AMY1A
gene geneOn this page
Summary
AMY1A (amylase alpha 1A, HGNC:474) is a protein-coding gene on chromosome 1p21.1, encoding Alpha-amylase 1A (P0DUB6). Calcium-binding enzyme that initiates starch digestion in the oral cavity.
Amylases are secreted proteins that hydrolyze 1,4-alpha-glucoside bonds in oligosaccharides and polysaccharides, and thus catalyze the first step in digestion of dietary starch and glycogen. The human genome has a cluster of several amylase genes that are expressed at high levels in either salivary gland or pancreas. This gene encodes an amylase isoenzyme produced by the salivary gland. Alternative splicing results in multiple transcript variants encoding the same protein.
Source: NCBI Gene 276 — RefSeq curated summary.
At a glance
- GWAS associations: 1
- Clinical variants (ClinVar): 30 total
- Druggable target: yes — 6 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_004038
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:474 |
| Approved symbol | AMY1A |
| Name | amylase alpha 1A |
| Location | 1p21.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000237763 |
| Ensembl biotype | protein_coding |
| OMIM | 104700 |
| Entrez | 276 |
Gene structure
Transcript identifiers
Ensembl transcripts: 10 — 8 protein_coding, 1 retained_intron, 1 protein_coding_CDS_not_defined
ENST00000370083, ENST00000422549, ENST00000461518, ENST00000494409, ENST00000872085, ENST00000872086, ENST00000872087, ENST00000962698, ENST00000962699, ENST00000962700
RefSeq mRNA: 6 — MANE Select: NM_004038
NM_001008221, NM_001422120, NM_001422123, NM_001422127, NM_001422129, NM_004038
CCDS: CCDS30782
Canonical transcript exons
ENST00000370083 — 11 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001615366 | 103662657 | 103662775 |
| ENSE00001618329 | 103656285 | 103656498 |
| ENSE00001669527 | 103660360 | 103660482 |
| ENSE00001786647 | 103660577 | 103660676 |
| ENSE00001800716 | 103655760 | 103655928 |
| ENSE00003512225 | 103657794 | 103657991 |
| ENSE00003594796 | 103662886 | 103663011 |
| ENSE00003627931 | 103659410 | 103659543 |
| ENSE00003628416 | 103658440 | 103658670 |
| ENSE00003740032 | 103664331 | 103664554 |
| ENSE00003790665 | 103656844 | 103656990 |
Expression profiles
Bgee: expression breadth ubiquitous, 124 present calls, max score 86.63.
Top tissues by expression
131 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| body of pancreas | UBERON:0001150 | 86.63 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 84.80 | gold quality |
| right uterine tube | UBERON:0001302 | 81.10 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 80.22 | gold quality |
| olfactory segment of nasal mucosa | UBERON:0005386 | 70.76 | gold quality |
| tonsil | UBERON:0002372 | 70.66 | gold quality |
| fallopian tube | UBERON:0003889 | 68.26 | gold quality |
| pancreas | UBERON:0001264 | 67.92 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 62.19 | gold quality |
| placenta | UBERON:0001987 | 60.89 | gold quality |
| left lobe of thyroid gland | UBERON:0001120 | 59.24 | gold quality |
| saliva-secreting gland | UBERON:0001044 | 58.60 | gold quality |
| endocervix | UBERON:0000458 | 57.44 | gold quality |
| thyroid gland | UBERON:0002046 | 57.44 | gold quality |
| calcaneal tendon | UBERON:0003701 | 57.07 | gold quality |
| right lung | UBERON:0002167 | 55.71 | gold quality |
| endometrium | UBERON:0001295 | 54.75 | gold quality |
| minor salivary gland | UBERON:0001830 | 54.54 | gold quality |
| gastrocnemius | UBERON:0001388 | 54.32 | gold quality |
| lung | UBERON:0002048 | 53.72 | gold quality |
| muscle of leg | UBERON:0001383 | 52.41 | gold quality |
| bone marrow | UBERON:0002371 | 52.17 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 51.97 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 51.90 | gold quality |
| cerebellar cortex | UBERON:0002129 | 51.27 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 51.08 | gold quality |
| cerebellum | UBERON:0002037 | 51.06 | gold quality |
| tibial nerve | UBERON:0001323 | 51.04 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 50.08 | gold quality |
| metanephros cortex | UBERON:0010533 | 49.98 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-6058 | no | 9.34 |
| E-ANND-3 | no | 1.74 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): GATA1, SP1
Literature-anchored findings (GeneRIF, showing 40)
- the binding region of human salivary alpha-amylase is composed of four glycone and three aglycone-binding sites, while that of mutant Tyr151Met is composed of four glycone and two aglycone-binding sites (PMID:12782315)
- This study reports on the effectiveness and specificity of glucopyranosylidene-spiro-thiohydantoin (G-TH) inhibitor on the 2-chloro-4-nitrophenyl-4-O-beta-D-galactopyranosyl-maltoside (GalG(2)CNP) hydrolysis catalysed by human salivary alpha-amylase. (PMID:14637141)
- These results suggest that the residue Trp58 plays a critical role in substrate binding and hydrolytic activity of human salivary alpha-amylase. (PMID:15182367)
- Data show that tannin is an effective inhibitor of human salivary alpha-amylase and indicate a higher stability for the enzyme-inhibitor complex than the enzyme-substrate-inhibitor complex. (PMID:15194503)
- A marked increasse in salivary alpha-amylase activity due to psychosocial stress and a reaction significantly different from a nonstress condition is observed. (PMID:15708646)
- The addition of salivary alpha-amylase to culture supernatants of S. gordonii precipitated a protein complex containing amylase, AbpA, amylase-binding protein B (AbpB), and the glucosyltransferase produced by S. gordonii (Gtf-G). (PMID:17593303)
- copy number of the salivary amylase gene (AMY1) is correlated positively with salivary amylase protein level and that individuals from populations with high-starch diets have, on average, more AMY1 copies than those with traditionally low-starch diets (PMID:17828263)
- Social evaluation-responders allocated significantly more money than controls; while there was no significant correlation between social evaluation-induced salivary amylase elevation and the allocated money. (PMID:17984929)
- The crystal structure of HSAmy-ar (multiple mutant) as an acarbose complex was determined at a resolution of 1.5 A and compared with the existing wild-type acarbose complex. (PMID:18951906)
- show that AMY1 copy number relates to salivary amylase concentration and enzymatic activity level, which, in turn, account for individual variation in the oral perception of starch viscosity (PMID:20967220)
- These findings confirm that sAA is sensitive to the effects of potentially stressful stimuli (state variance) and at the same time demonstrate its relative robustness and stability across time and conditions (trait variance). (PMID:21827821)
- salivary alpha-amylase increases may reflect levels of emotional arousal, including high arousal positive emotions (PMID:21840370)
- results show a strong association between acute physical stressor-induced elevations in sAA levels and patients with MDD. (PMID:22063648)
- Regression analyses demonstrated significant curvilinear relations and interactions between cortisol and sAA in the prediction of child functioning. (PMID:22100627)
- Salivary alpha-amylkase levels in the responder group were significantly elevated compared with the non-responder group and controls both before and after electrical stimulation in panic disorder patients. (PMID:22391145)
- High amylase individuals may be better adapted to ingest starches, whereas low amylase individuals may be at greater risk for insulin resistance and diabetes if chronically ingesting starch-rich diets. (PMID:22492122)
- Excercise significantly elevated salivary alpha-amylase in patients with mild cognitive impairment and normal aging controls. (PMID:22914593)
- A review of the possible impact of copy number polymorphism of the AMY1 gene on nutritional issues such as starch digestion, effect on glycemic response after starch consumption, effect on taste perception and satiety, influence on psychosocial stress and relation to oral health. (PMID:22965187)
- Adults who indicated that they would respond in a harsh way to the crying infant were significantly less likely to show a decrease in salivary alpha amylase. (PMID:23144191)
- AMY1A can be of great diagnostic utility when trying to differentiate Chromophobe renal cell carcinoma and oncocytoma (PMID:24225843)
- Salivary alpha amylase increased during wound care procedures of pediatric burn patients, and correlated with self-report of pain. (PMID:24433940)
- Low copy number of the salivary amylase gene predisposes to obesity. (PMID:24686848)
- findings suggest that both affective arousal andvalence should be accounted for when examining differences in salivary alpha Amylase reactivity and diurnal patterns. (PMID:25076484)
- Elevation in AMY1a following a second bout of downhill running may indicate an adaptive stress response which reduces the inflammatory events resulting from this type of exercise or an exercise-induced enhancement in innate secretory immunity. (PMID:25145588)
- Our current study suggests putative benefits of high number of AMY1 copies (and related production of salivary amylase) on energy metabolism in Mexican children. (PMID:25394825)
- Results suggest that AMY1 copy number and salivary alpha-amylase (sAA) amount played crucial roles in sAA activity; however, the roles were attenuated after stimulation due to fortified release of glycosylated sAA (PMID:25446200)
- Diurnal and stress-response salivary alpha amylase patterns were related to child adiposity: decreased morning alpha amylase was associated with increased BMI. (PMID:25588701)
- genetic association study in population in China: Data suggest that copy number variation of AMY1A gene is not associated with down-regulation of salivary response in thin children as compared to salivary response in normal weight children. (PMID:25784372)
- genetic association studies in a population of men in Republic of Korea: Data suggest that low AMY1A gene copy number is associated with high insulin resistance and thus with genetic predisposition to diabetes type 2 and metabolic syndrome. (PMID:25996848)
- The purpose of this study was to a) determine the heart rate variability (HRV) and saliva markers of immunity (salivary immunoglobulin A; sIgA) and stress (salivary alpha-amylase; sAA) responses to chronic training in elite swimmers with a disability. (PMID:26043224)
- Alpha-amylase in blood increases after pharmacological activation of the adrenergic pathways suggesting that sympathetic receptors are responsible for these changes. Psychological stress, however, does not seem to have an impact on alpha-amylase in blood (PMID:26110636)
- Splenic asthenia children had positive correlations between AMY1 copy number and sAA activity before or after citric acid stimulation. (PMID:26237829)
- low serum amylase level is significantly associated with increased risk of gestational diabetes mellitus (PMID:26642703)
- Data show that carcinoembryonic antigen (CEA) modestly differentiated between mucinous and nonmucinous lesions, and amylase did not distinguish intraductal papillary mucinous neoplasms (IPMNs) from mucinous cystadenomas (MCAs). (PMID:26646270)
- Results from 2 case-control cohorts of Chinese and Malays, show no previously reported association between AMY1 and obesity or body mass index. (PMID:27068483)
- Serum amylase levels in the normal range are positively associated with integrated islet beta cell function in patients with early type 2 diabetes. (PMID:27606813)
- AMY1 copy number was significantly correlated with the variation observed in salivary amylase production and enzyme activity but did not explain the majority of observed variation between individuals. AMY1-odd and AMY1-even haplotypes showed a different relationship between copy number and expression levels, but the difference was not statistically significant. (PMID:28219410)
- Alcohol dependent patients showed significantly lower stress-related salivary alpha-amylase activity than healthy controls. (PMID:28314952)
- higher levels of sAA in EHS participants (PMID:28466664)
- Our findings suggest an effect of the interaction between starch intake and AMY1 copy number on obesity. Individuals with high starch intake but low genetic capacity to digest starch had the lowest BMI, potentially because larger amounts of undigested starch are transported through the gastrointestinal tract, contributing to fewer calories extracted from ingested starch. (PMID:28539377)
Cross-species orthologs
12 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| drosophila_melanogaster | Amy-d | FBGN0000078 |
| drosophila_melanogaster | Amy-p | FBGN0000079 |
| drosophila_melanogaster | Mal-A2 | FBGN0002569 |
| drosophila_melanogaster | Mal-A3 | FBGN0002571 |
| drosophila_melanogaster | Amyrel | FBGN0020506 |
| drosophila_melanogaster | Mal-B1 | FBGN0032381 |
| drosophila_melanogaster | Mal-B2 | FBGN0032382 |
| drosophila_melanogaster | Mal-A4 | FBGN0033294 |
| drosophila_melanogaster | Mal-A7 | FBGN0033296 |
| drosophila_melanogaster | Mal-A8 | FBGN0033297 |
| drosophila_melanogaster | Mal-A6 | FBGN0050360 |
| caenorhabditis_elegans | WBGENE00008220 |
Paralogs (7): GBE1 (ENSG00000114480), SLC3A1 (ENSG00000138079), SLC3A2 (ENSG00000168003), AMY1B (ENSG00000174876), AMY1C (ENSG00000187733), AMY2B (ENSG00000240038), AMY2A (ENSG00000243480)
Protein
Protein identifiers
Alpha-amylase 1A — P0DUB6 (reviewed: P0DUB6)
Alternative names: 1,4-alpha-D-glucan glucanohydrolase 1, Salivary alpha-amylase
All UniProt accessions (2): P0DUB6, Q5T084
UniProt curated annotations — full annotation on UniProt →
Function. Calcium-binding enzyme that initiates starch digestion in the oral cavity. Catalyzes the hydrolysis of internal (1->4)-alpha-D-glucosidic bonds, yielding a mixture of maltose, isomaltose, small amounts of glucose as well as small linear and branched oligosaccharides called dextrins.
Subunit / interactions. Monomer.
Subcellular location. Secreted.
Cofactor. Binds 1 Ca(2+) ion per subunit. Binds 1 Cl(-) ion per subunit.
Similarity. Belongs to the glycosyl hydrolase 13 family.
RefSeq proteins (6): NP_001008222, NP_001409049, NP_001409052, NP_001409056, NP_001409058, NP_004029* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR006046 | Alpha_amylase | Family |
| IPR006047 | GH13_cat_dom | Domain |
| IPR006048 | A-amylase/branching_C | Domain |
| IPR013780 | Glyco_hydro_b | Homologous_superfamily |
| IPR017853 | GH_hydrolase_sf | Homologous_superfamily |
| IPR031319 | A-amylase_C | Domain |
Pfam: PF00128, PF02806
UniProt features (84 total): strand 28, helix 20, turn 12, binding site 7, disulfide bond 5, modified residue 4, glycosylation site 2, active site 2, signal peptide 1, chain 1, site 1, sequence conflict 1
Structure
Experimental structures (PDB)
13 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 3DHP | X-RAY DIFFRACTION | 1.5 |
| 1SMD | X-RAY DIFFRACTION | 1.6 |
| 1Z32 | X-RAY DIFFRACTION | 1.6 |
| 3BLP | X-RAY DIFFRACTION | 1.6 |
| 1JXK | X-RAY DIFFRACTION | 1.9 |
| 1JXJ | X-RAY DIFFRACTION | 1.99 |
| 1MFU | X-RAY DIFFRACTION | 2 |
| 1MFV | X-RAY DIFFRACTION | 2 |
| 3BLK | X-RAY DIFFRACTION | 2 |
| 1Q4N | X-RAY DIFFRACTION | 2.07 |
| 1NM9 | X-RAY DIFFRACTION | 2.1 |
| 1C8Q | X-RAY DIFFRACTION | 2.3 |
| 1XV8 | X-RAY DIFFRACTION | 3 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P0DUB6-F1 | 96.57 | 0.96 |
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): 315 (transition state stabilizer); 212 (nucleophile); 248 (proton donor)
Ligand- & substrate-binding residues (7): 352; 115; 173; 182; 210; 216; 313
Post-translational modifications (4): 16, 365, 427, 474
Disulfide bonds (5): 43–101, 85–130, 156–175, 393–399, 465–477
Glycosylation sites (2): 427, 476
Function
Pathways and Gene Ontology
Reactome pathways
3 pathways
| ID | Pathway |
|---|---|
| R-HSA-189085 | Digestion of dietary carbohydrate |
| R-HSA-8935690 | Digestion |
| R-HSA-8963743 | Digestion and absorption |
MSigDB gene sets: 40 (showing top):
GOBP_OLIGOSACCHARIDE_METABOLIC_PROCESS, LEE_NEURAL_CREST_STEM_CELL_DN, REACTOME_DIGESTION_OF_DIETARY_CARBOHYDRATE, GOBP_CARBOHYDRATE_METABOLIC_PROCESS, TURASHVILI_BREAST_DUCTAL_CARCINOMA_VS_DUCTAL_NORMAL_DN, KEGG_STARCH_AND_SUCROSE_METABOLISM, BASAKI_YBX1_TARGETS_DN, chr1p21, RODRIGUES_THYROID_CARCINOMA_POORLY_DIFFERENTIATED_DN, NAKAMURA_TUMOR_ZONE_PERIPHERAL_VS_CENTRAL_UP, BLALOCK_ALZHEIMERS_DISEASE_DN, GOMF_HYDROLASE_ACTIVITY_ACTING_ON_GLYCOSYL_BONDS, DODD_NASOPHARYNGEAL_CARCINOMA_DN, GOMF_HYDROLASE_ACTIVITY_HYDROLYZING_O_GLYCOSYL_COMPOUNDS, LIU_PROSTATE_CANCER_DN
GO Biological Process (2): carbohydrate metabolic process (GO:0005975), oligosaccharide metabolic process (GO:0009311)
GO Molecular Function (8): alpha-amylase activity (GO:0004556), calcium ion binding (GO:0005509), chloride ion binding (GO:0031404), catalytic activity (GO:0003824), hydrolase activity (GO:0016787), hydrolase activity, acting on glycosyl bonds (GO:0016798), cation binding (GO:0043169), metal ion binding (GO:0046872)
GO Cellular Component (3): obsolete extracellular space (GO:0005615), extracellular exosome (GO:0070062), extracellular region (GO:0005576)
Reactome top-level categories
Rollup of top-2 pathways:
| Category | Pathways |
|---|---|
| Digestion | 1 |
| Digestion and absorption | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| primary metabolic process | 1 |
| carbohydrate metabolic process | 1 |
| amylase activity | 1 |
| metal ion binding | 1 |
| anion binding | 1 |
| molecular_function | 1 |
| catalytic activity | 1 |
| hydrolase activity | 1 |
| ion binding | 1 |
| cation binding | 1 |
| extracellular vesicle | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
0 interactions, top by confidence (×1000):
IntAct
0 interactions, top by confidence:
ESM2 similar proteins: H2N0D4, O18344, O18345, O18408, O18420, O18552, O76260, O76261, O76262, O76263, O76264, O76265, O76284, O76459, O77011, O77012, O77013, O77014, O77015, O77016, O77018, O77019, O77020, O77021, O77022, O97396, P00687, P00688, P00689, P00690, P04063, P04746, P04750, P08144, P09107, P0DTE7, P0DTE8, P0DUB6, P19961, P54215
Diamond homologs: A0A096XJN4, B0KZK1, H2N0D4, O18344, O18345, O18408, O18420, O18552, O76260, O76261, O76262, O76263, O76264, O76265, O76284, O76459, O77011, O77012, O77013, O77014, O77015, O77016, O77018, O77019, O77020, O77021, O77022, O97396, P00687, P00688, P00689, P00690, P04746, P08144, P08486, P09107, P09794, P0DTE7, P0DTE8, P0DUB6
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
30 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 17 |
| Likely benign | 5 |
| Benign | 5 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
1380 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 1:103656839:TGTA:T | acceptor_loss | 1.0000 |
| 1:103656841:TAGGT:T | acceptor_loss | 1.0000 |
| 1:103656842:A:AC | acceptor_loss | 1.0000 |
| 1:103656843:GG:G | acceptor_loss | 1.0000 |
| 1:103656987:TGGGG:T | donor_loss | 1.0000 |
| 1:103656988:GGG:G | donor_gain | 1.0000 |
| 1:103656988:GGGGT:G | donor_loss | 1.0000 |
| 1:103656989:GG:G | donor_gain | 1.0000 |
| 1:103656989:GGG:G | donor_gain | 1.0000 |
| 1:103656989:GGGTA:G | donor_loss | 1.0000 |
| 1:103656990:GG:G | donor_gain | 1.0000 |
| 1:103656990:GGTA:G | donor_loss | 1.0000 |
| 1:103656991:G:GG | donor_gain | 1.0000 |
| 1:103656991:GTA:G | donor_loss | 1.0000 |
| 1:103656992:T:G | donor_loss | 1.0000 |
| 1:103657793:GGTTC:G | acceptor_gain | 1.0000 |
| 1:103658631:C:G | donor_gain | 1.0000 |
| 1:103658667:GGAG:G | donor_gain | 1.0000 |
| 1:103658668:G:GT | donor_gain | 1.0000 |
| 1:103659397:A:AG | acceptor_gain | 1.0000 |
| 1:103659398:A:G | acceptor_gain | 1.0000 |
| 1:103659405:TCTA:T | acceptor_loss | 1.0000 |
| 1:103659406:CTAG:C | acceptor_loss | 1.0000 |
| 1:103659407:TAGG:T | acceptor_loss | 1.0000 |
| 1:103659408:A:AG | acceptor_gain | 1.0000 |
| 1:103659408:AGG:A | acceptor_loss | 1.0000 |
| 1:103659409:G:GA | acceptor_loss | 1.0000 |
| 1:103659409:G:GG | acceptor_gain | 1.0000 |
| 1:103659409:GGT:G | acceptor_gain | 1.0000 |
| 1:103659409:GGTA:G | acceptor_gain | 1.0000 |
AlphaMissense
0 scored. Top likely-pathogenic:
dbSNP variants (sampled 300 via entrez): RS1003027647 (1:103660460 A>G), RS1004874086 (1:103655151 A>G), RS1005586971 (1:103660642 G>A), RS1016309644 (1:103655165 G>A,C), RS1029100176 (1:103660918 GAAAATA>G), RS1044735674 (1:103664067 G>A,T), RS1053446789 (1:103660373 G>T), RS1156428450 (1:103662098 G>A), RS1157156527 (1:103664305 G>A), RS1158049492 (1:103662267 C>A,T), RS1159402738 (1:103655373 C>T), RS1159914236 (1:103660509 T>A), RS1162278934 (1:103660316 T>C), RS1163508876 (1:103654902 C>T), RS1164316420 (1:103660070 T>C)
Disease associations
OMIM: gene MIM:104700 | disease phenotypes:
GenCC curated gene-disease
Mondo (1): primary ovarian failure (MONDO:0005387)
Orphanet (1): NON RARE IN EUROPE: Primary ovarian failure (Orphanet:619)
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
1 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST006585_2903 | Blood protein levels | 6.000000e-35 |
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D016649 | Primary Ovarian Insufficiency | C12.050.351.500.056.630.750; C12.100.250.056.630.750; C19.391.630.750 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL2478 (SINGLE PROTEIN), CHEMBL6066863 (PROTEIN FAMILY)
Molecules with ChEMBL bioactivity
6 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 162,315 (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 |
|---|---|---|---|
| CHEMBL404271 | ACARBOSE | 4 | 16 |
| CHEMBL50 | QUERCETIN | 3 | 74,559 |
| CHEMBL145 | CAFFEIC ACID | 3 | 36,305 |
| CHEMBL151 | LUTEOLIN | 2 | 23,523 |
| CHEMBL31574 | FISETIN | 2 | 7,745 |
| CHEMBL583912 | (-)-EPICATECHIN | 2 | 20,167 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
Binding affinities (BindingDB)
5 measured of 19 human assays (21 total across all organisms); most potent 5 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| YPYSCWVRH | IC50 | 34 nM |
| (3R,4R,5S,6R)-5-{[(2R,3R,4R,5S,6R)-5-{[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-{[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)cyclohex-2-en-1-yl]amino}oxan-2-yl]oxy}-3,4-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}-6-(hydroxymethyl)oxane-2,3,4-triol | IC50 | 996 nM |
| 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one | KI | 2200 nM |
| 2-(3,4-dihydroxyphenyl)-3,5,6,7-tetrahydroxy-4H-chromen-4-one | IC50 | 10200 nM |
| 2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-chromen-4-one | IC50 | 72800 nM |
ChEMBL bioactivities
243 potent at pChembl≥5 of 327 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 8.70 | EC50 | 2 | nM | CHEMBL3940413 |
| 8.52 | EC50 | 3 | nM | CHEMBL5613512 |
| 8.52 | EC50 | 3 | nM | CHEMBL3933500 |
| 7.40 | IC50 | 39.9 | nM | CHEMBL5590766 |
| 7.35 | IC50 | 44.77 | nM | CHEMBL5593047 |
| 7.32 | IC50 | 47.97 | nM | CHEMBL5595111 |
| 7.32 | IC50 | 48.08 | nM | CHEMBL5595096 |
| 7.31 | IC50 | 49.32 | nM | CHEMBL5592906 |
| 7.28 | IC50 | 52.97 | nM | CHEMBL5592459 |
| 7.27 | IC50 | 53.95 | nM | CHEMBL5595454 |
| 7.26 | IC50 | 55.21 | nM | CHEMBL5593276 |
| 7.24 | IC50 | 57.54 | nM | CHEMBL5591259 |
| 7.23 | IC50 | 59.29 | nM | CHEMBL5592359 |
| 7.22 | IC50 | 59.98 | nM | CHEMBL5594054 |
| 7.21 | IC50 | 60.95 | nM | CHEMBL5590296 |
| 7.18 | IC50 | 65.77 | nM | CHEMBL5594396 |
| 7.18 | IC50 | 65.77 | nM | CHEMBL5594825 |
| 7.18 | IC50 | 65.31 | nM | CHEMBL5596000 |
| 7.17 | IC50 | 67.76 | nM | CHEMBL5595749 |
| 7.16 | IC50 | 68.55 | nM | CHEMBL5592466 |
| 7.11 | IC50 | 77.98 | nM | CHEMBL5592801 |
| 7.09 | IC50 | 80.35 | nM | CHEMBL5590293 |
| 7.08 | IC50 | 83.75 | nM | CHEMBL5592637 |
| 7.04 | IC50 | 91.41 | nM | CHEMBL5592947 |
| 7.03 | IC50 | 93.11 | nM | CHEMBL5593659 |
| 7.03 | IC50 | 92.9 | nM | CHEMBL5594837 |
| 7.01 | IC50 | 97.72 | nM | CHEMBL5595658 |
| 7.00 | IC50 | 99.31 | nM | CHEMBL5593920 |
| 6.92 | IC50 | 120 | nM | ACARBOSE |
| 6.86 | IC50 | 138.4 | nM | CHEMBL5592880 |
| 6.72 | Ki | 190 | nM | CHEMBL3618492 |
| 6.72 | IC50 | 190 | nM | CHEMBL5624535 |
| 6.70 | IC50 | 201 | nM | CHEMBL5624476 |
| 6.68 | IC50 | 210 | nM | ACARBOSE |
| 6.64 | IC50 | 230 | nM | CHEMBL5267115 |
| 6.62 | IC50 | 240 | nM | CHEMBL5282550 |
| 6.62 | IC50 | 241 | nM | CHEMBL5630676 |
| 6.61 | IC50 | 243 | nM | CHEMBL5624847 |
| 6.58 | IC50 | 260 | nM | CHEMBL5290104 |
| 6.54 | IC50 | 290 | nM | CHEMBL5286589 |
| 6.54 | IC50 | 287 | nM | CHEMBL5631075 |
| 6.50 | IC50 | 320 | nM | CHEMBL5272639 |
| 6.50 | IC50 | 320 | nM | CHEMBL5275030 |
| 6.50 | IC50 | 319 | nM | CHEMBL5630566 |
| 6.47 | IC50 | 340 | nM | CHEMBL5286991 |
| 6.46 | IC50 | 350 | nM | CHEMBL5286580 |
| 6.43 | IC50 | 370 | nM | CHEMBL5271666 |
| 6.43 | IC50 | 367 | nM | CHEMBL5624515 |
| 6.42 | IC50 | 380 | nM | CHEMBL5279591 |
| 6.41 | IC50 | 390 | nM | CHEMBL5268343 |
PubChem BioAssay actives
266 with measured affinity, of 864 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| (2S)-2-[[(3S,8S)-3-[4-[(3,4-dichlorophenyl)methoxy]phenyl]-7-[1-[(2-methylpropan-2-yl)oxycarbonyl]piperidine-4-carbonyl]-3,6,8,9-tetrahydro-2H-[1,4]dioxino[2,3-g]isoquinoline-8-carbonyl]amino]-3-[4-(2,3-dimethyl-4-pyridinyl)phenyl]propanoic acid | 2124618: Inhibition of alpha-amylase (unknown origin) | ec50 | 0.0020 | uM |
| (2S)-2-[[(3S,8S)-3-[4-[(3,4-dichlorophenyl)methoxy]phenyl]-7-[(1S)-1-phenylpropyl]-3,6,8,9-tetrahydro-2H-[1,4]dioxino[2,3-g]isoquinoline-8-carbonyl]amino]-3-[4-(2,5-dimethylpyrazol-3-yl)phenyl]propanoic acid | 2124618: Inhibition of alpha-amylase (unknown origin) | ec50 | 0.0030 | uM |
| (2S)-2-[[(3S,8S)-3-[4-[(4-chlorophenyl)methoxy]phenyl]-7-[(1S)-1-phenylpropyl]-3,6,8,9-tetrahydro-2H-[1,4]dioxino[2,3-g]isoquinoline-8-carbonyl]amino]-3-[4-(2,3-dimethyl-4-pyridinyl)phenyl]propanoic acid | 2124618: Inhibition of alpha-amylase (unknown origin) | ec50 | 0.0030 | uM |
| (2S)-N-[(2S)-1-amino-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[(3S,10S,13S,16S)-10-(hydroxymethyl)-3,13-bis[(4-hydroxyphenyl)methyl]-2,5,9,12,15-pentaoxo-7-thia-1,4,8,11,14-pentazabicyclo[14.3.0]nonadecan-8-yl]-3-sulfanylpropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-methylbutanoyl]amino]pentanamide | 1802659: Inhibition Assay (piHA-Dm) from Article 10.1016/j.chembiol.2017.02.001: “Rapid Discovery of Potent and Selective Glycosidase-Inhibiting De Novo Peptides.” | ic50 | 0.0340 | uM |
| (5Z)-3-[[1-(7-chloroquinolin-4-yl)triazol-4-yl]methyl]-5-(dimethylaminomethylidene)-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0399 | uM |
| (5Z)-3-[[1-[(2,4-dichlorophenyl)methyl]triazol-4-yl]methyl]-5-(dimethylaminomethylidene)-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0448 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-[[1-[2-(trifluoromethyl)phenyl]triazol-4-yl]methyl]-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0480 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-[[1-(2,4-dimethylphenyl)triazol-4-yl]methyl]-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0481 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-[[1-(2-ethylphenyl)triazol-4-yl]methyl]-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0493 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-[[1-(4-methoxyphenyl)triazol-4-yl]methyl]-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0530 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-[[1-(4-propan-2-ylphenyl)triazol-4-yl]methyl]-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0539 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-[[1-[3-(trifluoromethyl)phenyl]triazol-4-yl]methyl]-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0552 | uM |
| (5Z)-3-[(1-butyltriazol-4-yl)methyl]-5-(dimethylaminomethylidene)-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0575 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-[[1-(4-nitrophenyl)triazol-4-yl]methyl]-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0593 | uM |
| (5Z)-3-[[1-(2,3-dichlorophenyl)triazol-4-yl]methyl]-5-(dimethylaminomethylidene)-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0600 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-[[1-(3-methylphenyl)triazol-4-yl]methyl]-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0609 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-[[1-(2-methoxyphenyl)triazol-4-yl]methyl]-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0653 | uM |
| (5Z)-3-[[1-(3-chlorophenyl)triazol-4-yl]methyl]-5-(dimethylaminomethylidene)-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0658 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-[[1-(3,5-dimethylphenyl)triazol-4-yl]methyl]-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0658 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-[[1-(4-ethylphenyl)triazol-4-yl]methyl]-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0678 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-[[1-(3-methoxyphenyl)triazol-4-yl]methyl]-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0685 | uM |
| (5Z)-3-[[1-[2-(4-bromophenyl)-2-oxoethyl]triazol-4-yl]methyl]-5-(dimethylaminomethylidene)-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0780 | uM |
| (5Z)-3-[(1-benzyltriazol-4-yl)methyl]-5-(dimethylaminomethylidene)-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0804 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-[[1-[4-(trifluoromethyl)phenyl]triazol-4-yl]methyl]-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0838 | uM |
| (5Z)-3-[[1-(2-chlorophenyl)triazol-4-yl]methyl]-5-(dimethylaminomethylidene)-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0914 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-[[1-(2,5-dimethylphenyl)triazol-4-yl]methyl]-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0929 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-[[1-(4-fluorophenyl)triazol-4-yl]methyl]-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0931 | uM |
| (5Z)-3-[[1-(4-chlorophenyl)triazol-4-yl]methyl]-5-(dimethylaminomethylidene)-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0977 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-[(1-phenyltriazol-4-yl)methyl]-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.0993 | uM |
| (3R,4R,5S,6R)-5-[(2R,3R,4R,5S,6R)-5-[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)cyclohex-2-en-1-yl]amino]oxan-2-yl]oxy-3,4-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-6-(hydroxymethyl)oxane-2,3,4-triol | 1942520: Inhibition of alpha-amylase (unknown origin) by HPLC analysis | ic50 | 0.1200 | uM |
| (5Z)-5-(dimethylaminomethylidene)-3-prop-2-ynyl-1,3-thiazolidine-2,4-dione | 2116899: Inhibition of alpha-amylase (unknown origin) using 1% starch as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by colorimetric analysis | ic50 | 0.1384 | uM |
| (7R,8S,9S,10R)-7-[[(2S,3R,4R,5S,6R)-5-[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)cyclohex-2-en-1-yl]amino]oxan-2-yl]oxy-3,4-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxymethyl]-8,9,10-trihydroxy-2-sulfanylidene-6-oxa-1,3-diazaspiro[4.5]decan-4-one | 1248395: Non-competitive inhibition of human salivary alpha-amylase using GalG2CNP as substrate assessed as CNP liberation by Lineweaver-Burk plot analysis | ki | 0.1900 | uM |
| N-[4-[(Z)-[3-[2-(1,3-dioxoisoindol-2-yl)acetyl]-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenyl]-3,4,5-trihydroxybenzamide | 2133787: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by absorbance based assay | ic50 | 0.1900 | uM |
| N-[4-[(Z)-[3-[2-[4-(benzenesulfonyl)piperazin-1-yl]acetyl]-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenyl]-3,4,5-trihydroxybenzamide | 2133787: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by absorbance based assay | ic50 | 0.2010 | uM |
| N-[(E)-(4-hydroxyphenyl)methylideneamino]-2-(4-nitroanilino)-1,3-thiazole-4-carboxamide | 1953050: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated with substrate for 15 mins followed by compound addition and measured after 15 mins by UV-VIS spectrophotometric analysis | ic50 | 0.2300 | uM |
| N-[(E)-(4-hydroxy-3-methoxyphenyl)methylideneamino]-2-(4-nitroanilino)-1,3-thiazole-4-carboxamide | 1953050: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated with substrate for 15 mins followed by compound addition and measured after 15 mins by UV-VIS spectrophotometric analysis | ic50 | 0.2400 | uM |
| 3,4,5-trihydroxy-N-[4-[(Z)-[3-[2-(2-methylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl)acetyl]-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenyl]benzamide | 2133787: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by absorbance based assay | ic50 | 0.2410 | uM |
| (5Z)-3-[2-(1,3-dioxoisoindol-2-yl)acetyl]-5-[(4-phenylmethoxyphenyl)methylidene]-1,3-thiazolidine-2,4-dione | 2133787: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by absorbance based assay | ic50 | 0.2430 | uM |
| 2-(4-nitroanilino)-N-[(E)-(3,4,5-trimethoxyphenyl)methylideneamino]-1,3-thiazole-4-carboxamide | 1953050: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated with substrate for 15 mins followed by compound addition and measured after 15 mins by UV-VIS spectrophotometric analysis | ic50 | 0.2600 | uM |
| N-[4-[(Z)-[2,4-dioxo-3-[2-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]acetyl]-1,3-thiazolidin-5-ylidene]methyl]phenyl]-3,4,5-trihydroxybenzamide | 2133787: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by absorbance based assay | ic50 | 0.2870 | uM |
| N-[(E)-(4-chlorophenyl)methylideneamino]-2-(4-nitroanilino)-1,3-thiazole-4-carboxamide | 1953050: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated with substrate for 15 mins followed by compound addition and measured after 15 mins by UV-VIS spectrophotometric analysis | ic50 | 0.2900 | uM |
| (5Z)-5-[(4-phenylmethoxyphenyl)methylidene]-3-[2-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]acetyl]-1,3-thiazolidine-2,4-dione | 2133787: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by absorbance based assay | ic50 | 0.3190 | uM |
| 2-(4-chloroanilino)-N-[(E)-(4-hydroxy-3-methoxyphenyl)methylideneamino]-1,3-thiazole-4-carboxamide | 1953050: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated with substrate for 15 mins followed by compound addition and measured after 15 mins by UV-VIS spectrophotometric analysis | ic50 | 0.3200 | uM |
| N-[(E)-(4-methoxyphenyl)methylideneamino]-2-(4-nitroanilino)-1,3-thiazole-4-carboxamide | 1953050: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated with substrate for 15 mins followed by compound addition and measured after 15 mins by UV-VIS spectrophotometric analysis | ic50 | 0.3200 | uM |
| N-[(E)-(4-fluorophenyl)methylideneamino]-2-(4-nitroanilino)-1,3-thiazole-4-carboxamide | 1953050: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated with substrate for 15 mins followed by compound addition and measured after 15 mins by UV-VIS spectrophotometric analysis | ic50 | 0.3400 | uM |
| 2-(4-chloroanilino)-N-[(E)-1-pyridin-2-ylethylideneamino]-1,3-thiazole-4-carboxamide | 1953050: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated with substrate for 15 mins followed by compound addition and measured after 15 mins by UV-VIS spectrophotometric analysis | ic50 | 0.3500 | uM |
| (5Z)-3-[2-[4-(benzenesulfonyl)piperazin-1-yl]acetyl]-5-[(4-phenylmethoxyphenyl)methylidene]-1,3-thiazolidine-2,4-dione | 2133787: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by absorbance based assay | ic50 | 0.3670 | uM |
| N-[(E)-benzylideneamino]-2-(4-nitroanilino)-1,3-thiazole-4-carboxamide | 1953050: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated with substrate for 15 mins followed by compound addition and measured after 15 mins by UV-VIS spectrophotometric analysis | ic50 | 0.3700 | uM |
| N-[(E)-benzylideneamino]-2-(4-chloroanilino)-1,3-thiazole-4-carboxamide | 1953050: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated with substrate for 15 mins followed by compound addition and measured after 15 mins by UV-VIS spectrophotometric analysis | ic50 | 0.3800 | uM |
| 2-(4-chloroanilino)-N-[(E)-(4-chlorophenyl)methylideneamino]-1,3-thiazole-4-carboxamide | 1953050: Inhibition of alpha-amylase (unknown origin) using starch as substrate preincubated with substrate for 15 mins followed by compound addition and measured after 15 mins by UV-VIS spectrophotometric analysis | ic50 | 0.3900 | uM |
CTD chemical–gene interactions
9 total (human), top 9 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Cadmium | increases abundance, increases expression, decreases expression | 2 |
| potassium persulfate | increases expression | 1 |
| beta-methylcholine | affects expression | 1 |
| cordycepin | decreases expression, decreases reaction, decreases secretion, increases expression | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| Estradiol | affects cotreatment, increases expression | 1 |
| Hydrogen Peroxide | decreases expression, decreases reaction, decreases secretion | 1 |
| Progesterone | affects cotreatment, increases expression | 1 |
| Cadmium Chloride | increases abundance, increases expression | 1 |
ChEMBL screening assays
94 unique, capped per target: 94 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1116865 | Binding | Activity of human salivary alpha amylase by FRET assay | Simple and conveniently accessible bi-fluorescence-labeled substrates for amylases. — Bioorg Med Chem Lett |
Clinical trials (associated diseases)
75 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00417066 | PHASE4 | COMPLETED | Flexible GnRH Antagonist vs Flare up GnRH Agonist Protocol in Poor Responders |
| NCT00732693 | PHASE4 | COMPLETED | Evaluation of Physiologic and Standard Sex Steroid Replacement Regimens in Women With Premature Ovarian Failure |
| NCT00837616 | PHASE4 | COMPLETED | Estrogen Dosing in Turner Syndrome: Pharmacology and Metabolism |
| NCT01853501 | PHASE4 | UNKNOWN | Effects of ADSC Therapy in Women With POF |
| NCT02783937 | PHASE4 | COMPLETED | Filgrastim for Premature Ovarian Insufficiency |
| NCT03535480 | PHASE4 | UNKNOWN | Autologous Bone Marrow Stem Cell Ovarian Transplantation to Restore Ovarian Function in Premature Ovarian Failure |
| NCT00140998 | PHASE3 | COMPLETED | Estrogen Treatment (Oral vs. Patches) in Turner Syndrome |
| NCT00001951 | PHASE2 | COMPLETED | Hormone Replacement in Young Women With Premature Ovarian Failure |
| NCT00370019 | PHASE2 | WITHDRAWN | Effects of an Estrogen Replacement Therapy Skin Patch on Ovulation in Women With Premature Ovarian Failure |
| NCT00429494 | PHASE2 | COMPLETED | GnRH Analogue for Ovarian Function Preservation in Hematopoietic Stem Cell Transplantation Patients |
| NCT03816852 | PHASE2 | SUSPENDED | The Safety and Efficiency Study of Mesenchymal Stem Cell (19#iSCLife®-POI) in Premature Ovarian Insufficiency |
| NCT04536467 | PHASE2 | UNKNOWN | Prevention of Chemotherapy-Induced Ovarian Failure With Goserelin in Premenopausal Lymphoma Patients |
| NCT06117982 | PHASE2 | COMPLETED | The Impact of Granulocyte Colony Stimulating Factor on Premature Ovarian Insufficiency |
| NCT02912104 | PHASE1 | COMPLETED | A Therapeutic Trial of Human Amniotic Epithelial Cells Transplantation for Primary Ovarian Failure |
| NCT03178695 | PHASE1 | COMPLETED | Inovium Ovarian Rejuvenation Trials |
| NCT04815213 | PHASE1 | ACTIVE_NOT_RECRUITING | The Use of Expandeded Mesenchymal Stromal Cells (MSC) in Premature Ovarian Failure (POF) in Adult Humans |
| NCT05138367 | PHASE1 | COMPLETED | Effects of UCA-PSCs in Women With POF |
| NCT06132542 | PHASE1 | UNKNOWN | Autologous ADMSC Transplantation in Patients With POI |
| NCT00948857 | PHASE2/PHASE3 | TERMINATED | Dehydroepiandrosterone (DHEA) Treatment and Premature Ovarian Failure (POF) |
| NCT04031456 | PHASE2/PHASE3 | RECRUITING | Autologous PRP Infusion May Restore Ovarian Function and May Promote Folliculogenesis in POI Patients |
| NCT02043743 | PHASE1/PHASE2 | UNKNOWN | Autologous Stem Cells Transplantation in Patients With Idiopathic and Drug Induced Premature Ovarian Failure |
| NCT02062931 | PHASE1/PHASE2 | UNKNOWN | Autologous Mesenchymal Stem Cells Transplantation In Women With Premature Ovarian Failure |
| NCT02151890 | PHASE1/PHASE2 | COMPLETED | Pregnancy After Stem Cell Transplantation in Premature Ovarian Failure |
| NCT02372474 | PHASE1/PHASE2 | COMPLETED | It is a Real The First Baby Of Autologous Stem Cell Therapy in Premature Ovarian Failure |
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| NCT03069209 | PHASE1/PHASE2 | UNKNOWN | Autologous Bone Marrow-Derived Stem Cell Transplantation in Patients With Premature Ovarian Failure (POF) |
| NCT03985462 | PHASE1/PHASE2 | WITHDRAWN | Very Small Embryonic-like Stem Cells for Ovary |
| NCT04009473 | PHASE1/PHASE2 | UNKNOWN | Stem Cell Therapy and Growth Factor Ovarian in Vitro Activation |
| NCT04071574 | PHASE1/PHASE2 | COMPLETED | Comparative Study on the Efficacy of Ovarian Stimulation Protocols on the Success Rate of ICSI in Female Infertility |
| NCT04922398 | PHASE1/PHASE2 | UNKNOWN | Ovarian Injection of PRP (Platelet -Rich Plasma) Vs Normal Saline in Premature Ovarian Insufficiency |
| NCT05462379 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Autologous Heterotopic Fresh Ovarian Graft in Woman With LACC Eligible for Pelvic Radiotherapy Treatment. |
| NCT06202547 | PHASE1/PHASE2 | UNKNOWN | Intra-ovarian Injection of MSC-EVs in Idiopathic Premature Ovarian Failure |
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| NCT05522634 | EARLY_PHASE1 | UNKNOWN | A Clinical Study of Chinese Herbal Compound TJAOA101 in the Treatment of Premature Ovarian Insufficiency |
| NCT07308327 | EARLY_PHASE1 | ACTIVE_NOT_RECRUITING | The Influence of Gut Microbiota on Ovarian Function: A Single-center, Randomized,Double Blind, Parallel-controlled, Exploratory Clinical Trial |
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| NCT00001306 | Not specified | COMPLETED | Steroid Therapy in Autoimmune Premature Ovarian Failure |
| NCT00006156 | Not specified | COMPLETED | Feasibility Study for Development of an Early Test for Ovarian Failure |
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Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.