Compound Detail
CHEMBL3989843
TRANYLCYPROMINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL3989843 |
| Name | TRANYLCYPROMINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | IGLYMJRIWWIQQE-QUOODJBBSA-N |
| Therapeutic | ✓ Yes |
16
Targets
141
Activities
4
Assay Types
11
PK Parameters
20
Publications
3
Known Names
9
Indications
Molecular Properties
266.4
MW (Da)
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1961 |
| Availability | Prescription |
| Chirality | Racemic |
Indications
Depressive Disorder Depressive Disorder Anxiety Dementia Schizophrenia Hypotension, Orthostatic Leukemia Leukemia, Myeloid, Acute Myelodysplastic Syndromes
ATC Classification
N06AF04
tranylcypromine
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOANALEPTICS
Activity Summary
IC50 107 meas. best 8.35
Ki 30 meas. best 7.58
Kd 3 meas. best 5.7
EC50 1 meas. best 5.57
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Lysine-specific histone demethylase 1A CHEMBL6136 | IC50 | 8.35 | 4.7888 | 4.5 | 26 |
| Amine oxidase [flavin-containing] B CHEMBL2039 | IC50 | 8.03 | 5.738 | 9.4 | 20 |
| Amine oxidase [flavin-containing] B CHEMBL2039 | Ki | 7.58 | 5.3075 | 26.0 | 4 |
| Cytochrome P450 2A6 CHEMBL5282 | IC50 | 7.1 | 6.446 | 80.0 | 5 |
| Amine oxidase [flavin-containing] A CHEMBL1951 | IC50 | 7.07 | 5.6242 | 85.0 | 19 |
| Cytochrome P450 2A6 CHEMBL5282 | Ki | 6.89 | 6.89 | 130.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL4153 | Ki | 5.75 | 5.75 | 1800.0 | 1 |
| Cytochrome P450 2C19 CHEMBL3622 | IC50 | 5.72 | 5.2716 | 1900.0 | 19 |
| Cytochrome P450 2A6 CHEMBL5282 | Kd | 5.7 | 5.7 | 2000.0 | 1 |
| Cytochrome P450 2A13 CHEMBL3542436 | Kd | 5.64 | 5.64 | 2300.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | EC50 | 5.57 | 5.57 | 2697.0 | 1 |
| Amine oxidase [flavin-containing] A CHEMBL1951 | Ki | 5.3 | 5.3 | 5000.0 | 1 |
| Sigma intracellular receptor 2 CHEMBL4105864 | Ki | 5.21 | 5.21 | 6200.0 | 1 |
| Cytochrome P450 2B6 CHEMBL4729 | IC50 | 5.21 | 5.1957 | 6200.0 | 7 |
| Cytochrome P450 2A13 CHEMBL3542436 | Ki | 5.19 | 5.19 | 6500.0 | 1 |
| 7-alpha-hydroxycholest-4-en-3-one 12-alpha-hydroxylase CHEMBL4523494 | IC50 | 5.11 | 5.11 | 7800.0 | 1 |
| LSD1/CoREST complex CHEMBL3137262 | IC50 | 5.06 | 4.75 | 8800.0 | 3 |
| D(3) dopamine receptor CHEMBL3138 | Ki | 4.89 | 4.89 | 12793.0 | 1 |
| Serine protease 1 CHEMBL3769 | Ki | 4.88 | 4.88 | 13300.0 | 1 |
| Lysine-specific histone demethylase 1A CHEMBL6136 | Ki | 4.68 | 4.496 | 21000.0 | 5 |
| D(2) dopamine receptor CHEMBL339 | Ki | 4.23 | 4.23 | 58737.0 | 1 |
| Lysine-specific histone demethylase 1A/REST corepressor CHEMBL4296114 | IC50 | 4.05 | 4.05 | 89080.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| Cmax | 490.0 | nM | Homo sapiens |
| Fu | 0.49 | - | Not specified |
| Fu | 0.53 | - | Not specified |
| Fu | 0.612 | - | Not specified |
| Fu | 0.63 | - | Not specified |
| Inhibition | 97.0 | % | Homo sapiens |
| Inhibition | 98.0 | % | Homo sapiens |
| Inhibition | 99.0 | % | Homo sapiens |
| Inhibition | 96.0 | % | Homo sapiens |
| Inhibition | 99.0 | % | Homo sapiens |
| Inhibition | 97.0 | % | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine