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| Stem definition | Drug id | CAS RN |
|---|---|---|
| antihyperglycaemics | 2845 | 83480-29-9 |
| Molecule | Description |
|---|---|
|
Synonyms:
|
|
| Dose | Unit | Route |
|---|---|---|
| 0.60 | mg | O |
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 6 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAP3K21,MAPK10,MAPK7,NTRK1,NTRK2,PDK2,PDK4,PIK3CB,PIK3CD,PRKDC,SIK2,STK33,TEK,TGFBR1 | 29 | |||
| kinase-selectivity-class | ACVRL1,AXL,BMX,CDK1,CDK16,CDK2,CDK3,CDK4,CDK6,CDK7,CDK8,CDK9,CHUK,DYRK1A,IGF1R,INSR,IRAK1,IRAK3,IRAK4,MAP2K6,MAP3K14,PDK1,PIK3CD,TGFBR1,ZAP70 | 25 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 20, 1994 | PMDA |
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Hypoglycaemia | 121.56 | 33.46 | 46 | 1582 | 69802 | 90557017 |
| Pneumatosis intestinalis | 73.06 | 33.46 | 16 | 1612 | 3421 | 90623398 |
| Renal impairment | 69.32 | 33.46 | 35 | 1593 | 105386 | 90521433 |
| Hepatic function abnormal | 54.34 | 33.46 | 23 | 1605 | 46265 | 90580554 |
| Hypoglycaemic coma | 53.01 | 33.46 | 12 | 1616 | 2978 | 90623841 |
| Lactic acidosis | 52.43 | 33.46 | 23 | 1605 | 50440 | 90576379 |
| Diabetes mellitus inadequate control | 46.24 | 33.46 | 16 | 1612 | 18668 | 90608151 |
| Glycosylated haemoglobin increased | 45.09 | 33.46 | 15 | 1613 | 15547 | 90611272 |
| Cerebral infarction | 44.28 | 33.46 | 17 | 1611 | 26579 | 90600240 |
| Altered state of consciousness | 38.10 | 33.46 | 16 | 1612 | 31516 | 90595303 |
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Cerebral infarction | 117.40 | 24.64 | 50 | 2467 | 31119 | 42587699 |
| Hypoglycaemia | 86.44 | 24.64 | 50 | 2467 | 59804 | 42559014 |
| Interstitial lung disease | 71.59 | 24.64 | 49 | 2468 | 78413 | 42540405 |
| Pemphigoid | 48.46 | 24.64 | 20 | 2497 | 11447 | 42607371 |
| Pneumatosis intestinalis | 45.01 | 24.64 | 15 | 2502 | 4737 | 42614081 |
| Renal impairment | 37.54 | 24.64 | 39 | 2478 | 110189 | 42508629 |
| Glycosylated haemoglobin increased | 30.48 | 24.64 | 15 | 2502 | 12909 | 42605909 |
| Hepatic function abnormal | 28.68 | 24.64 | 24 | 2493 | 51543 | 42567275 |
| Thrombotic cerebral infarction | 26.30 | 24.64 | 6 | 2511 | 463 | 42618355 |
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Hypoglycaemia | 199.78 | 26.06 | 96 | 4355 | 116008 | 110468840 |
| Cerebral infarction | 164.53 | 26.06 | 66 | 4385 | 51772 | 110533076 |
| Renal impairment | 100.37 | 26.06 | 73 | 4378 | 188372 | 110396476 |
| Pneumatosis intestinalis | 95.67 | 26.06 | 28 | 4423 | 8501 | 110576347 |
| Interstitial lung disease | 83.42 | 26.06 | 58 | 4393 | 139276 | 110445572 |
| Hepatic function abnormal | 77.64 | 26.06 | 47 | 4404 | 89248 | 110495600 |
| Glycosylated haemoglobin increased | 71.16 | 26.06 | 29 | 4422 | 23590 | 110561258 |
| Hypoglycaemic coma | 70.22 | 26.06 | 20 | 4431 | 5513 | 110579335 |
| Pemphigoid | 62.12 | 26.06 | 25 | 4426 | 19682 | 110565166 |
| Lactic acidosis | 56.36 | 26.06 | 39 | 4412 | 92772 | 110492076 |
| Diabetes mellitus inadequate control | 52.21 | 26.06 | 25 | 4426 | 29750 | 110555098 |
| Platelet count decreased | 48.87 | 26.06 | 53 | 4398 | 230390 | 110354458 |
| Altered state of consciousness | 46.65 | 26.06 | 29 | 4422 | 57597 | 110527251 |
| Decreased appetite | 45.52 | 26.06 | 74 | 4377 | 475772 | 110109076 |
| Ketoacidosis | 43.22 | 26.06 | 16 | 4435 | 10071 | 110574777 |
| Thrombotic cerebral infarction | 36.22 | 26.06 | 8 | 4443 | 786 | 110584062 |
| Diabetic ketoacidosis | 36.16 | 26.06 | 22 | 4429 | 42036 | 110542812 |
| Diabetes mellitus | 34.52 | 26.06 | 30 | 4421 | 99351 | 110485497 |
| Cerebral haemorrhage | 34.11 | 26.06 | 25 | 4426 | 64943 | 110519905 |
| Cardiac failure | 32.69 | 26.06 | 39 | 4412 | 187587 | 110397261 |
| Hyperglycaemia | 30.19 | 26.06 | 26 | 4425 | 85064 | 110499784 |
| Hyperglycaemic hyperosmolar nonketotic syndrome | 29.91 | 26.06 | 9 | 4442 | 3000 | 110581848 |
| Drug eruption | 28.97 | 26.06 | 21 | 4430 | 53638 | 110531210 |
| Dehydration | 27.38 | 26.06 | 44 | 4407 | 279467 | 110305381 |
| Fatigue | 26.64 | 26.06 | 8 | 4443 | 1215950 | 109368898 |
| Erythema multiforme | 26.11 | 26.06 | 14 | 4437 | 21083 | 110563765 |
None
| Source | Code | Description |
|---|---|---|
| ATC | A10BF03 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Alpha glucosidase inhibitors |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D007004 | Hypoglycemic Agents |
| MeSH PA | D065089 | Glycoside Hydrolase Inhibitors |
| CHEBI has role | CHEBI:35526 | hypoglycemic agent |
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Diabetes mellitus type 2 | indication | 44054006 | DOID:9352 |
| Glucosylceramide beta-glucosidase deficiency | indication | 190794006 | DOID:1926 |
| Impaired renal function disorder | contraindication | 197663003 | |
| Pregnancy, function | contraindication | 289908002 | |
| Peripheral nerve disease | contraindication | 302226006 | |
| Breastfeeding (mother) | contraindication | 413712001 |
None
None
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 11.5 | acidic |
| pKa2 | 12.5 | acidic |
| pKa3 | 8.5 | Basic |
None
None
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Lysosomal alpha-glucosidase | Enzyme | INHIBITOR | IC50 | 7.15 | CHEMBL | SCIENTIFIC LITERATURE | |||
| Maltase-glucoamylase, intestinal | Enzyme | IC50 | 5.89 | CHEMBL | |||||
| Sucrase-isomaltase, intestinal | Enzyme | IC50 | 7.15 | CHEMBL | |||||
| Lysosomal alpha-glucosidase | Enzyme | IC50 | 6.96 | CHEMBL | |||||
| Glycogen debranching enzyme | Enzyme | IC50 | 4.15 | CHEMBL |
| ID | Source |
|---|---|
| D01665 | KEGG_DRUG |
| C0532578 | UMLSCUI |
| CHEBI:32300 | CHEBI |
| VOG | PDB_CHEM_ID |
| CHEMBL476960 | ChEMBL_ID |
| DB04878 | DRUGBANK_ID |
| C102817 | MESH_SUPPLEMENTAL_RECORD_UI |
| 444020 | PUBCHEM_CID |
| 6797 | INN_ID |
| S77P977AG8 | UNII |
| 010940 | NDDF |
| 1163442006 | SNOMEDCT_US |
| 1172848007 | SNOMEDCT_US |
| C054577 | MESH_SUPPLEMENTAL_RECORD_UI |
None