Compound Detail
CHEMBL363295
TERODILINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL363295 |
| Name | TERODILINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | UISARWKNNNHPGI-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
3
Targets
4
Activities
1
Assay Types
15
PK Parameters
20
Publications
2
Known Names
2
Indications
Molecular Properties
281.4
MW (Da)
4.99
ALogP
1
HBA
1
HBD
12.0
PSA (Ų)
0.81
QED
0
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1986 |
| Availability | Withdrawn |
| Chirality | Racemic |
Indications
Polyuria Urinary Incontinence
ATC Classification
G04BD05
terodiline
Level 1: GENITO URINARY SYSTEM AND SEX HORMONES
Level 2: UROLOGICALS
Drug Warnings
Withdrawn
cardiotoxicity
cardiac adverse reactions, including ventricular tachycardia, heart block and bradycardia
Withdrawn
cardiotoxicity
cardiac adverse reactions, including ventricular tachycardia, heart block and bradycardia
Withdrawn
cardiotoxicity
cardiac adverse reactions, including ventricular tachycardia, heart block and bradycardia
Activity Summary
IC50 4 meas. best 6.3
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240 | IC50 | 6.3 | 5.77 | 500.0 | 2 |
| Voltage-gated L-type calcium channel CHEMBL2095229 | IC50 | 5.32 | 5.32 | 4800.0 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1C CHEMBL2366456 | IC50 | 4.47 | 4.47 | 33500.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 1.1 | mL.min-1.kg-1 | Homo sapiens |
| CL | 1.1 | mL.min-1.kg-1 | Homo sapiens |
| CL | 1.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 1.1 | mL.min-1.kg-1 | Homo sapiens |
| Fu | 0.08 | - | Homo sapiens |
| Fu | 0.08 | - | Homo sapiens |
| Fu | 0.028 | - | Homo sapiens |
| Fu | 0.071 | - | Macaca fascicularis |
| Fu | 0.148 | - | Canis lupus familiaris |
| Fu | 0.059 | - | Cavia porcellus |
| Fu | 0.049 | - | Mus musculus |
| Fu | 0.02 | - | Rattus norvegicus |
| Fu | 0.025 | - | Rattus norvegicus |
| MRT | 81.0 | hr | Homo sapiens |
| T1/2 | 56.0 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Voltage-gated inwardly rectifying potassium channel KCNH2 | IC50 | = | 500.0 | nM | 6.3 | Inhibitory concentration against IKr potassium channel | 15324906 |
| Voltage-gated L-type calcium channel | IC50 | = | 4800.0 | nM | 5.32 | Inhibition of Cav1.2 current measured using QPatch automatic path clamp system i... | 23812503 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 | IC50 | = | 5754.4 | nM | 5.24 | Inhibition of human ERG | 21185626 |
| Voltage-dependent L-type calcium channel subunit alpha-1C | IC50 | = | 33500.0 | nM | 4.47 | Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in gu... | - |
Literature References
Data from ChEMBL 36 via Core Engine