ADAM9
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Also known as MDC9KIAA0021MCMPMltng
Summary
ADAM9 (ADAM metallopeptidase domain 9, HGNC:216) is a protein-coding gene on chromosome 8p11.22, encoding Disintegrin and metalloproteinase domain-containing protein 9 (Q13443). Metalloprotease that cleaves and releases a number of molecules with important roles in tumorigenesis and angiogenesis, such as TEK, KDR, EPHB4, CD40, VCAM1 and CDH5.
This gene encodes a member of the ADAM (a disintegrin and metalloprotease domain) family. Members of this family are membrane-anchored proteins structurally related to snake venom disintegrins, and have been implicated in a variety of biological processes involving cell-cell and cell-matrix interactions, including fertilization, muscle development, and neurogenesis. The protein encoded by this gene interacts with SH3 domain-containing proteins, binds mitotic arrest deficient 2 beta protein, and is also involved in TPA-induced ectodomain shedding of membrane-anchored heparin-binding EGF-like growth factor. Several alternatively spliced transcript variants have been identified for this gene.
Source: NCBI Gene 8754 — RefSeq curated summary.
At a glance
- Gene–disease (curated): ADAM9-related retinopathy (Definitive, ClinGen) — +2 more curated relationships
- GWAS associations: 1
- Clinical variants (ClinVar): 599 total — 23 pathogenic, 9 likely-pathogenic
- Phenotypes (HPO): 17
- Druggable target: yes — 3 molecules with ChEMBL bioactivity
- Dosage sensitivity (ClinGen): haploinsufficiency autosomal recessive, triplosensitivity no evidence
- MANE Select transcript:
NM_003816
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:216 |
| Approved symbol | ADAM9 |
| Name | ADAM metallopeptidase domain 9 |
| Location | 8p11.22 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | MDC9, KIAA0021, MCMP, Mltng |
| Ensembl gene | ENSG00000168615 |
| Ensembl biotype | protein_coding |
| OMIM | 602713 |
| Entrez | 8754 |
Gene structure
Transcript identifiers
Ensembl transcripts: 33 — 15 nonsense_mediated_decay, 13 protein_coding, 4 retained_intron, 1 protein_coding_CDS_not_defined
ENST00000379917, ENST00000463437, ENST00000466936, ENST00000468065, ENST00000481058, ENST00000481513, ENST00000481873, ENST00000484143, ENST00000487273, ENST00000676489, ENST00000676617, ENST00000676643, ENST00000676669, ENST00000676765, ENST00000676919, ENST00000676936, ENST00000677004, ENST00000677137, ENST00000677165, ENST00000677359, ENST00000677582, ENST00000677908, ENST00000678253, ENST00000678474, ENST00000678540, ENST00000678730, ENST00000678863, ENST00000679268, ENST00000893524, ENST00000893525, ENST00000893526, ENST00000893527, ENST00000966952
RefSeq mRNA: 1 — MANE Select: NM_003816
NM_003816
CCDS: CCDS6112
Canonical transcript exons
ENST00000487273 — 22 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001129032 | 39082641 | 39082721 |
| ENSE00001129038 | 39071298 | 39071403 |
| ENSE00001129046 | 39055577 | 39055772 |
| ENSE00001155308 | 39026677 | 39026810 |
| ENSE00001155318 | 39025803 | 39025884 |
| ENSE00001155326 | 39023156 | 39023325 |
| ENSE00001155336 | 39021643 | 39021714 |
| ENSE00001155346 | 39017219 | 39017414 |
| ENSE00001155353 | 39016118 | 39016194 |
| ENSE00001157032 | 39041946 | 39042117 |
| ENSE00001196585 | 39082968 | 39083073 |
| ENSE00001274312 | 39054481 | 39054573 |
| ENSE00001274364 | 39013965 | 39014043 |
| ENSE00001274374 | 39011658 | 39011716 |
| ENSE00001274383 | 39007886 | 39007983 |
| ENSE00001882322 | 39103607 | 39105261 |
| ENSE00003467627 | 39091259 | 39091346 |
| ENSE00003476366 | 39101863 | 39101930 |
| ENSE00003610635 | 39077228 | 39077411 |
| ENSE00003642615 | 39090047 | 39090188 |
| ENSE00003644662 | 39018853 | 39018918 |
| ENSE00003845718 | 38996973 | 38997160 |
Expression profiles
Bgee: expression breadth ubiquitous, 215 present calls, max score 98.35.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 79.1277 / max 1133.3668, expressed in 1819 samples.
FANTOM5 promoters (5 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 88571 | 71.7903 | 1795 |
| 88569 | 3.8523 | 1255 |
| 88568 | 2.3438 | 1262 |
| 88570 | 0.9863 | 617 |
| 88575 | 0.1551 | 67 |
Top tissues by expression
237 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| stromal cell of endometrium | CL:0002255 | 98.35 | gold quality |
| islet of Langerhans | UBERON:0000006 | 97.59 | gold quality |
| gall bladder | UBERON:0002110 | 96.99 | gold quality |
| smooth muscle tissue | UBERON:0001135 | 96.42 | gold quality |
| right lung | UBERON:0002167 | 96.29 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 95.62 | gold quality |
| thoracic aorta | UBERON:0001515 | 95.33 | gold quality |
| calcaneal tendon | UBERON:0003701 | 95.33 | gold quality |
| ascending aorta | UBERON:0001496 | 95.29 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 95.18 | gold quality |
| rectum | UBERON:0001052 | 95.09 | gold quality |
| right coronary artery | UBERON:0001625 | 94.98 | gold quality |
| minor salivary gland | UBERON:0001830 | 94.96 | gold quality |
| vermiform appendix | UBERON:0001154 | 94.45 | gold quality |
| upper lobe of lung | UBERON:0008948 | 94.42 | gold quality |
| body of stomach | UBERON:0001161 | 94.34 | gold quality |
| left coronary artery | UBERON:0001626 | 94.26 | gold quality |
| aorta | UBERON:0000947 | 94.25 | gold quality |
| popliteal artery | UBERON:0002250 | 93.85 | gold quality |
| tibial artery | UBERON:0007610 | 93.85 | gold quality |
| adrenal tissue | UBERON:0018303 | 93.79 | gold quality |
| ventricular zone | UBERON:0003053 | 93.63 | gold quality |
| tendon | UBERON:0000043 | 93.03 | gold quality |
| colonic epithelium | UBERON:0000397 | 93.02 | gold quality |
| buccal mucosa cell | CL:0002336 | 92.65 | gold quality |
| stomach | UBERON:0000945 | 92.41 | gold quality |
| left adrenal gland | UBERON:0001234 | 92.40 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 92.31 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 92.19 | gold quality |
| heart left ventricle | UBERON:0002084 | 92.17 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 2.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-HCAD-13 | yes | 11.53 |
| E-ANND-3 | yes | 7.52 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): AR
miRNA regulators (miRDB)
157 targeting ADAM9, 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-126-5P | 100.00 | 72.71 | 3180 |
| HSA-MIR-30A-5P | 100.00 | 76.31 | 3233 |
| HSA-MIR-30B-5P | 100.00 | 76.29 | 3248 |
| HSA-MIR-30C-5P | 100.00 | 76.29 | 3248 |
| HSA-MIR-30D-5P | 100.00 | 76.32 | 3233 |
| HSA-MIR-30E-5P | 100.00 | 76.32 | 3242 |
| HSA-MIR-3924 | 100.00 | 72.09 | 2394 |
| HSA-MIR-518D-5P | 100.00 | 67.51 | 979 |
| HSA-MIR-518E-5P | 100.00 | 67.66 | 954 |
| HSA-MIR-518F-5P | 100.00 | 67.51 | 979 |
| HSA-MIR-519A-5P | 100.00 | 67.66 | 954 |
| HSA-MIR-519B-5P | 100.00 | 67.66 | 954 |
| HSA-MIR-519C-5P | 100.00 | 67.66 | 954 |
| HSA-MIR-520C-5P | 100.00 | 67.51 | 979 |
| HSA-MIR-522-5P | 100.00 | 67.66 | 954 |
| HSA-MIR-523-5P | 100.00 | 67.66 | 954 |
| HSA-MIR-526A-5P | 100.00 | 67.51 | 979 |
| HSA-MIR-513A-5P | 100.00 | 69.77 | 2465 |
| HSA-MIR-4795-3P | 100.00 | 74.62 | 4024 |
| HSA-MIR-5011-5P | 100.00 | 83.46 | 5820 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-548AW | 99.99 | 72.57 | 3559 |
| HSA-MIR-548C-3P | 99.99 | 74.01 | 7587 |
| HSA-MIR-4775 | 99.98 | 75.00 | 6394 |
| HSA-MIR-4789-5P | 99.98 | 70.76 | 2721 |
| HSA-MIR-5696 | 99.98 | 72.36 | 4487 |
| HSA-MIR-302E | 99.96 | 70.74 | 2669 |
| HSA-MIR-548AJ-3P | 99.96 | 73.38 | 5345 |
| HSA-MIR-548X-3P | 99.96 | 73.38 | 5345 |
| HSA-MIR-570-3P | 99.96 | 72.41 | 4910 |
Functional genomics
ClinGen dosage: haploinsufficiency 30 (autosomal recessive), triplosensitivity 0 (no evidence). ClinGen Gene Dosage Map
Literature-anchored findings (GeneRIF, showing 40)
- ADAM9 is involved in monocyte fusion. (PMID:11831872)
- The downregulated expression of ADAM9 may serve as a marker for anterior polar cataracts. (PMID:11955914)
- cloning of a novel form of human ADAM9 (hADAM9s) which has an alpha-secretase activity for Amyloid Protein Precursor (PMID:12054541)
- First evidence is presented of ADAM9 as an insulin-like growth factor binding protein-5 (IGFBP-5) protease produced and secreted by osteoblasts in culture, able to degrade IGFBP-5 with high potency, thereby regulating the critical activity of IGFBP-5. (PMID:12484779)
- The results indicate that ADAM9, ADAM10, and ADAM17, members of the disintegrin and metalloprotease family, catalyze alpha-secretory cleavage and therefore act as alpha-secretases in A172 cells. (PMID:12535668)
- Expression of ADAM-9 mRNA and protein in human breast cancer. (PMID:12767059)
- Cytoplasmic ADAM9 overexpression is associated with poor differentiation in ductal adenocarcinoma (PMID:14997207)
- ADAM9 overexpression enhances cell adhesion and invasion of non-small cell lung cancer cells via modulation of other adhesion molecules and changes in sensitivity to growth factors, thereby promoting metastatic capacity to the brain. (PMID:15205330)
- In melanoma ADAM-9 protein expression appeared to be restricted to the melanoma cells within the invading front. (PMID:15856464)
- In conclusion, our findings are consistent with the hypothesis that FHL-2 and ADAM-9 are important modulators of IGFBP-5 actions and are, in part, regulated in a coordinated manner in bone (PMID:16311053)
- ADAM9 does not behave as a genuine alpha-secretase but rather acts as an important upstream regulator of ADAM10 activity. (PMID:16806063)
- Intracellular ROS and/or hydrogen peroxide, generated by cell stress, regulate ADAM9 expression. ADAM9 may support prostate cancer cell survival and progression. (PMID:17018608)
- These findings suggest that reactive oxygen species is a common mediator responsible for ADAM9 protein induction in human prostate cancer cells, downstream from androgen receptor, and stress response signaling. (PMID:17342749)
- the ADAM-9 adhesive domain plays a role in regulating the motility of cells by interaction with beta1 integrins and modulates MMP synthesis. (PMID:17704059)
- ADAM9 is overexpressed in prostate cancer cases and is an independent prognostic marker of PSA relapse-free survival following radical prostatectomy. (PMID:18061337)
- ADAM9 plays a crucial role in UV-induced EGFR activation and is overexpressed in skin cancer cell lines (PMID:19003995)
- The data of this suggested that promoter polymorphisms which regulate ADAM9 transcription are protective against SAD. (PMID:19237226)
- involved in advanced atherosclerosis, in catalytically active form, most notably associated with cells of monocytic origin (PMID:19253070)
- Cell migration in response to the amino-terminal fragment of urokinase requires epidermal growth factor receptor activation through an ADAM9/10-mediated mechanism. (PMID:19394555)
- ADAM9 is a CRD gene and also is a form of pathology wherein retinal disease first manifests at the POS-RPE junction. (PMID:19409519)
- ADAM9 expression is low in the squamous epithelium of the cervix, but is increased in CIN3 lesions as well as SCCs being the increase in both cases statistically significant. (PMID:19473694)
- the role of the disintegrin domain of the human ADAM9 (ADAM9D) on the adhesion of breast tumor cells and platelets to collagen I (PMID:19505527)
- Data show that the expression levels MMP1, MMP9, ADAM9 and TIMP3 were altered in drug-resistant sublines. (PMID:19543729)
- Experiments revealed that ADAM9 and ADAM10, but not ADAM17, are involved in the shedding of PrP(C) and that ADAM9 exerts its effect on PrP(C) shedding via ADAM10. (PMID:19564338)
- disintegrin and metalloprotease-9 is overexpressed in hepatocellular carcinoma and can be used as a prognostic marker (PMID:20388695)
- is expressed in adenoid cystic carcinoma-associated metastasis (PMID:20422344)
- ADAM9 plays a crucial role in prostate cancer progression and therapeutic resistance in part by altering E-cadherin and integrin expression. (PMID:20672324)
- Secreted variants of ADAM9 are a key determinant in manifestation of aggressive migratory phenotypes associated with breast cancer progression. (PMID:20736367)
- ADAM-9 expression plays an important role in mediating cell-cell contacts between fibroblasts and melanoma cells and that these interactions contribute to proteolytic activities required during invasion of melanoma cells. (PMID:21135106)
- ADAM10 activity is regulated by inhibition of ADAM9, and this regulation may be used to control shedding of amyloid precursor protein by enhancing alpha-secretase activity, a key regulatory step in the etiology of Alzheimer disease (PMID:21956108)
- The miR-126/ADAM9 axis plays essential role in the inhibition of invasive growth of pancreatic cancer cells. (PMID:22064652)
- Transient transfection of ADAM9 and ACE cDNAs into HEK293 cells demonstrated that ADAM9 requires both membrane anchorage and its catalytic domain to shed ACE. (PMID:22480688)
- ADAM9 expression was low in castration resistant prostate cancer (CRPC), correlated with poor prognosis and might be involved in the succession from hormonal sensitive prostate cancer (HSPC) to CRPC by various functions. (PMID:23106877)
- a novel molecular mechanism of ADAM9 in the regulation of prostate cancer cell proliferation. (PMID:23342005)
- The over-expression of MGAM was confirmed with a 6.6 fold increase in expression at the mRNA level whereas the fold change in ADAM9 demonstrated a 1.6 fold increase. (PMID:23405089)
- ADAM19 was upregulated in patients with ulcerative colitis and, to a lesser extent, in patients with Crohn’s disease compared with normal controls. In contrast, ADAM9 and ADAM10 expression did not differ between patients with IBD and controls. (PMID:23429442)
- miR-126&126* restored expressions play a tumor suppressor role by directly regulating ADAM9 and MMP7 in melanoma. (PMID:23437250)
- ADAM9 is an important molecule in the processes of invasion and metastasis. (PMID:23499592)
- The expression of circulating ADAM9 is down-regulated in pulmonary sarcoidosis. (PMID:23857158)
- ADAM9 up-regulates N-cadherin via miR-218 suppression in lung adenocarcinoma cells. (PMID:24705471)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | adam9a | ENSDARG00000010070 |
| mus_musculus | Adam9 | ENSMUSG00000031555 |
| rattus_norvegicus | Adam9 | ENSRNOG00000017231 |
Paralogs (20): ADAM22 (ENSG00000008277), ADAM28 (ENSG00000042980), ADAM7 (ENSG00000069206), ADAM11 (ENSG00000073670), ADAM2 (ENSG00000104755), ADAM23 (ENSG00000114948), ADAM20 (ENSG00000134007), ADAMDEC1 (ENSG00000134028), ADAM30 (ENSG00000134249), ADAM19 (ENSG00000135074), ADAM10 (ENSG00000137845), ADAM21 (ENSG00000139985), ADAM15 (ENSG00000143537), ADAM12 (ENSG00000148848), ADAM33 (ENSG00000149451), ADAM8 (ENSG00000151651), ADAM17 (ENSG00000151694), ADAM29 (ENSG00000168594), ADAM18 (ENSG00000168619), ADAM32 (ENSG00000197140)
Protein
Protein identifiers
Disintegrin and metalloproteinase domain-containing protein 9 — Q13443 (reviewed: Q13443)
Alternative names: Cellular disintegrin-related protein, Meltrin-gamma, Metalloprotease/disintegrin/cysteine-rich protein 9, Myeloma cell metalloproteinase
All UniProt accessions (18): A0A7I2V2E1, A0A7I2V2Z6, A0A7I2V303, A0A7I2V3B5, A0A7I2V3C1, A0A7I2V3I3, A0A7I2V3W3, A0A7I2V4B3, A0A7I2V4T8, A0A7I2V5C0, A0A7I2V5N8, A0A7I2V5Q0, A0A7I2YQ97, A0AVL1, Q13443, C9J6H5, C9JPM3, F8WC54
UniProt curated annotations — full annotation on UniProt →
Function. Metalloprotease that cleaves and releases a number of molecules with important roles in tumorigenesis and angiogenesis, such as TEK, KDR, EPHB4, CD40, VCAM1 and CDH5. May mediate cell-cell, cell-matrix interactions and regulate the motility of cells via interactions with integrins. May act as alpha-secretase for amyloid precursor protein (APP).
Subunit / interactions. Interacts with SH3GL2 and SNX9 through its cytoplasmic tail. Interacts with ITGA6.
Subcellular location. Cell membrane Secreted.
Tissue specificity. Widely expressed. Expressed in chondrocytes. Isoform 2 is highly expressed in liver and heart.
Post-translational modifications. Proteolytically cleaved in the trans-Golgi network before it reaches the plasma membrane to generate a mature protein. The removal of the pro-domain occurs via cleavage at two different sites. Processed most likely by a pro-protein convertase such as furin, at the boundary between the pro-domain and the catalytic domain. An additional upstream cleavage pro-protein convertase site (Arg-56/Glu-57) has an important role in the activation of ADAM9. Phosphorylation is induced in vitro by phorbol-12-myristate-13-acetate (PMA).
Disease relevance. Cone-rod dystrophy 9 (CORD9) [MIM:612775] An inherited retinal dystrophy characterized by retinal pigment deposits visible on fundus examination, predominantly in the macular region, and initial loss of cone photoreceptors followed by rod degeneration. This leads to decreased visual acuity and sensitivity in the central visual field, followed by loss of peripheral vision. Severe loss of vision occurs earlier than in retinitis pigmentosa, due to cone photoreceptors degenerating at a higher rate than rod photoreceptors. The disease is caused by variants affecting the gene represented in this entry.
Activity regulation. Synthesized as an inactive form which is proteolytically cleaved to generate an active enzyme. Processing at the upstream site is particularly important for activation of the proenzyme, whereas processing at the boundary between the pro-domain and the catalytic domain does not appear to be essential. Inhibited by hydroxamic acid-based inhibitors.
Cofactor. Binds 1 zinc ion per subunit.
Miscellaneous. May be produced at very low levels due to a premature stop codon in the mRNA, leading to nonsense-mediated mRNA decay.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q13443-1 | 1 | yes |
| Q13443-2 | 2 |
RefSeq proteins (1): NP_003807* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000742 | EGF | Domain |
| IPR001590 | Peptidase_M12B | Domain |
| IPR001762 | Disintegrin_dom | Domain |
| IPR002870 | Peptidase_M12B_N | Domain |
| IPR006586 | ADAM_Cys-rich | Domain |
| IPR018358 | Disintegrin_CS | Conserved_site |
| IPR024079 | MetalloPept_cat_dom_sf | Homologous_superfamily |
| IPR034027 | Reprolysin_adamalysin | Domain |
| IPR036436 | Disintegrin_dom_sf | Homologous_superfamily |
Pfam: PF00200, PF01421, PF01562, PF08516
Enzyme classification (BRENDA):
- EC 3.4.24.B9 — (BRENDA: organisms, substrates, inhibitors, Km, kcat entries)
UniProt features (41 total): disulfide bond 7, sequence conflict 7, glycosylation site 6, binding site 3, domain 3, site 2, modified residue 2, topological domain 2, splice variant 2, region of interest 2, signal peptide 1, chain 1, compositionally biased region 1, active site 1, transmembrane region 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q13443-F1 | 76.14 | 0.40 |
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): 348; 56–57 (cleavage); 205–206 (cleavage; by furin-like protease)
Ligand- & substrate-binding residues (3): 347; 351; 357
Post-translational modifications (2): 758, 761
Disulfide bonds (7): 322–401, 363–385, 365–370, 473–493, 644–656, 650–662, 664–673
Glycosylation sites (6): 125, 144, 154, 231, 381, 487
Function
Pathways and Gene Ontology
Reactome pathways
3 pathways
| ID | Pathway |
|---|---|
| R-HSA-1442490 | Collagen degradation |
| R-HSA-1474228 | Degradation of the extracellular matrix |
| R-HSA-1474244 | Extracellular matrix organization |
MSigDB gene sets: 490 (showing top):
GSE18804_SPLEEN_MACROPHAGE_VS_BRAIN_TUMORAL_MACROPHAGE_DN, GSE18804_BRAIN_VS_COLON_TUMORAL_MACROPHAGE_DN, GSE18804_SPLEEN_MACROPHAGE_VS_TUMORAL_MACROPHAGE_DN, MODULE_172, AHRARNT_01, MODULE_52, GOBP_EPITHELIUM_DEVELOPMENT, TAATAAT_MIR126, RODRIGUES_THYROID_CARCINOMA_POORLY_DIFFERENTIATED_UP, GOMF_METALLOPEPTIDASE_ACTIVITY, GOBP_RESPONSE_TO_PEPTIDE, GOBP_CELLULAR_RESPONSE_TO_LIPID, GOBP_RESPONSE_TO_CORTICOSTEROID, GOBP_CELLULAR_RESPONSE_TO_BIOTIC_STIMULUS, MODULE_64
GO Biological Process (27): membrane protein ectodomain proteolysis (GO:0006509), cell adhesion (GO:0007155), cell-matrix adhesion (GO:0007160), transforming growth factor beta receptor signaling pathway (GO:0007179), integrin-mediated signaling pathway (GO:0007229), response to manganese ion (GO:0010042), cell migration (GO:0016477), protein processing (GO:0016485), keratinocyte differentiation (GO:0030216), positive regulation of cell migration (GO:0030335), membrane protein intracellular domain proteolysis (GO:0031293), cell adhesion mediated by integrin (GO:0033627), positive regulation of cell adhesion mediated by integrin (GO:0033630), cell-cell adhesion mediated by integrin (GO:0033631), positive regulation of macrophage fusion (GO:0034241), response to tumor necrosis factor (GO:0034612), monocyte activation (GO:0042117), response to hydrogen peroxide (GO:0042542), amyloid precursor protein catabolic process (GO:0042987), positive regulation of MAPK cascade (GO:0043410), positive regulation of protein secretion (GO:0050714), positive regulation of membrane protein ectodomain proteolysis (GO:0051044), response to glucocorticoid (GO:0051384), positive regulation of keratinocyte migration (GO:0051549), response to calcium ion (GO:0051592), cellular response to lipopolysaccharide (GO:0071222), proteolysis (GO:0006508)
GO Molecular Function (12): metalloendopeptidase activity (GO:0004222), protein kinase C binding (GO:0005080), integrin binding (GO:0005178), collagen binding (GO:0005518), metallopeptidase activity (GO:0008237), SH3 domain binding (GO:0017124), laminin binding (GO:0043236), metal ion binding (GO:0046872), metalloendopeptidase activity involved in amyloid precursor protein catabolic process (GO:1902945), protein binding (GO:0005515), peptidase activity (GO:0008233), hydrolase activity (GO:0016787)
GO Cellular Component (8): obsolete extracellular space (GO:0005615), plasma membrane (GO:0005886), focal adhesion (GO:0005925), external side of plasma membrane (GO:0009897), cell surface (GO:0009986), extracellular exosome (GO:0070062), extracellular region (GO:0005576), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-2 pathways:
| Category | Pathways |
|---|---|
| Degradation of the extracellular matrix | 1 |
| Extracellular matrix organization | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular anatomical structure | 3 |
| membrane protein proteolysis | 2 |
| cell adhesion mediated by integrin | 2 |
| protein-containing complex binding | 2 |
| cellular process | 1 |
| cell-substrate adhesion | 1 |
| cellular response to transforming growth factor beta stimulus | 1 |
| transforming growth factor beta receptor superfamily signaling pathway | 1 |
| cell surface receptor signaling pathway | 1 |
| response to metal ion | 1 |
| cell motility | 1 |
| proteolysis | 1 |
| protein maturation | 1 |
| epidermal cell differentiation | 1 |
| skin development | 1 |
| cell migration | 1 |
| regulation of cell migration | 1 |
| positive regulation of cell motility | 1 |
| cell adhesion | 1 |
| regulation of cell adhesion mediated by integrin | 1 |
| positive regulation of cell adhesion | 1 |
| cell-cell adhesion | 1 |
| macrophage fusion | 1 |
| regulation of macrophage fusion | 1 |
| positive regulation of syncytium formation by plasma membrane fusion | 1 |
| response to cytokine | 1 |
| myeloid leukocyte activation | 1 |
| response to reactive oxygen species | 1 |
| amyloid precursor protein metabolic process | 1 |
| MAPK cascade | 1 |
| regulation of MAPK cascade | 1 |
| positive regulation of intracellular signal transduction | 1 |
| endopeptidase activity | 1 |
| metallopeptidase activity | 1 |
| protein kinase binding | 1 |
| signaling receptor binding | 1 |
| cell adhesion molecule binding | 1 |
| peptidase activity | 1 |
| protein domain specific binding | 1 |
| protein binding | 1 |
Protein interactions and networks
STRING
1228 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| ADAM9 | SNX9 | Q9Y5X1 | 967 |
| ADAM9 | MAD2L2 | Q9UI95 | 859 |
| ADAM9 | MAD2L1 | Q13257 | 711 |
| ADAM9 | APP | P05067 | 691 |
| ADAM9 | PACSIN3 | Q9UKS6 | 681 |
| ADAM9 | SH3GL2 | Q99962 | 678 |
| ADAM9 | GP6 | Q9HCN6 | 659 |
| ADAM9 | CLEC1B | Q9P126 | 640 |
| ADAM9 | ADAM17 | P78536 | 633 |
| ADAM9 | SELP | P16109 | 632 |
| ADAM9 | PITPNM3 | Q9BZ71 | 629 |
| ADAM9 | ADAM10 | O14672 | 627 |
| ADAM9 | RPGRIP1 | Q96KN7 | 615 |
| ADAM9 | RAX2 | Q96IS3 | 613 |
| ADAM9 | EGF | P01133 | 611 |
IntAct
136 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| VEGFD | ADAM9 | psi-mi:“MI:0914”(association) | 0.640 |
| CRIPTO | AIP | psi-mi:“MI:0914”(association) | 0.640 |
| SNX9 | WASL | psi-mi:“MI:0914”(association) | 0.640 |
| MAD2L2 | ADAM9 | psi-mi:“MI:0915”(physical association) | 0.630 |
| ADAM9 | SNX9 | psi-mi:“MI:0407”(direct interaction) | 0.590 |
| CANX | PGRMC1 | psi-mi:“MI:0914”(association) | 0.570 |
| ADAM9 | SNX18 | psi-mi:“MI:0407”(direct interaction) | 0.560 |
| GPHA2 | PLXNA2 | psi-mi:“MI:0914”(association) | 0.530 |
| CD1B | TOR1B | psi-mi:“MI:0914”(association) | 0.530 |
| SCGB1D4 | EGFR | psi-mi:“MI:0914”(association) | 0.530 |
| PLOD2 | psi-mi:“MI:0914”(association) | 0.530 | |
| FBXO2 | TMEM131L | psi-mi:“MI:0914”(association) | 0.530 |
| ADGRG5 | KLRG2 | psi-mi:“MI:0914”(association) | 0.530 |
| HTR2C | KLRG2 | psi-mi:“MI:0914”(association) | 0.530 |
| CRP | QSOX1 | psi-mi:“MI:0914”(association) | 0.530 |
| TMX1 | NRP1 | psi-mi:“MI:0914”(association) | 0.530 |
| INSL5 | COCH | psi-mi:“MI:0914”(association) | 0.530 |
| OCLN | DNAJC13 | psi-mi:“MI:0914”(association) | 0.530 |
| EPPIN | UMPS | psi-mi:“MI:0914”(association) | 0.530 |
| TIMP3 | ZZEF1 | psi-mi:“MI:0914”(association) | 0.530 |
BioGRID (191): ADAM9 (Affinity Capture-MS), ADAM9 (Affinity Capture-MS), ADAM9 (Affinity Capture-MS), ADAM9 (Affinity Capture-MS), ADAM9 (Affinity Capture-MS), ADAM9 (Affinity Capture-MS), ADAM9 (Affinity Capture-MS), ADAM9 (Co-fractionation), ADAM9 (Affinity Capture-MS), ADAM9 (Affinity Capture-Western), ADAM9 (Affinity Capture-Western), ADAM9 (Affinity Capture-MS), ADAM9 (Affinity Capture-MS), ADAM9 (Affinity Capture-MS), ADAM9 (Affinity Capture-MS)
ESM2 similar proteins: O35674, O43184, O43506, O75173, O88839, O95450, P57110, P58459, P59384, P59511, P70505, P78325, P79331, P97857, Q05910, Q13443, Q13444, Q14114, Q1EHB3, Q4VC17, Q5RFQ8, Q60813, Q61072, Q61824, Q62179, Q64151, Q68SA9, Q69Z28, Q8BNJ2, Q8C9W3, Q8TE57, Q8TE58, Q8TE60, Q8WXS8, Q924X6, Q9ESP7, Q9H013, Q9H324, Q9JI76, Q9JLN6
Diamond homologs: A0A0B4U9L8, A0A6B7FMR5, A2CJE2, A2CJE3, A2CJE4, A3R0T9, A4PBQ9, A8QL48, A8QL49, A8QL59, B8K1W0, C0LZJ5, C5H5D1, C5H5D2, C5H5D3, C5H5D4, C5H5D5, C5H5D6, C9E1R8, C9E1S0, D3TTC1, D3TTC2, D5LMJ3, D6PXE8, D8VNS0, F8RKV9, F8RKW0, F8RKW1, F8S108, G5EFD5, J3S829, J3S830, J3SDW6, J3SDW8, O35227, O35674, O42138, O43184, O77780, O88839
SIGNOR signaling
2 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| ADAM9 | “down-regulates quantity by destabilization” | FGFR2 | cleavage |
| MMP14 | “down-regulates quantity by destabilization” | ADAM9 | cleavage |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 156 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.
Reactome pathways:
| Pathway | Partners | Fold | FDR |
|---|---|---|---|
| Metal ion SLC transporters | 5 | 31.0× | 6e-05 |
| Signaling by phosphorylated juxtamembrane, extracellular and kinase domain KIT mutants | 5 | 26.8× | 6e-05 |
| Downstream signal transduction | 5 | 19.6× | 2e-04 |
| Signaling by SCF-KIT | 6 | 15.4× | 1e-04 |
| NCAM signaling for neurite out-growth | 5 | 14.0× | 6e-04 |
| R-HSA-425366 | 5 | 9.3× | 2e-03 |
| Clathrin-mediated endocytosis | 8 | 7.0× | 5e-04 |
| Cargo recognition for clathrin-mediated endocytosis | 6 | 6.5× | 4e-03 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| zinc ion transmembrane transport | 5 | 25.4× | 7e-04 |
| T cell receptor signaling pathway | 7 | 7.7× | 5e-03 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
599 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 23 |
| Likely pathogenic | 9 |
| Uncertain significance | 259 |
| Likely benign | 220 |
| Benign | 29 |
Top pathogenic / likely-pathogenic (30)
| Variant ID | HGVS | Classification |
|---|---|---|
| 1184447 | NM_003816.3(ADAM9):c.1588_1591+10del | Pathogenic |
| 1410127 | NM_003816.3(ADAM9):c.543_546dup (p.Glu183fs) | Pathogenic |
| 1452105 | NM_003816.3(ADAM9):c.1420C>T (p.Arg474Ter) | Pathogenic |
| 1804635 | NM_003816.3(ADAM9):c.17_18del (p.Arg6fs) | Pathogenic |
| 1879709 | NC_000008.11:g.39018852GA[1] | Pathogenic |
| 189795 | NM_003816.3(ADAM9):c.1396-2A>G | Pathogenic |
| 2134415 | NM_003816.3(ADAM9):c.1284_1285del (p.Cys428_Asp429delinsTer) | Pathogenic |
| 2424769 | NC_000008.10:g.(?38911980)(38928942_?)del | Pathogenic |
| 2798666 | NM_003816.3(ADAM9):c.399T>A (p.Cys133Ter) | Pathogenic |
| 2811859 | NM_003816.3(ADAM9):c.1802G>A (p.Trp601Ter) | Pathogenic |
| 3068523 | NM_003816.3(ADAM9):c.702del (p.Ala234_Val235insTer) | Pathogenic |
| 3069202 | NM_003816.3(ADAM9):c.1189A>T (p.Lys397Ter) | Pathogenic |
| 3245572 | NC_000008.10:g.(?38913076)(38928942_?)del | Pathogenic |
| 3248796 | NM_003816.3(ADAM9):c.2020G>T (p.Glu674Ter) | Pathogenic |
| 3727419 | NM_003816.3(ADAM9):c.735C>A (p.Tyr245Ter) | Pathogenic |
| 373092 | NM_003816.3(ADAM9):c.196-1G>A | Pathogenic |
| 6876 | NM_003816.3(ADAM9):c.1130+1G>A | Pathogenic |
| 6877 | NM_003816.3(ADAM9):c.766C>T (p.Arg256Ter) | Pathogenic |
| 6878 | NM_003816.3(ADAM9):c.490C>T (p.Arg164Ter) | Pathogenic |
| 6879 | NM_003816.3(ADAM9):c.411-8A>G | Pathogenic |
| 812214 | NM_003816.3(ADAM9):c.1455C>A (p.Tyr485Ter) | Pathogenic |
| 862925 | NM_003816.3(ADAM9):c.1968T>A (p.Cys656Ter) | Pathogenic |
| 915360 | NM_003816.3(ADAM9):c.639T>G (p.Tyr213Ter) | Pathogenic |
| 1065690 | NM_003816.3(ADAM9):c.576del (p.Glu193fs) | Likely pathogenic |
| 2013020 | NM_003816.3(ADAM9):c.254+1G>A | Likely pathogenic |
| 2034457 | NM_003816.3(ADAM9):c.744+1G>A | Likely pathogenic |
| 3242299 | GRCh37/hg19 8p11.22(chr8:38933032-38935086)x1 | Likely pathogenic |
| 3248895 | NM_003816.3:c.(672+1_673-1)_(914+1_915-1)del | Likely pathogenic |
| 3341288 | NM_003816.3(ADAM9):c.1698-1715_1881+156del | Likely pathogenic |
| 3382263 | NM_003816.3(ADAM9):c.103C>T (p.Gln35Ter) | Likely pathogenic |
SpliceAI
3516 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 8:39007881:TGTA:T | acceptor_loss | 1.0000 |
| 8:39007882:GTAG:G | acceptor_loss | 1.0000 |
| 8:39007883:TA:T | acceptor_loss | 1.0000 |
| 8:39007884:A:AG | acceptor_gain | 1.0000 |
| 8:39007884:A:C | acceptor_loss | 1.0000 |
| 8:39007884:AG:A | acceptor_gain | 1.0000 |
| 8:39007885:G:GA | acceptor_gain | 1.0000 |
| 8:39007885:GG:G | acceptor_gain | 1.0000 |
| 8:39007885:GGCT:G | acceptor_gain | 1.0000 |
| 8:39007979:AACAA:A | donor_gain | 1.0000 |
| 8:39007980:ACAA:A | donor_gain | 1.0000 |
| 8:39007981:CAA:C | donor_gain | 1.0000 |
| 8:39007982:AA:A | donor_gain | 1.0000 |
| 8:39007983:AG:A | donor_loss | 1.0000 |
| 8:39007984:G:GG | donor_gain | 1.0000 |
| 8:39007985:TAAG:T | donor_loss | 1.0000 |
| 8:39011717:G:GG | donor_gain | 1.0000 |
| 8:39013960:TCCA:T | acceptor_loss | 1.0000 |
| 8:39013963:A:AG | acceptor_gain | 1.0000 |
| 8:39013964:G:GG | acceptor_gain | 1.0000 |
| 8:39013964:GA:G | acceptor_gain | 1.0000 |
| 8:39013964:GAGA:G | acceptor_gain | 1.0000 |
| 8:39013964:GAGAC:G | acceptor_gain | 1.0000 |
| 8:39014043:GGTAA:G | donor_loss | 1.0000 |
| 8:39014044:G:GG | donor_gain | 1.0000 |
| 8:39014044:GTA:G | donor_loss | 1.0000 |
| 8:39014045:T:A | donor_loss | 1.0000 |
| 8:39017188:A:AG | acceptor_gain | 1.0000 |
| 8:39017190:A:AG | acceptor_gain | 1.0000 |
| 8:39017190:AATTT:A | acceptor_gain | 1.0000 |
AlphaMissense
5385 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 8:39025852:T:A | C322S | 1.000 |
| 8:39025853:G:A | C322Y | 1.000 |
| 8:39025853:G:C | C322S | 1.000 |
| 8:39026719:C:G | H347D | 1.000 |
| 8:39026731:C:G | H351D | 1.000 |
| 8:39026733:T:A | H351Q | 1.000 |
| 8:39026733:T:G | H351Q | 1.000 |
| 8:39041960:T:G | F382C | 1.000 |
| 8:39055751:T:A | C524S | 1.000 |
| 8:39055751:T:C | C524R | 1.000 |
| 8:39055752:G:C | C524S | 1.000 |
| 8:39055753:T:G | C524W | 1.000 |
| 8:39077238:T:A | C570S | 1.000 |
| 8:39077239:G:C | C570S | 1.000 |
| 8:39077253:T:A | C575S | 1.000 |
| 8:39077253:T:C | C575R | 1.000 |
| 8:39077254:G:C | C575S | 1.000 |
| 8:39023274:G:C | R288P | 0.999 |
| 8:39025829:G:A | G314E | 0.999 |
| 8:39025837:T:C | F317L | 0.999 |
| 8:39025839:T:A | F317L | 0.999 |
| 8:39025839:T:G | F317L | 0.999 |
| 8:39025852:T:C | C322R | 0.999 |
| 8:39025853:G:T | C322F | 0.999 |
| 8:39025854:T:G | C322W | 0.999 |
| 8:39025871:G:A | G328D | 0.999 |
| 8:39026717:C:A | A346D | 0.999 |
| 8:39026719:C:A | H347N | 0.999 |
| 8:39026721:T:A | H347Q | 0.999 |
| 8:39026721:T:G | H347Q | 0.999 |
dbSNP variants (sampled 300 via entrez): RS1000007634 (8:39034243 A>G), RS1000037804 (8:39043965 G>A), RS1000075484 (8:39027502 G>C), RS1000093763 (8:39037097 C>T), RS1000120761 (8:39012196 C>T), RS1000152181 (8:39094300 T>C), RS1000159195 (8:39008517 T>C), RS1000192352 (8:39050830 G>T), RS1000245064 (8:39081848 A>C,G), RS1000247532 (8:39044929 T>C,G), RS1000260842 (8:39050734 G>C), RS1000313450 (8:39001959 C>T), RS1000316031 (8:39102860 A>T), RS1000325868 (8:39045464 G>A,C), RS1000326716 (8:39096340 A>T)
Disease associations
OMIM: gene MIM:602713 | disease phenotypes: MIM:612775, MIM:120970, MIM:615033, MIM:268000
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| cone-rod dystrophy 9 | Definitive | Autosomal recessive |
| cone-rod dystrophy | Supportive | Autosomal dominant |
ClinGen Gene-Disease Validity (1)
Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.
| Disease | Classification | Inheritance |
|---|---|---|
| ADAM9-related retinopathy | Definitive | AR |
Mondo (5): inherited retinal dystrophy (MONDO:0019118), cone-rod dystrophy 9 (MONDO:0013002), cone-rod dystrophy (MONDO:0015993), hereditary spastic paraplegia 54 (MONDO:0014018), retinitis pigmentosa (MONDO:0019200)
Orphanet (4): OBSOLETE: Inherited retinal disorder (Orphanet:71862), Cone rod dystrophy (Orphanet:1872), Autosomal recessive spastic paraplegia type 54 (Orphanet:320380), Retinitis pigmentosa (Orphanet:791)
HPO phenotypes
17 total (18 of 17 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0000007 | Autosomal recessive inheritance |
| HP:0000505 | Visual impairment |
| HP:0000529 | Progressive visual loss |
| HP:0000543 | Optic disc pallor |
| HP:0000548 | Cone/cone-rod dystrophy |
| HP:0000551 | Color vision defect |
| HP:0000603 | Central scotoma |
| HP:0000613 | Photophobia |
| HP:0000639 | Nystagmus |
| HP:0000662 | Nyctalopia |
| HP:0001105 | Retinal atrophy |
| HP:0007641 | Dyschromatopsia |
| HP:0007703 | Abnormal retinal pigmentation |
| HP:0007737 | Spicular pigmentation of the retina |
| HP:0007843 | Attenuation of retinal blood vessels |
| HP:0012508 | Metamorphopsia |
| HP:0030466 | Abnormal full-field electroretinogram |
| HP:0000556 | Retinal dystrophy |
GWAS associations
1 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST90002379_117 | Basophil count | 1.000000e-09 |
EFO canonical traits (1, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0005090 | basophil count |
MeSH disease descriptors (3)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D000071700 | Cone-Rod Dystrophies | C11.270.152; C11.768.585.658.250; C16.320.290.152 |
| D058499 | Retinal Dystrophies | C11.768.585.658 |
| D012174 | Retinitis Pigmentosa | C11.270.684; C11.768.585.658.500; C16.320.290.684 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL5982 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
3 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 38,415 (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 |
|---|---|---|---|
| CHEMBL19611 | ILOMASTAT | 2 | 12,065 |
| CHEMBL206815 | APRATASTAT | 2 | 256 |
| CHEMBL296588 | PEPSTATIN | 2 | 26,094 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — M12: Astacin/Adamalysin
Most potent curated ligand interactions (1 total), top 1:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| ilomastat | Inhibition | 9.0 | pIC50 |
Binding affinities (BindingDB)
13 measured of 19 human assays (19 total across all organisms); most potent 13 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| (2S)-N-hydroxy-3-[[4-[(2-methylquinolin-4-yl)methoxy]phenyl]sulfonylamino]-2-(4-methylsulfonylpiperazin-1-yl)propanamide | IC50 | 21 nM | US-8633196: Benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics |
| (2S)-N-hydroxy-3-[[4-[(2-methylquinolin-4-yl)methoxy]phenyl]sulfonylamino]-2-(4-propan-2-ylsulfonylpiperazin-1-yl)propanamide | IC50 | 33 nM | US-8633196: Benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics |
| (2S)-2-(4-ethylpiperazin-1-yl)-N-hydroxy-3-[[4-[(2-methylquinolin-4-yl)methoxy]phenyl]sulfonylamino]propanamide | IC50 | 41 nM | US-8633196: Benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics |
| (2S)-N-hydroxy-2-[4-(2-methylpropanoyl)piperazin-1-yl]-3-[[4-[(2-methylquinolin-4-yl)methoxy]phenyl]sulfonylamino]propanamide | IC50 | 53 nM | US-8633196: Benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics |
| (2S)-N-hydroxy-2-[4-[(4-methylphenyl)methyl]piperazin-1-yl]-3-[[4-[(2-methylquinolin-4-yl)methoxy]phenyl]sulfonylamino]propanamide | IC50 | 63 nM | US-8633196: Benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics |
| (2S)-2-[4-[(4-fluorophenyl)methyl]piperazin-1-yl]-N-hydroxy-3-[[4-[(2-methylquinolin-4-yl)methoxy]phenyl]sulfonylamino]propanamide | IC50 | 67 nM | US-8633196: Benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics |
| N-hydroxy-4-[4-(4-hydroxybut-2-ynoxy)phenyl]sulfonyl-2,2-dimethylthiomorpholine-3-carboxamide | IC50 | 71 nM | US-9115102: N-[2-hydroxycarbamoyl-2-(piperazinyl) ethyl] benzamide compounds, their preparation and their use as TACE inhibitors |
| (S)-N-hydroxy-4-(4-(4-hydroxybut-2-ynyloxy)phenylsulfonyl)-2,2-dimethylthiomorpholine-3-carboxamide | IC50 | 71 nM | US-9266848: 4-alkoxy-N-(2-hydroxycarbamoyl-2-piperidinyl-ethyl)-benzamide compounds as selective TACE-inhibitors for the treatment of inflammatory diseases |
| (2S)-N-hydroxy-2-[4-(2-methylpropylsulfonyl)piperazin-1-yl]-3-[[4-[(2-methylquinolin-4-yl)methoxy]phenyl]sulfonylamino]propanamide | IC50 | 86 nM | US-8633196: Benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics |
| 4-but-2-ynoxy-N-[(2S)-3-(hydroxyamino)-2-(4-methylsulfonylpiperazin-1-yl)-3-oxopropyl]benzamide | IC50 | 942 nM | US-9115102: N-[2-hydroxycarbamoyl-2-(piperazinyl) ethyl] benzamide compounds, their preparation and their use as TACE inhibitors |
| N-[(2S)-3-(hydroxyamino)-3-oxo-2-piperidin-1-ylpropyl]-4-(pyridin-4-ylmethoxy)benzamide | IC50 | 3090 nM | US-9266848: 4-alkoxy-N-(2-hydroxycarbamoyl-2-piperidinyl-ethyl)-benzamide compounds as selective TACE-inhibitors for the treatment of inflammatory diseases |
| N-[(2S)-3-(hydroxyamino)-2-(4-methylsulfonylpiperazin-1-yl)-3-oxopropyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide | IC50 | 5800 nM | US-9115102: N-[2-hydroxycarbamoyl-2-(piperazinyl) ethyl] benzamide compounds, their preparation and their use as TACE inhibitors |
| N-[(2S)-3-(hydroxyamino)-3-oxo-2-piperidin-1-ylpropyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide | IC50 | 6400 nM | US-9266848: 4-alkoxy-N-(2-hydroxycarbamoyl-2-piperidinyl-ethyl)-benzamide compounds as selective TACE-inhibitors for the treatment of inflammatory diseases |
ChEMBL bioactivities
46 potent at pChembl≥5 of 48 total, top 45 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.00 | IC50 | 1 | nM | ILOMASTAT |
| 7.25 | IC50 | 56.3 | nM | PEPSTATIN |
| 7.25 | IC50 | 56.3 | nM | ILOMASTAT |
| 7.16 | IC50 | 70 | nM | CHEMBL170315 |
| 7.16 | IC50 | 70 | nM | CHEMBL353536 |
| 7.07 | IC50 | 85 | nM | CHEMBL3392650 |
| 7.07 | IC50 | 85 | nM | APRATASTAT |
| 7.05 | IC50 | 90 | nM | CHEMBL4215407 |
| 6.75 | IC50 | 180 | nM | CHEMBL173027 |
| 6.72 | IC50 | 190 | nM | CHEMBL171962 |
| 6.64 | IC50 | 230 | nM | CHEMBL366478 |
| 6.58 | IC50 | 260 | nM | CHEMBL355797 |
| 6.52 | IC50 | 300 | nM | CHEMBL172885 |
| 6.43 | IC50 | 370 | nM | CHEMBL172548 |
| 6.37 | IC50 | 430 | nM | CHEMBL173235 |
| 6.32 | IC50 | 480 | nM | CHEMBL4208519 |
| 6.29 | IC50 | 510 | nM | CHEMBL368857 |
| 6.28 | IC50 | 520 | nM | CHEMBL173316 |
| 6.25 | IC50 | 560 | nM | CHEMBL177072 |
| 6.18 | IC50 | 660 | nM | CHEMBL436049 |
| 6.18 | IC50 | 660 | nM | CHEMBL173686 |
| 6.16 | IC50 | 700 | nM | CHEMBL175164 |
| 6.10 | IC50 | 800 | nM | CHEMBL172249 |
| 6.09 | IC50 | 810 | nM | CHEMBL368205 |
| 6.08 | IC50 | 830 | nM | CHEMBL172415 |
| 6.05 | IC50 | 890 | nM | CHEMBL367710 |
| 6.04 | IC50 | 910 | nM | CHEMBL172722 |
| 5.97 | IC50 | 1060 | nM | CHEMBL173326 |
| 5.94 | IC50 | 1140 | nM | CHEMBL171292 |
| 5.87 | IC50 | 1340 | nM | CHEMBL173846 |
| 5.80 | IC50 | 1600 | nM | CHEMBL170429 |
| 5.78 | IC50 | 1670 | nM | CHEMBL425316 |
| 5.72 | IC50 | 1890 | nM | CHEMBL172886 |
| 5.71 | IC50 | 1960 | nM | CHEMBL539171 |
| 5.66 | Ki | 2200 | nM | CHEMBL497985 |
| 5.65 | IC50 | 2240 | nM | CHEMBL173744 |
| 5.58 | IC50 | 2600 | nM | CHEMBL171986 |
| 5.51 | IC50 | 3110 | nM | CHEMBL174315 |
| 5.51 | IC50 | 3054 | nM | CHEMBL3648903 |
| 5.49 | IC50 | 3251 | nM | CHEMBL3704903 |
| 5.45 | IC50 | 3560 | nM | CHEMBL173754 |
| 5.07 | IC50 | 8448 | nM | CHEMBL4873384 |
| 5.03 | IC50 | 9254 | nM | CHEMBL3648902 |
| 5.00 | IC50 | 1e+04 | nM | GRASSYSTATIN A |
| 5.00 | Ki | 1e+04 | nM | CHEMBL1078396 |
PubChem BioAssay actives
40 with measured affinity, of 62 total; 39 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 |
|---|---|---|---|---|
| (2R)-N’-hydroxy-N-[(2S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl]-2-(2-methylpropyl)butanediamide | 241656: In vitro inhibition of A disintegrin and metalloprotease domain 9 (ADAM9) | ic50 | 0.0010 | uM |
| (3S,4S)-3-hydroxy-4-[[(2S)-2-[[(3S,4S)-3-hydroxy-6-methyl-4-[[(2S)-3-methyl-2-[[(2S)-3-methyl-2-(3-methylbutanoylamino)butanoyl]amino]butanoyl]amino]heptanoyl]amino]propanoyl]amino]-6-methylheptanoic acid | 448178: Inhibition of ADAM9 | ic50 | 0.0563 | uM |
| N-hydroxy-2-[methoxy-(4-methoxyphenyl)phosphoryl]-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.0700 | uM |
| 2-[ethoxy-[4-(2-ethoxyethoxy)phenyl]phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.0700 | uM |
| N-hydroxy-3-[methyl-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]sulfonylamino]-1-(2-methylpropanoyl)azetidine-3-carboxamide | 1371964: Inhibition of ADAM9 (unknown origin) | ic50 | 0.0900 | uM |
| N-hydroxy-2-[(4-methoxyphenyl)-(2-pyridin-2-ylethoxy)phosphoryl]-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.1800 | uM |
| 7-amino-2-[ethoxy-(4-methoxyphenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.1900 | uM |
| 2-[ethoxy-(4-methoxyphenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.2300 | uM |
| 2-[ethoxy-(4-phenoxyphenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.2600 | uM |
| 2-[ethoxy-(4-fluorophenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.3000 | uM |
| 2-[ethoxy(phenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.3700 | uM |
| benzyl 4-[ethoxy-(4-methoxyphenyl)phosphoryl]-3-(hydroxycarbamoyl)piperazine-1-carboxylate | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.4300 | uM |
| N-hydroxy-1-(3-methylbutanoyl)-3-[methyl-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]sulfonylamino]azetidine-3-carboxamide | 1371964: Inhibition of ADAM9 (unknown origin) | ic50 | 0.4800 | uM |
| 2-[2-ethoxyethoxy-(4-methoxyphenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.5100 | uM |
| 5-[ethoxy-(4-methoxyphenyl)phosphoryl]-N-hydroxy-6,7-dihydro-4H-thieno[3,2-c]pyridine-6-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.5200 | uM |
| 6-[ethoxy-(4-methoxyphenyl)phosphoryl]-N-hydroxy-7,8-dihydro-5H-pyrido[3,4-b]pyrazine-7-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.5600 | uM |
| 2-[ethoxy-(4-pyridin-4-yloxyphenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.6600 | uM |
| 2-[(4-aminophenyl)-ethoxyphosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.6600 | uM |
| 2-[ethoxy(2-phenylethyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.7000 | uM |
| 2-[ethoxy-(4-methoxyphenyl)phosphoryl]-N-hydroxy-1,3,4,9-tetrahydropyrido[3,4-b]indole-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.8000 | uM |
| 2-[butoxy-(4-methoxyphenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.8100 | uM |
| 2-[ethoxy-(3-fluorophenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.8300 | uM |
| 2-[ethoxy(thiophen-2-yl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.8900 | uM |
| 2-[ethoxy-[(E)-2-phenylethenyl]phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 0.9100 | uM |
| 2-[ethoxy-(2-fluorophenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 1.0600 | uM |
| 2-[2-(diethylamino)ethoxy-(4-methoxyphenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 1.1400 | uM |
| 2-[cyclohexylmethoxy-(4-methoxyphenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 1.3400 | uM |
| 2-[hexoxy-(4-methoxyphenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 1.6000 | uM |
| 2-[[4-(4-aminophenoxy)phenyl]-ethoxyphosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 1.6700 | uM |
| 2-[ethoxy-(4-methylphenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 1.8900 | uM |
| 2-[ethoxy-(4-phenylphenyl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 1.9600 | uM |
| (6S,7S)-N-hydroxy-5-methyl-6-[4-[5-(trifluoromethyl)-2-pyridinyl]piperazine-1-carbonyl]-5-azaspiro[2.5]octane-7-carboxamide | 1356429: Inhibition of recombinant human C-terminal His10-tagged ADAM9 (Ala206 to Asp697 residues) expressed in mouse cells using McaPLAQAV-Dpa-RSSSR-NH2 as substrate by fluorescence spectrophotometric method | ki | 2.2000 | uM |
| N-hydroxy-2-[(4-methoxyphenyl)-propan-2-yloxyphosphoryl]-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 2.2400 | uM |
| 2-[ethoxy(pyridin-4-yl)phosphoryl]-N-hydroxy-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 2.6000 | uM |
| N-hydroxy-2-[(4-methoxyphenyl)-(2-phenylethoxy)phosphoryl]-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 3.1100 | uM |
| N-hydroxy-2-[(4-methoxyphenyl)-[2-(4-phenylphenyl)ethoxy]phosphoryl]-3,4-dihydro-1H-isoquinoline-3-carboxamide | 66433: Inhibition of the heparin binding epidermal growth factor (HB-EGF) release from fibrosarcoma HT1080 transfectants expressing alkaline phosphate (AP) tagged HB-EGF stimulated by 12-O-tetradecanoylphorbol 13-acetate(TPA). | ic50 | 3.5600 | uM |
| (5R)-5-[3-[4-(3,5-dichlorophenyl)piperazin-1-yl]-3-oxopropyl]imidazolidine-2,4-dione | 1775686: Inhibition of ADAM-9 (unknown origin) | ic50 | 8.4480 | uM |
| 5-[(5-methoxy-3-oxo-1H-indazol-2-yl)methyl]-5-methylimidazolidine-2,4-dione | 464407: Inhibition of ADAM9 | ki | 10.0000 | uM |
| methyl (2S)-1-[(2R)-2-[[(2S)-2-[[(2S,3R)-2-[[(3S,4S)-4-[[(2S)-4-amino-2-[[(2S)-2-[[(2R)-2-[(2S)-2-[(2S)-2-(dimethylamino)-3-methylbutanoyl]oxy-3-methylbutanoyl]oxy-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxy-6-methylheptanoyl]amino]-3-hydroxybutanoyl]amino]propanoyl]-methylamino]-3-phenylpropanoyl]pyrrolidine-2-carboxylate | 448855: Inhibition of ADAM9 after 10 to 15 mins by fluorescence assay | ic50 | 10.0000 | uM |
CTD chemical–gene interactions
63 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Hydrogen Peroxide | decreases reaction, increases expression, affects expression | 3 |
| mercuric bromide | affects cotreatment, increases expression | 2 |
| Resveratrol | affects cotreatment, increases expression | 2 |
| Lead | affects expression, decreases expression | 2 |
| Phenylmercuric Acetate | affects cotreatment, increases expression | 2 |
| Dihydrotestosterone | increases expression, decreases reaction, affects reaction | 2 |
| Tobacco Smoke Pollution | affects expression, increases expression | 2 |
| Tretinoin | affects localization, increases expression | 2 |
| Valproic Acid | increases expression | 2 |
| tert-Butylhydroperoxide | decreases reaction, increases expression, affects cotreatment, affects expression | 2 |
| aristolochic acid I | decreases expression | 1 |
| FR900359 | affects phosphorylation | 1 |
| methylmercuric chloride | increases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| bisphenol A | affects expression | 1 |
| sodium arsenate | increases expression | 1 |
| sodium arsenite | decreases expression | 1 |
| sulindac sulfide | decreases expression | 1 |
| benazol P | affects expression | 1 |
| aluminum sulfate | decreases expression | 1 |
| ebselen | decreases reaction, increases expression | 1 |
| bicalutamide | increases expression, decreases reaction | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| perfluorooctane sulfonic acid | decreases expression | 1 |
| K 7174 | increases expression | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | affects cotreatment, increases expression | 1 |
| dorsomorphin | affects cotreatment, increases expression | 1 |
| Rosiglitazone | affects cotreatment, increases expression, decreases reaction | 1 |
| Pioglitazone | decreases reaction, increases expression | 1 |
| Fulvestrant | increases methylation | 1 |
ChEMBL screening assays
19 unique, capped per target: 18 binding, 1 admet
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1039217 | Binding | Inhibition of ADAM9 assessed as residual activity at 10 uM after 10 to 15 mins by fluorescence assay relative to control | Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. — J Med Chem |
| CHEMBL4186131 | ADMET | Inhibition of ADAM9 (unknown origin) | Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis. — Bioorg Med Chem |
Cellosaurus cell lines
9 cell lines: 6 cancer cell line, 2 transformed cell line, 1 spontaneously immortalized cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B1J0 | Abcam HeLa ADAM9 KO | Cancer cell line | Female |
| CVCL_D7JL | Ubigene A-549 ADAM9 KO | Cancer cell line | Male |
| CVCL_D8YQ | Ubigene HEK293 ADAM9 KO | Transformed cell line | Female |
| CVCL_E6P0 | Genomeditech CHO-K1 H_ADAM9 | Spontaneously immortalized cell line | Female |
| CVCL_E6TB | Genomeditech HEK-293 H_ADAM9 | Transformed cell line | Female |
| CVCL_SB49 | HAP1 ADAM9 (-) 1 | Cancer cell line | Male |
| CVCL_SB50 | HAP1 ADAM9 (-) 2 | Cancer cell line | Male |
| CVCL_SB51 | HAP1 ADAM9 (-) 3 | Cancer cell line | Male |
| CVCL_SB52 | HAP1 ADAM9 (-) 4 | Cancer cell line | Male |
Clinical trials (associated diseases)
263 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00717080 | PHASE4 | COMPLETED | The Role of Capsular Tension Ring (CTR) in Anterior Capsular Contraction |
| NCT04224207 | PHASE3 | COMPLETED | Management of Retinitis Pigmentosa by Mesenchymal Stem Cells by Wharton’s Jelly Derived Mesenchymal Stem Cells |
| NCT07082855 | PHASE3 | NOT_YET_RECRUITING | A Multicenter, Randomized, Double-Blind, Controlled Clinical Study of Minocycline for the Treatment of Retinitis Pigmentosa |
| NCT00000114 | PHASE3 | COMPLETED | Randomized Trial of Vitamin A and Vitamin E Supplementation for Retinitis Pigmentosa |
| NCT00000116 | PHASE3 | COMPLETED | Randomized Trial of DHA for Retinitis Pigmentosa Patients Receiving Vitamin A |
| NCT00346333 | PHASE3 | COMPLETED | Clinical Trial of Lutein for Patients With Retinitis Pigmentosa Receiving Vitamin A |
| NCT01786395 | PHASE3 | TERMINATED | Phase III Efficacy and Safety Clinical Study of UF-021 for Treatment of Retinitis Pigmentosa |
| NCT04636853 | PHASE3 | COMPLETED | CB-PRP in Retinitis Pigmentosa and Dry Age-related Macular Degeneration |
| NCT05537220 | PHASE3 | ACTIVE_NOT_RECRUITING | Oral N-acetylcysteine for Retinitis Pigmentosa |
| NCT05800301 | PHASE3 | COMPLETED | Management of Retinitis Pigmentosa Via Combination of Wharton’s Jelly-derived Mesenchymal Stem Cells and Magnovision |
| NCT05926583 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of AAV5-hRKp.RPGR for the Treatment of Japanese Participants With X-linked Retinitis Pigmentosa |
| NCT06388200 | PHASE3 | ACTIVE_NOT_RECRUITING | A Phase 3 Study Of OCU400 Gene Therapy for the Treatment Of Retinitis Pigmentosa |
| NCT07290530 | PHASE3 | NOT_YET_RECRUITING | 24-Month Trial of NPI-001 for the Preservation of Photoreceptors in Retinitis Pigmentosa Associated With Usher Syndrome |
| NCT01773278 | PHASE2 | RECRUITING | Cholesterol and Antioxidant Treatment in Patients With Smith-Lemli-Opitz Syndrome (SLOS) |
| NCT03763227 | PHASE2 | COMPLETED | Intravitreal Ranibizumab (Lucentis®) in the Treatment of Non-leaking Macular Cysts in Retinal Dystrophy |
| NCT04068207 | PHASE2 | COMPLETED | Minocycline Treatment in Retinitis Pigmentosa |
| NCT04945772 | PHASE2 | COMPLETED | Efficacy and Safety of MCO-010 Optogenetic Therapy in Adults With Retinitis Pigmentosa [RESTORE] |
| NCT00100230 | PHASE2 | COMPLETED | DHA and X-Linked Retinitis Pigmentosa |
| NCT00447980 | PHASE2 | COMPLETED | A Study of Encapsulated Cell Technology (ECT) Implant for Participants With Early Stage Retinitis Pigmentosa |
| NCT00447993 | PHASE2 | COMPLETED | A Study of Encapsulated Cell Technology (ECT) Implant for Patients With Late Stage Retinitis Pigmentosa |
| NCT01233609 | PHASE2 | COMPLETED | Trial of Oral Valproic Acid for Retinitis Pigmentosa |
| NCT01399515 | PHASE2 | COMPLETED | Efficacy and Safety of Oral Valproic Acid for Retinitis Pigmentosa |
| NCT01530659 | PHASE2 | COMPLETED | Retinal Imaging in CNTF -Releasing Encapsulated Cell Implant Treated Patients for Early-stage Retinitis Pigmentosa |
| NCT01560715 | PHASE2 | COMPLETED | Autologous Bone Marrow-Derived Stem Cells Transplantation For Retinitis Pigmentosa |
| NCT02609165 | PHASE2 | COMPLETED | Nerve Growth Factor Eye Drops Treatment in Patients With Retinitis Pigmentosa and Cystoid Macular Edema |
| NCT02661711 | PHASE2 | COMPLETED | Aflibercept for Macular Oedema With Underlying Retinitis Pigmentosa (AMOUR) Study |
| NCT02804360 | PHASE2 | UNKNOWN | Intravitreal Dexamethasone Implant in Retinitis Pigmentosa-related Macular Edema- a Retrospective Study |
| NCT02837640 | PHASE2 | UNKNOWN | Studying a Potential Protective Effect of L-Dopa on Retinitis Pigmentosa |
| NCT03073733 | PHASE2 | COMPLETED | Safety and Efficacy of Intravitreal Injection of Human Retinal Progenitor Cells in Adults With Retinitis Pigmentosa |
| NCT04356716 | PHASE2 | COMPLETED | Sildenafil for Treatment of Choroidal Ischemia |
| NCT04604899 | PHASE2 | COMPLETED | Safety of Repeat Intravitreal Injection of Human Retinal Progenitor Cells (jCell) in Adult Subjects With Retinitis Pigmentosa |
| NCT04763369 | PHASE2 | UNKNOWN | Investigation of Therapeutic Efficacy and Safety of UMSCs for the Management of Retinitis Pigmentosa (RP) |
| NCT04864496 | PHASE2 | UNKNOWN | Effects of Treatment With N- Acetylcysteine on Visual Outcomes in Patients With Retinitis Pigmentosa |
| NCT05085964 | PHASE2 | TERMINATED | An Open-Label Extension Study to Evaluate Safety & Tolerability of QR-421a in Subjects With Retinitis Pigmentosa |
| NCT05392179 | PHASE2 | COMPLETED | A Study in Subjects With Retinitis Pigmentosa |
| NCT06627179 | PHASE2 | RECRUITING | Study to Evaluate Ultevursen in Subjects With Retinitis Pigmentosa (RP) Due to Mutations in Exon 13 of the USH2A Gene |
| NCT06628947 | PHASE2 | RECRUITING | A Phase II Study of Intravitreal KIO-301 in Patients With Late-stage Retinitis Pigmentosa |
| NCT06912633 | PHASE2 | RECRUITING | Safety of a Single, Intravitreal Injection of 6.0M jCell (Famzeretcel) in Retinitis Pigmentosa (RP) |
| NCT05902962 | PHASE1 | COMPLETED | SAD of IVT VP-001 in PRPF31 Mutation-Associated Retinal Dystrophy Subjects |
| NCT06319872 | PHASE1 | RECRUITING | The Effects of Disulfiram (Antabuse®) on Visual Acuity in Patients With Retinal Degeneration |
Related Atlas pages
- Associated diseases: cone-rod dystrophy 9, Leber congenital amaurosis 4, ADAM9-related retinopathy
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): cone-rod dystrophy, cone-rod dystrophy 9, hereditary spastic paraplegia 54