MMP1
gene geneOn this page
Summary
MMP1 (matrix metallopeptidase 1, HGNC:7155) is a protein-coding gene on chromosome 11q22.2, encoding Interstitial collagenase (P03956). Cleaves collagens of types I, II, and III at one site in the helical domain. In precision oncology, MMP1 Overexpression is associated with resistance to Sacituzumab Govitecan in Estrogen-receptor Positive Breast Cancer (CIViC Level D).
This gene encodes a member of the peptidase M10 family of matrix metalloproteinases (MMPs). Proteins in this family are involved in the breakdown of extracellular matrix in normal physiological processes, such as embryonic development, reproduction, and tissue remodeling, as well as in disease processes, such as arthritis and metastasis. The encoded preproprotein is proteolytically processed to generate the mature protease. This secreted protease breaks down the interstitial collagens, including types I, II, and III. The gene is part of a cluster of MMP genes on chromosome 11. Mutations in this gene are associated with chronic obstructive pulmonary disease (COPD). Alternative splicing results in multiple transcript variants, at least one of which encodes an isoform that is proteolytically processed.
Source: NCBI Gene 4312 — RefSeq curated summary.
At a glance
- GWAS associations: 2
- Clinical variants (ClinVar): 146 total
- Phenotypes (HPO): 58
- Druggable target: yes — 21 molecules with ChEMBL bioactivity
- Precision-oncology evidence (CIViC): 1 curated variant–drug association
- MANE Select transcript:
NM_002421
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:7155 |
| Approved symbol | MMP1 |
| Name | matrix metallopeptidase 1 |
| Location | 11q22.2 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000196611 |
| Ensembl biotype | protein_coding |
| OMIM | 120353 |
| Entrez | 4312 |
Gene structure
Transcript identifiers
Ensembl transcripts: 4 — 2 protein_coding_CDS_not_defined, 1 protein_coding, 1 retained_intron
ENST00000315274, ENST00000680179, ENST00000681445, ENST00000681643
RefSeq mRNA: 2 — MANE Select: NM_002421
NM_001145938, NM_002421
CCDS: CCDS8322
Canonical transcript exons
ENST00000315274 — 10 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000993183 | 102795174 | 102795291 |
| ENSE00000993195 | 102792605 | 102792738 |
| ENSE00000993197 | 102795452 | 102795607 |
| ENSE00000993199 | 102791333 | 102791495 |
| ENSE00000993204 | 102790703 | 102790806 |
| ENSE00000993211 | 102797256 | 102797500 |
| ENSE00000993213 | 102797014 | 102797162 |
| ENSE00001105440 | 102796664 | 102796789 |
| ENSE00001234609 | 102797988 | 102798160 |
| ENSE00001234621 | 102789919 | 102790521 |
Expression profiles
Bgee: expression breadth ubiquitous, 172 present calls, max score 99.09.
FANTOM5 (CAGE): breadth broad, TPM avg 239.1385 / max 18368.5720, expressed in 879 samples.
FANTOM5 promoters (24 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 122018 | 231.0513 | 856 |
| 122001 | 3.1155 | 283 |
| 121998 | 0.7959 | 180 |
| 121995 | 0.5200 | 164 |
| 122009 | 0.4695 | 162 |
| 122012 | 0.4472 | 170 |
| 122008 | 0.4334 | 130 |
| 122007 | 0.2731 | 109 |
| 122011 | 0.2674 | 114 |
| 122015 | 0.2650 | 122 |
Top tissues by expression
274 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| epithelial cell of pancreas | CL:0000083 | 99.09 | gold quality |
| pancreatic ductal cell | CL:0002079 | 98.93 | gold quality |
| islet of Langerhans | UBERON:0000006 | 98.21 | gold quality |
| cartilage tissue | UBERON:0002418 | 98.20 | gold quality |
| type B pancreatic cell | CL:0000169 | 97.71 | gold quality |
| synovial membrane of synovial joint | UBERON:0002018 | 97.06 | gold quality |
| gall bladder | UBERON:0002110 | 94.66 | gold quality |
| stromal cell of endometrium | CL:0002255 | 90.21 | gold quality |
| amniotic fluid | UBERON:0000173 | 85.31 | gold quality |
| pylorus | UBERON:0001166 | 83.59 | gold quality |
| decidua | UBERON:0002450 | 83.35 | gold quality |
| mucosa of urinary bladder | UBERON:0001259 | 81.56 | gold quality |
| duodenum | UBERON:0002114 | 81.39 | gold quality |
| jejunal mucosa | UBERON:0000399 | 79.93 | gold quality |
| palpebral conjunctiva | UBERON:0001812 | 78.93 | gold quality |
| vermiform appendix | UBERON:0001154 | 78.27 | gold quality |
| rectum | UBERON:0001052 | 76.63 | gold quality |
| body of stomach | UBERON:0001161 | 75.96 | gold quality |
| caecum | UBERON:0001153 | 75.86 | gold quality |
| mucosa of sigmoid colon | UBERON:0004993 | 75.50 | gold quality |
| visceral pleura | UBERON:0002401 | 74.84 | gold quality |
| periodontal ligament | UBERON:0008266 | 74.37 | silver quality |
| stomach | UBERON:0000945 | 72.88 | gold quality |
| nasal cavity epithelium | UBERON:0005384 | 72.01 | gold quality |
| olfactory segment of nasal mucosa | UBERON:0005386 | 71.10 | gold quality |
| colonic mucosa | UBERON:0000317 | 70.80 | gold quality |
| colonic epithelium | UBERON:0000397 | 69.98 | gold quality |
| placenta | UBERON:0001987 | 68.08 | gold quality |
| pancreas | UBERON:0001264 | 68.00 | gold quality |
| jejunum | UBERON:0002115 | 67.73 | gold quality |
Single-cell (SCXA)
Detected in 4 experiment(s), a significant marker in 4.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-CURD-10 | yes | 2840.46 |
| E-MTAB-6308 | yes | 953.77 |
| E-MTAB-5061 | yes | 5.93 |
| E-ANND-3 | no | 0.00 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): AHR, AP1, AR, ATF2, ATF3, BACH1, BATF3, BCL3, CEBPA, CEBPB, CEBPG, CITED2, COP1, CREB1, CTNNB1, EGR1, EHF, ELF2, ERG, ESR1, ESR2, ETS1, ETS2, ETV1, ETV2, ETV3, ETV4, ETV7, EWSR1, FBN1, FLI1, FOS, FOSL1, FOXN1, FOXO1, FOXO3, GATA3, HIF1A, HOPX, HR
miRNA regulators (miRDB)
38 targeting MMP1, 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-520G-5P | 99.99 | 66.76 | 658 |
| HSA-MIR-4500 | 99.99 | 72.72 | 2367 |
| HSA-LET-7F-5P | 99.98 | 72.56 | 1784 |
| HSA-MIR-4803 | 99.98 | 71.99 | 3117 |
| HSA-MIR-6888-3P | 99.97 | 65.95 | 1170 |
| HSA-LET-7D-5P | 99.96 | 71.76 | 1632 |
| HSA-MIR-4458 | 99.96 | 71.64 | 1650 |
| HSA-MIR-7162-3P | 99.89 | 68.16 | 1682 |
| HSA-MIR-6124 | 99.87 | 69.78 | 3551 |
| HSA-MIR-202-3P | 99.84 | 71.41 | 1290 |
| HSA-MIR-5010-3P | 99.83 | 70.60 | 2357 |
| HSA-MIR-4799-5P | 99.82 | 70.60 | 2663 |
| HSA-MIR-875-3P | 99.63 | 69.47 | 2548 |
| HSA-MIR-4743-3P | 99.62 | 68.12 | 2095 |
| HSA-MIR-488-3P | 99.61 | 68.79 | 1731 |
| HSA-MIR-6833-5P | 99.50 | 68.93 | 1161 |
| HSA-MIR-4251 | 99.40 | 69.19 | 3363 |
| HSA-MIR-3176 | 99.25 | 64.35 | 954 |
| HSA-MIR-3922-3P | 99.25 | 64.96 | 1136 |
| HSA-MIR-5190 | 99.15 | 67.76 | 1234 |
| HSA-MIR-3152-3P | 99.10 | 66.35 | 678 |
| HSA-MIR-936 | 98.87 | 70.51 | 1124 |
| HSA-MIR-655-5P | 98.74 | 65.93 | 888 |
| HSA-MIR-330-5P | 98.73 | 67.63 | 1788 |
| HSA-MIR-5197-3P | 98.71 | 67.05 | 1905 |
| HSA-MIR-5094 | 98.63 | 67.11 | 1062 |
| HSA-MIR-518C-5P | 98.53 | 69.20 | 1640 |
| HSA-MIR-3136-5P | 98.53 | 67.68 | 793 |
| HSA-MIR-4439 | 98.53 | 67.53 | 793 |
| HSA-MIR-326 | 98.25 | 66.44 | 1565 |
Literature-anchored findings (GeneRIF, showing 40)
- Patients with detectable concentrations of urinary MMP-1 had higher rates of disease progression and death from bladder cancer than patients with undetectable urinary MMP-1. (PMID:11705862)
- members of the forkhead family of transcription factors play a role in regulation of the collagenase promoter and increased activity of forkhead transcription factors underlie the increase in collagenase expression observed during replicative senescence (PMID:11751876)
- 17beta-estradiol represses MMP-1 synthesis, and this effect may contribute to its action on the inhibition of bone resorption (PMID:11762702)
- role in degradation of extracellular matrix and joint destruction (PMID:11831026)
- induction in fibroblasts by basic calcium phosphate crystals (PMID:11836255)
- These data suggest that polymorphisms in the MMP1 and MMP12 genes, but not MMP9, are either causative factors in smoking-related lung injury or are in linkage disequilibrium with causative polymorphisms (PMID:11875051)
- Membrane type 1 matrix metalloproteinase regulates cellular invasiveness and survival in cutaneous epidermal cells. (PMID:11918701)
- in the late healing period of radiation-impaired wounds, increased expression of MMP1 may be related to overdegradation of matrixes and difficulty in granulation tissue formation (PMID:11934016)
- A newly identified single nucleotide polymorphism at position -519 in the promoter region of the MMP-1 gene is reported. This polymorphism consists in a guanine to adenine substitution. A linkage between polymorphisms -519A/G and -1607 1G/2G was studied. (PMID:12005449)
- Reduction of cytokine-induced expression and activity of MMP-1 and MMP-13 by mechanical strain in MH7A rheumatoid synovial cells (PMID:12009332)
- Accessory elements, flanking DNA sequence, and promoter context play key roles in determining the efficacy of insulin and phorbol ester signaling through the enzyme motifs (PMID:12032154)
- destruction of the surrounding matrix by endometriosis might be caused by various MMPs, which are mainly produced in stromal cells. (PMID:12034345)
- Oxidized low-density and high-density lipoproteins regulate the production by activated monocytes (PMID:12050187)
- lack of expression in Ewing sarcoma may be due to loss of accessibility of regulatory element to the specific fusion protein in vivo (PMID:12054564)
- Activation of p38 alpha MAPK enhances its expression by mRNA stabilization (PMID:12060661)
- Activation of protein kinase CK2 is an early step in the ultraviolet B-mediated increase in interstitial collagenase (matrix metalloproteinase-1; MMP-1) and stromelysin-1 (MMP-3) protein levels in human dermal fibroblasts. (PMID:12071839)
- Results demonstrate that generation of the 44-kDa membrane type-1 matrix metalloproteinase (MT1-MMP) autolysis product regulates collagenolytic activity and subsequent invasive potential. (PMID:12145314)
- keratinocyte-fibroblast interactions are mediated by multiple stimulating agents acting on specific receptors to induce signalling through different mitogen-activated protein kinase pathways leading to altered expression of key biological functions. (PMID:12177784)
- Association of a polymorphism of the matrix metalloproteinase-1 gene with bone mineral density.Bone density for the distal radius was significantly lower in postmenopausal women with the GG/GG genotype. (PMID:12225803)
- MMP1 may play a pivotal role in the formation of capillarylike tubular structures in a collagen-containing fibrin matrix in vitro and may be involved in angiogenesis in a fibrinous exudate in vivo. (PMID:12393408)
- Genotyping was carried out using PCR-RFLP and direct sequencing. In the MMP-1 gene polymorphism, the frequency of the 2G/2G genotype that is associated with higher enzyme activity was significantly increased in colorectal cancer patients (PMID:12432557)
- viral LMP1 and Zta proteins regulate the expression and activity of MMP-1; first evidence that viral proteins are capable of regulating MMP-1 and clues for the role of EBV in nasopharyngeal carcinoma progression (PMID:12517806)
- A novel promoter element was detected in the human MMP1 gene, and the inflammation-responsive transcription factor SAF-1 was found to interact with it in osteoarthritis (PMID:12528113)
- a polymorphism in the promoter region is associated with the severe chronic periodontitis phenotype in non-smokers (PMID:12622858)
- expression and regulation by intestinal myofibroblasts in inflammatory bowel disease (PMID:12651627)
- catalytic activity on the cell surface is regulated through a vacuolar H(+)-ATPase-dependent degradation process (PMID:12667140)
- MMP-1 induces progressive adult-onset emphysema by the selective degradation of type III collagen within the alveolar wall. (PMID:12676763)
- Gene expression for MMP-1 after UVA1 irradiation was induced in all fibroblasts, but the induction rate was greater in systemic sclerosis fibroblasts than in normal ones. (PMID:12692352)
- MMP1 has a role in tumor invasion [review] (PMID:12706853)
- MT1-MMP-catalyzed release of beta-amyloid precursor protein leads to reduction of the extracellular matrix-associated gelatinase A inhibitor, sAPP, thus making it feasible for gelatinase A to exert proteolytic activity only near its activator, MT1-MMP (PMID:12767235)
- MMP-1 epitope increased interleukin 4 (IL-4) production of rheumatoid arthritis lymphocytes and decreased IL-4 production by control lymphocytes (PMID:12784383)
- These data provide evidence that tissue factor pathway inhibitor-2 does not bind to matrix metalloproteinases-2, -9 or -1, or regulate matrix metalloproteinase-1, in the extracellular matrix. (PMID:12787920)
- Hypoxia may be responsible for delayed wound healing by inducing an increase of MMP-1 synthesis. (PMID:12788533)
- MMP1 is a senescence-associated gene in normal human oral keratinocytes. (PMID:12837283)
- A single nucleotide polymorphism in the matrix metalloproteinase-1 promoter is associated with renal cell carcinoma (PMID:12845675)
- study showed no change in metalloproteinase-1 production in response to varying estrogen levels in fibroblasts that were derived from incontinent women (PMID:12861139)
- Patients with deteriorating heart failure have increased expression of TIMP1 and MMP1 mRNA. Correlation with pro-inflammatory cytokines suggests common pathways of regulation and potential activation by IL-6 and IL1-beta. (PMID:12873541)
- Upregulation of mmp-1 ia assiciated with neoplasm invasiveness in Hereditary nonpolyposis colorectal cancers (PMID:12949792)
- monocyte matrix metalloproteinase-1 and -9 are differentially regulated by interferon gamma through tumor necrosis factor-alpha and caspase 8 (PMID:12960156)
- reported association between the matrix metalloproteinase 1 promoter polymorphism and ovarian cancer risk was not supported by our (PMID:12969782)
Cross-species orthologs
12 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | ENSDARG00000012395 | |
| danio_rerio | ENSDARG00000108401 | |
| danio_rerio | ENSDARG00000114451 | |
| mus_musculus | Mmp1b | ENSMUSG00000041620 |
| mus_musculus | Mmp1a | ENSMUSG00000043089 |
| rattus_norvegicus | Mmp1b | ENSRNOG00000008881 |
| rattus_norvegicus | Mmp1 | ENSRNOG00000032353 |
| caenorhabditis_elegans | WBGENE00010524 | |
| caenorhabditis_elegans | WBGENE00012185 | |
| caenorhabditis_elegans | WBGENE00012364 | |
| caenorhabditis_elegans | WBGENE00016283 | |
| caenorhabditis_elegans | WBGENE00194737 |
Paralogs (23): MMP25 (ENSG00000008516), MMP2 (ENSG00000087245), MMP11 (ENSG00000099953), MMP9 (ENSG00000100985), MMP15 (ENSG00000102996), HPX (ENSG00000110169), MMP8 (ENSG00000118113), MMP19 (ENSG00000123342), MMP24 (ENSG00000125966), MMP7 (ENSG00000137673), MMP20 (ENSG00000137674), MMP27 (ENSG00000137675), MMP13 (ENSG00000137745), MMP3 (ENSG00000149968), MMP21 (ENSG00000154485), MMP16 (ENSG00000156103), MMP14 (ENSG00000157227), MMP10 (ENSG00000166670), MMP26 (ENSG00000167346), MMP23B (ENSG00000189409), MMP17 (ENSG00000198598), MMP12 (ENSG00000262406), MMP28 (ENSG00000271447)
Protein
Protein identifiers
Interstitial collagenase — P03956 (reviewed: P03956)
Alternative names: Fibroblast collagenase, Matrix metalloproteinase-1
All UniProt accessions (1): P03956
UniProt curated annotations — full annotation on UniProt →
Function. Cleaves collagens of types I, II, and III at one site in the helical domain. Also cleaves collagens of types VII and X. In case of HIV infection, interacts and cleaves the secreted viral Tat protein, leading to a decrease in neuronal Tat’s mediated neurotoxicity.
Subunit / interactions. (Microbial infection) Interacts with HIV-1 Tat.
Subcellular location. Secreted. Extracellular space. Extracellular matrix.
Post-translational modifications. Undergoes autolytic cleavage to two major forms (22 kDa and 27 kDa). A minor form (25 kDa) is the glycosylated form of the 22 kDa form. The 27 kDa form has no activity while the 22/25 kDa form can act as activator for collagenase. Tyrosine phosphorylated in platelets by PKDCC/VLK.
Activity regulation. Can be activated without removal of the activation peptide.
Cofactor. Binds 4 Ca(2+) ions per subunit. Binds 2 Zn(2+) ions per subunit.
Domain organisation. There are two distinct domains in this protein; the catalytic N-terminal, and the C-terminal which is involved in substrate specificity and in binding TIMP (tissue inhibitor of metalloproteinases). The conserved cysteine present in the cysteine-switch motif binds the catalytic zinc ion, thus inhibiting the enzyme. The dissociation of the cysteine from the zinc ion upon the activation-peptide release activates the enzyme.
Similarity. Belongs to the peptidase M10A family.
RefSeq proteins (2): NP_001139410, NP_002412* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000585 | Hemopexin-like_dom | Domain |
| IPR001818 | Pept_M10_metallopeptidase | Domain |
| IPR002477 | Peptidoglycan-bd-like | Domain |
| IPR006026 | Peptidase_Metallo | Domain |
| IPR018486 | Hemopexin_CS | Conserved_site |
| IPR018487 | Hemopexin-like_repeat | Repeat |
| IPR021158 | Pept_M10A_Zn_BS | Binding_site |
| IPR021190 | Pept_M10A | Family |
| IPR024079 | MetalloPept_cat_dom_sf | Homologous_superfamily |
| IPR033739 | M10A_MMP | Domain |
| IPR036365 | PGBD-like_sf | Homologous_superfamily |
| IPR036375 | Hemopexin-like_dom_sf | Homologous_superfamily |
Pfam: PF00045, PF00413, PF01471
Enzyme classification (BRENDA):
- EC 3.4.24.7 — interstitial collagenase (BRENDA: 11 organisms, 121 substrates, 166 inhibitors, 52 Km, 47 kcat entries)
Substrate kinetics (BRENDA)
28 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| COLLAGEN I ALPHA-1 CHAIN | 0.0009–0.74 | 8 |
| COLLAGEN I ALPHA-2 CHAIN | 0.0003–0.53 | 8 |
| HUMAN TYPE I COLLAGEN | 0.0005–0.0011 | 4 |
| HUMAN TYPE III COLLAGEN | 0.0013–0.0024 | 3 |
| ALPHA1(I)772-786 TRIPLE-HELICAL PEPTIDE | 0.063–0.2076 | 2 |
| FTHP-3 | 0.0612–0.0666 | 2 |
| HUMAN TYPE II COLLAGEN | 0.001–0.0021 | 2 |
| 2,4-DINITROPHENYL-PRO-BETA-CYCLOHEXYL-ALA-GLY-CY | 0.013 | 1 |
| 2,4-DINITROPHENYL-PRO-LEU-ALA-LEU-TRP-ALA-ARG-OH | 0.026 | 1 |
| ACETYL-PRO-LEU-GLY-ILE-LEU-GLY-OC2H5 | 0.0013 | 1 |
| ACETYL-PRO-LEU-GLY-LEU-LEU-GLY-OC2H5 | 0.0012 | 1 |
| ACETYL-PRO-LEU-GLY-SCH[CH2CH(CH3)2CO]-LEU-LEU-OC | 0.0039 | 1 |
| BOVINE TYPE I COLLAGEN | 0.0002 | 1 |
| GLY-PRO-GLN-GLY-ILE-ALA-GLY-GLN-GLN | 3.3 | 1 |
| GLY-PRO-GLN-GLY-ILE-ALA-GLY-GLN-GLN-ARG-GLY-VAL- | 0.63 | 1 |
UniProt features (103 total): strand 31, binding site 24, helix 10, sequence conflict 7, sequence variant 6, turn 5, repeat 4, chain 3, modified residue 3, site 2, signal peptide 1, propeptide 1, short sequence motif 1, active site 1, glycosylation site 1, disulfide bond 1, mutagenesis site 1, region of interest 1
Structure
Experimental structures (PDB)
15 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 1HFC | X-RAY DIFFRACTION | 1.5 |
| 1CGE | X-RAY DIFFRACTION | 1.9 |
| 966C | X-RAY DIFFRACTION | 1.9 |
| 1CGF | X-RAY DIFFRACTION | 2.1 |
| 1SU3 | X-RAY DIFFRACTION | 2.2 |
| 2TCL | X-RAY DIFFRACTION | 2.2 |
| 3SHI | X-RAY DIFFRACTION | 2.2 |
| 1CGL | X-RAY DIFFRACTION | 2.4 |
| 2J0T | X-RAY DIFFRACTION | 2.54 |
| 2CLT | X-RAY DIFFRACTION | 2.67 |
| 4AUO | X-RAY DIFFRACTION | 3 |
| 1AYK | SOLUTION NMR | |
| 2AYK | SOLUTION NMR | |
| 3AYK | SOLUTION NMR | |
| 4AYK | SOLUTION NMR |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P03956-F1 | 91.29 | 0.85 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Catalytic / active sites (3): 219; 143 (not glycosylated); 269–270 (cleavage; by autolysis)
Ligand- & substrate-binding residues (24): 92 (in inhibited form); 124; 158; 168; 170; 175; 176; 178; 180; 183; 190; 192 …
Post-translational modifications (3): 57, 274, 360
Disulfide bonds (1): 278–466
Glycosylation sites (1): 120
Mutagenesis-validated functional residues (1):
| Position | Phenotype |
|---|---|
| 360 | partial reduction of tyrosine phosphorylation in the presence of pkdcc/vlk. |
Function
Pathways and Gene Ontology
Reactome pathways
13 pathways
| ID | Pathway |
|---|---|
| R-HSA-1442490 | Collagen degradation |
| R-HSA-1474228 | Degradation of the extracellular matrix |
| R-HSA-1592389 | Activation of Matrix Metalloproteinases |
| R-HSA-210991 | Basigin interactions |
| R-HSA-381426 | Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs) |
| R-HSA-6785807 | Interleukin-4 and Interleukin-13 signaling |
| R-HSA-109582 | Hemostasis |
| R-HSA-1280215 | Cytokine Signaling in Immune system |
| R-HSA-1474244 | Extracellular matrix organization |
| R-HSA-168256 | Immune System |
| R-HSA-202733 | Cell surface interactions at the vascular wall |
| R-HSA-392499 | Metabolism of proteins |
| R-HSA-449147 | Signaling by Interleukins |
MSigDB gene sets: 448 (showing top):
MODULE_172, AHRARNT_01, TONKS_TARGETS_OF_RUNX1_RUNX1T1_FUSION_MONOCYTE_UP, MODULE_52, MCLACHLAN_DENTAL_CARIES_UP, YAGI_AML_WITH_INV_16_TRANSLOCATION, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, GOMF_METALLOPEPTIDASE_ACTIVITY, GOBP_CELLULAR_RESPONSE_TO_UV, chr11q22, GOBP_CELLULAR_RESPONSE_TO_LIGHT_STIMULUS, MODULE_128, SATO_SILENCED_BY_DEACETYLATION_IN_PANCREATIC_CANCER, GNF2_PTX3, PID_REG_GR_PATHWAY
GO Biological Process (6): proteolysis (GO:0006508), extracellular matrix disassembly (GO:0022617), extracellular matrix organization (GO:0030198), collagen catabolic process (GO:0030574), positive regulation of protein-containing complex assembly (GO:0031334), cellular response to UV-A (GO:0071492)
GO Molecular Function (8): endopeptidase activity (GO:0004175), metalloendopeptidase activity (GO:0004222), serine-type endopeptidase activity (GO:0004252), peptidase activity (GO:0008233), zinc ion binding (GO:0008270), metallopeptidase activity (GO:0008237), hydrolase activity (GO:0016787), metal ion binding (GO:0046872)
GO Cellular Component (2): extracellular region (GO:0005576), extracellular matrix (GO:0031012)
Reactome top-level categories
Rollup of top-8 pathways:
| Category | Pathways |
|---|---|
| Degradation of the extracellular matrix | 2 |
| Extracellular matrix organization | 1 |
| Cell surface interactions at the vascular wall | 1 |
| Metabolism of proteins | 1 |
| Signaling by Interleukins | 1 |
| Immune System | 1 |
| Hemostasis | 1 |
| Cytokine Signaling in Immune system | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| peptidase activity | 2 |
| endopeptidase activity | 2 |
| protein metabolic process | 1 |
| cellular component disassembly | 1 |
| extracellular matrix organization | 1 |
| extracellular structure organization | 1 |
| external encapsulating structure organization | 1 |
| catabolic process | 1 |
| collagen metabolic process | 1 |
| regulation of protein-containing complex assembly | 1 |
| positive regulation of cellular component biogenesis | 1 |
| positive regulation of cellular component organization | 1 |
| protein-containing complex assembly | 1 |
| cellular response to UV | 1 |
| response to UV-A | 1 |
| metallopeptidase activity | 1 |
| serine-type peptidase activity | 1 |
| hydrolase activity | 1 |
| catalytic activity, acting on a protein | 1 |
| transition metal ion binding | 1 |
| catalytic activity | 1 |
| cation binding | 1 |
| cellular anatomical structure | 1 |
| external encapsulating structure | 1 |
Protein interactions and networks
STRING
2902 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| MMP1 | TIMP1 | P01033 | 985 |
| MMP1 | TIMP2 | P16035 | 921 |
| MMP1 | IL1B | P01584 | 849 |
| MMP1 | F2R | P25116 | 828 |
| MMP1 | PLAU | P00749 | 822 |
| MMP1 | PITRM1 | Q5JRX3 | 801 |
| MMP1 | ELN | P15502 | 796 |
| MMP1 | IL1A | P01583 | 779 |
| MMP1 | EGF | P01133 | 779 |
| MMP1 | FN1 | P02751 | 777 |
| MMP1 | CCL2 | P13500 | 754 |
| MMP1 | TIMP4 | Q99727 | 754 |
| MMP1 | ADAMTS3 | O15072 | 751 |
| MMP1 | COL1A1 | P02452 | 739 |
| MMP1 | IL6 | P05231 | 732 |
IntAct
4 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| MMP1 | SOX8 | psi-mi:“MI:0915”(physical association) | 0.370 |
| NEK4 | QSOX1 | psi-mi:“MI:0914”(association) | 0.350 |
| F2R | MMP1 | psi-mi:“MI:2364”(proximity) | 0.270 |
BioGRID (27): F2R (Co-localization), MMP1 (Co-localization), MMP1 (Affinity Capture-MS), MMP1 (Synthetic Lethality), MMP1 (Reconstituted Complex), MMP1 (Affinity Capture-MS), MMP1 (Reconstituted Complex), BCAN (Biochemical Activity), MMP1 (Affinity Capture-Western), ITGA2 (Affinity Capture-Western), MMP1 (Affinity Capture-MS), MMP1 (Affinity Capture-MS), MMP1 (Affinity Capture-MS), MMP2 (Negative Genetic), MMP24 (Negative Genetic)
ESM2 similar proteins: A0A0C5PRQ1, A0FKN6, C9D7R2, C9D7R3, D2KBH9, D5FM34, D5FM37, K7Z9Q9, O13065, O17264, O35548, O62243, P03956, P07584, P0DJJ2, P0DM62, P31580, P31581, P42662, P42664, P50280, P51512, P55112, P55113, P55114, P91828, P98060, P98061, P98068, P98070, Q10738, Q18206, Q18439, Q20191, Q20459, Q20958, Q21178, Q21181, Q21252, Q22396
Diamond homologs: A4KX75, D0EM77, G5EBU3, O04529, O18733, O18767, O18927, O23507, O55123, O55761, O60882, O62806, O77656, P03956, P03957, P07152, P08253, P08254, P09237, P09238, P13943, P14780, P21692, P22757, P23097, P28862, P28863, P29136, P33434, P33435, P33436, P34960, P39900, P41245, P41246, P45452, P50280, P50281, P50282, P50757
SIGNOR signaling
14 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| FBN1 | “up-regulates quantity by expression” | MMP1 | “transcriptional regulation” |
| MMP1 | up-regulates | Angiogenesis | |
| CITED2 | “down-regulates quantity by repression” | MMP1 | “transcriptional regulation” |
| MMP1 | “down-regulates quantity by destabilization” | COL2A1 | cleavage |
| ZMYND8 | “down-regulates quantity by repression” | MMP1 | “transcriptional regulation” |
| MMP1 | “up-regulates activity” | HBEGF | cleavage |
| WNT7A | “up-regulates quantity by expression” | MMP1 | “transcriptional regulation” |
| ZNF384 | “up-regulates quantity by expression” | MMP1 | “transcriptional regulation” |
| MMP1 | “down-regulates quantity by destabilization” | COL1A1 | cleavage |
| MMP1 | “down-regulates quantity by destabilization” | COL1A2 | cleavage |
| MMP1 | “down-regulates quantity by destabilization” | COL3A1 | cleavage |
| MMP1 | up-regulates | ECM_disassembly | |
| MMP1 | down-regulates | ECM |
Disease & clinical
Cancer significance
Clinical variants and AI predictions
ClinVar
146 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 81 |
| Likely benign | 17 |
| Benign | 38 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
742 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 11:102790697:ACTT:A | donor_loss | 1.0000 |
| 11:102790699:TTA:T | donor_loss | 1.0000 |
| 11:102790700:TA:T | donor_loss | 1.0000 |
| 11:102790701:A:AC | donor_gain | 1.0000 |
| 11:102790701:AC:A | donor_gain | 1.0000 |
| 11:102790701:ACCAT:A | donor_gain | 1.0000 |
| 11:102790702:C:A | donor_loss | 1.0000 |
| 11:102790702:C:CA | donor_gain | 1.0000 |
| 11:102790702:CC:C | donor_gain | 1.0000 |
| 11:102790702:CCA:C | donor_gain | 1.0000 |
| 11:102790702:CCAT:C | donor_gain | 1.0000 |
| 11:102790702:CCATC:C | donor_gain | 1.0000 |
| 11:102790802:CATAC:C | acceptor_gain | 1.0000 |
| 11:102790803:ATAC:A | acceptor_gain | 1.0000 |
| 11:102790804:TAC:T | acceptor_gain | 1.0000 |
| 11:102790805:AC:A | acceptor_gain | 1.0000 |
| 11:102790806:CC:C | acceptor_gain | 1.0000 |
| 11:102790807:C:CC | acceptor_gain | 1.0000 |
| 11:102790812:C:CT | acceptor_gain | 1.0000 |
| 11:102791328:CTTA:C | donor_loss | 1.0000 |
| 11:102791329:TTACC:T | donor_loss | 1.0000 |
| 11:102791330:TACCT:T | donor_loss | 1.0000 |
| 11:102791331:A:AC | donor_gain | 1.0000 |
| 11:102791331:A:C | donor_loss | 1.0000 |
| 11:102791331:ACCT:A | donor_gain | 1.0000 |
| 11:102791332:C:A | donor_loss | 1.0000 |
| 11:102791332:C:CC | donor_gain | 1.0000 |
| 11:102791332:CCT:C | donor_gain | 1.0000 |
| 11:102791332:CCTC:C | donor_gain | 1.0000 |
| 11:102791492:TTCC:T | acceptor_gain | 1.0000 |
AlphaMissense
3141 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 11:102796734:A:C | F185L | 0.997 |
| 11:102796734:A:T | F185L | 0.997 |
| 11:102796736:A:G | F185L | 0.997 |
| 11:102796767:A:C | F174L | 0.997 |
| 11:102796767:A:T | F174L | 0.997 |
| 11:102796769:A:G | F174L | 0.997 |
| 11:102797024:A:C | F163L | 0.996 |
| 11:102797024:A:T | F163L | 0.996 |
| 11:102797026:A:G | F163L | 0.996 |
| 11:102797279:C:A | W109C | 0.995 |
| 11:102797279:C:G | W109C | 0.995 |
| 11:102796680:C:A | W203C | 0.994 |
| 11:102796680:C:G | W203C | 0.994 |
| 11:102795549:A:C | H228Q | 0.993 |
| 11:102795549:A:T | H228Q | 0.993 |
| 11:102795567:A:C | H222Q | 0.993 |
| 11:102795567:A:T | H222Q | 0.993 |
| 11:102797092:A:G | W141R | 0.993 |
| 11:102797092:A:T | W141R | 0.993 |
| 11:102795479:C:G | D252H | 0.992 |
| 11:102795569:G:C | H222D | 0.992 |
| 11:102795581:G:C | H218D | 0.992 |
| 11:102796682:A:G | W203R | 0.992 |
| 11:102796682:A:T | W203R | 0.992 |
| 11:102795525:C:A | M236I | 0.991 |
| 11:102795525:C:G | M236I | 0.991 |
| 11:102795525:C:T | M236I | 0.991 |
| 11:102795559:C:T | G225E | 0.991 |
| 11:102795576:T:A | E219D | 0.991 |
| 11:102795576:T:G | E219D | 0.991 |
dbSNP variants (sampled 300 via entrez): RS1000350191 (11:102796292 A>C), RS1000803147 (11:102791440 G>A), RS1000986045 (11:102792025 T>C), RS1001036252 (11:102797883 A>G), RS1001267121 (11:102793484 A>G), RS1001333506 (11:102792254 T>C), RS1001371280 (11:102798928 G>A,T), RS1001424911 (11:102798643 C>G), RS1001718338 (11:102793221 G>A), RS1001927369 (11:102798742 A>G), RS1002422733 (11:102792985 A>C), RS1002987656 (11:102794722 A>G), RS1003092169 (11:102799843 G>A), RS1003175954 (11:102794452 C>A,T), RS1003777678 (11:102790498 T>C)
Disease associations
OMIM: gene MIM:120353 | disease phenotypes: MIM:178500, MIM:226600, MIM:610504
GenCC curated gene-disease
Mondo (4): interstitial lung disease 2 (MONDO:0800497), recessive dystrophic epidermolysis bullosa (MONDO:0009179), COPD, severe early onset (MONDO:0011751), preterm premature rupture of the membranes (MONDO:0012511)
Orphanet (4): Idiopathic pulmonary fibrosis (Orphanet:2032), Acute interstitial pneumonia (Orphanet:79126), Autosomal recessive generalized dystrophic epidermolysis bullosa, severe form (Orphanet:79408), Recessive dystrophic epidermolysis bullosa inversa (Orphanet:79409)
HPO phenotypes
58 total (30 of 58 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0000079 | Abnormality of the urinary system |
| HP:0000083 | Renal insufficiency |
| HP:0000099 | Glomerulonephritis |
| HP:0000160 | Narrow mouth |
| HP:0000478 | Abnormality of the eye |
| HP:0000572 | Visual loss |
| HP:0000670 | Carious teeth |
| HP:0000716 | Depression |
| HP:0000739 | Anxiety |
| HP:0000794 | IgA deposition in the glomerulus |
| HP:0000823 | Delayed puberty |
| HP:0000938 | Osteopenia |
| HP:0000939 | Osteoporosis |
| HP:0000982 | Palmoplantar keratoderma |
| HP:0001030 | Fragile skin |
| HP:0001056 | Milia |
| HP:0001057 | Aplasia cutis congenita |
| HP:0001075 | Atrophic scars |
| HP:0001371 | Flexion contracture |
| HP:0001510 | Growth delay |
| HP:0001581 | Recurrent skin infections |
| HP:0001644 | Dilated cardiomyopathy |
| HP:0001798 | Anonychia |
| HP:0001891 | Iron deficiency anemia |
| HP:0001903 | Anemia |
| HP:0001917 | Renal amyloidosis |
| HP:0001965 | Abnormal scalp morphology |
| HP:0002015 | Dysphagia |
| HP:0002020 | Gastroesophageal reflux |
| HP:0002671 | Basal cell carcinoma |
GWAS associations
2 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST006585_1874 | Blood protein levels | 7.000000e-107 |
| GCST009731_49 | Blood protein levels in cardiovascular risk | 2.000000e-82 |
EFO canonical traits (1, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0008193 | interstitial collagenase measurement |
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| C563032 | Preterm Premature Rupture of the Membranes (supp.) |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (4): CHEMBL2095216 (PROTEIN FAMILY), CHEMBL2111422 (SELECTIVITY GROUP), CHEMBL332 (SINGLE PROTEIN), CHEMBL4523984 (SELECTIVITY GROUP)
Molecules with ChEMBL bioactivity
21 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 529,513 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL1200448 | TILUDRONATE DISODIUM | 4 | 5,476 |
| CHEMBL2 | PRAZOSIN | 4 | 31,107 |
| CHEMBL421 | SULFASALAZINE | 4 | 73,629 |
| CHEMBL481 | IRINOTECAN | 4 | 159,900 |
| CHEMBL56367 | NIMESULIDE | 4 | 25,455 |
| CHEMBL707 | DOXAZOSIN | 4 | 24,931 |
| CHEMBL145 | CAFFEIC ACID | 3 | 36,305 |
| CHEMBL279785 | MARIMASTAT | 3 | 29,447 |
| CHEMBL297453 | EPIGALOCATECHIN GALLATE | 3 | 22,804 |
| CHEMBL50 | QUERCETIN | 3 | 74,559 |
| CHEMBL75094 | PRINOMASTAT | 3 | 8,839 |
| CHEMBL115653 | CIPEMASTAT | 2 | 359 |
| CHEMBL19611 | ILOMASTAT | 2 | 12,065 |
| CHEMBL206815 | APRATASTAT | 2 | 256 |
| CHEMBL2107228 | SOLIMASTAT | 2 | 104 |
| CHEMBL261932 | TANOMASTAT | 2 | 1,980 |
| CHEMBL279786 | BATIMASTAT | 2 | 21,247 |
| CHEMBL368347 | (+)-SECOISOLARICIRESINOL | 2 | 91 |
| CHEMBL440498 | CTS-1027 | 2 | 615 |
| CHEMBL76222 | REBIMASTAT | 2 | 344 |
| CHEMBL87223 | AMINOQUINURIDE | 2 |
Clinical evidence (CIViC)
Drug × variant × indication: 1 predictive associations from 1 curated evidence items.
| Variant | Therapy | Indication | Effect | Level | CIViC |
|---|---|---|---|---|---|
| MMP1 Overexpression | Sacituzumab Govitecan | Estrogen-receptor Positive Breast Cancer | Resistance | CIViC D | EID12597 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB variants
2 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs2071230 | MMP1, MMP10 | 0.00 | 0 | ||
| rs7945189 | MMP1, MMP10 | 0.00 | 0 |
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — M10: Matrix metallopeptidase
Most potent curated ligand interactions (6 total), top 6:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| ilomastat | Inhibition | 9.25 | pIC50 |
| batimastat | Inhibition | 9.0 | pIC50 |
| cipemastat | Inhibition | 8.5 | pKi |
| marimastat | Inhibition | 8.3 | pIC50 |
| apratastat | Inhibition | 7.48 | pIC50 |
| CGS-27023A | Inhibition | 7.25 | pIC50 |
Binding affinities (BindingDB)
241 measured of 287 human assays (287 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| N-hydroxy-1-(2-methoxyethyl)-4-[(4-phenoxybenzene)sulfonyl]piperidine-4-carboxamide hydrochloride | KI | 0.1 nM | |
| 1-Cyclopropyl-N-hydroxy-4-{[4-(phenylthio)phenyl]-sulfonyl}piperidine-4-carboxamide Hydrochloride | KI | 0.1 nM | |
| N-hydroxy-2-methyl-2-[(4-phenoxybenzene)sulfonyl]propanamide | KI | 0.1 nM | |
| N-Hydroxy-4-{[4-(phenoxyphenyl]sulfonyl}-1- (2-propynyl)4-piperidinecarboxamide, Monohydrochloride | KI | 0.13 nM | |
| N-hydroxy-4-{[4-(phenylsulfanyl)benzene]sulfonyl}-1-(prop-2-en-1-yl)piperidine-4-carboxamide hydrochloride | KI | 0.15 nM | |
| piperidinyl glycine derivative, 24f | KI | 0.19 nM | |
| tert-Butyl 4-[(Hydroxyamino)carbonyl]-4-{[(4-phenoxyphenyl)sulfonyl]methyl}piperidine-1-carboxylate | KI | 0.2 nM | |
| N-hydroxy-1-[(3-methoxyphenyl)methyl]-4-{[(4-phenoxybenzene)sulfonyl]methyl}piperidine-4-carboxamide hydrochloride | KI | 0.2 nM | |
| tert-butyl 4-(hydroxycarbamoyl)-4-[(4-phenoxybenzene)sulfonyl]piperidine-1-carboxylate | KI | 0.2 nM | |
| 1-cyclopropyl-N-hydroxy-4-[(4-phenoxybenzene)sulfonyl]piperidine-4-carboxamide hydrochloride | KI | 0.2 nM | |
| N-hydroxy-4-[(4-phenoxybenzene)sulfonyl]piperidine-4-carboxamide | KI | 0.22 nM | |
| N-hydroxy-4-{[(4-phenoxybenzene)sulfonyl]methyl}-1-(prop-2-yn-1-yl)piperidine-4-carboxamide hydrochloride | KI | 0.25 nM | |
| N-Hydroxy-4-{[(4-phenoxyphenyl)sulfonyl]methyl}-1-(2-phenylethyl)piperidine-4-carboxamide Hydrochloride | KI | 0.3 nM | |
| N-hydroxy-1-methanesulfonyl-4-[(4-phenoxybenzene)sulfonyl]piperidine-4-carboxamide | KI | 0.3 nM | |
| N-hydroxy-1-(2-methoxyethyl)-4-{[4-(phenylsulfanyl)benzene]sulfonyl}piperidine-4-carboxamide hydrochloride | KI | 0.3 nM | |
| BOC-piperidinyl glycine derivative, 9 | IC50 | 0.3 nM | |
| N-hydroxy-4-{[4-(phenylsulfanyl)benzene]sulfonyl}-1-(prop-2-yn-1-yl)piperidine-4-carboxamide hydrochloride | KI | 0.33 nM | |
| (3R)-N-hydroxy-2-{[4-(4-methoxyphenyl)phenyl]methyl}-1,1-dioxo-1,2-thiazinane-3-carboxamide | KI | 0.4 nM | |
| alpha-tetrahydropyran beta-sulfone 1B | KI | 0.4 nM | |
| 1-acetyl-N-hydroxy-4-{[4-(phenylsulfanyl)benzene]sulfonyl}piperidine-4-carboxamide | KI | 0.4 nM | |
| piperidinyl glycine derivative, 24q | IC50 | 0.4 nM | |
| piperidinyl glycine derivative, 24u | IC50 | 0.4 nM | |
| N-Hydroxy-1-methyl-4-{[4-(phenylthio)phenyl]sulfonyl}-piperidine-4-carboxamide Hydrochloride | KI | 0.5 nM | |
| piperidinyl glycine derivative, 24t | IC50 | 0.5 nM | |
| Trocade | KI | 0.53 nM | |
| piperidinyl glycine derivative, 24d | IC50 | 0.6 nM | |
| piperidinyl glycine derivative, 24p | IC50 | 0.6 nM | |
| piperidinyl glycine derivative, 24s | IC50 | 0.6 nM | |
| N-Pentafluorophenylsulfonyl-N-4-nitrobenzyl-glycine hydroxamate | KI | 0.7 nM | |
| N-hydroxy-2-{(4-nitrophenyl)methylsulfonamido}propanamide | KI | 0.7 nM | |
| piperidinyl glycine derivative, 27c | IC50 | 0.7 nM | |
| piperidinyl glycine derivative, 27d | IC50 | 0.7 nM | |
| BOC-piperidinyl glycine derivative, 22a | IC50 | 0.75 nM | |
| 2-[benzyl(2,3,4,5,6-pentafluorobenzene)sulfonamido]-N-hydroxy-3-methylbutanamide | KI | 0.8 nM | |
| 2-[benzyl(2,3,4,5,6-pentafluorobenzene)sulfonamido]-N-hydroxy-4-methylpentanamide | KI | 0.8 nM | |
| N-hydroxy-2-{(2-nitrophenyl)methylsulfonamido}propanamide | KI | 0.8 nM | |
| 1-ethyl-N-hydroxy-4-{[4-(phenylsulfanyl)benzene]sulfonyl}piperidine-4-carboxamide hydrochloride | KI | 0.8 nM | |
| piperidinyl glycine derivative, 24g | IC50 | 0.8 nM | |
| piperidinyl glycine derivative, 24o | IC50 | 0.8 nM | |
| piperidinyl glycine derivative, 25c | IC50 | 0.8 nM | |
| 2-[benzyl(2,3,4,5,6-pentafluorobenzene)sulfonamido]-N-hydroxypropanamide | KI | 0.9 nM | |
| 4-({[4-(3,4-Dimethylphenoxy)phenyl]sulfonyl}methyl)-N-hydroxy-1-prop-2-ynylpiperidine-4-carboxamide Hydrochloride | KI | 0.9 nM | |
| piperidinyl glycine derivative, 24i | IC50 | 0.9 nM | |
| piperidinyl glycine derivative, 24r | IC50 | 0.9 nM | |
| piperidinyl glycine derivative, 26d | IC50 | 0.9 nM | |
| (3R)-N-hydroxy-1,1-dioxo-2-{[4-(pyridin-4-yl)phenyl]methyl}-1,2-thiazinane-3-carboxamide | KI | 1 nM | |
| piperidinyl glycine derivative, 24n | IC50 | 1 nM | |
| (R)-N4-Hydroxy-N1-[(S)-2-(1H-indol-3-yl)-1-methylcarbamoyl-ethyl]-2-isobutyl-succinamide | IC50 | 1 nM | US-9487462: Inhibitors of matrix metalloproteinases |
| piperidinyl glycine derivative, 27b | IC50 | 1.2 nM | |
| piperidinyl glycine derivative, 24a | IC50 | 1.3 nM |
ChEMBL bioactivities
2751 potent at pChembl≥5 of 3190 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 10.00 | Ki | 0.1 | nM | CHEMBL281795 |
| 10.00 | EC50 | 0.1 | nM | CHEMBL526566 |
| 9.70 | IC50 | 0.2 | nM | ILOMASTAT |
| 9.59 | IC50 | 0.26 | nM | CHEMBL321180 |
| 9.52 | Ki | 0.3 | nM | CIPEMASTAT |
| 9.52 | IC50 | 0.3 | nM | CHEMBL279078 |
| 9.40 | IC50 | 0.4 | nM | CHEMBL4088630 |
| 9.40 | Ki | 0.4 | nM | ILOMASTAT |
| 9.40 | IC50 | 0.4 | nM | ILOMASTAT |
| 9.40 | IC50 | 0.4 | nM | BATIMASTAT |
| 9.40 | IC50 | 0.4 | nM | CHEMBL141080 |
| 9.30 | Ki | 0.5 | nM | BATIMASTAT |
| 9.30 | IC50 | 0.5 | nM | ILOMASTAT |
| 9.30 | IC50 | 0.5 | nM | CHEMBL74670 |
| 9.30 | IC50 | 0.5 | nM | CHEMBL139886 |
| 9.25 | IC50 | 0.56 | nM | ILOMASTAT |
| 9.22 | Ki | 0.6 | nM | CHEMBL353382 |
| 9.22 | Ki | 0.6 | nM | CHEMBL433314 |
| 9.15 | Ki | 0.7 | nM | CHEMBL382705 |
| 9.15 | Ki | 0.7 | nM | CHEMBL208181 |
| 9.15 | Ki | 0.7 | nM | MARIMASTAT |
| 9.15 | IC50 | 0.7 | nM | CHEMBL140511 |
| 9.12 | IC50 | 0.75 | nM | BATIMASTAT |
| 9.11 | IC50 | 0.78 | nM | MARIMASTAT |
| 9.10 | IC50 | 0.8 | nM | CHEMBL140970 |
| 9.10 | EC50 | 0.8 | nM | CHEMBL526106 |
| 9.06 | IC50 | 0.88 | nM | CHEMBL144611 |
| 9.06 | Ki | 0.87 | nM | CHEMBL417537 |
| 9.01 | Ki | 0.97 | nM | CHEMBL172885 |
| 9.00 | Ki | 1 | nM | CHEMBL30980 |
| 9.00 | IC50 | 0.99 | nM | BATIMASTAT |
| 9.00 | IC50 | 1 | nM | CHEMBL207776 |
| 9.00 | Ki | 1 | nM | CHEMBL72511 |
| 9.00 | Ki | 1 | nM | CHEMBL324947 |
| 9.00 | Ki | 1 | nM | CHEMBL114458 |
| 9.00 | Ki | 1 | nM | CHEMBL389020 |
| 9.00 | IC50 | 1 | nM | MARIMASTAT |
| 9.00 | IC50 | 1 | nM | CHEMBL73763 |
| 9.00 | IC50 | 1 | nM | CHEMBL344633 |
| 9.00 | IC50 | 1 | nM | CHEMBL337594 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL144843 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL432991 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL4785595 |
| 8.96 | Ki | 1.1 | nM | CHEMBL72511 |
| 8.96 | Ki | 1.1 | nM | MARIMASTAT |
| 8.96 | IC50 | 1.1 | nM | MARIMASTAT |
| 8.92 | IC50 | 1.2 | nM | CHEMBL344759 |
| 8.92 | Ki | 1.2 | nM | CHEMBL45631 |
| 8.92 | IC50 | 1.2 | nM | CHEMBL6572 |
| 8.92 | IC50 | 1.2 | nM | BATIMASTAT |
PubChem BioAssay actives
2553 with measured affinity, of 5328 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 |
|---|---|---|---|---|
| N,6-dihydroxy-2-(4-nitrophenyl)sulfonyl-3,4-dihydro-1H-isoquinoline-1-carboxamide | 731524: Inhibition of MMP1 (unknown origin) | ic50 | <0.0001 | uM |
| [(8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl] N-(2,2-dimethylpropyl)carbamate | 362585: Inhibition of glucocorticoid-mediated human MMP1 expression in PMA stimulated A549 cells assessed as MMP1 protein level by ELISA | ec50 | 0.0001 | uM |
| (2R)-N’-hydroxy-N-[(2S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl]-2-(2-methylpropyl)butanediamide | 628300: Inhibition of MMP1 | ic50 | 0.0002 | uM |
| (2S,3R)-N-hydroxy-2-methyl-N’-[(2S)-1-(methylamino)-1-oxo-3-(5,6,7,8-tetrahydronaphthalen-1-yl)propan-2-yl]-3-(2-methylpropyl)butanediamide | 108731: Activity against Matrix metalloprotease-1 (MMP-1). | ic50 | 0.0003 | uM |
| (2S,3R)-N,2-dihydroxy-N’-[(2S)-1-(1H-indol-3-yl)-3,3-dimethyl-1-oxobutan-2-yl]-3-(2-methylpropyl)butanediamide | 104923: In vitro inhibitory activity against matrix metalloprotease 1 isolated from the culture medium of human skin fibroblasts induced with PMA | ic50 | 0.0003 | uM |
| (2R,3R)-3-(cyclopentylmethyl)-N-hydroxy-4-oxo-4-piperidin-1-yl-2-[(3,4,4-trimethyl-2,5-dioxoimidazolidin-1-yl)methyl]butanamide | 264663: Binding affinity to recombinant MMP1 | ki | 0.0003 | uM |
| (3S)-N-hydroxy-4-(4-methoxyphenyl)sulfonyl-2,2-dimethylthiomorpholine-3-carboxamide | 108733: In vitro inhibitory activity against truncated collagenase-1 (matrix metalloprotease-1). | ic50 | 0.0004 | uM |
| N-hydroxy-4-(4-methoxyphenyl)sulfonyl-2,2-dimethylthiomorpholine-3-carboxamide | 1454754: Inhibition of human interstitial recombinant N-terminal MMP1 expressed in Escherichia coli BL21(DE3) using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 as substrate after 20 to 30 mins by spectrofluorimetric analysis | ic50 | 0.0004 | uM |
| (2S,3R)-N-hydroxy-N’-[(2S)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl]-3-(2-methylpropyl)-2-(thiophen-2-ylsulfanylmethyl)butanediamide | 108731: Activity against Matrix metalloprotease-1 (MMP-1). | ic50 | 0.0004 | uM |
| (3S)-4-(4-bromo-2-methylphenyl)sulfonyl-N-hydroxy-2,2-dimethyl-1,4-thiazepane-3-carboxamide | 108733: In vitro inhibitory activity against truncated collagenase-1 (matrix metalloprotease-1). | ic50 | 0.0005 | uM |
| (2R,3R)-N-[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-N’-hydroxy-3-(hydroxymethyl)-2-(2-methylpropyl)butanediamide | 109221: Inhibitory potency against Matrix metalloprotease-1 (MMP-1) | ki | 0.0006 | uM |
| (2R,3R)-N,2-dihydroxy-N’-[(2S)-3-(4-methoxyphenyl)-1-(methylamino)-1-oxopropan-2-yl]-2-methyl-3-(2-methylpropyl)butanediamide | 104557: Binding affinity was evaluated against matrix metalloprotease-1 | ki | 0.0006 | uM |
| (3S)-4-(4-bromophenyl)sulfonyl-N-hydroxy-2,2-dimethyl-1,4-thiazepane-3-carboxamide | 108733: In vitro inhibitory activity against truncated collagenase-1 (matrix metalloprotease-1). | ic50 | 0.0007 | uM |
| (2S)-1-[(2S,3S)-2-(4-chlorophenyl)-3-(hydroxycarbamoyl)pentanoyl]-N-methylpiperidine-2-carboxamide | 264663: Binding affinity to recombinant MMP1 | ki | 0.0007 | uM |
| (2R,3S)-N-[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-N’,3-dihydroxy-2-(2-methylpropyl)butanediamide | 109221: Inhibitory potency against Matrix metalloprotease-1 (MMP-1) | ki | 0.0007 | uM |
| (2S,3R)-N-[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-N’-hydroxy-2-(4-methoxyphenyl)-3-[(3,4,4-trimethyl-2,5-dioxoimidazolidin-1-yl)methyl]butanediamide | 264663: Binding affinity to recombinant MMP1 | ki | 0.0007 | uM |
| [(8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl] N-butan-2-ylcarbamate | 362585: Inhibition of glucocorticoid-mediated human MMP1 expression in PMA stimulated A549 cells assessed as MMP1 protein level by ELISA | ec50 | 0.0008 | uM |
| (3S)-N-hydroxy-4-(4-methoxyphenyl)sulfonyl-2,2-dimethyl-1,4-thiazepane-3-carboxamide | 108733: In vitro inhibitory activity against truncated collagenase-1 (matrix metalloprotease-1). | ic50 | 0.0008 | uM |
| (2S,3R)-N-hydroxy-N’-[(2R)-3-(4-methoxyphenyl)-1-(methylamino)-1-oxopropan-2-yl]-2-methyl-3-(2-methylpropyl)butanediamide | 109228: Inhibition of MMP-1 (Matrix metalloprotease-1) | ki | 0.0009 | uM |
| (2R,3S)-N-[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-N’-hydroxy-3-[(1-methyl-2-oxoquinolin-6-yl)methoxy]-2-(2-methylpropyl)butanediamide | 108749: Inhibitory activity against MMP-1 (Matrix metalloprotease-1) | ic50 | 0.0009 | uM |
| (2R)-N-[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-N’-hydroxy-2-[4-(4-methoxyphenoxy)butyl]butanediamide | 52368: Inhibitory potency against human fibroblast collagenase, MMP-1 | ki | 0.0010 | uM |
| (2S,11S,12R)-11-N-hydroxy-2-N-methyl-7-(1-methylimidazol-4-yl)sulfonyl-12-(2-methylpropyl)-13-oxo-1,7-diazacyclotridecane-2,11-dicarboxamide | 104564: Inhibition of MMP-1 (human fibroblast collagenase) | ki | 0.0010 | uM |
| (3R)-6-cyclohexyl-N-hydroxy-3-[3-(methanesulfonamidomethyl)-1,2,4-oxadiazol-5-yl]hexanamide | 349373: Inhibition of MMP1 | ki | 0.0010 | uM |
| (6S)-N-hydroxy-7-(4-methoxyphenyl)sulfonyl-5,5-dimethyl-1,4,7-oxathiazonane-6-carboxamide | 108733: In vitro inhibitory activity against truncated collagenase-1 (matrix metalloprotease-1). | ic50 | 0.0010 | uM |
| (3S)-N-hydroxy-2,2-dimethyl-4-(5-pyridin-2-ylthiophen-2-yl)sulfonyl-1,4-thiazepane-3-carboxamide | 108733: In vitro inhibitory activity against truncated collagenase-1 (matrix metalloprotease-1). | ic50 | 0.0010 | uM |
| (8S,11R,12S)-12-N-hydroxy-8-N-methyl-11-(2-methylpropyl)-2,10-dioxo-1-oxa-3,9-diazacyclopentadecane-8,12-dicarboxamide | 108935: In vitro inhibition of human MMP-1. | ki | 0.0010 | uM |
| (2S,11S,12R)-11-N-hydroxy-2-N-methyl-12-(2-methylpropyl)-13-oxo-1,7-diazacyclotridecane-2,11-dicarboxamide | 108935: In vitro inhibition of human MMP-1. | ki | 0.0010 | uM |
| tert-butyl (6S,9R,10S)-10-(hydroxycarbamoyl)-6-(methylcarbamoyl)-9-(2-methylpropyl)-8-oxo-1,7-diazacyclotridecane-1-carboxylate | 104564: Inhibition of MMP-1 (human fibroblast collagenase) | ki | 0.0010 | uM |
| (7S,8R,11S)-7-N-hydroxy-11-N-methyl-8-(2-methylpropyl)-9-oxo-6-oxa-1,10-diazatricyclo[11.6.1.014,19]icosa-13(20),14,16,18-tetraene-7,11-dicarboxamide | 108935: In vitro inhibition of human MMP-1. | ki | 0.0010 | uM |
| (4R,7R,8S)-8-N-hydroxy-4-N-methyl-7-(2-methylpropyl)-6,11-dioxo-9-oxa-2-thia-5,12-diazabicyclo[11.4.0]heptadeca-1(17),13,15-triene-4,8-dicarboxamide | 108935: In vitro inhibition of human MMP-1. | ki | 0.0010 | uM |
| (2S,11S,12R)-7-(benzenesulfonyl)-11-N-hydroxy-2-N-methyl-12-(2-methylpropyl)-13-oxo-1,7-diazacyclotridecane-2,11-dicarboxamide | 104564: Inhibition of MMP-1 (human fibroblast collagenase) | ki | 0.0010 | uM |
| (9S,12R,13S)-13-N-hydroxy-9-N,4-dimethyl-12-(2-methylpropyl)-3,11-dioxo-1-oxa-4,10-diazacyclotridecane-9,13-dicarboxamide | 108935: In vitro inhibition of human MMP-1. | ki | 0.0010 | uM |
| (8S,11R,12S)-12-N-hydroxy-8-N,3-dimethyl-11-(2-methylpropyl)-2,10-dioxo-1-oxa-3,9-diazacyclopentadecane-8,12-dicarboxamide | 108935: In vitro inhibition of human MMP-1. | ki | 0.0010 | uM |
| (2R)-N’-hydroxy-N-[(2S)-3-(4-methoxyphenyl)-1-(methylamino)-1-oxopropan-2-yl]-2-(2-methylpropyl)butanediamide | 108923: Inhibition of matrix metalloprotease-1 | ki | 0.0010 | uM |
| (3S)-N-hydroxy-2,2-dimethyl-4-(4-prop-2-ynoxyphenyl)sulfonylthiomorpholine-3-carboxamide | 261911: Inhibition of MMP1 | ic50 | 0.0010 | uM |
| (3S)-N-hydroxy-6-(methoxymethoxy)-4-(4-methoxyphenyl)sulfonyl-2,2-dimethyl-1,4-thiazepane-3-carboxamide | 108733: In vitro inhibitory activity against truncated collagenase-1 (matrix metalloprotease-1). | ic50 | 0.0010 | uM |
| 2-[ethoxy-(4-fluorophenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 108920: Inhibitory activity against matrix metalloprotease-1 (MMP-1)(recombinant human collagenase-1). | ki | 0.0010 | uM |
| (2S,11S,12R)-7-(4-aminophenyl)sulfonyl-11-N-hydroxy-2-N-methyl-12-(2-methylpropyl)-13-oxo-1,7-diazacyclotridecane-2,11-dicarboxamide | 104564: Inhibition of MMP-1 (human fibroblast collagenase) | ki | 0.0010 | uM |
| (2S,11S,12R)-11-N-hydroxy-2-N-methyl-12-(2-methylpropyl)-13-oxo-1,7-diazacyclotridecane-2,11-dicarboxamide;hydrochloride | 104564: Inhibition of MMP-1 (human fibroblast collagenase) | ki | 0.0010 | uM |
| (2S,3R)-N-[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-N’-hydroxy-3-(hydroxymethyl)-2-(4-methoxyphenyl)butanediamide | 264663: Binding affinity to recombinant MMP1 | ki | 0.0010 | uM |
| (2R,3S)-N-[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-N’-hydroxy-2-(2-methylpropyl)-3-(quinolin-8-ylsulfonylamino)butanediamide | 108749: Inhibitory activity against MMP-1 (Matrix metalloprotease-1) | ic50 | 0.0011 | uM |
| (2S,3R)-N-hydroxy-N’-[(2S)-1-(1H-indol-3-yl)-1-oxo-3-phenylpropan-2-yl]-3-(2-methylpropyl)-2-prop-2-enylbutanediamide | 104923: In vitro inhibitory activity against matrix metalloprotease 1 isolated from the culture medium of human skin fibroblasts induced with PMA | ic50 | 0.0011 | uM |
| (2R,3S)-N-[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-N’-hydroxy-2-(2-methylpropyl)-3-prop-2-enylbutanediamide | 1727020: Inhibition of PMA-induced human skin fibroblast derived MMP1 by fluorometric assay | ic50 | 0.0011 | uM |
| (3R,9aS)-N-hydroxy-2-(4-methoxyphenyl)sulfonyl-5-oxo-3,4,7,8,9,9a-hexahydro-1H-pyrrolo[1,2-a][1,4]diazepine-3-carboxamide | 108752: Inhibition of human Matrix metalloprotease-1 | ic50 | 0.0012 | uM |
| (2R,3S)-N-[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-N’-hydroxy-2-(2-methylpropyl)-3-(quinolin-6-ylsulfonylamino)butanediamide | 108749: Inhibitory activity against MMP-1 (Matrix metalloprotease-1) | ic50 | 0.0012 | uM |
| (3S)-4-(4-bromophenyl)sulfonyl-N-hydroxy-2,2-dimethyl-1,1-dioxo-1,4-thiazepane-3-carboxamide | 108733: In vitro inhibitory activity against truncated collagenase-1 (matrix metalloprotease-1). | ic50 | 0.0012 | uM |
| (6S,7R,10S)-6-N-hydroxy-10-N-methyl-7-(2-methylpropyl)-8-oxo-2-oxa-9-azabicyclo[10.2.2]hexadeca-1(14),12,15-triene-6,10-dicarboxamide | 108935: In vitro inhibition of human MMP-1. | ki | 0.0012 | uM |
| (2S,3R)-N-hydroxy-N’-[(2S)-1-(1H-indol-3-yl)-3,3-dimethyl-1-oxobutan-2-yl]-3-(2-methylpropyl)-2-prop-2-enylbutanediamide | 104923: In vitro inhibitory activity against matrix metalloprotease 1 isolated from the culture medium of human skin fibroblasts induced with PMA | ic50 | 0.0012 | uM |
| (2R,3S)-N-[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-N’-hydroxy-2-(2-methylpropyl)-3-[(4-oxo-3H-quinazolin-6-yl)sulfonylamino]butanediamide | 108749: Inhibitory activity against MMP-1 (Matrix metalloprotease-1) | ic50 | 0.0013 | uM |
| (2S,3R)-N-hydroxy-2-methyl-N’-[(2S)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl]-3-(2-methylpropyl)butanediamide | 108735: Inhibition of matrix metalloprotease-1 (MMP-1) | ic50 | 0.0013 | uM |
CTD chemical–gene interactions
315 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Particulate Matter | affects response to substance, affects binding, decreases reaction, increases expression, affects reaction (+6 more) | 25 |
| sodium arsenite | increases reaction, affects expression, decreases expression, affects cotreatment, increases abundance (+1 more) | 14 |
| Tobacco Smoke Pollution | decreases reaction, increases expression, affects reaction, affects expression, decreases secretion (+1 more) | 13 |
| Tetrachlorodibenzodioxin | affects reaction, affects binding, decreases reaction, increases expression, increases activity (+1 more) | 12 |
| 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one | decreases activity, decreases expression, decreases reaction, increases activity, increases expression (+1 more) | 9 |
| Estradiol | decreases reaction, increases expression, affects cotreatment, decreases expression, affects binding (+1 more) | 8 |
| Vehicle Emissions | increases expression, increases secretion, affects reaction, increases reaction, decreases reaction (+3 more) | 7 |
| Benzo(a)pyrene | affects methylation, increases expression | 6 |
| Lipopolysaccharides | affects response to substance, affects cotreatment, decreases expression, increases reaction, decreases reaction (+3 more) | 6 |
| U 0126 | decreases reaction, increases expression, increases secretion, decreases expression, increases reaction | 5 |
| (+)-JQ1 compound | affects cotreatment, decreases expression | 5 |
| Acetylcysteine | decreases reaction, increases abundance, increases activity, increases expression | 5 |
| Air Pollutants | increases abundance, increases expression, decreases expression, increases secretion, decreases reaction | 5 |
| Hydrogen Peroxide | affects expression, decreases expression, decreases reaction, increases expression | 5 |
| Quercetin | decreases expression, decreases reaction, increases expression, increases secretion | 5 |
| Silicon Dioxide | increases expression, increases reaction | 5 |
| cobaltiprotoporphyrin | decreases expression, increases reaction, decreases reaction, increases expression | 4 |
| Resveratrol | decreases reaction, increases activity, increases expression, increases secretion | 4 |
| Plant Extracts | increases abundance, decreases reaction, increases expression, decreases expression | 4 |
| Smoke | decreases nitrosation, increases expression, increases secretion | 4 |
| Tetradecanoylphorbol Acetate | increases expression, increases reaction, decreases reaction | 4 |
| Cyclosporine | increases expression, decreases expression | 4 |
| Cadmium Chloride | decreases expression, decreases reaction, increases expression, increases secretion | 4 |
| Simvastatin | decreases secretion, decreases reaction, increases expression, increases secretion, decreases expression | 4 |
| 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one | decreases reaction, increases expression, increases secretion, increases reaction | 3 |
| SB 203580 | decreases reaction, increases activity, increases expression | 3 |
| pyrazolanthrone | decreases reaction, increases activity, increases expression | 3 |
| 2,2’,4,4’-tetrabromodiphenyl ether | increases expression, increases secretion | 3 |
| Arsenic Trioxide | decreases expression, increases secretion, affects cotreatment, decreases activity, decreases secretion (+3 more) | 3 |
| Dexamethasone | decreases reaction, increases expression, decreases expression, decreases secretion | 3 |
ChEMBL screening assays
588 unique, capped per target: 574 binding, 10 admet, 3 functional, 1 toxicity
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL4481593 | Binding | Inhibition of collagenase (unknown origin) at 200 uM relative to control | Deleting a Chromatin Remodeling Gene Increases the Diversity of Secondary Metabolites Produced by Colletotrichum higginsianum. — J Nat Prod |
| CHEMBL663111 | Functional | In vitro antagonist activity against collagenase induced gel-filtered platelet (GFP) aggregation at 50 uM; NA=Inactive | Discovery and optimization of a novel series of thrombin receptor (par-1) antagonists: potent, selective peptide mimetics based on indole and indazole templates. — J Med Chem |
| CHEMBL3868398 | ADMET | Inhibition of recombinant human AMPA-activated MMP1 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method | Design, synthesis, and biological activity of novel, potent, and highly selective fused pyrimidine-2-carboxamide-4-one-based matrix metalloproteinase (MMP)-13 zinc-binding inhibitors. — Bioorg Med Chem |
Cellosaurus cell lines
6 cell lines: 5 cancer cell line, 1 spontaneously immortalized cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_AB52 | BHK-MMP1 | Spontaneously immortalized cell line | Male |
| CVCL_B8KL | Abcam HCT 116 MMP1 KO | Cancer cell line | Male |
| CVCL_B8YX | Abcam MCF-7 MMP1 KO | Cancer cell line | Female |
| CVCL_B9MU | Abcam A-549 MMP1 KO | Cancer cell line | Male |
| CVCL_E0I7 | Ubigene HeLa MMP1 KO | Cancer cell line | Female |
| CVCL_F1P4 | HyCyte HCT 116 KO-hMMP1 | Cancer cell line | Male |
Clinical trials (associated diseases)
300 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00106821 | PHASE4 | COMPLETED | Efficacy of Tiotropium in Patients of African Descent With Chronic Obstructive Pulmonary Disease |
| NCT00115492 | PHASE4 | COMPLETED | Advair® DISKUS® Versus Serevent® DISKUS® For Chronic Obstructive Pulmonary Disease Exacerbations |
| NCT00132860 | PHASE4 | UNKNOWN | Prophylactic Antibiotic Treatment of Patients With Chronic Obstructive Lung Disease (COLD) |
| NCT00139932 | PHASE4 | COMPLETED | Tiotropium Bromide Alone vs Tiotropium Bromide and Formoterol Fumarate in Subjects With COPD (Study P04272) |
| NCT00144196 | PHASE4 | COMPLETED | 12 Week Efficacy of Tiotropium Versus Placebo in Patients With Mild COPD According to Swedish Guidelines (SPIRIMILD) |
| NCT00144911 | PHASE4 | COMPLETED | ADVAIR® DISKUS® Inhaler (Fluticasone Propionate/Salmeterol) Versus SEREVENT® DISKUS® Inhaler (Salmeterol) For The Treatment Of Chronic Obstructive Pulmonary Disease Exacerbations. ADVAIR® DISKUS® Inhaler and SEREVENT® DISKUS® Inhaler Are Trademarks of the GSK Group of Companies. |
| NCT00152984 | PHASE4 | COMPLETED | Efficacy and Safety of Tiotropium in Patients With COPD and Concomitant Diagnosis of Asthma |
| NCT00153075 | PHASE4 | COMPLETED | Flow Rate Effect Respimat Inhaler Versus a Metered Dose Inhaler Using Berodual in Patients With Chronic Obstructive Pulmonary Disease (COPD) |
| NCT00181207 | PHASE4 | COMPLETED | Airway Clearance for Prevention of Chronic Obstructive Pulmonary Disease (COPD) Exacerbation |
| NCT00184977 | PHASE4 | COMPLETED | COPD on Primary Care Treatment (COOPT) |
| NCT00239408 | PHASE4 | COMPLETED | Spiriva (Tiotropium Bromide) Assessment of FEV1 - (SAFE-Portugal). |
| NCT00239421 | PHASE4 | COMPLETED | A Six-week Study Comparing the Efficacy and Safety of Tiotropium Plus Formoterol to Salmeterol Plus Fluticasone in Chronic Obstructive Pulmonary Disease (COPD) |
| NCT00239499 | PHASE4 | COMPLETED | Pilot Study Comparing Tiotropium (Spiriva) to Salmeterol (Serevent) Plus Fluticasone (Flixotide) in Chronic Obstructive Pulmonary Disease (COPD) |
| NCT00267917 | PHASE4 | COMPLETED | Evaluation of the Respimat Inhaler vs. a HFA MDI Using Berodual in Patients With COPD With Poor MDI Technique. |
| NCT00274079 | PHASE4 | COMPLETED | SPIRIVA in Ususal Care |
| NCT00291460 | PHASE4 | UNKNOWN | Inspiratory Muscle Training in Hypercapnic COPD |
| NCT00346749 | PHASE4 | TERMINATED | ADVAIR DISKUS® (Fluticasone Propionate/Salmeterol) Inhaler Versus SEREVENT DISKUS® (Salmeterol) Inhlaer On Inflammatory Cells And Markers In Chronic Obstructive Pulmonary Disease. ADVAIR DISKUS® and SEREVENT DISKUS® Inhalers Are Trademarks of the GSK Group of Companies. |
| NCT00351676 | PHASE4 | COMPLETED | Capturing Outcomes of Clinical Activities Performed by a Rounding Pharmacist Practising in a Team Environment |
| NCT00355342 | PHASE4 | COMPLETED | Bone Mineral Density Study In Patients With Chronic Obstructive Pulmonary Disease. DISKUS® Inhaler is a Trademark of the GSK Group of Companies. |
| NCT00358358 | PHASE4 | COMPLETED | Chronic Obstructive Pulmonary Disease Endpoints Study |
| NCT00359788 | PHASE4 | COMPLETED | A Trial Comparing Treatment With Tiotropium Inhalation Capsules to Combivent Inhalation Aerosol in COPD Patients. |
| NCT00361959 | PHASE4 | COMPLETED | SERETIDE 50/500mcg Versus Tiotropium Bromide On Exacerbation Rates In Severe Chronic Obstructive Pulmonary Disease |
| NCT00388882 | PHASE4 | COMPLETED | Trial Comparing Treatment With Tiotropium Inhalation Capsules to Combivent® Inhalation Aerosol in COPD Patients. |
| NCT00394485 | PHASE4 | TERMINATED | Tiotropium + Procaterol vs Tiotropium + Placebo in COPD Patients |
| NCT00412204 | PHASE4 | COMPLETED | Study to Evaluate the Effects of Tiotropium Bromide on Chronic Obstructive Pulmonary Disease (COPD) During Exercise |
| NCT00440245 | PHASE4 | COMPLETED | Bronchoprotection of Salbutamol in Asthma and Chronic Obstructive Pulmonary Disease |
| NCT00523991 | PHASE4 | COMPLETED | Trial Comparing Tiotropium Inhalation Capsules vs Placebo in Chronic Obstructive Pulmonary Disease (COPD). |
| NCT00525512 | PHASE4 | COMPLETED | Tiotropium In Exercise |
| NCT00527826 | PHASE4 | COMPLETED | Influence Of Salmeterol Xinafoate/Fluticasone Propionate (50/500 µg BID) On The Course Of The Disease And Exacerbation Frequency In COPD Patients Gold Stage III And IV |
| NCT00530842 | PHASE4 | COMPLETED | Effect of Tiotropium Plus Salmeterol vs. Fluticasone/Salmeterol on Static Lung Volumes and Exercise Endurance in COPD |
| NCT00563381 | PHASE4 | COMPLETED | Tiotropium Once Daily 18 Mcg Versus Salmeterol Twice Daily 50 Mcg on Time to First Exacerbation in COPD Patients. |
| NCT00569270 | PHASE4 | COMPLETED | Dynamic Hyperinflation and Tiotropium |
| NCT00578968 | PHASE4 | COMPLETED | Cardiac Limitations in Chronic Obstructive Pulmonary Disease: Benefits of Bronchodilation |
| NCT00592033 | PHASE4 | COMPLETED | Effect of Oxygen in Normoxaemic COPD Patients Who Desaturate During Exercise |
| NCT00633217 | PHASE4 | COMPLETED | Advair HFA For Chronic Obstructive Pulmonary Disease(COPD) |
| NCT00633776 | PHASE4 | WITHDRAWN | Perforomist Versus Foradil Evaluated by Inspiratory Capacity and High Resolution Computed Tomography (HRCT) |
| NCT00667797 | PHASE4 | COMPLETED | Costs & Outcomes of Hospitalization/Treatment With Levalbuterol & Albuterol in Asthma or Chronic Obstructive Pulmonary Disease (COPD) Subjects |
| NCT00680056 | PHASE4 | COMPLETED | Add-on Effects of Tiotropium Over Formoterol in Exercise Tolerance on Chronic Obstructive Pulmonary Disease Patients |
| NCT00680641 | PHASE4 | UNKNOWN | Simvastatin in Chronic Obstructive Pulmonary Disease (COPD) |
| NCT00720226 | PHASE4 | COMPLETED | Efficacy of Losartan in Preventing Progression of COPD |
Related Atlas pages
- Associated diseases: estrogen-receptor positive breast cancer
- Biomarker drugs (CIViC) (drugs whose response is associated with variants in this gene — CIViC predictive evidence, not targeting): Sacituzumab Govitecan
- Targeted by drugs: Marimastat
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): COPD, severe early onset, estrogen-receptor positive breast cancer, interstitial lung disease 2, preterm premature rupture of the membranes, recessive dystrophic epidermolysis bullosa