KLK7
gene geneOn this page
Also known as SCCE
Summary
KLK7 (kallikrein related peptidase 7, HGNC:6368) is a protein-coding gene on chromosome 19q13.41, encoding Kallikrein-7 (P49862). May catalyze the degradation of intercellular cohesive structures in the cornified layer of the skin in the continuous shedding of cells from the skin surface.
This gene encodes a member of the kallikrein subfamily of serine proteases. These enzymes have diverse physiological functions and many kallikrein genes are biomarkers for cancer. The encoded protein has chymotrypsin-like activity and plays a role in the proteolysis of intercellular cohesive structures that precedes desquamation, the shedding of the outermost layer of the epidermis. The encoded protein may play a role in cancer invasion and metastasis, and increased expression of this gene is associated with unfavorable prognosis and progression of several types of cancer. Polymorphisms in this gene may play a role in the development of atopic dermatitis. Alternatively spliced transcript variants encoding multiple isoforms have been observed for this gene, which is one of fifteen kallikrein subfamily members located in a gene cluster on chromosome 19.
Source: NCBI Gene 5650 — RefSeq curated summary.
At a glance
- Clinical variants (ClinVar): 58 total
- Druggable target: yes
- MANE Select transcript:
NM_005046
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:6368 |
| Approved symbol | KLK7 |
| Name | kallikrein related peptidase 7 |
| Location | 19q13.41 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | SCCE |
| Ensembl gene | ENSG00000169035 |
| Ensembl biotype | protein_coding |
| OMIM | 604438 |
| Entrez | 5650 |
Gene structure
Transcript identifiers
Ensembl transcripts: 12 — 10 protein_coding, 1 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined
ENST00000304045, ENST00000391807, ENST00000593904, ENST00000595638, ENST00000595820, ENST00000597707, ENST00000900087, ENST00000900088, ENST00000900089, ENST00000900090, ENST00000900091, ENST00000900092
RefSeq mRNA: 4 — MANE Select: NM_005046
NM_001207053, NM_001243126, NM_005046, NM_139277
CCDS: CCDS12812, CCDS59414
Canonical transcript exons
ENST00000595820 — 6 exons
| Exon | Start | End |
|---|---|---|
| ENSE00003131682 | 50976468 | 50977691 |
| ENSE00003493301 | 50980240 | 50980487 |
| ENSE00003505310 | 50979788 | 50979924 |
| ENSE00003594479 | 50982327 | 50982457 |
| ENSE00003621659 | 50981767 | 50981914 |
| ENSE00003848246 | 50983851 | 50983917 |
Expression profiles
Bgee: expression breadth ubiquitous, 218 present calls, max score 99.08.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 2.8328 / max 477.3739, expressed in 181 samples.
FANTOM5 promoters (3 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 182314 | 2.4142 | 138 |
| 182316 | 0.3902 | 86 |
| 182315 | 0.0284 | 17 |
Top tissues by expression
276 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| gingival epithelium | UBERON:0001949 | 99.08 | gold quality |
| gingiva | UBERON:0001828 | 99.02 | gold quality |
| mammalian vulva | UBERON:0000997 | 98.96 | gold quality |
| penis | UBERON:0000989 | 98.86 | gold quality |
| upper arm skin | UBERON:0004263 | 98.83 | gold quality |
| upper leg skin | UBERON:0004262 | 98.44 | gold quality |
| skin of abdomen | UBERON:0001416 | 97.80 | gold quality |
| skin of leg | UBERON:0001511 | 97.47 | gold quality |
| zone of skin | UBERON:0000014 | 97.36 | gold quality |
| nipple | UBERON:0002030 | 96.93 | gold quality |
| skin of hip | UBERON:0001554 | 96.11 | gold quality |
| pharyngeal mucosa | UBERON:0000355 | 94.43 | gold quality |
| body of tongue | UBERON:0011876 | 94.31 | gold quality |
| esophagus squamous epithelium | UBERON:0006920 | 93.60 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 93.29 | gold quality |
| epithelium of esophagus | UBERON:0001976 | 93.23 | gold quality |
| squamous epithelium | UBERON:0006914 | 93.05 | gold quality |
| oral cavity | UBERON:0000167 | 92.74 | gold quality |
| esophagus mucosa | UBERON:0002469 | 92.07 | gold quality |
| tongue | UBERON:0001723 | 90.12 | gold quality |
| buccal mucosa cell | CL:0002336 | 87.70 | gold quality |
| renal glomerulus | UBERON:0000074 | 87.18 | gold quality |
| metanephric glomerulus | UBERON:0004736 | 87.18 | gold quality |
| amygdala | UBERON:0001876 | 87.16 | gold quality |
| oviduct epithelium | UBERON:0004804 | 86.90 | gold quality |
| temporal lobe | UBERON:0001871 | 85.96 | gold quality |
| superior surface of tongue | UBERON:0007371 | 85.71 | gold quality |
| tongue squamous epithelium | UBERON:0006919 | 85.56 | silver quality |
| middle temporal gyrus | UBERON:0002771 | 85.43 | silver quality |
| cervix epithelium | UBERON:0004801 | 85.17 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 0.00 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
70 targeting KLK7, 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-5692A | 100.00 | 74.40 | 6850 |
| HSA-MIR-200B-3P | 100.00 | 73.31 | 2693 |
| HSA-MIR-200C-3P | 100.00 | 73.35 | 2685 |
| HSA-MIR-429 | 100.00 | 73.44 | 2698 |
| HSA-MIR-3667-3P | 99.99 | 67.17 | 1636 |
| HSA-MIR-5696 | 99.98 | 72.36 | 4487 |
| HSA-MIR-6888-3P | 99.97 | 65.95 | 1170 |
| HSA-MIR-1250-3P | 99.96 | 70.04 | 4038 |
| HSA-MIR-335-3P | 99.93 | 73.36 | 4958 |
| HSA-MIR-106A-5P | 99.90 | 73.94 | 2683 |
| HSA-MIR-153-5P | 99.89 | 73.86 | 6317 |
| HSA-MIR-17-5P | 99.89 | 73.83 | 2665 |
| HSA-MIR-6780A-5P | 99.88 | 66.69 | 2776 |
| HSA-MIR-106B-5P | 99.88 | 74.72 | 2795 |
| HSA-MIR-20A-5P | 99.88 | 74.76 | 2769 |
| HSA-MIR-20B-5P | 99.88 | 74.01 | 2621 |
| HSA-MIR-519D-3P | 99.88 | 73.97 | 2607 |
| HSA-MIR-526B-3P | 99.88 | 74.06 | 2587 |
| HSA-MIR-93-5P | 99.88 | 73.98 | 2606 |
| HSA-MIR-579-3P | 99.86 | 71.66 | 3628 |
| HSA-MIR-383-3P | 99.85 | 65.84 | 1359 |
| HSA-MIR-4728-5P | 99.85 | 69.39 | 4718 |
| HSA-MIR-6079 | 99.84 | 68.54 | 1170 |
| HSA-MIR-5010-3P | 99.83 | 70.60 | 2357 |
| HSA-MIR-6785-5P | 99.82 | 68.68 | 4428 |
| HSA-MIR-548AG | 99.77 | 69.25 | 1492 |
| HSA-MIR-1273H-5P | 99.77 | 66.32 | 2471 |
| HSA-MIR-4679 | 99.76 | 69.19 | 1229 |
| HSA-MIR-548M | 99.70 | 68.87 | 1749 |
| HSA-MIR-377-5P | 99.70 | 65.28 | 712 |
Literature-anchored findings (GeneRIF, showing 40)
- High expression of KLK7 transcript with a long 3’-untranslated region is associated with ovarian cancer (PMID:12738725)
- human kallikrein 7 may have a role in breast carcnoma (PMID:14691584)
- Among all kallikreins measured, detectable levels in cerebrospinal fluid are identified for kallikrein K7. The most notable difference is seen between controls and frontotemperol dementia patients and controls and Alzheimer patients. (PMID:14972646)
- SCCE directly cleaved corneodesmosin and desmocollin 1 but was unable to degrade desmoglein 1. (PMID:15140227)
- The AACC insertion in the SCCE gene may result in a change to SCCE activity within the skin barrier so SCCE could have an important role in the development of atopic dermatitis. (PMID:15191543)
- Squamous cervical cancer expressed high levels of SCCE, suggesting that this protease may play an important role in invasion and metastasis. (PMID:15297163)
- 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)
- variability in KLK5 and KLK7 gene expression might be involved in lung tumorigenesis (PMID:15766562)
- 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)
- x-ray structures of recombinant active K7 at medium and atomic resolution (PMID:17909180)
- in 99 children and adults with atopic dermatitis found that an association with KLK7 4bp insertion polymorphism was not confirmed. (PMID:17989887)
- 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)
- Expression of KLK7, a novel biomarker for advanced ovarian carcinoma, was determined by a novel in situ quantitative method. (PMID:18325919)
- Data show that hK7 was crystallized, and its three-dimensional structure was solved in the absence of protease inhibitors. A model of the interaction between the protease and its inhibitor is proposed. (PMID:18329042)
- KLK7 is able to cleave fibronectin in a time-dependent manner, but not laminin. (PMID:18343220)
- KLK7 insertion appears to confer no risk of eczema; no interaction between the SPINK5 risk allele or the putative KLK7 risk allele and FLG mutations was found (PMID:18774391)
- Expression of kallikrein 7 diminishes pancreatic cancer cell adhesion to vitronectin and enhances urokinase-type plasminogen activator receptor shedding. (PMID:18953252)
- hK7 and ALP were decreased in malignant prostate epithelium. (PMID:18976018)
- kallikreins 5, 7, 8, and 10 are abundantly expressed in human OSCC and may be implicated in malignant progression (PMID:19085836)
- expression of K7 in BxPC-3 cells resulted in increase in shedding of soluble desmoglein 2 consistent with notion that aberrant expression of K7 in pancreatic tumors may result in diminished cell adhesion & facilitate tumor cell invasion (PMID:19091121)
- 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)
- Data suggest that KLK7 gene is up-regulated in colon cancer and its expression predicts poor prognosis for colon cancer patients. (PMID:19350120)
- 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)
- Overexpression of kallikrein 7 is associated with cervical neoplasia. (PMID:19921697)
- 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)
- in the high-KLK7-expression group there was more progressive liver metastasis and more advanced clinical staging compared with the low-KLK7-expression group (PMID:20544292)
- hK7 plays an important role in mediating prostate cancer progression (PMID:20944116)
- Our evidence suggests that the AACCins5874 insertion in the 3’untranslated region of the SCCE gene causes an over-expression in COS-7 and HeLa cells but does not have an effect on mRNA stability. (PMID:21168996)
- Both KLK7 (P=0.026) and KLK11 (P<0.001) expressions were decreased in prostate cancer cells compared to normal/benign prostate cells (PMID:21520985)
- Stromal cells can suppress the expression of the KLK7 gene in the epithelial cells in benign prostate hyperplasia. (PMID:21548205)
- KLK7 may play an important role in the activation of MMP-9 in tumors that express high levels of both these proteases (PMID:21616098)
- 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)
- The enhancement of protease activity through increased KLK7 expression by the TH2 cytokines IL-4 and IL-13 might be an important factor for mechanical and chemical epidermal barrier dysfunction in patients with atopic dermatitis. (PMID:22521249)
- High KLK7 expression is associated with pancreatic ductal adenocarcinoma. (PMID:22573795)
- regulation of procaspase-14 maturation during terminal differentiation is a unique two-step process involving KLK7 and an activation intermediate of caspase-14. (PMID:22825846)
- KLK7 and KLK14 gene expression can be regarded as markers of poor prognosis for colorectal cancer patients with discriminating power between CC and adenoma patients. (PMID:23224034)
- Early-stage oral squamous cell carcinoma and high KLK7 mRNA levels were correlated with the rs10581213(wt/ins + ins/ins) genotypes (PMID:23413953)
- Prochemerin processing protease converts prochemerin into active chemerinF; the activating truncation by the protease may trigger a structural C-terminal rearrangement leading to increased affinity of chemerin to chemokine-like receptor (CMKLR)1. (PMID:23495698)
Cross-species orthologs
13 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Klk7 | ENSMUSG00000030713 |
| rattus_norvegicus | Klk7 | ENSRNOG00000018664 |
| 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), KLK5 (ENSG00000167754), KLK11 (ENSG00000167757), KLK12 (ENSG00000186474), PRSS58 (ENSG00000258223)
Protein
Protein identifiers
Kallikrein-7 — P49862 (reviewed: P49862)
Alternative names: Serine protease 6, Stratum corneum chymotryptic enzyme
All UniProt accessions (4): A0A024R4H6, P49862, M0QYU8, Q6DTY1
UniProt curated annotations — full annotation on UniProt →
Function. May catalyze the degradation of intercellular cohesive structures in the cornified layer of the skin in the continuous shedding of cells from the skin surface. Specific for amino acid residues with aromatic side chains in the P1 position. Cleaves insulin A chain at ‘14-Tyr-|-Gln-15’ and insulin B chain at ‘6-Leu-|-Cys-7’, ‘16-Tyr-|-Leu-17’, ‘25-Phe-|-Tyr-26’ and ‘26-Tyr-|-Thr-27’. Could play a role in the activation of precursors to inflammatory cytokines.
Subcellular location. Secreted.
Tissue specificity. Abundantly expressed in the skin and is expressed by keratinocytes in the epidermis. Also expressed in the brain, mammary gland, cerebellum, spinal cord and kidney. Lower levels in salivary glands, uterus, thymus, thyroid, placenta, trachea and testis. Up-regulated in ovarian carcinoma, especially late-stage serous carcinoma, compared with normal ovaries and benign adenomas (at protein level).
Activity regulation. Inhibited by Zn2+ and Cu2+ at low micromolar concentrations. Inhibited by SERPINA12.
Induction. By estrogens and glucocorticoids in a breast carcinoma cell line.
Similarity. Belongs to the peptidase S1 family. Kallikrein subfamily.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P49862-1 | 1, Long | yes |
| P49862-2 | 2, Short |
RefSeq proteins (4): NP_001193982, NP_001230055, NP_005037, NP_644806 (=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 3.4.21.117 — stratum corneum chymotryptic enzyme (BRENDA: 4 organisms, 176 substrates, 117 inhibitors, 38 Km, 36 kcat entries)
Substrate kinetics (BRENDA)
34 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| METHOXY-SUCCINYL-ARG-PRO-TYR-4-NITROANILIDE | 0.65 | 2 |
| METHOXY-SUCCINYL-ARG-PRO-TYR-7-AMIDO-4-METHYLCOU | 0.304–0.43 | 2 |
| PHE-7-AMIDO-4-METHYLCOUMARIN | 0.0402–0.0443 | 2 |
| ABZ-AIKFFSA-Q-N-[2,4-DINITROPHENYL]-ETHYLENEDIAM | 0.0009 | 1 |
| ABZ-ALFSSK-Q-N-[2,4-DINITROPHENYL]-ETHYLENEDIAMI | 0.0043 | 1 |
| ABZ-FLFSSK-Q-N-[2,4-DINITROPHENYL]-ETHYLENEDIAMI | 0.0032 | 1 |
| ABZ-GFSPFRSSRI-Q-N-[2,4-DINITROPHENYL]-ETHYLENED | 0.002 | 1 |
| ABZ-GFSPFRSSRIGEIKEETT-Q-N-[2,4-DINITROPHENYL]-E | 0.069 | 1 |
| ABZ-GLFSSK-Q-N-[2,4-DINITROPHENYL]-ETHYLENEDIAMI | 0.0062 | 1 |
| ABZ-HLFSSK-Q-N-[2,4-DINITROPHENYL]-ETHYLENEDIAMI | 0.0034 | 1 |
| ABZ-ILFSSK-Q-N-[2,4-DINITROPHENYL]-ETHYLENEDIAMI | 0.0027 | 1 |
| ABZ-KAFSSK-Q-N-[2,4-DINITROPHENYL]-ETHYLENEDIAMI | 0.0035 | 1 |
| ABZ-KFFSSK-Q-N-[2,4-DINITROPHENYL]-ETHYLENEDIAMI | 0.003 | 1 |
| ABZ-KLFSSK-Q-N-[2,4-DINITROPHENYL]-ETHYLENEDIAMI | 0.0018 | 1 |
| ABZ-KLYSSK-Q-N-[2,4-DINITROPHENYL]-ETHYLENEDIAMI | 0.0034 | 1 |
UniProt features (41 total): strand 16, disulfide bond 6, helix 5, active site 3, mutagenesis site 2, signal peptide 1, propeptide 1, splice variant 1, sequence conflict 1, chain 1, turn 1, domain 1, site 1, glycosylation site 1
Structure
Experimental structures (PDB)
12 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 2QXI | X-RAY DIFFRACTION | 1 |
| 5FAH | X-RAY DIFFRACTION | 1.1 |
| 6SHI | X-RAY DIFFRACTION | 1.85 |
| 6SJU | X-RAY DIFFRACTION | 1.97 |
| 2QXH | X-RAY DIFFRACTION | 2 |
| 6SHH | X-RAY DIFFRACTION | 2 |
| 2QXJ | X-RAY DIFFRACTION | 2.1 |
| 5Y9L | X-RAY DIFFRACTION | 2.15 |
| 6Y4S | X-RAY DIFFRACTION | 2.23 |
| 5YJK | X-RAY DIFFRACTION | 2.4 |
| 2QXG | X-RAY DIFFRACTION | 2.6 |
| 3BSQ | X-RAY DIFFRACTION | 2.8 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P49862-F1 | 91.74 | 0.87 |
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): 70 (charge relay system); 112 (charge relay system); 205 (charge relay system); 109 (major binding site for inhibitory zinc or copper)
Disulfide bonds (6): 55–71, 137–239, 144–211, 176–190, 201–226, 36–165
Glycosylation sites (1): 246
Mutagenesis-validated functional residues (2):
| Position | Phenotype |
|---|---|
| 54 | no effect on zinc inhibition. |
| 109 | no zinc inhibition. |
Function
Pathways and Gene Ontology
Reactome pathways
5 pathways
| ID | Pathway |
|---|---|
| R-HSA-1474228 | Degradation of the extracellular matrix |
| R-HSA-9725554 | Differentiation of Keratinocytes in Interfollicular Epidermis in Mammalian Skin |
| R-HSA-1266738 | Developmental Biology |
| R-HSA-1474244 | Extracellular matrix organization |
| R-HSA-9734767 | Developmental Cell Lineages |
MSigDB gene sets: 107 (showing top):
WANG_CLIM2_TARGETS_UP, GOBP_ANTIMICROBIAL_HUMORAL_RESPONSE, GOMF_METALLOPEPTIDASE_ACTIVITY, JAEGER_METASTASIS_DN, GOCC_SECRETORY_GRANULE, GGGTGGRR_PAX4_03, ONDER_CDH1_TARGETS_3_DN, CHANG_IMMORTALIZED_BY_HPV31_DN, GOBP_PEPTIDE_METABOLIC_PROCESS, GOBP_PROTEIN_MATURATION, GOBP_DEFENSE_RESPONSE_TO_OTHER_ORGANISM, RICKMAN_TUMOR_DIFFERENTIATED_WELL_VS_POORLY_DN, GOBP_HUMORAL_IMMUNE_RESPONSE, GOBP_EPIDERMIS_DEVELOPMENT, TURASHVILI_BREAST_DUCTAL_CARCINOMA_VS_DUCTAL_NORMAL_DN
GO Biological Process (6): antibacterial peptide biosynthetic process (GO:0002780), proteolysis (GO:0006508), epidermis development (GO:0008544), extracellular matrix disassembly (GO:0022617), protein maturation (GO:0051604), positive regulation of antibacterial peptide production (GO:0002803)
GO Molecular Function (5): metalloendopeptidase activity (GO:0004222), serine-type endopeptidase activity (GO:0004252), peptidase activity (GO:0008233), serine-type peptidase activity (GO:0008236), hydrolase activity (GO:0016787)
GO Cellular Component (5): cornified envelope (GO:0001533), extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), secretory granule (GO:0030141), epidermal lamellar body (GO:0097209)
Reactome top-level categories
Rollup of top-3 pathways:
| Category | Pathways |
|---|---|
| Extracellular matrix organization | 1 |
| Developmental Cell Lineages of the Integumentary System | 1 |
| Developmental Biology | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| antibacterial peptide production | 2 |
| protein metabolic process | 2 |
| endopeptidase activity | 2 |
| antimicrobial peptide biosynthetic process | 1 |
| tissue development | 1 |
| cellular component disassembly | 1 |
| extracellular matrix organization | 1 |
| gene expression | 1 |
| positive regulation of antimicrobial peptide production | 1 |
| regulation of antibacterial peptide production | 1 |
| positive regulation of defense response to bacterium | 1 |
| metallopeptidase activity | 1 |
| serine-type peptidase activity | 1 |
| hydrolase activity | 1 |
| catalytic activity, acting on a protein | 1 |
| peptidase activity | 1 |
| serine hydrolase activity | 1 |
| catalytic activity | 1 |
| plasma membrane | 1 |
| cellular anatomical structure | 1 |
| endomembrane system | 1 |
| secretory vesicle | 1 |
| lamellar body | 1 |
Protein interactions and networks
STRING
1130 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| KLK7 | SPINK5 | Q9NQ38 | 893 |
| KLK7 | DSG1 | Q02413 | 819 |
| KLK7 | CDSN | Q15517 | 804 |
| KLK7 | A2ML1 | A8K2U0 | 802 |
| KLK7 | FLG2 | Q5D862 | 776 |
| KLK7 | FLG | P20930 | 766 |
| KLK7 | SPRR1B | P22528 | 753 |
| KLK7 | GLIS1 | Q8NBF1 | 681 |
| KLK7 | TGM1 | P22735 | 668 |
| KLK7 | IVL | P07476 | 660 |
| KLK7 | DSC1 | Q08554 | 647 |
| KLK7 | SERPINA12 | Q8IW75 | 586 |
| KLK7 | SPINK9 | Q5DT21 | 523 |
| KLK7 | CASP14 | P31944 | 458 |
| KLK7 | LORICRIN | P23490 | 447 |
IntAct
71 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CCNC | MED19 | psi-mi:“MI:0914”(association) | 0.640 |
| ALDH3A1 | RCCD1 | psi-mi:“MI:0914”(association) | 0.640 |
| FTH1 | A2ML1 | psi-mi:“MI:0914”(association) | 0.530 |
| TBC1D22B | A2ML1 | psi-mi:“MI:0914”(association) | 0.530 |
| GMCL1 | A2ML1 | psi-mi:“MI:0914”(association) | 0.530 |
| CA8 | IGLL5 | psi-mi:“MI:0914”(association) | 0.530 |
| KIR3DS1 | PPL | psi-mi:“MI:0914”(association) | 0.530 |
| DTL | DNAJA2 | psi-mi:“MI:0914”(association) | 0.530 |
| KLK7 | BAG4 | psi-mi:“MI:0915”(physical association) | 0.370 |
| KLK7 | CCND1 | psi-mi:“MI:0915”(physical association) | 0.370 |
| KLK7 | CHEK2 | psi-mi:“MI:0915”(physical association) | 0.370 |
| PTPN1 | KLK7 | psi-mi:“MI:0915”(physical association) | 0.370 |
| PTPRJ | KLK7 | psi-mi:“MI:0915”(physical association) | 0.370 |
| STK11 | KLK7 | psi-mi:“MI:0915”(physical association) | 0.370 |
| KLK7 | TGFB1 | psi-mi:“MI:0915”(physical association) | 0.370 |
| KLK7 | WT1 | psi-mi:“MI:0915”(physical association) | 0.370 |
| ATG16L1 | psi-mi:“MI:0914”(association) | 0.350 | |
| KLHL11 | PIPSL | psi-mi:“MI:0914”(association) | 0.350 |
| STX17 | A2ML1 | psi-mi:“MI:0914”(association) | 0.350 |
| PI4KAP1 | A2ML1 | psi-mi:“MI:0914”(association) | 0.350 |
| ST6GALNAC6 | A2ML1 | psi-mi:“MI:0914”(association) | 0.350 |
| LRRC10 | A2ML1 | psi-mi:“MI:0914”(association) | 0.350 |
| CDK15 | A2ML1 | psi-mi:“MI:0914”(association) | 0.350 |
| GABPA | A2ML1 | psi-mi:“MI:0914”(association) | 0.350 |
| ZNF154 | A2ML1 | psi-mi:“MI:0914”(association) | 0.350 |
| PTDSS1 | IGLL5 | psi-mi:“MI:0914”(association) | 0.350 |
| FCF1 | SULT2B1 | psi-mi:“MI:0914”(association) | 0.350 |
| VNN2 | ATP2A1 | psi-mi:“MI:0914”(association) | 0.350 |
| PRSS16 | KLK10 | psi-mi:“MI:0914”(association) | 0.350 |
| SFR1 | CTSV | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (88): KLK7 (Affinity Capture-MS), KLK7 (Affinity Capture-MS), KLK7 (Affinity Capture-MS), KLK7 (Affinity Capture-MS), KLK7 (Affinity Capture-MS), KLK7 (Affinity Capture-MS), KLK7 (Two-hybrid), KLK7 (Two-hybrid), KLK7 (Two-hybrid), KLK7 (Two-hybrid), KLK7 (Two-hybrid), KLK7 (Two-hybrid), KLK7 (Two-hybrid), KLK7 (Two-hybrid), KLK7 (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: 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
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
58 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 46 |
| Likely benign | 0 |
| Benign | 4 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
0 predictions. Top by Δscore:
AlphaMissense
1640 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 19:50980262:C:A | W149C | 1.000 |
| 19:50980262:C:G | W149C | 1.000 |
| 19:50977566:C:A | W244C | 0.999 |
| 19:50977566:C:G | W244C | 0.999 |
| 19:50979825:C:G | C190S | 0.999 |
| 19:50979826:A:T | C190S | 0.999 |
| 19:50980374:T:A | D112V | 0.999 |
| 19:50980374:T:G | D112A | 0.999 |
| 19:50977635:C:A | W221C | 0.998 |
| 19:50977635:C:G | W221C | 0.998 |
| 19:50977687:T:A | D204V | 0.998 |
| 19:50977687:T:G | D204A | 0.998 |
| 19:50979792:C:G | C201S | 0.998 |
| 19:50979792:C:T | C201Y | 0.998 |
| 19:50979793:A:T | C201S | 0.998 |
| 19:50980261:C:A | G150C | 0.998 |
| 19:50980264:A:G | W149R | 0.998 |
| 19:50980264:A:T | W149R | 0.998 |
| 19:50980277:A:C | C144W | 0.998 |
| 19:50980374:T:C | D112G | 0.998 |
| 19:50981776:C:G | C71S | 0.998 |
| 19:50981776:C:T | C71Y | 0.998 |
| 19:50981777:A:T | C71S | 0.998 |
| 19:50981824:C:T | C55Y | 0.998 |
| 19:50977621:C:G | C226S | 0.997 |
| 19:50977622:A:T | C226S | 0.997 |
| 19:50977681:C:A | G206V | 0.997 |
| 19:50977681:C:T | G206E | 0.997 |
| 19:50977682:C:A | G206W | 0.997 |
| 19:50977688:C:G | D204H | 0.997 |
dbSNP variants (sampled 300 via entrez): RS1000183595 (19:50982751 C>A,T), RS1000193891 (19:50976126 G>A), RS1000482602 (19:50976405 G>A), RS1000622042 (19:50977801 A>C,G), RS1001623718 (19:50979087 T>C), RS1001676246 (19:50984162 G>A), RS1001705954 (19:50976477 C>T), RS1001988373 (19:50976858 A>G), RS1002530178 (19:50979864 G>A,C,T), RS1002626633 (19:50980184 T>A,C), RS1004187068 (19:50985569 C>T), RS1004549578 (19:50983730 C>T), RS1004614391 (19:50977044 GA>G,GAA), RS1004645507 (19:50985293 T>C,G), RS1004776599 (19:50977262 A>G)
Disease associations
OMIM: gene MIM:604438 | 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): CHEMBL2443 (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 | 7.4 | pIC50 |
| compound 4d [PMID: 25489658] | Inhibition | 7.19 | pIC50 |
Binding affinities (BindingDB)
227 measured of 350 human assays (364 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| [1-[(5-methyl-1,2-oxazol-3-yl)amino]-1-oxopropan-2-yl] 2-(4-chlorophenyl)acetate | IC50 | 39 nM | US-9744148: Kallikrein 7 inhibitors |
| CHEMBL5175954 | KI | 66 nM | |
| [1-(4-fluoroanilino)-1-oxopropan-2-yl] 2-(4-chlorophenyl)acetate | IC50 | 70 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-[(5-methyl-1,2-oxazol-3-yl)amino]-1-oxobutan-2-yl] 2-(4-chlorophenyl)acetate | IC50 | 80 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-(4-methoxyanilino)-1-oxopropan-2-yl] 2-(4-chlorophenyl)acetate | IC50 | 80 nM | US-9744148: Kallikrein 7 inhibitors |
| (1-anilino-1-oxopropan-2-yl) 2-(4-chlorophenyl)acetate | IC50 | 90 nM | US-9744148: Kallikrein 7 inhibitors |
| CHEMBL5172075 | KI | 96 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 |
| [1-(4-methoxyanilino)-1-oxobutan-2-yl] 2-(4-chlorophenyl)acetate | IC50 | 120 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-[(5-methyl-1,2-oxazol-3-yl)amino]-1-oxopropan-2-yl] 2-(4-methoxyphenyl)acetate | IC50 | 130 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-(4-fluoroanilino)-1-oxobutan-2-yl] 2-(4-chlorophenyl)acetate | IC50 | 140 nM | US-9744148: Kallikrein 7 inhibitors |
| (1-anilino-1-oxobutan-2-yl) 2-(4-chlorophenyl)acetate | IC50 | 150 nM | US-9744148: Kallikrein 7 inhibitors |
| (1-anilino-1-oxopropan-2-yl) 3-cyclopentylpropanoate | IC50 | 150 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-(4-methoxyanilino)-1-oxobutan-2-yl] 3-cyclopentylpropanoate | IC50 | 150 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-[(5-methyl-1,2-oxazol-3-yl)amino]-1-oxobutan-2-yl] 2-(4-methoxyphenyl)acetate | IC50 | 150 nM | US-9744148: Kallikrein 7 inhibitors |
| [2-(4-methoxyanilino)-2-oxo-1-phenylethyl] 2-(4-chlorophenyl)acetate | IC50 | 170 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-[(5-methyl-1,2-oxazol-3-yl)amino]-1-oxopropan-2-yl] 3-cyclopentylpropanoate | IC50 | 180 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-(4-methoxyanilino)-1-oxopropan-2-yl] 2-(4-methoxyphenyl)acetate | IC50 | 180 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-[(5-methyl-1,2-oxazol-3-yl)amino]-1-oxobutan-2-yl] 3-cyclopentylpropanoate | IC50 | 190 nM | US-9744148: Kallikrein 7 inhibitors |
| [2-[(5-methyl-1,2-oxazol-3-yl)amino]-2-oxo-1-phenylethyl] 2-(4-chlorophenyl)acetate | IC50 | 190 nM | US-9744148: Kallikrein 7 inhibitors |
| 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 |
| [1-[(5-methyl-1,2-oxazol-3-yl)amino]-1-oxopentan-2-yl] 2,2-diphenylacetate | IC50 | 220 nM | US-9744148: Kallikrein 7 inhibitors |
| [2-(4-methoxyanilino)-2-oxo-1-phenylethyl] 3-cyclopentylpropanoate | IC50 | 230 nM | US-9744148: Kallikrein 7 inhibitors |
| [2-[(5-methyl-1,2-oxazol-3-yl)amino]-2-oxo-1-phenylethyl] 3-cyclopentylpropanoate | IC50 | 230 nM | US-9744148: Kallikrein 7 inhibitors |
| 7-(4-methoxyphenyl)-5-phenyl-pyrido[2,3-d]pyrimidin-4-amine | IC50 | 237 nM | |
| (1-anilino-1-oxopropan-2-yl) 2-(4-methoxyphenyl)acetate | IC50 | 260 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-(4-fluoroanilino)-1-oxopropan-2-yl] 3-cyclopentylpropanoate | IC50 | 260 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-(4-methoxyanilino)-1-oxobutan-2-yl] 2-(4-methoxyphenyl)acetate | IC50 | 280 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-(4-fluoroanilino)-1-oxobutan-2-yl] 3-cyclopentylpropanoate | IC50 | 310 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-[(5-methyl-1,2-oxazol-3-yl)amino]-1-oxobutan-2-yl] 2-(1,3-benzodioxol-5-yl)acetate | IC50 | 320 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-[(5-methyl-1,2-oxazol-3-yl)amino]-1-oxohexan-2-yl] 2,2-diphenylacetate | IC50 | 330 nM | US-9744148: Kallikrein 7 inhibitors |
| [(2S)-1-[(5-methyl-1,2-oxazol-3-yl)amino]-1-oxobutan-2-yl] 2,2-diphenylacetate | IC50 | 340 nM | US-9744148: Kallikrein 7 inhibitors |
| [2-(4-fluoroanilino)-2-oxo-1-phenylethyl] 2-(4-chlorophenyl)acetate | IC50 | 350 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-(4-fluoroanilino)-1-oxobutan-2-yl] 2-(4-methoxyphenyl)acetate | IC50 | 360 nM | US-9744148: Kallikrein 7 inhibitors |
| (2-anilino-2-oxo-1-phenylethyl) 2-(4-chlorophenyl)acetate | IC50 | 380 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-[(5-methyl-1,2-oxazol-3-yl)amino]-1-oxobutan-2-yl] 2,2-diphenylacetate | IC50 | 390 nM | US-9744148: Kallikrein 7 inhibitors |
| (1-anilino-1-oxobutan-2-yl) 2-(4-methoxyphenyl)acetate | IC50 | 390 nM | US-9744148: Kallikrein 7 inhibitors |
| 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-(4-methoxyanilino)-2-oxo-1-phenylethyl] 2-(4-methoxyphenyl)acetate | IC50 | 410 nM | US-9744148: Kallikrein 7 inhibitors |
| [2-[(5-methyl-1,2-oxazol-3-yl)amino]-2-oxo-1-phenylethyl] 2-(4-methoxyphenyl)acetate | IC50 | 430 nM | US-9744148: Kallikrein 7 inhibitors |
| [2-(benzylamino)-2-oxo-1-phenylethyl] 3-cyclopentylpropanoate | IC50 | 460 nM | US-9744148: Kallikrein 7 inhibitors |
| [4-methoxy-1-[(5-methyl-1,2-oxazol-3-yl)amino]-1-oxobutan-2-yl] 2,2-diphenylacetate | IC50 | 470 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-[(5-methyl-1,2-oxazol-3-yl)amino]-1-oxobutan-2-yl] 2-(3,4-dichlorophenyl)acetate | IC50 | 480 nM | US-9744148: Kallikrein 7 inhibitors |
| 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-(4-methoxyanilino)-2-oxoethyl] 2-(4-chlorophenyl)acetate | IC50 | 550 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-[(5-methyl-1,2-oxazol-3-yl)amino]-1-oxobutan-2-yl] 2-(3,4-dimethoxyphenyl)acetate | IC50 | 580 nM | US-9744148: Kallikrein 7 inhibitors |
| [1-(4-fluoroanilino)-1-oxopropan-2-yl] 2-(4-methoxyphenyl)acetate | IC50 | 590 nM | US-9744148: Kallikrein 7 inhibitors |
| 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 |
| [1-(4-methoxyanilino)-1-oxobutan-2-yl] 2,2-diphenylacetate | IC50 | 630 nM | US-9744148: Kallikrein 7 inhibitors |
ChEMBL bioactivities
264 potent at pChembl≥5 of 424 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
114 with measured affinity, of 417 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 |
|---|---|---|---|---|
| (2S)-N-[(2S,5S,8R,11R,12S,15S,18S,21R)-2,8-bis[(2R)-butan-2-yl]-21-hydroxy-4,11-dimethyl-15-(2-methylpropyl)-5-[[4-[(1-methylpyrazol-3-yl)methoxy]phenyl]methyl]-3,6,9,13,16,22-hexaoxo-10-oxa-1,4,7,14,17-pentazabicyclo[16.3.1]docosan-12-yl]-2-(2-methylpropanoylamino)pentanediamide | 1942958: Inhibition of KLK7 (unknown origin) | ic50 | 0.0002 | 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 | 1251579: Inhibition of KLK7 (unknown origin) expressed in Pichia pastoris X33 using KHLY-pNA substrate by spectrophotometry method | ki | 0.0008 | uM |
| (2S)-N-[(2S,5S,8R,11R,12S,15S,18S,21R)-2,8-bis[(2R)-butan-2-yl]-21-hydroxy-5-[(4-hydroxyphenyl)methyl]-4,11-dimethyl-15-(2-methylpropyl)-3,6,9,13,16,22-hexaoxo-10-oxa-1,4,7,14,17-pentazabicyclo[16.3.1]docosan-12-yl]-2-(2-methylpropanoylamino)pentanediamide | 1942958: Inhibition of KLK7 (unknown origin) | ic50 | 0.0010 | uM |
| (2S)-N-[(2S,5S,8S,11R,12S,15Z,18S,21R)-2-benzyl-15-ethylidene-21-hydroxy-5-[(4-hydroxyphenyl)methyl]-4,11-dimethyl-3,6,9,13,16,22-hexaoxo-8-propan-2-yl-10-oxa-1,4,7,14,17-pentazabicyclo[16.3.1]docosan-12-yl]-2-(hexanoylamino)pentanediamide | 1942945: Inhibition of human recombinant kallikrein 7 (23 to 252 residues) using MCA-RPKPVE-Nval-WRK(Dnp)-NH2 as substrate by fluorescence based analysis | ic50 | 0.0031 | uM |
| (2S,3S)-N-[(2S,5S,8S,11R,12S,15Z,18S,21R)-2-benzyl-15-ethylidene-21-hydroxy-5-[(4-hydroxyphenyl)methyl]-4,11-dimethyl-3,6,9,13,16,22-hexaoxo-8-propan-2-yl-10-oxa-1,4,7,14,17-pentazabicyclo[16.3.1]docosan-12-yl]-2-[[(2S)-2-[[(E)-4-chloro-3-methylbut-3-enoyl]amino]propanoyl]amino]-3-methylpentanamide | 1942945: Inhibition of human recombinant kallikrein 7 (23 to 252 residues) using MCA-RPKPVE-Nval-WRK(Dnp)-NH2 as substrate by fluorescence based analysis | ic50 | 0.0050 | uM |
| 5-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[2-[2-[2-[[(5S)-6-[(2-amino-2-oxoethyl)amino]-5-[[2-[[(3R,6S,9S,12S,15S,18S,21R)-12-butyl-6-(3-carbamimidamidopropyl)-15-[(4-hydroxyphenyl)methyl]-9-methyl-18-(2-methylpropyl)-5,8,11,14,17,20,25-heptaoxo-21-[[(2S)-pyrrolidine-2-carbonyl]amino]-1,23-dithia-4,7,10,13,16,19-hexazacyclohexacosane-3-carbonyl]amino]acetyl]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 | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0070 | uM |
| (2S)-2-[[(5R,8S,11S,14S,17S,20R)-20-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-8-(hydroxymethyl)-14-[(4-hydroxyphenyl)methyl]-11,17-bis(2-methylpropyl)-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-carbonyl]amino]-3-hydroxypropanoic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0088 | uM |
| (2S)-5-amino-2-[[(3R,11R,14S,17S,20S,23S)-17,20-bis(3-amino-3-oxopropyl)-3-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(3R,6S,9S,12S,15S,18S,21R)-6-(3-carbamimidamidopropyl)-21-[[(2S)-2,5-diamino-5-oxopentanoyl]amino]-15-[(4-hydroxyphenyl)methyl]-9-methyl-18-(2-methylpropyl)-12-(2-methylsulfanylethyl)-5,8,11,14,17,20,25-heptaoxo-1,23-dithia-4,7,10,13,16,19-hexazacyclohexacosane-3-carbonyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-14-[(4-hydroxyphenyl)methyl]-2,7,13,16,19,22-hexaoxo-5,9-dithia-1,12,15,18,21-pentazabicyclo[21.3.0]hexacosane-11-carbonyl]amino]-5-oxopentanoic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0090 | uM |
| (2S)-2-[[(3R,6S,9S,12S,15S,18S,21R)-6-[3-(diaminomethylideneamino)propyl]-15-[(4-hydroxyphenyl)methyl]-9-methyl-18-(2-methylpropyl)-12-(2-methylsulfanylethyl)-5,8,11,14,17,20,25-heptaoxo-21-[[(2S)-pyrrolidine-2-carbonyl]amino]-1,23-dithia-4,7,10,13,16,19-hexazacyclohexacosane-3-carbonyl]amino]-3-hydroxypropanoic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0101 | uM |
| (2S)-2-[[(5R,8S,11S,14S,17S,20R)-20-[[(2S)-2,5-diamino-5-oxopentanoyl]amino]-8-(hydroxymethyl)-14-[(4-hydroxyphenyl)methyl]-11,17-bis(2-methylpropyl)-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-carbonyl]amino]-3-hydroxypropanoic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0120 | uM |
| (2S)-2-[[(3R,6S,9S,12S,15S,18S,21S)-6-[3-(diaminomethylideneamino)propyl]-15-[(4-hydroxyphenyl)methyl]-9-methyl-12,18-bis(2-methylpropyl)-5,8,11,14,17,20,25-heptaoxo-21-[[(2S)-pyrrolidine-2-carbonyl]amino]-1,23-dithia-4,7,10,13,16,19-hexazacyclohexacosane-3-carbonyl]amino]-3-hydroxypropanoic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0160 | 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 | 1251579: Inhibition of KLK7 (unknown origin) expressed in Pichia pastoris X33 using KHLY-pNA substrate by spectrophotometry method | ki | 0.0168 | uM |
| (2S)-3-hydroxy-2-[[(5R,8S,11S,14S,17S,20R)-14-[(4-hydroxyphenyl)methyl]-8-methyl-11,17-bis(2-methylpropyl)-7,10,13,16,19-pentaoxo-20-[[(2S)-pyrrolidine-2-carbonyl]amino]-3,22-dithia-6,9,12,15,18,28-hexazabicyclo[22.3.1]octacosa-1(27),24(28),25-triene-5-carbonyl]amino]propanoic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0175 | uM |
| (5R,8S,11S,14S,17S,20R)-14-[(4-hydroxyphenyl)methyl]-8-methyl-11,17-bis(2-methylpropyl)-7,10,13,16,19-pentaoxo-20-[[(2S)-pyrrolidine-2-carbonyl]amino]-3,22-dithia-6,9,12,15,18,28-hexazabicyclo[22.3.1]octacosa-1(27),24(28),25-triene-5-carboxylic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0190 | uM |
| (3R,6S,9S,12S,15S,18S,21R)-6-[3-(diaminomethylideneamino)propyl]-15-[(4-hydroxyphenyl)methyl]-9-methyl-12,18-bis(2-methylpropyl)-5,8,11,14,17,20,25-heptaoxo-21-[[(2S)-pyrrolidine-2-carbonyl]amino]-1,23-dithia-4,7,10,13,16,19-hexazacyclohexacosane-3-carboxylic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0290 | uM |
| (2S)-3-hydroxy-2-[[(5R,8S,11S,14S,17S,20R)-8-(hydroxymethyl)-14-[(4-hydroxyphenyl)methyl]-11,17-bis(2-methylpropyl)-7,10,13,16,19-pentaoxo-20-[[(2S)-pyrrolidine-2-carbonyl]amino]-3,22-dithia-6,9,12,15,18,28-hexazabicyclo[22.3.1]octacosa-1(27),24(28),25-triene-5-carbonyl]amino]propanoic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0294 | uM |
| 5-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[2-[2-[2-[[(5S)-6-[(2-amino-2-oxoethyl)amino]-5-[[2-[[(3R,6S,9S,12S,15S,18S,21R)-6-(3-carbamimidamidopropyl)-15-[(4-hydroxyphenyl)methyl]-9-methyl-12,18-bis(2-methylpropyl)-5,8,11,14,17,20,25-heptaoxo-21-[[(2S)-pyrrolidine-2-carbonyl]amino]-1,23-dithia-4,7,10,13,16,19-hexazacyclohexacosane-3-carbonyl]amino]acetyl]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 | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0310 | uM |
| 2-[(5R,11S,14S,17R)-17-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(5R,8S,11S,14S,17S,20R)-11-[(2S)-butan-2-yl]-20-[[(2S)-2,5-diamino-5-oxopentanoyl]amino]-14-[(4-hydroxyphenyl)methyl]-8-methyl-17-(2-methylpropyl)-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-carbonyl]pyrrolidine-2-carbonyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]propanoyl]amino]hexanoyl]amino]-11-(2-amino-2-oxoethyl)-5-[[(2S)-1,5-diamino-1,5-dioxopentan-2-yl]carbamoyl]-7,10,13,16-tetraoxo-3,19-dithia-6,9,12,15,25-pentazabicyclo[19.3.1]pentacosa-1(24),21(25),22-trien-14-yl]acetic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0320 | uM |
| (2S)-2-[[(3R,6S,9S,12S,15S,18S,21R)-6-(3-amino-3-oxopropyl)-15-[(4-hydroxyphenyl)methyl]-9-methyl-12,18-bis(2-methylpropyl)-5,8,11,14,17,20,25-heptaoxo-21-[[(2S)-pyrrolidine-2-carbonyl]amino]-1,23-dithia-4,7,10,13,16,19-hexazacyclohexacosane-3-carbonyl]amino]-3-hydroxypropanoic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0360 | uM |
| (5-amino-3-pyridin-3-yl-1,2,4-triazol-1-yl)-(4-methylphenyl)methanone | 762641: Inhibition of human kallikrein 7 measured after 15 mins at pH 8 by fluorescence assay | ic50 | 0.0400 | uM |
| (2S)-2-[(6R)-6-[(5-chloro-2-methoxyphenyl)methyl]-3-(2,2-dimethylhydrazinyl)-7-oxo-5,6-dihydro-2H-1,4-diazepin-1-yl]-N-[3-(1-methylpyrazol-4-yl)phenyl]pentanamide | 1391053: Inhibition of recombinant human KLK7 using MOCAc-Arg-Pro-Lys-Pro-Val-Glu-Nva-Trp-Arg-Lys(Dnp)-NH2 as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence assay | ic50 | 0.0480 | uM |
| 6-ethoxy-7-methoxy-2-(2-methoxyphenyl)-3,1-benzoxazin-4-one | 1624363: Inhibition of recombinant human KLK7 using S-2586 substrate | ic50 | 0.0480 | uM |
| (2S)-N-[(5R,8S,11S,14S,17S,20R)-5-[(2S)-2-acetylpyrrolidine-1-carbonyl]-8-(hydroxymethyl)-14-[(4-hydroxyphenyl)methyl]-11,17-bis(2-methylpropyl)-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-trien-20-yl]pyrrolidine-2-carboxamide | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0500 | uM |
| (2S)-3-hydroxy-2-[[(5R,8S,11S,14S,17S,20R)-8-[(1R)-1-hydroxyethyl]-14-[(4-hydroxyphenyl)methyl]-11,17-bis(2-methylpropyl)-7,10,13,16,19-pentaoxo-20-[[(2S)-pyrrolidine-2-carbonyl]amino]-3,22-dithia-6,9,12,15,18,28-hexazabicyclo[22.3.1]octacosa-1(27),24(28),25-triene-5-carbonyl]amino]propanoic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0520 | uM |
| (2S)-2-[[(5R,8S,11S,14S,17S,20R)-11-[3-(diaminomethylideneamino)propyl]-8-(hydroxymethyl)-14-[(4-hydroxyphenyl)methyl]-17-(2-methylpropyl)-7,10,13,16,19-pentaoxo-20-[[(2S)-pyrrolidine-2-carbonyl]amino]-3,22-dithia-6,9,12,15,18,28-hexazabicyclo[22.3.1]octacosa-1(27),24(28),25-triene-5-carbonyl]amino]-3-hydroxypropanoic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0530 | uM |
| (2S)-2-[(6R)-6-[(5-chloro-2-methoxyphenyl)methyl]-3-(2,2-dimethylhydrazinyl)-7-oxo-5,6-dihydro-2H-1,4-diazepin-1-yl]-N-[3-(1-methylpyrazol-4-yl)phenyl]propanamide | 1391053: Inhibition of recombinant human KLK7 using MOCAc-Arg-Pro-Lys-Pro-Val-Glu-Nva-Trp-Arg-Lys(Dnp)-NH2 as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence assay | ic50 | 0.0580 | uM |
| 2-[(5R,8S,11S,14S,20S,23S,26R)-5-[(2S)-2-[[(2S)-5-amino-1-[[(5R,8S,11S,14S,17S,20R)-5-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]carbamoyl]-8-[(2S)-butan-2-yl]-11-(3-carbamimidamidopropyl)-14-[(4-hydroxyphenyl)methyl]-17-(2-methylpropyl)-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-trien-20-yl]amino]-1,5-dioxopentan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]-20-(4-aminobutyl)-26-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-8,23-bis(3-carbamimidamidopropyl)-14-(2-methylpropyl)-7,10,13,16,19,22,25-heptaoxo-3,28-dithia-6,9,12,15,18,21,24,34-octazabicyclo[28.3.1]tetratriaconta-1(33),30(34),31-trien-11-yl]acetic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0660 | 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 | 1483611: Inhibition of recombinant KLK7 (unknown origin) expressed in zymogen form in Pichia pastorisstrain X-33 using KHLY-pNA as substrate after 30 mins | ki | 0.0690 | uM |
| (2S)-2-[[(3S,6S,9S,12S,15S,18S,21S)-6-[3-(diaminomethylideneamino)propyl]-9-(hydroxymethyl)-15-[(4-hydroxyphenyl)methyl]-12,18-bis(2-methylpropyl)-5,8,11,14,17,20,25-heptaoxo-21-[[(2S)-pyrrolidine-2-carbonyl]amino]-1,23-dithia-4,7,10,13,16,19-hexazacyclohexacosane-3-carbonyl]amino]-3-hydroxypropanoic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0900 | uM |
| (2S)-1-[(5R,8S,11S,14S,17S,20R)-20-[[(2S)-5-amino-2-[[2-[[(2S)-5-amino-2-[[(2S)-2-[[(5R,8S,11S,14S,17S,20R)-20-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-8-(3-amino-3-oxopropyl)-17-(carboxymethyl)-11,14-bis(hydroxymethyl)-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-carbonyl]amino]-4-methylsulfanylbutanoyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]-11-(3-carbamimidamidopropyl)-8-(hydroxymethyl)-14-[(4-hydroxyphenyl)methyl]-17-(2-methylpropyl)-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-carbonyl]pyrrolidine-2-carboxylic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0940 | uM |
| (3S)-3-[[(2S)-2-[[(2S,3S)-2-[[(3R,6S,9S,12S,16S,19S,22S,25R)-9-(3-amino-3-oxopropyl)-6-benzyl-19,22-bis[(2S)-butan-2-yl]-25-[[(2S)-2,5-diamino-5-oxopentanoyl]amino]-16-[(1R)-1-hydroxyethyl]-12-[(4-hydroxyphenyl)methyl]-5,8,11,14,18,21,24,29-octaoxo-1,27-dithia-4,7,10,13,15,17,20,23-octazacyclotriacontane-3-carbonyl]amino]-3-hydroxybutanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[[2-[[(3R,6R)-3-[[(1S)-1-carboxy-2-hydroxyethyl]carbamoyl]-5,10-dioxo-1,8-dithia-4-azacycloundec-6-yl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-4-oxobutanoic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.0960 | uM |
| 5-[2-[2-[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[2-[2-[2-[(2S)-2-[[(3R,6S,9S,12S,15S,18S,21R)-3-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]carbamoyl]-6-(3-carbamimidamidopropyl)-15-[(4-hydroxyphenyl)methyl]-9-methyl-12,18-bis(2-methylpropyl)-5,8,11,14,17,20,25-heptaoxo-1,23-dithia-4,7,10,13,16,19-hexazacyclohexacos-21-yl]carbamoyl]pyrrolidin-1-yl]-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 | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.1060 | uM |
| (2S)-2-[(6R)-6-[(5-chloro-2-methoxyphenyl)methyl]-3-(2,2-dimethylhydrazinyl)-7-oxo-5,6-dihydro-2H-1,4-diazepin-1-yl]-N-[3-(1-methylpyrazol-4-yl)phenyl]hexanamide | 1391053: Inhibition of recombinant human KLK7 using MOCAc-Arg-Pro-Lys-Pro-Val-Glu-Nva-Trp-Arg-Lys(Dnp)-NH2 as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence assay | ic50 | 0.1100 | 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 | 1483611: Inhibition of recombinant KLK7 (unknown origin) expressed in zymogen form in Pichia pastorisstrain X-33 using KHLY-pNA as substrate after 30 mins | ki | 0.1300 | uM |
| (2S)-2-[[(5R,8S,11S,14S,17S,20R)-20-amino-14-[(4-hydroxyphenyl)methyl]-8-methyl-11,17-bis(2-methylpropyl)-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-carbonyl]amino]-3-hydroxypropanoic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.2000 | uM |
| (2S)-2-[[(5R,8S,11S,14S,17S,20R)-14-benzyl-8-(hydroxymethyl)-11,17-bis(2-methylpropyl)-7,10,13,16,19-pentaoxo-20-[[(2S)-pyrrolidine-2-carbonyl]amino]-3,22-dithia-6,9,12,15,18,28-hexazabicyclo[22.3.1]octacosa-1(27),24(28),25-triene-5-carbonyl]amino]-3-hydroxypropanoic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.2200 | uM |
| (5-amino-3-pyridin-3-yl-1,2,4-triazol-1-yl)-(4-chlorophenyl)methanone | 762641: Inhibition of human kallikrein 7 measured after 15 mins at pH 8 by fluorescence assay | ic50 | 0.2200 | uM |
| (5-amino-3-phenyl-1,2,4-triazol-1-yl)-(3,4-dimethoxyphenyl)methanone | 762641: Inhibition of human kallikrein 7 measured after 15 mins at pH 8 by fluorescence assay | ic50 | 0.2300 | uM |
| 2-[6-[(2,6-dichlorophenyl)methyl]-3-(2,2-dimethylhydrazinyl)-7-oxo-5,6-dihydro-2H-1,4-diazepin-1-yl]-N-[3-(1-methylpyrazol-4-yl)phenyl]acetamide | 1498386: Inhibition of recombinant human C-terminal His10-tagged KLK7 (E23 to H252 residues) using MOCAcArg-Pro-Lys-Pro-Val-Glu-Nva-Trp-Arg-Lys(Dnp)-NH2 as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence assay | ic50 | 0.3800 | uM |
| 1-(2-bromophenyl)sulfonyl-5-methyl-3-(2-methyl-4,5-dihydro-1H-imidazol-5-yl)indole | 1574120: Inhibition of thermolysin activated recombinant human C-terminal 10-His tagged KLK7 (E23 to H252 residues) using MOCAc-Arg-Pro-Lys-Pro-Val-Glu-Nva-Trp-Arg-Lys(Dnp)-NH2 as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence analysis | ic50 | 0.3900 | uM |
| (2S)-2-[[(5R,8S,11S,14S,17S,20R)-11-(3-amino-3-oxopropyl)-8-(hydroxymethyl)-14-[(4-hydroxyphenyl)methyl]-17-(2-methylpropyl)-7,10,13,16,19-pentaoxo-20-[[(2S)-pyrrolidine-2-carbonyl]amino]-3,22-dithia-6,9,12,15,18,28-hexazabicyclo[22.3.1]octacosa-1(27),24(28),25-triene-5-carbonyl]amino]-3-hydroxypropanoic acid | 1884312: Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay | ki | 0.4400 | uM |
| (2S)-2-[(6R)-6-[(5-chloro-2-methoxyphenyl)methyl]-3-(2,2-dimethylhydrazinyl)-7-oxo-5,6-dihydro-2H-1,4-diazepin-1-yl]-N-[3-(1-methylpyrazol-4-yl)phenyl]butanamide | 1391053: Inhibition of recombinant human KLK7 using MOCAc-Arg-Pro-Lys-Pro-Val-Glu-Nva-Trp-Arg-Lys(Dnp)-NH2 as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence assay | ic50 | 0.4500 | uM |
| 2-[(6R)-6-[(5-chloro-2-methoxyphenyl)methyl]-3-(2,2-dimethylhydrazinyl)-7-oxo-5,6-dihydro-2H-1,4-diazepin-1-yl]-N-[3-(1-methylpyrazol-4-yl)phenyl]acetamide | 1391053: Inhibition of recombinant human KLK7 using MOCAc-Arg-Pro-Lys-Pro-Val-Glu-Nva-Trp-Arg-Lys(Dnp)-NH2 as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence assay | ic50 | 0.5200 | uM |
| 2-[(6R)-6-[(5-chloro-2-methoxyphenyl)methyl]-3-(2,2-dimethylhydrazinyl)-7-oxo-5,6-dihydro-2H-1,4-diazepin-1-yl]-N-[3-(furan-2-yl)phenyl]acetamide | 1391053: Inhibition of recombinant human KLK7 using MOCAc-Arg-Pro-Lys-Pro-Val-Glu-Nva-Trp-Arg-Lys(Dnp)-NH2 as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence assay | ic50 | 0.5900 | uM |
| (3-amino-1,2,4-triazol-4-yl)-(4-methoxyphenyl)methanone | 762641: Inhibition of human kallikrein 7 measured after 15 mins at pH 8 by fluorescence assay | ic50 | 0.6100 | uM |
| [3-(4-chlorophenyl)-5-methylsulfanyl-1,2,4-triazol-1-yl]-phenylmethanone | 762641: Inhibition of human kallikrein 7 measured after 15 mins at pH 8 by fluorescence assay | ic50 | 0.6600 | uM |
| 2-[(6R)-6-[(5-chloro-2-methoxyphenyl)methyl]-3-(2,2-dimethylhydrazinyl)-7-oxo-5,6-dihydro-2H-1,4-diazepin-1-yl]-N-[3-(furan-3-yl)phenyl]acetamide | 1391053: Inhibition of recombinant human KLK7 using MOCAc-Arg-Pro-Lys-Pro-Val-Glu-Nva-Trp-Arg-Lys(Dnp)-NH2 as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence assay | ic50 | 0.6700 | uM |
| (2S)-2-N-[2-(4-methoxyphenyl)ethyl]-1-N-(naphthalen-1-ylmethyl)pyrrolidine-1,2-dicarboxamide | 1802173: Human KLK7 Fluorescence-Lifetime Assay from Article 10.1038/nchembio.2208: “Small-molecule factor D inhibitors targeting the alternative complement pathway.” | ic50 | 0.7000 | 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 | 1483611: Inhibition of recombinant KLK7 (unknown origin) expressed in zymogen form in Pichia pastorisstrain X-33 using KHLY-pNA as substrate after 30 mins | ki | 0.7400 | uM |
| 2-[(6R)-6-[(5-chloro-2-methoxyphenyl)methyl]-3-(2,2-dimethylhydrazinyl)-7-oxo-5,6-dihydro-2H-1,4-diazepin-1-yl]-N-(3-methylsulfonylphenyl)acetamide | 1367551: Inhibition of thermolysin activated recombinant human C-terminal 10-His tagged KLK7 preincubated for 10 mins followed by MOCAc-Arg-Pro-Lys-Pro-Val-Glu-Nva-Trp-Arg-Lys(Dnp)-NH2 peptide substrate addition measured after 30 mins by fluorescence analysis | ic50 | 0.8200 | uM |
CTD chemical–gene interactions
25 total (human), top 25 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Tobacco Smoke Pollution | affects expression, decreases expression, increases expression | 4 |
| Smoke | decreases expression, increases abundance | 2 |
| sodium arsenate | decreases expression, increases abundance | 1 |
| sodium arsenite | decreases expression | 1 |
| pentanal | increases expression | 1 |
| exemestane | increases expression | 1 |
| CGP 52608 | increases reaction, affects binding | 1 |
| ICG 001 | increases expression | 1 |
| (+)-JQ1 compound | decreases expression | 1 |
| 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acid | increases expression | 1 |
| Resveratrol | affects cotreatment, decreases expression | 1 |
| Air Pollutants | decreases expression, increases abundance | 1 |
| Arsenic | decreases expression, increases abundance | 1 |
| Benzo(a)pyrene | increases methylation | 1 |
| Cadmium | increases expression | 1 |
| Calcitriol | increases expression | 1 |
| Carbamazepine | affects expression | 1 |
| Cisplatin | affects response to substance | 1 |
| Copper | affects cotreatment, decreases expression | 1 |
| Diethylhexyl Phthalate | decreases expression | 1 |
| Estradiol | decreases expression, affects cotreatment | 1 |
| Formaldehyde | decreases expression | 1 |
| Dihydrotestosterone | increases expression | 1 |
| Tretinoin | increases expression | 1 |
| Triclosan | increases expression | 1 |
ChEMBL screening assays
75 unique, capped per target: 74 binding, 1 admet
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1837531 | Binding | Inhibition of human kallikrein 7 using Abz-KLYSSKQ-EDDnp as substrate by spectrofluorimetric assay | Biological evaluation and docking studies of natural isocoumarins as inhibitors for human kallikrein 5 and 7. — Bioorg Med Chem Lett |
| CHEMBL4388473 | ADMET | Inhibition of recombinant C-terminal 10His-tagged human KLK7 (Glu23 to His252 residues) expressed in mouse NS0 cells using 5-FAM-E-A-L-Y-L-V-S-G-C as substrate after 40 mins by fluorescence intensity assay | Structure guided drug design to develop kallikrein 5 inhibitors to treat Netherton syndrome. — Bioorg Med Chem Lett |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.