ADAMTS7
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Also known as ADAM-TS7DKFZp434H204
Summary
ADAMTS7 (ADAM metallopeptidase with thrombospondin type 1 motif 7, HGNC:223) is a protein-coding gene on chromosome 15q25.1, encoding A disintegrin and metalloproteinase with thrombospondin motifs 7 (Q9UKP4). Metalloprotease.
The protein encoded by this gene is a member of the ADAMTS (a disintegrin and metalloproteinase with thrombospondin motifs) family. Members of this family share several distinct protein modules, including a propeptide region, a metalloproteinase domain, a disintegrin-like domain, and a thrombospondin type 1 (TS) motif. Individual members of this family differ in the number of C-terminal TS motifs, and some have unique C-terminal domains. The encoded preproprotein is proteolytically processed to generate the mature enzyme. This enzyme contains two C-terminal TS motifs and may regulate vascular smooth muscle cell (VSMC) migration. Mutations in this gene may be associated with susceptibility to coronary artery disease.
Source: NCBI Gene 11173 — RefSeq curated summary.
At a glance
- GWAS associations: 83
- Clinical variants (ClinVar): 402 total
- Druggable target: yes
- MANE Select transcript:
NM_014272
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:223 |
| Approved symbol | ADAMTS7 |
| Name | ADAM metallopeptidase with thrombospondin type 1 motif 7 |
| Location | 15q25.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | ADAM-TS7, DKFZp434H204 |
| Ensembl gene | ENSG00000136378 |
| Ensembl biotype | protein_coding |
| OMIM | 605009 |
| Entrez | 11173 |
Gene structure
Transcript identifiers
Ensembl transcripts: 11 — 7 protein_coding, 3 retained_intron, 1 protein_coding_CDS_not_defined
ENST00000388820, ENST00000565793, ENST00000566303, ENST00000568712, ENST00000569934, ENST00000917170, ENST00000917171, ENST00000917172, ENST00000972106, ENST00000972107, ENST00000972108
RefSeq mRNA: 1 — MANE Select: NM_014272
NM_014272
CCDS: CCDS32303
Canonical transcript exons
ENST00000388820 — 24 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000942809 | 78771585 | 78771829 |
| ENSE00001161375 | 78811121 | 78811464 |
| ENSE00001207358 | 78767379 | 78767592 |
| ENSE00001207445 | 78771162 | 78771303 |
| ENSE00001593573 | 78759206 | 78759578 |
| ENSE00001603311 | 78763699 | 78763845 |
| ENSE00001647921 | 78765645 | 78767051 |
| ENSE00001692702 | 78763926 | 78764099 |
| ENSE00001725652 | 78762403 | 78762565 |
| ENSE00001753106 | 78764555 | 78764707 |
| ENSE00003506582 | 78776749 | 78776841 |
| ENSE00003511965 | 78774167 | 78774300 |
| ENSE00003521526 | 78791140 | 78791223 |
| ENSE00003535197 | 78776188 | 78776333 |
| ENSE00003542882 | 78790670 | 78790794 |
| ENSE00003556999 | 78789689 | 78789838 |
| ENSE00003570807 | 78788231 | 78788374 |
| ENSE00003595990 | 78797948 | 78798113 |
| ENSE00003603457 | 78774624 | 78774793 |
| ENSE00003644817 | 78796590 | 78796786 |
| ENSE00003688907 | 78800192 | 78800547 |
| ENSE00003692389 | 78773083 | 78773203 |
| ENSE00003692472 | 78777444 | 78777588 |
| ENSE00003693704 | 78768133 | 78768259 |
Expression profiles
Bgee: expression breadth ubiquitous, 151 present calls, max score 92.69.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 6.5979 / max 176.7369, expressed in 1168 samples.
FANTOM5 promoters (4 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 151129 | 5.5481 | 1129 |
| 151128 | 0.5390 | 251 |
| 151127 | 0.3791 | 201 |
| 151130 | 0.1316 | 30 |
Top tissues by expression
245 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| right atrium auricular region | UBERON:0006631 | 92.69 | gold quality |
| cardiac atrium | UBERON:0002081 | 91.36 | gold quality |
| apex of heart | UBERON:0002098 | 89.32 | gold quality |
| stromal cell of endometrium | CL:0002255 | 86.98 | gold quality |
| ganglionic eminence | UBERON:0004023 | 86.88 | gold quality |
| right coronary artery | UBERON:0001625 | 86.11 | gold quality |
| ascending aorta | UBERON:0001496 | 84.06 | gold quality |
| thoracic aorta | UBERON:0001515 | 83.66 | gold quality |
| heart | UBERON:0000948 | 82.06 | gold quality |
| heart left ventricle | UBERON:0002084 | 82.06 | gold quality |
| left coronary artery | UBERON:0001626 | 81.95 | gold quality |
| cardiac ventricle | UBERON:0002082 | 80.95 | gold quality |
| coronary artery | UBERON:0001621 | 80.03 | gold quality |
| aorta | UBERON:0000947 | 79.73 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 79.59 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 78.58 | gold quality |
| cortical plate | UBERON:0005343 | 78.14 | gold quality |
| sural nerve | UBERON:0015488 | 77.99 | gold quality |
| right adrenal gland | UBERON:0001233 | 77.56 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 77.53 | gold quality |
| tibial nerve | UBERON:0001323 | 77.19 | gold quality |
| popliteal artery | UBERON:0002250 | 77.15 | gold quality |
| tibial artery | UBERON:0007610 | 77.12 | gold quality |
| left adrenal gland | UBERON:0001234 | 77.09 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 77.07 | gold quality |
| right ovary | UBERON:0002118 | 77.00 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 76.16 | gold quality |
| body of uterus | UBERON:0009853 | 76.12 | gold quality |
| omental fat pad | UBERON:0010414 | 76.05 | gold quality |
| peritoneum | UBERON:0002358 | 75.98 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 5.64 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): HR, HTATIP2, SSRP1, TFAP2A, ZBTB16
miRNA regulators (miRDB)
24 targeting ADAMTS7, 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-29A-3P | 100.00 | 73.11 | 1835 |
| HSA-MIR-29B-3P | 100.00 | 73.18 | 1833 |
| HSA-MIR-29C-3P | 100.00 | 73.15 | 1833 |
| HSA-MIR-3924 | 100.00 | 72.09 | 2394 |
| HSA-MIR-767-5P | 99.95 | 70.85 | 993 |
| HSA-MIR-6753-3P | 99.93 | 66.57 | 637 |
| HSA-MIR-7107-3P | 99.93 | 66.73 | 627 |
| HSA-MIR-5682 | 99.89 | 72.56 | 1005 |
| HSA-MIR-7162-3P | 99.89 | 68.16 | 1682 |
| HSA-MIR-380-3P | 99.89 | 70.18 | 1978 |
| HSA-MIR-4495 | 99.82 | 72.08 | 3080 |
| HSA-MIR-4729 | 99.69 | 72.18 | 4233 |
| HSA-MIR-379-3P | 99.69 | 69.60 | 1524 |
| HSA-MIR-411-3P | 99.69 | 69.63 | 1524 |
| HSA-MIR-548G-3P | 99.48 | 68.67 | 2159 |
| HSA-MIR-6871-3P | 99.43 | 68.85 | 741 |
| HSA-MIR-5589-5P | 98.34 | 64.82 | 1148 |
| HSA-MIR-6782-3P | 97.60 | 67.75 | 931 |
| HSA-MIR-585-5P | 97.54 | 69.02 | 955 |
| HSA-MIR-596 | 97.48 | 63.13 | 469 |
| HSA-MIR-6849-3P | 97.25 | 64.57 | 1371 |
| HSA-MIR-541-3P | 96.07 | 66.11 | 1271 |
| HSA-MIR-654-5P | 96.07 | 66.18 | 1280 |
| HSA-MIR-6734-5P | 95.70 | 65.56 | 950 |
Literature-anchored findings (GeneRIF, showing 40)
- ADAMTS-7 is the first metalloproteinase found to bind directly to and degrade COMP (PMID:16585064)
- ADAMTS-7 and ADAMTS-12 are newly identified enzymes responsible for cartilage oligomeric matrix protein degradation in arthritis. (PMID:19098927)
- Findings demonstrate that ADAMTS-7, a direct target of PTHrP signaling, negatively regulates endochondral bone formation by associating with and inactivating GEP chondrogenic growth factor. (PMID:19487464)
- identified ADAMTS7 as novel locus for CAD and association of ABO with MI in the presence of CAD (PMID:21239051)
- statistically significant increase in mRNA expression of ADAMTS-7 and ADAMTS-12 was observed in the endplate cells in degenerative discs compared with nondegenerative discs (PMID:22247065)
- There was a reduction in the amount of cleaved ADAMTS7 prodomain in media conditioned by VSMCs of the G/G genotype. (PMID:23415669)
- Data conclude that ADAMTS-7 level appears to be positively associated with expression of TNF-alpha and Phospho-NF-kappaB P65 in cartilage, which may imply its association with cartilage destruction of ONFH. (PMID:25653475)
- ADAMTS7 localized to cells having smooth muscle cell markers in human coronary artery disease lesions. Cultured vascular smooth muscle cells had ADAMTS7 at the cytoplasm and cell membrane, where it colocalized with markers of podosomes. (PMID:25712206)
- Logistic regression analysis indicated that the association between ADAMTS-7 and heart failure after AMI was independent from traditional cardiovascular risk factors and other biomarkers (PMID:25885961)
- The significant associations observed between this coding variant in ADAMTS7 and the risk of CAD development. (PMID:26189211)
- Our results indicate the presence of ADAMTS-7 in human NP cells and imply its potential role in disc degeneration. (PMID:26446668)
- miR-105/Runx2 axis mediates FGF2-induced ADAMTS expression in osteoarthritis cartilage. (PMID:26816250)
- The main contribution of this study is the proposal of a pharmacophore for ADAMTS7. (PMID:26872430)
- Expression of miR-26a and miR-29a was significantly down regulated in leukoplakia and cancer tissues but up regulated in lichen planus tissues. Expression of target genes such as, ADAMTS7, ATP1B1, COL4A2, CPEB3, CDK6, DNMT3a and PI3KR1 was significantly down regulated in at least two of three disease types with respect to normal tissues. (PMID:27515006)
- During inflammatory conditions, AP-1 and Sp1 sustained the expression of ADAMTS7, and ADAMTS7 sustained the expression of catabolic genes in nucleus pulposus cells (PMID:27516213)
- The native overfunctional ADAMTS7 allele (A) may accelerate VSMC migration and lead to neointimal thickening, atherosclerosis progression and acute plaque events. (PMID:27614204)
- ADAMTS7 and LPA single nucleotide polymorphisms are related to a 24-h ambulatory systolic-diastolic pressure regression index. (PMID:28092973)
- Studied gene expression of genetic variants of ADAMTS7 in atherosclerotic occlusive peripheral arterial disease (PAD). Found mRNA levels of ADAMTS7 to be significantly higher in PAD patients than controls, and that the rs1994016 CC and rs3825807 TT genotypes may upregulate ADAMTS7 mRNA levels and may influence PAD development. (PMID:28205274)
- Allelic variation that associates with reduced ADAMTS7 expression confers stronger coronary heart disease protection in never-smokers than in ever-smokers. (PMID:28461624)
- data show that ADAMTS-7 is associated with a vulnerable plaque phenotype in human carotid lesions. These data support previous observations of a potential proatherogenic role of ADAMTS-7. (PMID:28623250)
- The findings suggest that upregulation of ADAMTS-7 and down regulation of COMP are associated with human AA. (PMID:28849199)
- Genetic variation at the ADAMTS7 locus is associated with reduced severity of coronary artery disease. (PMID:29089340)
- Multivariate analysis showed that DeltaADAMTS-7(day 7 minus day 1) was independently associated with left ventricular reverse remodeling (PMID:29523183)
- Degenerated human biceps tendons had reduced ADAMTS7 mRNA compared with healthy biceps tendons, which expressed both ADAMTS7 and ADAMTS12. These results suggest that ADAMTS7 and ADAMTS12 may be essential for human tendon health. (PMID:29618652)
- Serum ADAMTS7 level is positively associated with acute coronary syndrome, and patients with the CT/TT genotype at the rs1994016 allele are less prone to suffer from ACS. (PMID:29980058)
- presents the expression levels of ADAMTS-7 and COMP in the decidual tissues of mice and humans suffering from SA. (PMID:30720083)
- findings reveal LTBP4 as an ADAMTS7 substrate, whose cleavage may potentially impact elastogenesis in the cardiovascular system. (PMID:30926607)
- ADAMTS7 tagSNP rs3825807 contributes to MI susceptibility in the Chinese Han population. (PMID:31292280)
- Genetic variants of ADAMTS7 confer risk for ischaemic stroke in the Chinese population. (PMID:31460868)
- ADAMTS7 polymorphisms of both rs7173743 and rs3825807 were associated with carotid plaque vulnerability but not the prevalence of ischemic stroke. The T/T genotype of rs7173743 and A/A genotype of rs3825807 were considered as risk genotypes for vulnerable plaque susceptibility. In conclusion, ADAMTS7 variants rs3825807 and rs7173743 are associated with the risk for carotid plaque vulnerability. (PMID:31651847)
- Data show that common variants in A disintegrin and metalloproteinase with thrombospondin motifs 7 protein (ADAMTS7) and zinc finger, C3HC-type containing 1 protein (ZC3HC1) genes contribute to an increased risk for both coronary artery disease (CAD) and large artery ischemic stroke (LA atherosclerotic) IS. (PMID:31679296)
- Upregulation of miR423 improves autologous vein graft restenosis via targeting ADAMTS7. (PMID:31894258)
- Effect of a coronary-heart-disease-associated variant of ADAMTS7 on endothelial cell angiogenesis. (PMID:32005000)
- ADATMS-7 regulates the focal adhesion kinase signaling and promotes invasiveness of trophoblasts in early pregnancy. (PMID:32148246)
- Hypomethylation of DNA promoter upregulates ADAMTS7 and contributes to HTR-8/SVneo and JEG-3 cells abnormalities in pre-eclampsia. (PMID:32250736)
- ADAMTS7 degrades Comp to fuel BMP2-dependent osteogenic differentiation and ameliorate oncogenic potential in osteosarcomas. (PMID:32692461)
- Association of polymorphisms in ADAMTS-7 gene with the susceptibility to coronary artery disease - a systematic review and meta-analysis. (PMID:33122452)
- Coronary Disease Association With ADAMTS7 Is Due to Protease Activity. (PMID:34176299)
- Genome-wide pleiotropy analysis of coronary artery disease and pneumonia identifies shared immune pathways. (PMID:35452290)
- miR-654-5p Suppresses Migration and Proliferation of Vascular Smooth Muscle Cells by Targeting ADAMTS-7. (PMID:35462367)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | adamts7 | ENSDARG00000102478 |
| mus_musculus | Adamts7 | ENSMUSG00000032363 |
| rattus_norvegicus | Adamts7 | ENSRNOG00000028036 |
Paralogs (25): ADAMTS6 (ENSG00000049192), ADAMTS2 (ENSG00000087116), PAPLN (ENSG00000100767), ADAMTS8 (ENSG00000134917), ADAMTS14 (ENSG00000138316), ADAMTS17 (ENSG00000140470), ADAMTS18 (ENSG00000140873), ADAMTS10 (ENSG00000142303), ADAMTSL4 (ENSG00000143382), ADAMTS16 (ENSG00000145536), ADAMTS19 (ENSG00000145808), ADAMTS12 (ENSG00000151388), ADAMTS1 (ENSG00000154734), ADAMTS5 (ENSG00000154736), ADAMTS3 (ENSG00000156140), ADAMTSL3 (ENSG00000156218), ADAMTS4 (ENSG00000158859), ADAMTS13 (ENSG00000160323), ADAMTS9 (ENSG00000163638), ADAMTS15 (ENSG00000166106), ADAMTS20 (ENSG00000173157), ADAMTSL1 (ENSG00000178031), ADAMTSL5 (ENSG00000185761), THSD4 (ENSG00000187720), ADAMTSL2 (ENSG00000197859)
Protein
Protein identifiers
A disintegrin and metalloproteinase with thrombospondin motifs 7 — Q9UKP4 (reviewed: Q9UKP4)
All UniProt accessions (1): Q9UKP4
UniProt curated annotations — full annotation on UniProt →
Function. Metalloprotease. Was previously shown to degrade COMP. However, a later study found no activity against COMP.
Subunit / interactions. Interacts with COMP.
Subcellular location. Secreted. Extracellular space. Extracellular matrix.
Tissue specificity. Expressed in heart, brain, placenta, lung, liver, skeletal muscle, kidney and pancreas. Detected in meniscus, bone, tendon, cartilage, synovium, fat and ligaments.
Post-translational modifications. N-glycosylated. Can be O-fucosylated by POFUT2 on a serine or a threonine residue found within the consensus sequence C1-X(2)-(S/T)-C2-G of the TSP type-1 repeat domains where C1 and C2 are the first and second cysteine residue of the repeat, respectively. Fucosylated repeats can then be further glycosylated by the addition of a beta-1,3-glucose residue by the glucosyltransferase, B3GALTL. Fucosylation mediates the efficient secretion of ADAMTS family members. Can also be C-glycosylated with one or two mannose molecules on tryptophan residues within the consensus sequence W-X-X-W of the TPRs. N- and C-glycosylations can also facilitate secretion. O-glycosylated proteoglycan; contains chondroitin sulfate. May be cleaved by a furin endopeptidase. The precursor is sequentially processed.
Cofactor. Binds 1 zinc ion per subunit.
Domain organisation. The spacer domain and the TSP type-1 domains are important for a tight interaction with the extracellular matrix. 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.
Induction. Up-regulated in articular cartilage and synovium from arthritis patients.
RefSeq proteins (1): NP_055087* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000884 | TSP1_rpt | Repeat |
| IPR001590 | Peptidase_M12B | Domain |
| IPR002870 | Peptidase_M12B_N | Domain |
| IPR010294 | ADAMTS_spacer1 | Domain |
| IPR010909 | PLAC | Domain |
| IPR013273 | ADAMTS/ADAMTS-like | Family |
| IPR024079 | MetalloPept_cat_dom_sf | Homologous_superfamily |
| IPR036383 | TSP1_rpt_sf | Homologous_superfamily |
| IPR041645 | ADAMTS_CR_2 | Domain |
| IPR045371 | ADAMTS_CR_3 | Domain |
| IPR050439 | ADAMTS_ADAMTS-like | Family |
Pfam: PF00090, PF01421, PF01562, PF05986, PF17771, PF19030, PF19236
UniProt features (52 total): domain 11, disulfide bond 11, region of interest 5, sequence variant 5, sequence conflict 5, binding site 4, compositionally biased region 3, glycosylation site 3, signal peptide 1, propeptide 1, short sequence motif 1, chain 1, active site 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9UKP4-F1 | 64.26 | 0.08 |
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 (1): 389
Ligand- & substrate-binding residues (4): 204 (in inhibited form); 388; 392; 398
Disulfide bonds (11): 318–372, 347–354, 366–447, 405–431, 474–497, 485–503, 492–522, 516–527, 550–587, 554–592, 565–577
Glycosylation sites (3): 94, 693, 778
Function
Pathways and Gene Ontology
Reactome pathways
9 pathways
| ID | Pathway |
|---|---|
| R-HSA-5083635 | Defective B3GALTL causes PpS |
| R-HSA-5173214 | O-glycosylation of TSR domain-containing proteins |
| R-HSA-1643685 | Disease |
| R-HSA-3781865 | Diseases of glycosylation |
| R-HSA-3906995 | Diseases associated with O-glycosylation of proteins |
| R-HSA-392499 | Metabolism of proteins |
| R-HSA-5173105 | O-linked glycosylation |
| R-HSA-5668914 | Diseases of metabolism |
| R-HSA-597592 | Post-translational protein modification |
MSigDB gene sets: 106 (showing top):
GOBP_COLLAGEN_FIBRIL_ORGANIZATION, GOBP_CARTILAGE_DEVELOPMENT, GOBP_SKELETAL_SYSTEM_DEVELOPMENT, GOMF_METALLOPEPTIDASE_ACTIVITY, GOBP_REGULATION_OF_CARTILAGE_DEVELOPMENT, GOBP_RESPONSE_TO_PEPTIDE, SP3_Q3, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_UP, GOBP_MACROMOLECULE_CATABOLIC_PROCESS, GOCC_CELL_SURFACE, GOBP_CARBOHYDRATE_DERIVATIVE_METABOLIC_PROCESS, TERAMOTO_OPN_TARGETS_CLUSTER_6, GOBP_ANATOMICAL_STRUCTURE_MATURATION, GOBP_BONE_DEVELOPMENT
GO Biological Process (12): chondrocyte differentiation (GO:0002062), proteoglycan metabolic process (GO:0006029), proteolysis (GO:0006508), extracellular matrix organization (GO:0030198), collagen fibril organization (GO:0030199), negative regulation of chondrocyte differentiation (GO:0032331), ossification involved in bone maturation (GO:0043931), obsolete proteolysis involved in protein catabolic process (GO:0051603), cellular response to interleukin-1 (GO:0071347), cellular response to tumor necrosis factor (GO:0071356), cellular response to BMP stimulus (GO:0071773), ossification (GO:0001503)
GO Molecular Function (6): metalloendopeptidase activity (GO:0004222), metallopeptidase activity (GO:0008237), metal ion binding (GO:0046872), protein binding (GO:0005515), peptidase activity (GO:0008233), hydrolase activity (GO:0016787)
GO Cellular Component (4): endoplasmic reticulum lumen (GO:0005788), cell surface (GO:0009986), extracellular matrix (GO:0031012), extracellular region (GO:0005576)
Reactome top-level categories
Rollup of top-7 pathways:
| Category | Pathways |
|---|---|
| Diseases associated with O-glycosylation of proteins | 1 |
| O-linked glycosylation | 1 |
| Diseases of metabolism | 1 |
| Diseases of glycosylation | 1 |
| Post-translational protein modification | 1 |
| Disease | 1 |
| Metabolism of proteins | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular response to cytokine stimulus | 2 |
| cellular anatomical structure | 2 |
| cell differentiation | 1 |
| cartilage development | 1 |
| glycoprotein metabolic process | 1 |
| protein metabolic process | 1 |
| extracellular structure organization | 1 |
| external encapsulating structure organization | 1 |
| extracellular matrix organization | 1 |
| chondrocyte differentiation | 1 |
| regulation of chondrocyte differentiation | 1 |
| negative regulation of cell differentiation | 1 |
| negative regulation of cartilage development | 1 |
| ossification | 1 |
| bone maturation | 1 |
| response to interleukin-1 | 1 |
| response to tumor necrosis factor | 1 |
| cellular response to growth factor stimulus | 1 |
| response to BMP | 1 |
| multicellular organismal process | 1 |
| endopeptidase activity | 1 |
| metallopeptidase activity | 1 |
| peptidase activity | 1 |
| cation binding | 1 |
| binding | 1 |
| hydrolase activity | 1 |
| catalytic activity, acting on a protein | 1 |
| catalytic activity | 1 |
| endoplasmic reticulum | 1 |
| intracellular organelle lumen | 1 |
| external encapsulating structure | 1 |
Protein interactions and networks
STRING
906 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| ADAMTS7 | COMP | P49747 | 912 |
| ADAMTS7 | FURIN | P09958 | 744 |
| ADAMTS7 | PHACTR1 | Q9C0D0 | 702 |
| ADAMTS7 | GRN | P23781 | 691 |
| ADAMTS7 | A2M | P01023 | 545 |
| ADAMTS7 | COL4A2 | P08572 | 528 |
| ADAMTS7 | MMP9 | P14780 | 521 |
| ADAMTS7 | PTHLH | P12272 | 521 |
| ADAMTS7 | HHIPL1 | Q96JK4 | 515 |
| ADAMTS7 | ZC3HC1 | Q86WB0 | 507 |
| ADAMTS7 | JCAD | Q9P266 | 507 |
| ADAMTS7 | ADAMTS12 | P58397 | 495 |
| ADAMTS7 | MMP2 | P08253 | 482 |
| ADAMTS7 | ACAN | P16112 | 481 |
| ADAMTS7 | SORT1 | Q99523 | 446 |
IntAct
59 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CRIPTO | AIP | psi-mi:“MI:0914”(association) | 0.640 |
| FBXO6 | MAN2B1 | psi-mi:“MI:0914”(association) | 0.640 |
| FBXO2 | TMEM131L | psi-mi:“MI:0914”(association) | 0.530 |
| CTSG | MANBA | psi-mi:“MI:0914”(association) | 0.530 |
| CMA1 | MANBA | psi-mi:“MI:0914”(association) | 0.530 |
| TIMP3 | ZZEF1 | psi-mi:“MI:0914”(association) | 0.530 |
| A2M | ADAMTS7 | psi-mi:“MI:0570”(protein cleavage) | 0.440 |
| ADAMTS7 | COMP | psi-mi:“MI:0570”(protein cleavage) | 0.440 |
| HTRA1 | ADAMTS7 | psi-mi:“MI:0915”(physical association) | 0.370 |
| Comp | ADAMTS7 | psi-mi:“MI:0915”(physical association) | 0.370 |
| SCGB2A2 | RTL8C | psi-mi:“MI:0914”(association) | 0.350 |
| GPIHBP1 | SAC3D1 | psi-mi:“MI:0914”(association) | 0.350 |
| IGFL3 | CBX4 | psi-mi:“MI:0914”(association) | 0.350 |
| DEFB136 | MANBA | psi-mi:“MI:0914”(association) | 0.350 |
| VEGFD | RPSA2 | psi-mi:“MI:0914”(association) | 0.350 |
| LY86 | TMEM131L | psi-mi:“MI:0914”(association) | 0.350 |
| IL5RA | POTEF | psi-mi:“MI:0914”(association) | 0.350 |
| NCR3 | POTEF | psi-mi:“MI:0914”(association) | 0.350 |
| LYPD4 | POTEF | psi-mi:“MI:0914”(association) | 0.350 |
| CFC1 | POTEF | psi-mi:“MI:0914”(association) | 0.350 |
| EDN3 | POTEF | psi-mi:“MI:0914”(association) | 0.350 |
| PI15 | psi-mi:“MI:0914”(association) | 0.350 | |
| MFAP4 | QSOX1 | psi-mi:“MI:0914”(association) | 0.350 |
| CA6 | QSOX1 | psi-mi:“MI:0914”(association) | 0.350 |
| ELSPBP1 | QSOX1 | psi-mi:“MI:0914”(association) | 0.350 |
| PRG2 | QSOX1 | psi-mi:“MI:0914”(association) | 0.350 |
| DNASE1L1 | QSOX1 | psi-mi:“MI:0914”(association) | 0.350 |
| INHBE | MANBA | psi-mi:“MI:0914”(association) | 0.350 |
| PRTN3 | MANBA | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (56): ADAMTS7 (Affinity Capture-MS), ADAMTS7 (Affinity Capture-MS), ADAMTS7 (Affinity Capture-MS), ADAMTS7 (Affinity Capture-MS), ADAMTS7 (Affinity Capture-MS), ADAMTS7 (Affinity Capture-MS), ADAMTS7 (Affinity Capture-MS), ADAMTS7 (Affinity Capture-MS), ADAMTS7 (Affinity Capture-MS), ADAMTS7 (Affinity Capture-MS), ADAMTS7 (Affinity Capture-MS), ADAMTS7 (Affinity Capture-MS), ADAMTS7 (Affinity Capture-MS), ADAMTS7 (Affinity Capture-MS), ADAMTS7 (Affinity Capture-MS)
ESM2 similar proteins: A1A5Y0, A1KZ92, A2AJ76, B0S5N4, D3YXG0, D3ZPX4, F1MMS9, O00187, O55005, O60500, O75093, O88279, O88280, P11627, P17852, P26006, P32004, P51805, P57110, P59511, P70208, P85171, Q05695, Q0PMG2, Q13219, Q3UH53, Q4KMG0, Q62470, Q62918, Q7Z5N4, Q80TR4, Q8AV58, Q8AXZ4, Q8CIY2, Q8HZK2, Q8HZK3, Q8NDA2, Q8R4K8, Q8TE57, Q91WP0
Diamond homologs: A2VEC9, B3EWY9, B3EWZ3, B3EWZ8, C0HL12, C5IAW9, D3YXF5, D3YXG0, D3Z7H8, D3ZTD8, E9Q6D8, F1LW30, G1FC92, G5ECS8, O08721, O08722, O08747, O14514, O15072, O60241, O60242, O95185, O95450, P07358, P07996, P10643, P11680, P13671, P27918, P35440, P35441, P35442, P35448, P48960, P55314, P57110, P58397, P59384, P61134, P61135
SIGNOR signaling
0 interactions.
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 85 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 |
|---|---|---|---|
| Degradation of the extracellular matrix | 8 | 16.8× | 6e-06 |
| Post-translational modification: synthesis of GPI-anchored proteins | 5 | 15.0× | 2e-03 |
| Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs) | 6 | 9.3× | 3e-03 |
| Extracellular matrix organization | 8 | 9.0× | 4e-04 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
402 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 319 |
| Likely benign | 40 |
| Benign | 9 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
5192 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 15:78762563:GCA:G | acceptor_gain | 1.0000 |
| 15:78762564:CA:C | acceptor_gain | 1.0000 |
| 15:78762564:CAC:C | acceptor_gain | 1.0000 |
| 15:78762566:C:CC | acceptor_gain | 1.0000 |
| 15:78768257:CAC:C | acceptor_gain | 1.0000 |
| 15:78773085:AGGC:A | donor_gain | 1.0000 |
| 15:78773097:T:TA | donor_gain | 1.0000 |
| 15:78773115:A:AC | donor_gain | 1.0000 |
| 15:78773116:C:CC | donor_gain | 1.0000 |
| 15:78773199:ACGTT:A | acceptor_gain | 1.0000 |
| 15:78773200:CGTT:C | acceptor_gain | 1.0000 |
| 15:78773200:CGTTC:C | acceptor_gain | 1.0000 |
| 15:78773202:TT:T | acceptor_gain | 1.0000 |
| 15:78773203:TC:T | acceptor_loss | 1.0000 |
| 15:78773204:C:CC | acceptor_gain | 1.0000 |
| 15:78773204:C:T | acceptor_loss | 1.0000 |
| 15:78774151:T:TA | donor_gain | 1.0000 |
| 15:78774165:A:AT | donor_loss | 1.0000 |
| 15:78774166:C:CT | donor_loss | 1.0000 |
| 15:78774170:A:AC | donor_gain | 1.0000 |
| 15:78774171:C:CC | donor_gain | 1.0000 |
| 15:78774297:TTCA:T | acceptor_gain | 1.0000 |
| 15:78774298:TCA:T | acceptor_gain | 1.0000 |
| 15:78774299:CA:C | acceptor_gain | 1.0000 |
| 15:78774299:CAC:C | acceptor_gain | 1.0000 |
| 15:78774299:CACT:C | acceptor_loss | 1.0000 |
| 15:78774301:C:CC | acceptor_gain | 1.0000 |
| 15:78774302:T:A | acceptor_loss | 1.0000 |
| 15:78774310:C:CT | acceptor_gain | 1.0000 |
| 15:78774310:C:T | acceptor_gain | 1.0000 |
AlphaMissense
10925 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 15:78776818:G:C | C497W | 0.999 |
| 15:78776819:C:G | C497S | 0.999 |
| 15:78776820:A:T | C497S | 0.999 |
| 15:78776821:C:A | W496C | 0.999 |
| 15:78776821:C:G | W496C | 0.999 |
| 15:78777490:C:G | C474S | 0.999 |
| 15:78777491:A:T | C474S | 0.999 |
| 15:78788269:C:A | W428C | 0.999 |
| 15:78788269:C:G | W428C | 0.999 |
| 15:78788271:A:G | W428R | 0.999 |
| 15:78788271:A:T | W428R | 0.999 |
| 15:78763932:C:A | W1529C | 0.998 |
| 15:78763932:C:G | W1529C | 0.998 |
| 15:78771753:G:C | F736L | 0.998 |
| 15:78771753:G:T | F736L | 0.998 |
| 15:78771755:A:G | F736L | 0.998 |
| 15:78771756:G:C | N735K | 0.998 |
| 15:78771756:G:T | N735K | 0.998 |
| 15:78774643:C:A | W619C | 0.998 |
| 15:78774643:C:G | W619C | 0.998 |
| 15:78776329:C:G | C522S | 0.998 |
| 15:78776330:A:T | C522S | 0.998 |
| 15:78776820:A:G | C497R | 0.998 |
| 15:78777489:G:C | C474W | 0.998 |
| 15:78777490:C:A | C474F | 0.998 |
| 15:78777491:A:G | C474R | 0.998 |
| 15:78788257:G:C | S432R | 0.998 |
| 15:78788257:G:T | S432R | 0.998 |
| 15:78788259:T:G | S432R | 0.998 |
| 15:78789751:G:C | C372W | 0.998 |
dbSNP variants (sampled 300 via entrez): RS1000008302 (15:78799052 C>A), RS1000179486 (15:78758934 C>T), RS1000282700 (15:78768265 G>A), RS1000411137 (15:78807100 G>A), RS1000446333 (15:78798714 G>A), RS1000691907 (15:78787599 G>A), RS1001032532 (15:78773940 G>A), RS1001067907 (15:78811425 A>G), RS1001185856 (15:78778798 G>C,T), RS1001438428 (15:78811614 C>G,T), RS1001453031 (15:78769836 A>G), RS1001531099 (15:78807001 A>G,T), RS1001789361 (15:78794181 G>C), RS1001863400 (15:78808138 G>A), RS1001961930 (15:78806764 G>A)
Disease associations
OMIM: gene MIM:605009 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
83 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST000945_1 | Coronary artery disease | 5.000000e-13 |
| GCST000998_21 | Coronary heart disease | 1.000000e-12 |
| GCST000999_1 | Coronary heart disease | 4.000000e-09 |
| GCST001902_1 | Coronary artery calcification | 7.000000e-06 |
| GCST002287_9 | Coronary artery disease or ischemic stroke | 2.000000e-09 |
| GCST002289_17 | Coronary artery disease | 7.000000e-08 |
| GCST002290_16 | Coronary artery disease or large artery stroke | 2.000000e-08 |
| GCST003116_16 | Coronary artery disease | 4.000000e-16 |
| GCST003117_31 | Myocardial infarction | 3.000000e-09 |
| GCST003262_1010 | Post bronchodilator FEV1 | 8.000000e-07 |
| GCST003262_1025 | Post bronchodilator FEV1 | 7.000000e-07 |
| GCST003262_1027 | Post bronchodilator FEV1 | 1.000000e-06 |
| GCST003262_1116 | Post bronchodilator FEV1 | 4.000000e-06 |
| GCST003262_1117 | Post bronchodilator FEV1 | 5.000000e-06 |
| GCST003262_1126 | Post bronchodilator FEV1 | 2.000000e-06 |
| GCST003262_157 | Post bronchodilator FEV1 | 7.000000e-07 |
| GCST003262_37 | Post bronchodilator FEV1 | 3.000000e-06 |
| GCST003262_65 | Post bronchodilator FEV1 | 3.000000e-06 |
| GCST003262_670 | Post bronchodilator FEV1 | 3.000000e-06 |
| GCST003262_782 | Post bronchodilator FEV1 | 7.000000e-08 |
| GCST003262_787 | Post bronchodilator FEV1 | 2.000000e-07 |
| GCST003262_802 | Post bronchodilator FEV1 | 1.000000e-06 |
| GCST003262_831 | Post bronchodilator FEV1 | 2.000000e-07 |
| GCST003262_954 | Post bronchodilator FEV1 | 2.000000e-06 |
| GCST003262_955 | Post bronchodilator FEV1 | 2.000000e-06 |
| GCST003264_1119 | Post bronchodilator FEV1/FVC ratio | 5.000000e-07 |
| GCST003264_1124 | Post bronchodilator FEV1/FVC ratio | 9.000000e-07 |
| GCST003264_1183 | Post bronchodilator FEV1/FVC ratio | 1.000000e-06 |
| GCST003264_1240 | Post bronchodilator FEV1/FVC ratio | 4.000000e-07 |
| GCST003264_1241 | Post bronchodilator FEV1/FVC ratio | 5.000000e-07 |
EFO canonical traits (8, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004723 | coronary artery calcification |
| EFO:0004314 | forced expiratory volume |
| EFO:0004713 | FEV/FVC ratio |
| EFO:0006336 | diastolic blood pressure |
| EFO:0004318 | smoking behavior |
| EFO:0004340 | body mass index |
| EFO:0005763 | pulse pressure measurement |
| EFO:0009369 | diffusing capacity of the lung for carbon monoxide |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL5724789 (SINGLE PROTEIN)
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 |
|---|---|---|---|
| BAY-9835 | Inhibition | 8.24 | pIC50 |
Binding affinities (BindingDB)
241 measured of 269 human assays (269 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| Ent-4’,5-Dichloro-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}[Biphenyl]-2-Carboxamide | IC50 | 463 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-5-Chloro-4’-Methyl-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}[Biphenyl]-2-Carboxamide | IC50 | 510 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-4-Fluoro-4’-Methyl-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}[Biphenyl]-2-Carboxamide | IC50 | 705 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-5-Chloro-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 728 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-4’-Chloro-4-Fluoro-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}[Biphenyl]-2-Carboxamide | IC50 | 830 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-5-Methyl-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 1020 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-4-Fluoro-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 1150 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| 4’-(2,2-Difluorocyclopropyl)-5-Methyl-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}[1,1’-Biphenyl]-2-Carboxamide (Mixture of Diastereoisomers) | IC50 | 1300 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-6-Fluoro-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 1300 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-4’,6-Dimethyl-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazoidin-4-Yl]Methyl}[1,1’-Biphenyl]-2-Carboxamide | IC50 | 1400 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-4’,5-Dichloro-N-{[4-(1-Methyl-1H-Pyrazol-5-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}[Biphenyl]-2-Carboxamide | IC50 | 1570 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-6-Methyl-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[1,1’-Biphenyl]-2-Carboxamide | IC50 | 1600 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-5-Fluoro-4’-Methyl-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}[Biphenyl]-2-Carboxamide | IC50 | 1700 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| N-[[4-(1-methylimidazol-2-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | IC50 | 1840 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-5-Fluoro-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 1850 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-4’-Methyl-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}[Biphenyl]-2-Carboxamide | IC50 | 1900 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-5-Methyl-N-{[4-(5-Methyl-1,3-Thiazol-4-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 1900 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-N-[(4-Cyclobutyl-2,5-Dioxoimidazolidin-4-Yl)Methyl]-5-Methyl-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 2000 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-5-Chloro-N-{[4-(1,5-Dimethyl-1H-Pyrazol-4-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 2100 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| 4’-(2,2-Difluorocyclopropyl)-4-Fluoro-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}[1,1’-Biphenyl]-2-Carboxamide (Mixture of Diastereoisomers) | IC50 | 2100 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| 4’-Cyclobutyl-N-{[(4R)-4-Cyclopropyl-2,5-Dioxoimidazolidin-4-Yl]Methyl}[Biphenyl]-2-Carboxamide | IC50 | 2200 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-4’-Chloro-4-Fluoro-N-{[4-(5-Methyl-1,3-Thiazol-4-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}[Biphenyl]-2-Carboxamide | IC50 | 2600 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-N-{[4-(5-Cyclopropyl-1,3-Thiazol-4-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 2700 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-5-Chloro-N-{[4-(1-Methyl-1H-Pyrazol-5-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 2730 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| N-{[(4R)-4-Cyclopropyl-2,5-Dioxoimidazolidin-4-Yl]Methyl}-5,6-Dimethyl-4’-(Trifluoromethyl)[1,1’-Biphenyl]-2-Carboxamide | IC50 | 2800 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| N-{[(4R)-4-Cyclopropyl-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4-Fluoro-4-Methyl[Biphenyl]-2-Carboxamide | IC50 | 2800 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-4’-Chloro-5-Fluoro-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}[Biphenyl]-2-Carboxamide | IC50 | 3000 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| 3-Chloro-N-{[(4R)-4-Cyclopropyl-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-Methyl[1,1’-Biphenyl]-2-Carboxamide | IC50 | 3000 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-2-[6-(Trifluoromethyl)Pyridin-3-Yl]Benzamide | IC50 | 3050 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-4’-Chloro-N-{[4-(5-Methyl-1,3-Thiazol-4-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}[Biphenyl]-2-Carboxamide | IC50 | 3100 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| N-{[(4R)-4-Cyclopropyl-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’,6-Dimethyl[Biphenyl]-2-Carboxamide | IC50 | 3200 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-4-Fluoro-N-{[4-(5-Methyl-1,3-Thiazol-4-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 3250 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| 5-Chloro-N-{[(4R)-4-Cyclopropyl-2,5-Dioxoimidazolidin-4-Yl]Methyl}-6-Fluoro-4’-(Trifluoromethyl)[1,1’-Biphenyl]-2-Carboxamide | IC50 | 3400 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-5-Chloro-N-{[4-(5-Methyl-1,3-Thiazol-4-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 3500 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| 5-Chloro-N-{[(4R)-4-Cyclopropyl-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-Methyl[Biphenyl]-2-Carboxamide | IC50 | 3500 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-4’-Chloro-4-Fluoro-N-{[4-(1-Methyl-1H-Pyrazol-5-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}[Biphenyl]-2-Carboxamide | IC50 | 3550 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| 4’-(2,2-Difluorocyclopropyl)-5-Fluoro-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}[1,1’-Biphenyl]-2-Carboxamide (Mixture of Diastereoisomers) | IC50 | 3600 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-3,4’-Dichloro-N-{[4-(1-Methyl-1H-Pyrazol-5-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}[Biphenyl]-2-Carboxamide | IC50 | 3650 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-5-Chloro-N-{[4-(4-Methyl-1,3-Thiazol-5-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 3700 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| 4’,5-Dichloro-N-{[(4R)-4-Cyclopropyl-2,5-Dioxoimidazolidin-4-Yl]Methyl}[1,1’-Biphenyl]-2-Carboxamide | IC50 | 3700 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-3-Fluoro-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 3750 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-5-Methyl-N-{[4-(4-Methyl-1,3-Thiazol-5-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 3800 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-N-{[4-(5-Cyclopropyl-1,3-Thiazol-4-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-2-[6-(Trifluoromethyl)Pyridin-3-Yl]Benzamide | IC50 | 3800 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| N-{[(4R)-4-Cyclopropyl-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’,5-Dimethyl[Biphenyl]-2-Carboxamide | IC50 | 3900 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-4,5-Difluoro-N-{[4-(1-Methyl-1H-Imidazol-2-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 3950 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| N-{[(4R)-4-Cyclopropyl-2,5-Dioxoimidazolidin-4-Yl]Methyl}-5-Methyl-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 4000 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-4’-Chloro-N-{[4-(1-Methyl-1H-Pyrazol-5-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}[Biphenyl]-2-Carboxamide | IC50 | 4030 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-5-Fluoro-N-{[4-(5-Methyl-1,3-Thiazol-4-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 4130 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Ent-N-{[4-(2,4-Dimethyl-1,3-Thiazol-5-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 4150 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
| Rac-5-Methyl-N-{[4-(5-Methyl-1,3-Thiazol-4-Yl)-2,5-Dioxoimidazolidin-4-Yl]Methyl}-4’-(Trifluoromethyl)[Biphenyl]-2-Carboxamide | IC50 | 4400 nM | US-12398120: Substituted hydantoinamides as ADAMTS7 antagonists |
ChEMBL bioactivities
51 potent at pChembl≥5 of 52 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
50 with measured affinity, of 54 total; 48 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-[[4-(1-methylimidazol-2-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0030 | uM |
| 4-chloro-3-fluoro-N-[[(4S)-4-(2-methylpyrazol-3-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0030 | uM |
| 3-fluoro-N-[[(4S)-4-(2-methylpyrazol-3-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0050 | uM |
| N-[[4-(5-methyl-1,3-thiazol-4-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0060 | uM |
| (2R)-2-(1-benzoylpiperidin-4-yl)-2-[[4-(4-fluorophenyl)phenyl]sulfonylamino]-N-hydroxyacetamide | 2114991: Inhibition of recombinant human full-length ADAMTS7 truncated before the C-terminal PLAC domain using FAM-Glu-Ala-Ala-Ala-Arg-Ala-Glu-Ala-Ala-Ala-Lys-TAMRA as substrate measured after 24 hrs by FRET assay | ki | 0.0060 | uM |
| 3,4-difluoro-N-[[4-(4-methyl-1-phenylpyrazol-3-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0080 | uM |
| (2R)-2-(1-benzoylpiperidin-4-yl)-N-hydroxy-2-[[4-[4-(trifluoromethyl)phenyl]phenyl]sulfonylamino]acetamide | 2114991: Inhibition of recombinant human full-length ADAMTS7 truncated before the C-terminal PLAC domain using FAM-Glu-Ala-Ala-Ala-Arg-Ala-Glu-Ala-Ala-Ala-Lys-TAMRA as substrate measured after 24 hrs by FRET assay | ki | 0.0090 | uM |
| 3,4-difluoro-N-[[4-(5-methyl-2-pyridin-3-yl-1,3-thiazol-4-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0090 | uM |
| 3-fluoro-N-[[(4S)-4-(2-methylpyrazol-3-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-4-(trifluoromethyl)-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0100 | uM |
| N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]-2-(3-fluorophenyl)triazole-4-carboxamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0130 | uM |
| N-[[2,5-dioxo-4-(1,3-thiazol-4-yl)imidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0140 | uM |
| N-[[4-(2,5-dimethyl-1,3-thiazol-4-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0150 | uM |
| 3-chloro-N-[[(4S)-4-(2-methylpyrazol-3-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0160 | uM |
| N-[[4-(2-ethylpyrazol-3-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0180 | uM |
| 4-fluoro-N-[[(4S)-4-(2-methylpyrazol-3-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0190 | uM |
| 5-fluoro-N-[[(4S)-4-(2-methylpyrazol-3-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0190 | uM |
| 2-(3-chlorophenyl)-N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]triazole-4-carboxamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0210 | uM |
| N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]-2-(4-fluorophenyl)triazole-4-carboxamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0260 | uM |
| 2-(4-chlorophenyl)-N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]triazole-4-carboxamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0260 | uM |
| 3-methoxy-N-[[(4S)-4-(2-methylpyrazol-3-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0290 | uM |
| (2R)-2-(1-benzoylpiperidin-4-yl)-2-[[4-[(2-chloro-4-fluorophenyl)methoxy]phenyl]sulfonylamino]-N-hydroxyacetamide | 2114991: Inhibition of recombinant human full-length ADAMTS7 truncated before the C-terminal PLAC domain using FAM-Glu-Ala-Ala-Ala-Arg-Ala-Glu-Ala-Ala-Ala-Lys-TAMRA as substrate measured after 24 hrs by FRET assay | ki | 0.0400 | uM |
| (2R)-2-(1-benzoylpiperidin-4-yl)-N-hydroxy-2-[[4-(4-methoxyphenyl)phenyl]sulfonylamino]acetamide | 2114991: Inhibition of recombinant human full-length ADAMTS7 truncated before the C-terminal PLAC domain using FAM-Glu-Ala-Ala-Ala-Arg-Ala-Glu-Ala-Ala-Ala-Lys-TAMRA as substrate measured after 24 hrs by FRET assay | ki | 0.0400 | uM |
| N-[[4-(1,5-dimethylpyrazol-4-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0460 | uM |
| N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]-2-(4-methylphenyl)triazole-4-carboxamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0470 | uM |
| 3,4-difluoro-N-[[4-(5-methyl-2-phenyl-1,3-thiazol-4-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0470 | uM |
| N-[4-[[4-[(2-chloro-4-fluorophenyl)methoxy]phenyl]sulfonylamino]-5-(hydroxyamino)-3-methyl-5-oxopentyl]benzamide | 2114991: Inhibition of recombinant human full-length ADAMTS7 truncated before the C-terminal PLAC domain using FAM-Glu-Ala-Ala-Ala-Arg-Ala-Glu-Ala-Ala-Ala-Lys-TAMRA as substrate measured after 24 hrs by FRET assay | ki | 0.0500 | uM |
| (2R)-2-(1-benzoylpiperidin-4-yl)-N-hydroxy-2-[methyl-[4-[4-(trifluoromethyl)phenyl]phenyl]sulfonylamino]acetamide | 2114991: Inhibition of recombinant human full-length ADAMTS7 truncated before the C-terminal PLAC domain using FAM-Glu-Ala-Ala-Ala-Arg-Ala-Glu-Ala-Ala-Ala-Lys-TAMRA as substrate measured after 24 hrs by FRET assay | ki | 0.0500 | uM |
| N-[[2,5-dioxo-4-[2-(2,2,2-trifluoroethyl)pyrazol-3-yl]imidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0600 | uM |
| N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]-2-phenyltriazole-4-carboxamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0610 | uM |
| N-[(4R)-4-[[4-[(2-chloro-4-fluorophenyl)methoxy]phenyl]sulfonylamino]-5-(hydroxyamino)-5-oxopentyl]benzamide | 2114991: Inhibition of recombinant human full-length ADAMTS7 truncated before the C-terminal PLAC domain using FAM-Glu-Ala-Ala-Ala-Arg-Ala-Glu-Ala-Ala-Ala-Lys-TAMRA as substrate measured after 24 hrs by FRET assay | ki | 0.0700 | uM |
| N-[[2,5-dioxo-4-[5-(trifluoromethyl)-1,3-thiazol-4-yl]imidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0720 | uM |
| 2-fluoro-N-[[(4S)-4-(2-methylpyrazol-3-yl)-2,5-dioxoimidazolidin-4-yl]methyl]-6-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0790 | uM |
| N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]-2-[4-(trifluoromethyl)phenyl]benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.0990 | uM |
| N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]-2-(5-fluoro-2-pyridinyl)triazole-4-carboxamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.1150 | uM |
| N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]-1-phenylpyrazole-4-carboxamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.1290 | uM |
| N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]-2-(2-fluorophenyl)triazole-4-carboxamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.1800 | uM |
| (2R)-3-(1-benzoylpiperidin-4-yl)-2-[[4-[(2-chloro-4-fluorophenyl)methoxy]phenyl]sulfonylamino]-N-hydroxypropanamide | 2114991: Inhibition of recombinant human full-length ADAMTS7 truncated before the C-terminal PLAC domain using FAM-Glu-Ala-Ala-Ala-Arg-Ala-Glu-Ala-Ala-Ala-Lys-TAMRA as substrate measured after 24 hrs by FRET assay | ki | 0.2200 | uM |
| N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]-2-(1,2-thiazol-4-yl)triazole-4-carboxamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.2300 | uM |
| 1-[(4-chlorophenyl)methyl]-N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]pyrazole-4-carboxamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.2800 | uM |
| 1-benzoyl-4-[[4-[(2-chloro-4-fluorophenyl)methoxy]phenyl]sulfonylamino]-N-hydroxypiperidine-4-carboxamide | 2114991: Inhibition of recombinant human full-length ADAMTS7 truncated before the C-terminal PLAC domain using FAM-Glu-Ala-Ala-Ala-Arg-Ala-Glu-Ala-Ala-Ala-Lys-TAMRA as substrate measured after 24 hrs by FRET assay | ki | 0.3800 | uM |
| (2R)-2-(1-benzoylpiperidin-4-yl)-2-[[4-[4-(dimethylamino)phenyl]phenyl]sulfonylamino]-N-hydroxyacetamide | 2114991: Inhibition of recombinant human full-length ADAMTS7 truncated before the C-terminal PLAC domain using FAM-Glu-Ala-Ala-Ala-Arg-Ala-Glu-Ala-Ala-Ala-Lys-TAMRA as substrate measured after 24 hrs by FRET assay | ki | 0.5500 | uM |
| N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]-4-(4-methylphenyl)benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.5800 | uM |
| N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]-2-[(1-methylpyrazol-4-yl)methyl]triazole-4-carboxamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.8500 | uM |
| N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]-2-(1,3-thiazol-2-ylmethyl)triazole-4-carboxamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.9100 | uM |
| N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]-2-[(2-methyl-1,3-thiazol-4-yl)methyl]triazole-4-carboxamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 0.9300 | uM |
| (2R)-2-(1-benzoylpiperidin-4-yl)-N-hydroxy-2-[[4-(4-morpholin-4-ylphenyl)phenyl]sulfonylamino]acetamide | 2114991: Inhibition of recombinant human full-length ADAMTS7 truncated before the C-terminal PLAC domain using FAM-Glu-Ala-Ala-Ala-Arg-Ala-Glu-Ala-Ala-Ala-Lys-TAMRA as substrate measured after 24 hrs by FRET assay | ki | 0.9400 | uM |
| (2R)-2-(1-benzoylpiperidin-4-yl)-N-hydroxy-2-[[4-[3-(trifluoromethyl)phenyl]phenyl]sulfonylamino]acetamide | 2114991: Inhibition of recombinant human full-length ADAMTS7 truncated before the C-terminal PLAC domain using FAM-Glu-Ala-Ala-Ala-Arg-Ala-Glu-Ala-Ala-Ala-Lys-TAMRA as substrate measured after 24 hrs by FRET assay | ki | 1.0000 | uM |
| N-[[(4R)-4-cyclopropyl-2,5-dioxoimidazolidin-4-yl]methyl]-3-(4-methylphenyl)benzamide | 2089697: Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | ic50 | 2.3000 | uM |
CTD chemical–gene interactions
25 total (human), top 25 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Particulate Matter | decreases expression, increases abundance, affects expression | 3 |
| Cisplatin | affects cotreatment, increases expression, decreases expression | 2 |
| Doxorubicin | increases expression | 2 |
| sodium arsenite | decreases expression | 1 |
| 3,4,5,3’,4’-pentachlorobiphenyl | increases expression | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| nutlin 3 | affects cotreatment, increases expression | 1 |
| abrine | decreases expression | 1 |
| jinfukang | affects cotreatment, increases expression | 1 |
| Resveratrol | affects cotreatment, decreases expression | 1 |
| Sunitinib | decreases expression | 1 |
| Air Pollutants | decreases expression, increases abundance | 1 |
| Benzo(a)pyrene | increases expression | 1 |
| Camptothecin | increases expression | 1 |
| Dactinomycin | affects cotreatment, increases expression | 1 |
| Estradiol | affects cotreatment, increases expression | 1 |
| Methotrexate | decreases expression | 1 |
| Phthalic Acids | increases methylation | 1 |
| Plant Extracts | affects cotreatment, decreases expression | 1 |
| Smoke | decreases expression | 1 |
| Tobacco Smoke Pollution | increases expression | 1 |
| Tretinoin | decreases expression | 1 |
| Paclitaxel | affects cotreatment, decreases expression | 1 |
| Genistein | increases expression | 1 |
| Acrylamide | decreases expression | 1 |
ChEMBL screening assays
6 unique, capped per target: 6 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL5530428 | Binding | Inhibition of recombinant ADAMTS7 (unknown origin) using HiLyteFluor-488 DELSSMVLELRGLRT-K(QXL520)-E-NH2 as substrate incubated for 120 mins by FRET assay | BAY-9835: Discovery of the First Orally Bioavailable ADAMTS7 Inhibitor. — J Med Chem |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): large artery stroke, stroke disorder