Compound Detail
CHEMBL266510
FLINDOKALNER 🧪 Phase III
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🧪 Phase III
Basic Information
| ChEMBL ID | CHEMBL266510 |
| Name | FLINDOKALNER |
| Phase | Phase III |
| Structure Type | MOL |
| InChI Key | ULYONBAOIMCNEH-HNNXBMFYSA-N |
6
Targets
6
Activities
2
Assay Types
19
PK Parameters
20
Publications
4
Known Names
6
Mechanisms
Molecular Properties
359.7
MW (Da)
4.53
ALogP
2
HBA
1
HBD
38.3
PSA (Ų)
0.80
QED
0
Ro5 Violations
2
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Calcium-activated potassium channel subunit alpha-1 opener | OPENER | Calcium-activated potassium channel subunit alpha-1 | ✓ | ✓ |
| Voltage-gated potassium channel subunit Kv7.5 activator | ACTIVATOR | Potassium voltage-gated channel subfamily KQT member 5 | ✓ | ✓ |
| Voltage-gated potassium channel subunit Kv7.4 activator | ACTIVATOR | Potassium voltage-gated channel subfamily KQT member 4 | ✓ | ✓ |
| Voltage-gated potassium channel subunit Kv7.2 activator | ACTIVATOR | Potassium voltage-gated channel subfamily KQT member 2 | ✓ | ✓ |
| Voltage-gated potassium channel, KQT; KCNQ2(Kv7.2)/KCNQ3(Kv7.3) activator | ACTIVATOR | Voltage-gated potassium channel, KQT; KCNQ2(Kv7.2)/KCNQ3(Kv7.3) | ✓ | ✓ |
| Voltage-gated potassium channel KCNQ3/KCNQ4 activator | ACTIVATOR | Voltage-gated potassium channel KCNQ3/KCNQ4 | ✓ | ✓ |
Activity Summary
EC50 5 meas. best 6.45
IC50 1 meas. best 6.45
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| NON-PROTEIN TARGET CHEMBL3879801 | IC50 | 6.45 | 6.45 | 352.0 | 1 |
| Calcium-activated potassium channel subunit alpha-1 CHEMBL4304 | EC50 | 6.45 | 6.45 | 352.0 | 1 |
| Potassium voltage-gated channel subfamily KQT member 2 CHEMBL2476 | EC50 | 5.62 | 5.62 | 2400.0 | 1 |
| Potassium voltage-gated channel subfamily KQT member 3 CHEMBL2684 | EC50 | 5.62 | 5.62 | 2400.0 | 1 |
| Potassium voltage-gated channel subfamily KQT member 5 CHEMBL2925 | EC50 | 5.62 | 5.62 | 2400.0 | 1 |
| Potassium voltage-gated channel subfamily KQT member 4 CHEMBL3576 | EC50 | 5.62 | 5.62 | 2400.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 3000.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 28800.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 320.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | - | ng.hr.mL-1 | Rattus norvegicus |
| CL | 51.5 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 40.2 | mL.min-1.kg-1 | Macaca |
| CL | 3.1 | mL.min-1.kg-1 | Canis lupus familiaris |
| CL | 7.63 | mL.min-1.kg-1 | Homo sapiens |
| CL | 15.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 29.9 | mL.min-1.kg-1 | Rattus norvegicus |
| Fu | 0.0038 | - | Homo sapiens |
| MRT | 11.0 | hr | Homo sapiens |
| T1/2 | 1.9 | hr | Rattus norvegicus |
| T1/2 | 1.6 | hr | Rattus norvegicus |
| T1/2 | 1.8 | hr | Rattus norvegicus |
| T1/2 | - | hr | Rattus norvegicus |
| T1/2 | 37.0 | hr | Homo sapiens |
| T1/2 | 168.0 | hr | Homo sapiens |
| Vd | 5.8 | L.kg-1 | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Calcium-activated potassium channel subunit alpha-1 | EC50 | = | 352.0 | nM | 6.45 | Positive modulation of Kca 1.1 (unknown origin) | 23121096 |
| NON-PROTEIN TARGET | IC50 | = | 352.0 | nM | 6.45 | In vitro reduction of glutamate release in hippocampal slices | 11356099 |
| Potassium voltage-gated channel subfamily KQT member 5 | EC50 | = | 2400.0 | nM | 5.62 | Positive modulatory activity at voltage-gated K channel 7.5 (unknown origin) | 23121096 |
| Potassium voltage-gated channel subfamily KQT member 4 | EC50 | = | 2400.0 | nM | 5.62 | Positive modulatory activity at voltage-gated K channel 7.4 (unknown origin) | 23121096 |
| Potassium voltage-gated channel subfamily KQT member 3 | EC50 | = | 2400.0 | nM | 5.62 | Positive modulatory activity at voltage-gated K channel 7.3 (unknown origin) | 23121096 |
| Potassium voltage-gated channel subfamily KQT member 2 | EC50 | = | 2400.0 | nM | 5.62 | Positive modulatory activity at voltage-gated K channel 7.2 (unknown origin) | 23121096 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.6019/CHEMBL5724801 | U2OS | 320 |
| - | 10.6019/CHEMBL5724801 | Fibroblast | 320 |
| - | 10.6019/CHEMBL5724801 | HEK-293T | 320 |
| 11909708 | 10.1016/s0960-894x(02)00101-4 | Rattus norvegicus | 10 |
| - | 10.6019/CHEMBL5303304 | HEK-293T | 9 |
| 16621936 | 10.1124/dmd.105.006619 | ADMET | 8 |
| - | 10.6019/CHEMBL5303304 | U2OS | 7 |
| - | 10.6019/CHEMBL5303304 | Fibroblast | 6 |
| 18426954 | 10.1124/dmd.108.020479 | ADMET | 4 |
| 11909708 | 10.1016/s0960-894x(02)00101-4 | HEK293 | 3 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| 15781124 | 10.1016/j.pharmthera.2004.10.013 | UDP-glucuronosyltransferase 2B7 | 2 |
| 23121096 | 10.1021/jm3011433 | Calcium-activated potassium channel subunit alpha-1 | 1 |
| 23121096 | 10.1021/jm3011433 | Potassium voltage-gated channel subfamily KQT member 2 | 1 |
| 23121096 | 10.1021/jm3011433 | Potassium voltage-gated channel subfamily KQT member 3 | 1 |
| 23121096 | 10.1021/jm3011433 | Potassium voltage-gated channel subfamily KQT member 4 | 1 |
| 18426954 | 10.1124/dmd.108.020479 | NON-PROTEIN TARGET | 1 |
| 11909708 | 10.1016/s0960-894x(02)00101-4 | ADMET | 1 |
Data from ChEMBL 36 via Core Engine