1185 predictions. Top by Δscore:

Variant	Effect	Δscore
19:50949852:CA:C	donor_loss	1.0000
19:50949853:A:AC	donor_gain	1.0000
19:50949853:ACT:A	donor_loss	1.0000
19:50949854:C:CA	donor_gain	1.0000
19:50949854:CTT:C	donor_gain	1.0000
19:50949856:T:TA	donor_gain	1.0000
19:50949859:T:TA	donor_gain	1.0000
19:50948772:CA:C	acceptor_gain	0.9900
19:50948854:CTCA:C	donor_loss	0.9900
19:50948855:TCACC:T	donor_loss	0.9900
19:50948856:CACC:C	donor_loss	0.9900
19:50948857:A:AT	donor_loss	0.9900
19:50949846:C:CA	donor_gain	0.9900
19:50949850:CTCA:C	donor_gain	0.9900
19:50949853:ACTT:A	donor_gain	0.9900
19:50949854:CT:C	donor_gain	0.9900
19:50949854:CTTC:C	donor_gain	0.9900
19:50949854:CTTCT:C	donor_gain	0.9900
19:50950057:C:CT	acceptor_gain	0.9900
19:50950071:T:TC	acceptor_gain	0.9900
19:50950113:TGCT:T	acceptor_gain	0.9900
19:50950115:CT:C	acceptor_gain	0.9900
19:50950117:C:CC	acceptor_gain	0.9900
19:50952042:G:C	donor_gain	0.9900
19:50952083:AG:A	donor_gain	0.9900
19:50952084:G:C	donor_gain	0.9900
19:50952586:TGTG:T	donor_gain	0.9900
19:50943782:TCACC:T	acceptor_gain	0.9800
19:50943783:CACC:C	acceptor_gain	0.9800
19:50943783:CACCC:C	acceptor_gain	0.9800

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000100544 (19:50954133 C>T), RS1000240368 (19:50948567 G>A), RS1000310379 (19:50954543 A>G), RS1000359265 (19:50944775 C>T), RS1000420913 (19:50949300 T>C), RS1000535694 (19:50949037 T>C), RS1000608863 (19:50954770 C>A,T), RS1000647418 (19:50945005 T>C), RS1000694330 (19:50945069 T>C), RS1001127286 (19:50954177 G>A), RS1001374785 (19:50950196 C>A,T), RS1001758979 (19:50946715 A>G,T), RS1001869792 (19:50945039 T>C), RS1002240173 (19:50951173 T>C), RS1002650294 (19:50947256 C>A,G,T)

Disease associations

OMIM: gene MIM:605643 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4447 (SINGLE PROTEIN)

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 (2 total), top 2:

Ligand	Action	Affinity	Parameter
compound 3 [PMID: 23849879]	Inhibition	6.57	pIC50
compound 4d [PMID: 25489658]	Inhibition	6.04	pIC50

Binding affinities (BindingDB)

1047 measured of 1264 human assays (1291 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(E)-3-(1-cyclohex-3-enyl)-2-(1-methyl-2-benzimidazolyl)-2-propenenitrile	EC50	0.0152 nM
MLS000053281	EC50	0.0172 nM
3-(1-ethyl-5-methyl-4-pyrazolyl)-N-(phenylmethyl)-4,5-dihydroisoxazole-5-carboxamide	EC50	0.0992 nM
CHEMBL5199103	KI	1.4 nM
CHEMBL5198215	KI	1.5 nM
CHEMBL5176455	KI	1.9 nM
CHEMBL5177587	KI	2 nM
CHEMBL5203034	KI	2.7 nM
CHEMBL5192991	KI	2.7 nM
CHEMBL5175408	KI	3.6 nM
CHEMBL5194536	KI	5.1 nM
CHEMBL5209454	KI	6.1 nM
CHEMBL5181364	KI	11 nM
CHEMBL5196523	KI	24 nM
(4-methylphenyl)-(5-methylsulfanyl-3-phenyl-1,2,4-triazol-1-yl)methanone	IC50	28 nM
CHEMBL5172332	KI	28 nM
CHEMBL5203584	KI	29 nM
1-(6-bromopyrazolo[1,5-a]pyrimidine-2-carbonyl)nipecotic acid ethyl ester	IC50	69.4 nM
(E)-2-(4-bromophenyl)-3-(2,5-dimethoxy-4-pyrrolidin-1-yl-phenyl)prop-2-enenitrile	EC50	74.5 nM
CHEMBL5185690	KI	79 nM
3-benzamido-1H-1,2,4-triazole-5-carboxylic acid methyl ester	IC50	92.4 nM
2-(2,4-dimethoxyphenyl)-6,7-dimethoxy-3,1-benzoxazin-4-one	KI	100 nM	US-9695194: Benzoxazinone derivatives for treatment of skin diseases
MLS000706208	IC50	159 nM
5-amino-1-(4-methoxybenzoyl)pyrazole-4-carbonitrile	IC50	195 nM
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
SMR000120438	IC50	450 nM
MLS000419584	IC50	455 nM
MLS000711688	EC50	481 nM
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
(5-amino-3-pyridin-3-yl-1,2,4-triazol-1-yl)-(2-methoxyphenyl)methanone	IC50	503 nM
MLS000043693	IC50	525 nM
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
(5-Amino-3-furan-2-yl-[1,2,4]triazol-1-yl)-phenyl-methanone	IC50	643 nM
5-methyl-2-phenyl-4-[[2-(4-phenyl-2-oxazolin-2-yl)pyrrol-1-yl]methyl]oxazole	EC50	692 nM
(2,4-difluorophenyl)-(2-quinolyl)amine	EC50	698 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
(4-chlorophenyl)-(5-methylsulfanyl-3-phenyl-1,2,4-triazol-1-yl)methanone	IC50	725 nM
1-benzotriazolyl-(3,4-dimethoxyphenyl)methanone	IC50	755 nM
2-Furan-2-yl-benzo[d][1,3]oxazin-4-one	IC50	793 nM
2-(4-fluorobenzoyl)-4,4-dimethyl-1-phenyl-pyrazolidin-3-one	IC50	837 nM
(5-methylsulfanyl-3-phenyl-1,2,4-triazol-1-yl)-phenyl-methanone	IC50	896 nM
(4-methoxyphenyl)-(5-methylsulfanyl-3-phenyl-1,2,4-triazol-1-yl)methanone	IC50	913 nM
2-furancarboxylic acid [5-amino-1-(4-methoxyphenyl)sulfonyl-3-pyrazolyl] ester	IC50	924 nM
2-[(5-benzamido-1H-1,2,4-triazol-3-yl)thio]acetic acid ethyl ester	IC50	945 nM
2-[[5-(m-toluoylamino)-1H-1,2,4-triazol-3-yl]thio]acetic acid ethyl ester	IC50	965 nM

ChEMBL bioactivities

147 potent at pChembl≥5 of 191 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.47	Ki	0.34	nM	CHEMBL4466351
9.30	IC50	0.5012	nM	CHEMBL4447752
9.14	Ki	0.73	nM	CHEMBL4550494
8.92	Ki	1.2	nM	CHEMBL5203652
8.90	IC50	1.259	nM	CHEMBL4461533
8.85	Ki	1.4	nM	CHEMBL5199103
8.82	Ki	1.5	nM	CHEMBL5198215
8.80	IC50	1.585	nM	CHEMBL4543039
8.72	Ki	1.9	nM	CHEMBL5176455
8.70	Ki	2	nM	CHEMBL5177587
8.68	Ki	2.1	nM	CHEMBL3623776
8.66	Ki	2.2	nM	CHEMBL5205331
8.62	Ki	2.4	nM	CHEMBL4575658
8.60	IC50	2.512	nM	CHEMBL4473069
8.57	Ki	2.7	nM	CHEMBL5203034
8.57	Ki	2.7	nM	CHEMBL5192991
8.50	IC50	3.162	nM	CHEMBL4447752
8.49	Ki	3.2	nM	CHEMBL5174330
8.44	Ki	3.6	nM	CHEMBL5175408
8.43	Ki	3.7	nM	CHEMBL4456620
8.40	IC50	3.981	nM	CHEMBL4579813
8.30	IC50	5.012	nM	CHEMBL4558285
8.30	IC50	5.012	nM	CHEMBL4465265
8.30	IC50	5.012	nM	CHEMBL4517343
8.29	Ki	5.1	nM	CHEMBL5194536
8.28	Ki	5.2	nM	CHEMBL3623779
8.24	Ki	5.8	nM	CHEMBL5194019
8.21	Ki	6.1	nM	CHEMBL5209454
8.20	IC50	6.31	nM	CHEMBL4579813
8.20	IC50	6.31	nM	CHEMBL4543039
8.20	IC50	6.31	nM	CHEMBL4436048
8.19	Ki	6.4	nM	CHEMBL5172150
8.15	Ki	7	nM	CHEMBL5192120
8.10	IC50	7.943	nM	CHEMBL4517343
8.10	IC50	7.943	nM	CHEMBL4461533
8.10	IC50	7.943	nM	CHEMBL4535907
8.10	IC50	7.943	nM	CHEMBL4464120
8.10	IC50	7.943	nM	CHEMBL4536142
8.05	Ki	8.9	nM	CHEMBL4513520
8.00	IC50	10	nM	CHEMBL4535907
8.00	IC50	10	nM	CHEMBL4448315
7.97	Ki	10.8	nM	CHEMBL5181364
7.90	IC50	12.59	nM	CHEMBL4464120
7.90	IC50	12.59	nM	CHEMBL4473069
7.80	IC50	15.85	nM	CHEMBL4448315
7.70	IC50	19.95	nM	CHEMBL4436048
7.70	IC50	19.95	nM	CHEMBL4536142
7.64	Ki	23	nM	CHEMBL5172861
7.62	Ki	24	nM	CHEMBL5196523
7.60	IC50	25.12	nM	CHEMBL4460168

PubChem BioAssay actives

134 with measured affinity, of 308 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)-28,40-bis(2-amino-2-oxoethyl)-49-benzyl-25-(3-carbamimidamidopropyl)-22-(hydroxymethyl)-19,34-bis[(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	1557491: Inhibition of recombinant human KLK5 expressed in expressed in Pichia pastoris X-33 cells using Boc-VPR-MCA as susbtrate measured every 60 secs for 10 mins by fluorescence based assay	ki	0.0003	uM
4-[(3R)-1-hydroxy-7-(trifluoromethyl)-3,4-dihydro-2,1-benzoxaborinin-3-yl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride	1601474: Inhibition of human recombinant 6His-Q-FLAG-tagged KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins using 1 x 10'10M enzyme by FLINT assay	ic50	0.0003	uM
4-[1-hydroxy-7-(trifluoromethyl)-3,4-dihydro-2,1-benzoxaborinin-3-yl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride	1601474: Inhibition of human recombinant 6His-Q-FLAG-tagged KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins using 1 x 10'10M enzyme by FLINT assay	ic50	0.0005	uM
2-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,40S,43S,49S)-28,40-bis(2-amino-2-oxoethyl)-49-benzyl-25-(3-carbamimidamidopropyl)-22-(hydroxymethyl)-19,34-bis[(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]acetic acid	1557491: Inhibition of recombinant human KLK5 expressed in expressed in Pichia pastoris X-33 cells using Boc-VPR-MCA as susbtrate measured every 60 secs for 10 mins by fluorescence based assay	ki	0.0007	uM
4-[(3S)-1-hydroxy-7-(trifluoromethyl)-3,4-dihydro-2,1-benzoxaborinin-3-yl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride	1601474: Inhibition of human recombinant 6His-Q-FLAG-tagged KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins using 1 x 10'10M enzyme by FLINT assay	ic50	0.0008	uM
5-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[2-[2-[2-[[(5S)-5-[[2-[[(3S,6S,9S,12S,15R,23R,26S)-15-[(2-aminoacetyl)amino]-6-(3-amino-3-oxopropyl)-9-(3-carbamimidamidopropyl)-12-[(1R)-1-hydroxyethyl]-3-[(4-hydroxyphenyl)methyl]-2,5,8,11,14,19,25-heptaoxo-17,21-dithia-1,4,7,10,13,24-hexazabicyclo[24.3.0]nonacosane-23-carbonyl]amino]acetyl]amino]-6-[(2-amino-2-oxoethyl)amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-4-carboxy-1-oxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylcarbamoyl]-2-(3-hydroxy-6-oxoxanthen-9-yl)benzoic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0012	uM
4-(6-chloro-7-fluoro-1-hydroxy-3,4-dihydro-2,1-benzoxaborinin-3-yl)-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride	1601474: Inhibition of human recombinant 6His-Q-FLAG-tagged KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins using 1 x 10'10M enzyme by FLINT assay	ic50	0.0013	uM
(5R,8S,11S,17S,20S,23S,26S,29S,32R)-32-[(2-aminoacetyl)amino]-23-(3-amino-3-oxopropyl)-17-(carboxymethyl)-26-[3-(diaminomethylideneamino)propyl]-29-[(1R)-1-hydroxyethyl]-8-(hydroxymethyl)-20-(1H-indol-3-ylmethyl)-7,10,16,19,22,25,28,31-octaoxo-3,34-dithia-6,9,15,18,21,24,27,30,40-nonazatricyclo[34.3.1.011,15]tetraconta-1(39),36(40),37-triene-5-carboxylic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0014	uM
(3S,6S,9S,12S,15S,18R,26R,29S,32S,35S)-18-[(2-aminoacetyl)amino]-9-(3-amino-3-oxopropyl)-3-(carboxymethyl)-12-[3-(diaminomethylideneamino)propyl]-15-[(1R)-1-hydroxyethyl]-32-(hydroxymethyl)-6-(1H-indol-3-ylmethyl)-29-(2-methylpropyl)-2,5,8,11,14,17,22,28,31,34-decaoxo-20,24-dithia-1,4,7,10,13,16,27,30,33-nonazabicyclo[33.3.0]octatriacontane-26-carboxylic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0015	uM
4-[(6-fluoro-1-hydroxy-3H-2,1-benzoxaborol-3-yl)methyl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride	1601474: Inhibition of human recombinant 6His-Q-FLAG-tagged KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins using 1 x 10'10M enzyme by FLINT assay	ic50	0.0016	uM
(2S)-2-[[(3S,6S,9S,12S,15R,23R,26S)-15-[(2-aminoacetyl)amino]-6-(3-amino-3-oxopropyl)-9-[3-(diaminomethylideneamino)propyl]-12-[(1R)-1-hydroxyethyl]-3-(1H-indol-3-ylmethyl)-2,5,8,11,14,19,25-heptaoxo-17,21-dithia-1,4,7,10,13,24-hexazabicyclo[24.3.0]nonacosane-23-carbonyl]amino]butanedioic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0019	uM
(2S)-2-[[(5S,8S,11S)-11-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(5R,8S,14S,17S,20S,23S,26S)-26-[(2-aminoacetyl)amino]-17-(3-amino-3-oxopropyl)-20-(3-carbamimidamidopropyl)-23-[(1R)-1-hydroxyethyl]-14-(1H-indol-3-ylmethyl)-7,13,16,19,22,25-hexaoxo-3,28-dithia-6,12,15,18,21,24,34-heptazatricyclo[28.3.1.08,12]tetratriaconta-1(33),30(34),31-triene-5-carbonyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-8-[(1R)-1-hydroxyethyl]-7,10-dioxo-3,13-dithia-6,9,19-triazabicyclo[13.3.1]nonadeca-1(18),15(19),16-triene-5-carbonyl]amino]-3-methylbutanoic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0020	uM
2-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,40S,43S,49S)-49-(2-amino-2-oxoethyl)-4,19-bis[(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-40-yl]acetamide	1251577: Inhibition of KLK5 (unknown origin) expressed in Pichia pastoris X33 using Ac-YRSR-pNA by spectrophotometry method	ki	0.0021	uM
(3S,6S,9S,12S,15R,23R,26S)-15-[(2-aminoacetyl)amino]-6-(3-amino-3-oxopropyl)-9-[3-(diaminomethylideneamino)propyl]-12-[(1R)-1-hydroxyethyl]-3-[(4-hydroxyphenyl)methyl]-2,5,8,11,14,19,25-heptaoxo-17,21-dithia-1,4,7,10,13,24-hexazabicyclo[24.3.0]nonacosane-23-carboxylic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0022	uM
3-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,40S,43S,49S)-40-(2-amino-2-oxoethyl)-34-benzyl-25-(3-carbamimidamidopropyl)-22-(hydroxymethyl)-19-[(4-hydroxyphenyl)methyl]-28-(1H-imidazol-5-ylmethyl)-49-(1H-indol-3-ylmethyl)-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	1557491: Inhibition of recombinant human KLK5 expressed in expressed in Pichia pastoris X-33 cells using Boc-VPR-MCA as susbtrate measured every 60 secs for 10 mins by fluorescence based assay	ki	0.0024	uM
4-[[1-hydroxy-6-(trifluoromethyl)-3H-2,1-benzoxaborol-3-yl]methyl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride	1601474: Inhibition of human recombinant 6His-Q-FLAG-tagged KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins using 1 x 10'10M enzyme by FLINT assay	ic50	0.0025	uM
(5R,8S,14S,17S,20S,23S,26S,29R)-29-[(2-aminoacetyl)amino]-20-(3-amino-3-oxopropyl)-14-(carboxymethyl)-23-[3-(diaminomethylideneamino)propyl]-26-[(1R)-1-hydroxyethyl]-17-(1H-indol-3-ylmethyl)-7,13,16,19,22,25,28-heptaoxo-3,31-dithia-6,12,15,18,21,24,27,37-octazatricyclo[31.3.1.08,12]heptatriaconta-1(36),33(37),34-triene-5-carboxylic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0027	uM
(2S)-2-[[(5S,8S,11S)-11-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(5R,8S,14S,17S,20S,23S,26R)-26-[(2-aminoacetyl)amino]-17-(3-amino-3-oxopropyl)-20-(3-carbamimidamidopropyl)-23-[(1R)-1-hydroxyethyl]-14-(1H-indol-3-ylmethyl)-7,13,16,19,22,25-hexaoxo-3,28-dithia-6,12,15,18,21,24,34-heptazatricyclo[28.3.1.08,12]tetratriaconta-1(33),30(34),31-triene-5-carbonyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-8-[(1R)-1-hydroxyethyl]-7,10-dioxo-3,13-dithia-6,9,19-triazabicyclo[13.3.1]nonadeca-1(18),15(19),16-triene-5-carbonyl]amino]-3-methylbutanoic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0027	uM
(3S,6S,9S,12S,15R,23R,26S)-15-[(2-aminoacetyl)amino]-6-(2-carboxyethyl)-9-[3-(diaminomethylideneamino)propyl]-12-[(1R)-1-hydroxyethyl]-3-[(4-hydroxyphenyl)methyl]-2,5,8,11,14,19,25-heptaoxo-17,21-dithia-1,4,7,10,13,24-hexazabicyclo[24.3.0]nonacosane-23-carboxylic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0032	uM
(3S,6S,9S,12S,15R,23R,26S)-15-[(2-aminoacetyl)amino]-6-(3-amino-3-oxopropyl)-9-[3-(diaminomethylideneamino)propyl]-12-[(1R)-1-hydroxyethyl]-3-(1H-indol-3-ylmethyl)-2,5,8,11,14,19,25-heptaoxo-17,21-dithia-1,4,7,10,13,24-hexazabicyclo[24.3.0]nonacosane-23-carboxylic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0036	uM
3-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,40S,43S,49S)-40-(2-amino-2-oxoethyl)-34,49-dibenzyl-25-(3-carbamimidamidopropyl)-22-(hydroxymethyl)-19-[(4-hydroxyphenyl)methyl]-28-(1H-imidazol-5-ylmethyl)-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	1557491: Inhibition of recombinant human KLK5 expressed in expressed in Pichia pastoris X-33 cells using Boc-VPR-MCA as susbtrate measured every 60 secs for 10 mins by fluorescence based assay	ki	0.0037	uM
4-(1-hydroxy-3,4-dihydro-2,1-benzoxaborinin-3-yl)-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride	1601474: Inhibition of human recombinant 6His-Q-FLAG-tagged KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins using 1 x 10'10M enzyme by FLINT assay	ic50	0.0040	uM
2-[(3-chlorophenyl)methoxy]-4-(1-hydroxy-3,4-dihydro-2,1-benzoxaborinin-3-yl)benzenecarboximidamide;hydrochloride	1601474: Inhibition of human recombinant 6His-Q-FLAG-tagged KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins using 1 x 10'10M enzyme by FLINT assay	ic50	0.0050	uM
(3S,6S,9S,12S,15R,23R,26S)-15-[(2-aminoacetyl)amino]-6-(2-carboxyethyl)-9-[3-(diaminomethylideneamino)propyl]-12-[(1R)-1-hydroxyethyl]-3-(1H-indol-3-ylmethyl)-2,5,8,11,14,19,25-heptaoxo-17,21-dithia-1,4,7,10,13,24-hexazabicyclo[24.3.0]nonacosane-23-carboxylic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0051	uM
2-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,40S,43S,49S)-19,49-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-40-yl]acetamide	1251577: Inhibition of KLK5 (unknown origin) expressed in Pichia pastoris X33 using Ac-YRSR-pNA by spectrophotometry method	ki	0.0052	uM
(5R,8S,11S,14S,17S,20R)-20-[(2-aminoacetyl)amino]-11-(3-amino-3-oxopropyl)-14-[3-(diaminomethylideneamino)propyl]-17-[(1R)-1-hydroxyethyl]-7,10,13,16,19-pentaoxo-8-propan-2-yl-3,22-dithia-6,9,12,15,18,28-hexazabicyclo[22.3.1]octacosa-1(27),24(28),25-triene-5-carboxylic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0058	uM
(2S)-2-[[(5R,8S,11R)-11-[[(2S)-5-amino-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-[[(5R,8S,11S,17S,20S,23S,26S,29S,32R)-17-(2-amino-2-oxoethyl)-8-(3-amino-3-oxopropyl)-32-[[(2S)-2-aminopropanoyl]amino]-26-(3-carbamimidamidopropyl)-23-(2-carboxyethyl)-29-[(1R)-1-hydroxyethyl]-20-[(4-hydroxyphenyl)methyl]-7,10,16,19,22,25,28,31-octaoxo-3,34-dithia-6,9,15,18,21,24,27,30,40-nonazatricyclo[34.3.1.011,15]tetraconta-1(39),36(40),37-triene-5-carbonyl]amino]propanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-8-(2-methylpropyl)-7,10-dioxo-3,13-dithia-6,9,19-triazabicyclo[13.3.1]nonadeca-1(18),15(19),16-triene-5-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0061	uM
4-[(1-hydroxy-3H-2,1-benzoxaborol-3-yl)methyl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride	1601474: Inhibition of human recombinant 6His-Q-FLAG-tagged KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins using 1 x 10'10M enzyme by FLINT assay	ic50	0.0063	uM
(5R,8S,11S,14S,17S,20R)-20-[(2-aminoacetyl)amino]-11-(2-carboxyethyl)-14-[3-(diaminomethylideneamino)propyl]-17-[(1R)-1-hydroxyethyl]-7,10,13,16,19-pentaoxo-8-propan-2-yl-3,22-dithia-6,9,12,15,18,28-hexazabicyclo[22.3.1]octacosa-1(27),24(28),25-triene-5-carboxylic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0064	uM
(2S)-4-amino-2-[[(5R,11S,14S,17S,20R)-5-[[(2S)-2-[[(2S)-1-[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S)-5-amino-2-[[(5R,8S,11S,14S,17S,20R)-20-[(2-aminoacetyl)amino]-11-(3-amino-3-oxopropyl)-14-(3-carbamimidamidopropyl)-17-[(1R)-1-hydroxyethyl]-7,10,13,16,19-pentaoxo-8-propan-2-yl-3,22-dithia-6,9,12,15,18,28-hexazabicyclo[22.3.1]octacosa-1(27),24(28),25-triene-5-carbonyl]amino]-5-oxopentanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]-14-(hydroxymethyl)-17-methyl-6,12,15,18-tetraoxo-3,22-dithia-7,13,16,19,28-pentazatricyclo[22.3.1.07,11]octacosa-1(28),24,26-triene-20-carbonyl]amino]-4-oxobutanoic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0070	uM
4-(7-fluoro-1-hydroxy-3,4-dihydro-2,1-benzoxaborinin-3-yl)-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride	1601474: Inhibition of human recombinant 6His-Q-FLAG-tagged KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins using 1 x 10'10M enzyme by FLINT assay	ic50	0.0079	uM
2-[(2-chlorophenyl)methoxy]-4-(1-hydroxy-3,4-dihydro-2,1-benzoxaborinin-3-yl)benzenecarboximidamide;hydrochloride	1601474: Inhibition of human recombinant 6His-Q-FLAG-tagged KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins using 1 x 10'10M enzyme by FLINT assay	ic50	0.0079	uM
4-[(1-hydroxy-5-methyl-3H-2,1-benzoxaborol-3-yl)methyl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride	1601474: Inhibition of human recombinant 6His-Q-FLAG-tagged KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins using 1 x 10'10M enzyme by FLINT assay	ic50	0.0079	uM
2-[(1R,4S,7S,13S,19S,22S,25S,28S,31R,34S,40S,43S,49S)-40-(2-amino-2-oxoethyl)-34,49-dibenzyl-25-(3-carbamimidamidopropyl)-22-(hydroxymethyl)-19-[(4-hydroxyphenyl)methyl]-28-(1H-imidazol-5-ylmethyl)-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]acetic acid	1557491: Inhibition of recombinant human KLK5 expressed in expressed in Pichia pastoris X-33 cells using Boc-VPR-MCA as susbtrate measured every 60 secs for 10 mins by fluorescence based assay	ki	0.0089	uM
4-[(5-fluoro-1-hydroxy-3H-2,1-benzoxaborol-3-yl)methyl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride	1601474: Inhibition of human recombinant 6His-Q-FLAG-tagged KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins using 1 x 10'10M enzyme by FLINT assay	ic50	0.0100	uM
4-[(5-phenyl-1H-imidazol-2-yl)methylamino]-2-phenylmethoxybenzenecarboximidamide	1589829: Inhibition of recombinant 6His-Q-FLAG tagged human KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins by fluorescence intensity assay	ic50	0.0100	uM
(5R,8S,11S,14S,17S,20R)-20-[(2-aminoacetyl)amino]-11-(2-carboxyethyl)-14-[3-(diaminomethylideneamino)propyl]-17-[(1R)-1-hydroxyethyl]-8-(1H-indol-3-ylmethyl)-7,10,13,16,19-pentaoxo-3,22-dithia-6,9,12,15,18,28-hexazabicyclo[22.3.1]octacosa-1(27),24(28),25-triene-5-carboxylic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0108	uM
5-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[2-[2-[2-[[(3S,6S,9S,12S,15R,23R,26S)-6-(3-amino-3-oxopropyl)-9-(3-carbamimidamidopropyl)-23-carbamoyl-12-[(1R)-1-hydroxyethyl]-3-[(4-hydroxyphenyl)methyl]-2,5,8,11,14,19,25-heptaoxo-17,21-dithia-1,4,7,10,13,24-hexazabicyclo[24.3.0]nonacosan-15-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-4-carboxy-1-oxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-(hexadecanoylamino)-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylcarbamoyl]-2-(3-hydroxy-6-oxoxanthen-9-yl)benzoic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0230	uM
(2S)-1-[(3R,11R,14S,17S,20S,23S)-3-[[(3S,6S,9S,12S,15S,18R,26R,29S,32S,35S)-18-[[(2S)-2-amino-4-methylsulfanylbutanoyl]amino]-9-(3-amino-3-oxopropyl)-12-(3-carbamimidamidopropyl)-3-(carboxymethyl)-15,32-bis(hydroxymethyl)-6-(1H-indol-3-ylmethyl)-29-(2-methylpropyl)-2,5,8,11,14,17,22,28,31,34-decaoxo-20,24-dithia-1,4,7,10,13,16,27,30,33-nonazabicyclo[33.3.0]octatriacontane-26-carbonyl]amino]-20-(3-amino-3-oxopropyl)-17-(3-carbamimidamidopropyl)-14-[(1R)-1-hydroxyethyl]-2,7,13,16,19,22-hexaoxo-5,9-dithia-1,12,15,18,21-pentazabicyclo[21.3.0]hexacosane-11-carbonyl]pyrrolidine-2-carboxylic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0240	uM
4-(1-hydroxy-8-methyl-3,4-dihydro-2,1-benzoxaborinin-3-yl)-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride	1601456: Inhibition of human recombinant 6His-Q-FLAG-tagged KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins by FLINT assay	ic50	0.0251	uM
4-[(1-hydroxy-5-methoxy-3H-2,1-benzoxaborol-3-yl)methyl]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide;hydrochloride	1601474: Inhibition of human recombinant 6His-Q-FLAG-tagged KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins using 1 x 10'10M enzyme by FLINT assay	ic50	0.0251	uM
(2S)-2-[[(3R,6S,9R)-9-[[(2S)-5-amino-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-[[(3S,6S,9S,12S,15S,18R,26R,29S,32S)-3-(2-amino-2-oxoethyl)-29-(3-amino-3-oxopropyl)-18-[[(2S)-2-aminopropanoyl]amino]-12-(3-carbamimidamidopropyl)-9-(2-carboxyethyl)-15-[(1R)-1-hydroxyethyl]-6-[(4-hydroxyphenyl)methyl]-2,5,8,11,14,17,22,28,31-nonaoxo-20,24-dithia-1,4,7,10,13,16,27,30-octazabicyclo[30.3.0]pentatriacontane-26-carbonyl]amino]propanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-6-(2-methylpropyl)-5,8,13-trioxo-1,11-dithia-4,7-diazacyclotetradecane-3-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0280	uM
(5R,8S,11S,14S,17S,20R)-20-[(2-aminoacetyl)amino]-11-(3-amino-3-oxopropyl)-14-[3-(diaminomethylideneamino)propyl]-17-(hydroxymethyl)-7,10,13,16,19-pentaoxo-8-propan-2-yl-3,22-dithia-6,9,12,15,18,28-hexazabicyclo[22.3.1]octacosa-1(27),24(28),25-triene-5-carboxylic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0290	uM
(5R,8S,11S,14S,17S,20R)-20-[(2-aminoacetyl)amino]-11-(3-amino-3-oxopropyl)-14-[3-(diaminomethylideneamino)propyl]-17-[(1R)-1-hydroxyethyl]-8-(1H-indol-3-ylmethyl)-7,10,13,16,19-pentaoxo-3,22-dithia-6,9,12,15,18,28-hexazabicyclo[22.3.1]octacosa-1(27),24(28),25-triene-5-carboxylic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0290	uM
2-[(2-chlorophenyl)methoxy]-4-[(5-phenyl-1H-imidazol-2-yl)methylamino]benzenecarboximidamide	1589829: Inhibition of recombinant 6His-Q-FLAG tagged human KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins by fluorescence intensity assay	ic50	0.0316	uM
2-[2-carbamimidoyl-5-[(5-phenyl-1H-imidazol-2-yl)methylamino]phenoxy]-N-(cyclopropylmethyl)acetamide	1589829: Inhibition of recombinant 6His-Q-FLAG tagged human KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins by fluorescence intensity assay	ic50	0.0398	uM
2-[(4-chlorophenyl)methoxy]-4-[(5-phenyl-1H-imidazol-2-yl)methylamino]benzenecarboximidamide	1589829: Inhibition of recombinant 6His-Q-FLAG tagged human KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins by fluorescence intensity assay	ic50	0.0631	uM
(3S,6S,9S,12S,15S,18R,26R,29S)-18-[(2-aminoacetyl)amino]-9-(3-amino-3-oxopropyl)-3-(carboxymethyl)-12-[3-(diaminomethylideneamino)propyl]-15-[(1R)-1-hydroxyethyl]-6-(1H-indol-3-ylmethyl)-2,5,8,11,14,17,22,28-octaoxo-20,24-dithia-1,4,7,10,13,16,27-heptazabicyclo[27.3.0]dotriacontane-26-carboxylic acid	1884311: Inhibition of C-terminal poly-His-tagged human recombinant KLK5 (30 to 293 residues) transfected in CHO cells assessed as inhibition constant using Boc-VPR-AMC as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay	ki	0.0790	uM
4-[(5-phenyl-1H-imidazol-2-yl)methylamino]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide	1589829: Inhibition of recombinant 6His-Q-FLAG tagged human KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins by fluorescence intensity assay	ic50	0.0794	uM
2-[2-carbamimidoyl-5-[(5-phenyl-1H-imidazol-2-yl)methylamino]phenoxy]-N-cyclopropylacetamide	1589829: Inhibition of recombinant 6His-Q-FLAG tagged human KLK5 expressed in baculovirus infected Sf9 insect cells using (Tos-Gly-Pro-Arg)2[R110].2TFA as substrate measured at 30 secs interval for 5 mins by fluorescence intensity assay	ic50	0.0794	uM

CTD chemical–gene interactions

21 total (human), top 21 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Tobacco Smoke Pollution	decreases expression, increases expression	2
3,19-(2-bromobenzylidene)andrographolide	decreases response to substance, increases expression	1
bisphenol A	affects cotreatment, increases methylation	1
pentanal	decreases expression	1
bisphenol S	decreases expression	1
Resveratrol	affects cotreatment, decreases expression	1
Fulvestrant	affects cotreatment, increases methylation	1
Benzo(a)pyrene	affects methylation, decreases methylation, increases methylation	1
Calcitriol	increases expression	1
Cisplatin	affects response to substance	1
Copper	affects cotreatment, decreases expression	1
Dichlorodiphenyl Dichloroethylene	decreases expression	1
Diazinon	increases methylation	1
Nicotine	increases expression	1
Smoke	decreases expression	1
Triclosan	increases expression	1
Valproic Acid	increases methylation	1
Zinc	decreases activity, decreases reaction	1
Copper Sulfate	increases expression	1
Citric Acid	increases activity	1
Lactic Acid	decreases expression	1

ChEMBL screening assays

57 unique, capped per target: 57 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1039261	Binding	Inhibition of kallikrein 5 after 10 to 15 mins by fluorescence assay	Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. — J Med Chem

Clinical trials (associated diseases)

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