AMY1B

Summary

AMY1B (amylase alpha 1B, HGNC:475) is a protein-coding gene on chromosome 1p21.1, encoding Alpha-amylase 1B (P0DTE7). 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.

Source: NCBI Gene 277 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 9 total
• GTEx eGene: eQTL in 1 tissue, sQTL in 1 (q < 0.05)
• MANE Select transcript: NM_001008218

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:475
Approved symbol	AMY1B
Name	amylase alpha 1B
Location	1p21.1
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000174876
Ensembl biotype	protein_coding
OMIM	104701
Entrez	277

Gene structure

Transcript identifiers

Ensembl transcripts: 12 — 11 protein_coding, 1 retained_intron

MANE Select: ENST00000330330

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 1, TSL 2: 1, TSL 3: 1

ENST00000330330, ENST00000370080, ENST00000425410, ENST00000464691, ENST00000903269, ENST00000903270, ENST00000903271, ENST00000903272, ENST00000942052, ENST00000942053, ENST00000942054, ENST00001144683

RefSeq mRNA: 6 — MANE Select: NM_001008218 NM_001008218, NM_001386925, NM_001422120, NM_001422123, NM_001422127, NM_001422129

CCDS: CCDS30783

Canonical transcript exons

ENST00000330330 — 11 exons

Exon	Start	End
ENSE00001681850	103689194	103689312
ENSE00001720483	103691488	103691610
ENSE00001738141	103691294	103691393
ENSE00001760424	103696042	103696210
ENSE00001765498	103695472	103695685
ENSE00001926974	103687415	103687638
ENSE00003466783	103692427	103692560
ENSE00003575864	103693979	103694176
ENSE00003597392	103693300	103693530
ENSE00003670179	103688958	103689083
ENSE00003785906	103694980	103695126

Expression profiles

Bgee: expression breadth broad, 75 present calls, max score 80.02.

Highest expression (Bgee): uterine tube, primordial germ cell in gonad, male germ line stem cell (sensu Vertebrata) in testis, tonsil, olfactory segment of nasal mucosa.

Genetic regulation across tissues (GTEx eQTL / sQTL)

AMY1B is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 1 tissue and its splicing (sQTL) in 1 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

2 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Pancreas	eqtl	2.9e-05	-0.47	1:103593955:TC:T
Pancreas	sqtl	1.8e-02	-1.65	1:103619572:A:T

Top tissues by expression

showing 100 of 108 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
right uterine tube	UBERON:0001302	80.02	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	78.98	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	77.37	gold quality
tonsil	UBERON:0002372	75.54	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	75.49	gold quality
fallopian tube	UBERON:0003889	66.95	gold quality
body of pancreas	UBERON:0001150	58.84	gold quality
saliva-secreting gland	UBERON:0001044	58.74	gold quality
right lobe of thyroid gland	UBERON:0001119	55.58	gold quality
minor salivary gland	UBERON:0001830	54.71	gold quality
endometrium	UBERON:0001295	54.06	gold quality
lung	UBERON:0002048	52.33	gold quality
pancreas	UBERON:0001264	50.84	gold quality
upper lobe of left lung	UBERON:0008952	50.58	gold quality
thyroid gland	UBERON:0002046	50.48	gold quality
left lobe of thyroid gland	UBERON:0001120	49.86	gold quality
stromal cell of endometrium	CL:0002255	49.00	gold quality
endocervix	UBERON:0000458	47.76	gold quality
placenta	UBERON:0001987	45.29	gold quality
skeletal muscle tissue	UBERON:0001134	44.37	gold quality
sural nerve	UBERON:0015488	43.88	gold quality
ventricular zone	UBERON:0003053	43.29	gold quality
ganglionic eminence	UBERON:0004023	42.29	gold quality
uterine cervix	UBERON:0000002	40.77	gold quality
muscle tissue	UBERON:0002385	40.44	gold quality
cortical plate	UBERON:0005343	39.76	gold quality
urinary bladder	UBERON:0001255	39.02	gold quality
bone marrow cell	CL:0002092	38.65	gold quality
monocyte	CL:0000576	38.23	gold quality
bone marrow	UBERON:0002371	38.12	silver quality
leukocyte	CL:0000738	37.77	gold quality
colonic epithelium	UBERON:0000397	37.20	gold quality
thoracic mammary gland	UBERON:0005200	36.89	gold quality
right lung	UBERON:0002167	36.78	gold quality
left uterine tube	UBERON:0001303	36.56	silver quality
blood	UBERON:0000178	35.99	gold quality
hindlimb stylopod muscle	UBERON:0004252	35.74	gold quality
islet of Langerhans	UBERON:0000006	35.34	gold quality
ectocervix	UBERON:0012249	34.91	gold quality
ovary	UBERON:0000992	34.80	gold quality
testis	UBERON:0000473	34.59	gold quality
left testis	UBERON:0004533	34.06	gold quality
gastrocnemius	UBERON:0001388	34.00	gold quality
muscle of leg	UBERON:0001383	33.61	gold quality
left ovary	UBERON:0002119	33.58	gold quality
skin of abdomen	UBERON:0001416	33.19	gold quality
liver	UBERON:0002107	33.10	gold quality
lymph node	UBERON:0000029	33.09	gold quality
multicellular organism	UBERON:0000468	33.08	gold quality
esophagus mucosa	UBERON:0002469	33.08	silver quality
zone of skin	UBERON:0000014	33.06	gold quality
skin of leg	UBERON:0001511	32.64	silver quality
right adrenal gland	UBERON:0001233	32.00	silver quality
thoracic aorta	UBERON:0001515	31.85	gold quality
metanephros cortex	UBERON:0010533	31.73	silver quality
esophagus	UBERON:0001043	31.72	gold quality
ascending aorta	UBERON:0001496	31.49	gold quality
body of uterus	UBERON:0009853	31.43	gold quality
right lobe of liver	UBERON:0001114	31.12	gold quality
nucleus accumbens	UBERON:0001882	30.45	silver quality
omental fat pad	UBERON:0010414	30.21	silver quality
right ovary	UBERON:0002118	30.20	silver quality
descending thoracic aorta	UBERON:0002345	30.13	silver quality
stomach	UBERON:0000945	30.10	gold quality
superior frontal gyrus	UBERON:0002661	29.95	gold quality
tibial nerve	UBERON:0001323	29.88	gold quality
adrenal gland	UBERON:0002369	29.82	silver quality
lower esophagus	UBERON:0013473	29.77	gold quality
lower esophagus muscularis layer	UBERON:0035833	29.75	gold quality
frontal cortex	UBERON:0001870	29.60	gold quality
body of stomach	UBERON:0001161	29.45	gold quality
vermiform appendix	UBERON:0001154	29.43	gold quality
substantia nigra	UBERON:0002038	29.37	silver quality
right adrenal gland cortex	UBERON:0035827	29.29	gold quality
left adrenal gland cortex	UBERON:0035825	29.25	silver quality
right frontal lobe	UBERON:0002810	29.06	gold quality
right testis	UBERON:0004534	28.89	gold quality
heart left ventricle	UBERON:0002084	28.80	gold quality
transverse colon	UBERON:0001157	28.78	silver quality
heart	UBERON:0000948	28.76	gold quality
spleen	UBERON:0002106	28.65	silver quality
cerebral cortex	UBERON:0000956	28.34	silver quality
smooth muscle tissue	UBERON:0001135	28.33	silver quality
left adrenal gland	UBERON:0001234	28.15	silver quality
duodenum	UBERON:0002114	28.14	gold quality
brain	UBERON:0000955	28.05	silver quality
caudate nucleus	UBERON:0001873	27.41	silver quality
right coronary artery	UBERON:0001625	27.37	gold quality
primary visual cortex	UBERON:0002436	27.37	gold quality
fundus of stomach	UBERON:0001160	27.29	gold quality
prostate gland	UBERON:0002367	27.05	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	26.59	gold quality
anterior cingulate cortex	UBERON:0009835	26.53	gold quality
right atrium auricular region	UBERON:0006631	26.02	silver quality
gall bladder	UBERON:0002110	25.98	gold quality
corpus callosum	UBERON:0002336	25.32	gold quality
pituitary gland	UBERON:0000007	24.71	gold quality
Brodmann (1909) area 9	UBERON:0013540	24.54	gold quality
hypothalamus	UBERON:0001898	24.44	silver quality
adenohypophysis	UBERON:0002196	24.18	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	24.54

HPA expression

RNA tissue specificity: Tissue enriched

16 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Salivary gland	tissue	9825.3	high
Cervix	tissue	101.7	not detected
Fallopian tube	tissue	27.4	not detected
Lung	tissue	3.6	not detected
Tonsil	tissue	2.6	not detected
Pancreas	tissue	2.0	not detected
Breast	tissue	1.4	not detected
Thymus	tissue	1.4
Bone marrow	tissue	1.0	not detected
Thyroid gland	tissue	0.9	not detected
Skin 1	tissue	0.7	not detected
Heart muscle	tissue	0.5	not detected
Testis	tissue	0.3	not detected
Placenta	tissue	0.3	not detected
Ovary	tissue	0.2	not detected
Esophagus	tissue	0.2	not detected

Regulation

Is transcription factor: no

Functional genomics

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000330330 — one region, missense o/e 0.02.

Literature-anchored findings (GeneRIF, showing 6)

• 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)
• results show a strong association between acute physical stressor-induced elevations in sAA levels and patients with MDD. (PMID:22063648)
• Diurnal and stress-response salivary alpha amylase patterns were related to child adiposity: decreased morning alpha amylase was associated with increased BMI. (PMID:25588701)
• 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)
• At baseline, a modest association between AMY1 gene copy number and BMI (P = 0.04) was observed but AMY1 gene copy was not associated with baseline glycemic variables. (PMID:30982860)
• AMY1 Gene Copy Number Correlates With Glucose Absorption and Visceral Fat Volume, but Not with Insulin Resistance. (PMID:32697825)

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), AMY1C (ENSG00000187733), AMY1A (ENSG00000237763), AMY2B (ENSG00000240038), AMY2A (ENSG00000243480)

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

Organism	UniProt	Identity	Method
Drosophila ananassae	O18345	99.8%	Diamond
Drosophila yakuba	P83833	99.8%	Diamond
Streptomyces limosus	P09794	99.6%	Diamond
Streptomyces griseus	P30270	99.6%	Diamond
Drosophila lini	O76262	99.0%	Diamond
Drosophila kikkawai	O77013	99.0%	Diamond
Drosophila sechellia	O76261	98.6%	Diamond
Drosophila simulans	O77016	98.6%	Diamond
Drosophila mauritiana	O77014	98.4%	Diamond
Drosophila bakoue	O77019	98.4%	Diamond
Drosophila jambulina	Q9GQV3	98.4%	Diamond
Drosophila punjabiensis	O77022	98.2%	Diamond
Drosophila bocqueti	O76284	97.8%	Diamond
Drosophila dossoui	O77021	97.8%	Diamond
Drosophila teissieri	O76260	97.6%	Diamond
Drosophila serrata	O76459	97.6%	Diamond
Drosophila erecta	O76265	97.2%	Diamond
Drosophila orena	O77015	97.2%	Diamond
Drosophila atripex	O77011	96.4%	Diamond
Drosophila bipectinata	Q9NJN8	96.4%	Diamond
Drosophila takahashii	O77018	95.5%	Diamond
Drosophila auraria	O77020	94.7%	Diamond
Drosophila varians	Q9NJN7	94.5%	Diamond
Drosophila ercepeae	O77012	94.1%	Diamond
Mus musculus	P00688	93.7%	Diamond
Rattus norvegicus	P00689	93.7%	Diamond
Drosophila elegans	Q9NJP0	93.7%	Diamond
Drosophila subobscura	O18420	91.5%	Diamond
Drosophila pseudoobscura pseudoobscura	O18552	91.5%	Diamond
Sus scrofa	P00690	86.5%	Diamond
Struthio camelus	P83053	84.5%	Diamond
Drosophila willistoni	O76263	83.8%	Diamond
Tribolium castaneum	P09107	78.7%	Diamond
Tenebrio molitor	P56634	78.7%	Diamond
Oryzias latipes	H2N0D4	74.0%	Diamond
Streptomyces violaceus	P22998	73.8%	Diamond
Pseudoalteromonas haloplanktis	P29957	70.4%	Diamond
Tityus serrulatus	P85843	70.4%	Diamond
Streptomyces thermoviolaceus	P27350	69.3%	Diamond
Phaedon cochleariae	O97396	67.8%	Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

Symbol	Type	Entrez
AMY1C	protein-coding	278
AMY1A	protein-coding	276
AMY2A	protein-coding	279
AMY2B	protein-coding	280

Protein

Protein identifiers

Alpha-amylase 1B — P0DTE7 (reviewed: P0DTE7)

All UniProt accessions (4): P0DTE7, P0DTE8, 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_001008219, NP_001373854, NP_001409049, NP_001409052, NP_001409056, NP_001409058 (=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

Enzyme classification (BRENDA)

• EC 3.2.1.1 — alpha-amylase (BRENDA: 280 organisms, 645 substrates, 924 inhibitors, 310 Km, 239 kcat entries)

Substrate kinetics (BRENDA)

43 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
2-CHLORO-4-NITROPHENYL BETA-D-MALTOHEPTAOSIDE	0.6–10	25
4,6-ETHYLIDENE-[G7]-P-NITROPHENYL-[G1]-ALPHA-D-M	0.01–0.281	16
STARCH	0.005–167.6	14
AMYLOSE	0.0002–18.2	10
AMYLOSE DP17	0.12–2.36	9
INSOLUBLE BLUE STARCH	0.3–1.5	9
MALTOTRIOSE	0.198–62.9	9
SOLUBLE STARCH	0.0006–3.05	9
2-CHLORO-4-NITROPHENYL ALPHA-MALTOTRIOSIDE	0.45–1.3	8
MALTOHEPTAOSE	0.21–3.37	7
MALTOPENTAOSE	0.12–3.1	7
4-NITROPHENYL ALPHA-D-MALTOHEPTAOSIDE-4,6-O-ETHY	0.065–0.26	6
MALTOHEXAOSE	0.43–6.37	4
PULLULAN	0.57–20	4
ALPHA-CYCLODEXTRIN	2.61–52	3

UniProt features (23 total): binding site 7, disulfide bond 5, modified residue 4, glycosylation site 2, active site 2, signal peptide 1, chain 1, site 1

Structure

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P0DTE7-F1	96.57	0.96

Human Protein Atlas

Protein class: Enzymes, ENZYME proteins, Hydrolases, Metabolic proteins, Predicted secreted proteins

Protein evidence: Evidence at protein level

Subcellular location (HPA, imaging): cytosol; golgi apparatus

Antibody reliability (HPA): IH supported · IF approved

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)

Position	Role
315	transition state stabilizer
212	nucleophile
248	proton donor

Ligand- & substrate-binding residues (7)

Position	Role
352	chloride
115	Ca(2+)
173	Ca(2+)
182	Ca(2+)
210	chloride
216	Ca(2+)
313	chloride

Post-translational modifications (4)

Type	Positions
Pyrrolidone carboxylic acid	16
Deamidated asparagine	365, 427, 474

Disulfide bonds (5)

Type	Positions
Disulfide bond	43–101, 85–130, 156–175, 393–399, 465–477

Glycosylation sites (2)

Type	Positions
N-linked (glcnac…) asparagine	427, 476

Function

Pathways and Gene Ontology

Reactome pathways

1 curated (TAS) of 3; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

3 pathways:

ID	Pathway	Evidence
R-HSA-189085	Digestion of dietary carbohydrate	curated
R-HSA-8935690	Digestion	—
R-HSA-8963743	Digestion and absorption	—

MSigDB gene sets: 26 (showing top): GOBP_OLIGOSACCHARIDE_METABOLIC_PROCESS, REACTOME_DIGESTION_OF_DIETARY_CARBOHYDRATE, GOBP_CARBOHYDRATE_METABOLIC_PROCESS, KEGG_STARCH_AND_SUCROSE_METABOLISM, chr1p21, GOMF_HYDROLASE_ACTIVITY_ACTING_ON_GLYCOSYL_BONDS, GOMF_HYDROLASE_ACTIVITY_HYDROLYZING_O_GLYCOSYL_COMPOUNDS, LU_EZH2_TARGETS_DN, GOMF_AMYLASE_ACTIVITY, GOMF_CHLORIDE_ION_BINDING, REACTOME_DIGESTION, REACTOME_DIGESTION_AND_ABSORPTION, ANDERSON_BLOOD_CN54GP140_ADJUVANTED_WITH_GLA_AF_AGE_18_45YO_3DY_UP, KANNAN_BLOOD_2012_2013_TIV_AGE_65PLS_REVACCINATED_IN_6_9_MO_VS_REVACCINATED_IN_12_13_MOS_DN, HOFT_CD4_POSITIVE_ALPHA_BETA_MEMORY_T_CELL_BCG_VACCINE_AGE_18_45YO_ID_7DY_TOP_100_DEG_EX_VIVO_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 (2): extracellular exosome (GO:0070062), extracellular region (GO:0005576)

Reactome top-level categories

2 top-level categories:

Category	Pathways
Digestion	1
Digestion and absorption	1

GO top-level categories

12 GO namespaces:

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

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 5 of 13 annotations. The rest are phylogenetic / computational / electronic (IEA).

5 experimentally-supported GO terms:

GO term	NS	Evidence
oligosaccharide metabolic process	BP	direct assay
extracellular exosome	CC	high-throughput assay
alpha-amylase activity	MF	direct assay
calcium ion binding	MF	direct assay
chloride ion binding	MF	direct assay

Disease & clinical

Genetic variants

Variant evidence for AMY1B: 9 ClinVar records (0 pathogenic / likely pathogenic).

ClinVar

9 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	7
Likely benign	2
Benign	0

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 19 predictions of 819):

Position(s)	Effect	Δscore	Sites
1:103688956–103688957	donor_loss	1.0000	5
1:103689084–103689085	acceptor_loss	1.0000	3
1:103689318	acceptor_gain	1.0000
1:103689322	acceptor_gain	1.0000
1:103691491	donor_gain	1.0000
1:103692447	donor_gain	1.0000
1:103692561	acceptor_loss	1.0000
1:103692572	acceptor_gain	1.0000
1:103693339	donor_gain	1.0000
1:103694978–103694979	donor_loss	1.0000	4

HPA cancer prognostics

RNA cancer specificity: Cancer enriched (Ovary Serous Cystadenocarcinoma)

Disease associations

OMIM: gene MIM:104701 | disease phenotypes:

Drugs & pharmacology

Drug and pharmacology data

Is drug target: no

PharmGKB: 1 entry (CPIC guideline: no)

PubChem BioAssay actives

20 with measured affinity, of 184 total; 6 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
(2S)-N-[(2S)-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
(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
(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	1248385: Inhibition of human salivary alpha-amylase using GalG2CNP as substrate by UV-Vis spectrophotometric analysis	ic50	0.5000	uM
5-[5-[[4-[5-[3,4-dihydroxy-6-methyl-5-[[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-5,6-dihydroxy-3-(hydroxymethyl)cyclohex-2-en-1-yl]amino]-3,4-dihydroxy-6-methyloxan-2-yl]oxy-6-(hydroxymethyl)oxane-2,3,4-triol	1248392: Inhibition of human salivary alpha-amylase using GalG2CNP as substrate	ki	0.7000	uM
[(2R,3R,4S,5R,6S)-3,4,5,6-tetrakis[(3,4,5-trihydroxybenzoyl)oxy]oxan-2-yl]methyl 3,4,5-trihydroxybenzoate	1248394: Inhibition of human salivary alpha-amylase using GalG2CNP as substrate assessed as CNP liberation by spectrophotometric analysis	ic50	2.3500	uM
5,6,7-trihydroxy-2-(4-hydroxyphenyl)chromen-4-one	1798320: In Vitro alpha-Amylase Activity Assay from Article 10.1021/jm800115x: “Flavonoids for controlling starch digestion: structural requirements for inhibiting human alpha-amylase.”	ic50	9.6400	uM

CTD chemical–gene interactions

11 total (human), top 11 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
CGP 52608	affects binding, increases reaction	1
Air Pollutants	increases abundance, increases expression	1
Ethanol	affects cotreatment, decreases expression, increases abundance	1
Arsenicals	decreases expression	1
Gasoline	increases abundance, affects cotreatment, decreases expression	1
Ozone	increases abundance, increases expression	1
Polycyclic Aromatic Hydrocarbons	affects cotreatment, decreases expression, increases abundance	1
Tunicamycin	decreases expression	1
Thapsigargin	decreases expression	1
1-Butanol	affects cotreatment, decreases expression, increases abundance	1
Particulate Matter	affects cotreatment, decreases expression, increases abundance	1

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.