Compound Detail
CHEMBL604710
Z160 🧪 Phase II
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🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL604710 |
| Name | Z160 |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | VCPMZDWBEWTGNW-UHFFFAOYSA-N |
6
Targets
6
Activities
1
Assay Types
11
PK Parameters
18
Publications
6
Known Names
2
Indications
1
Mechanisms
Molecular Properties
460.6
MW (Da)
6.14
ALogP
2
HBA
0
HBD
23.6
PSA (Ų)
0.33
QED
1
Ro5 Violations
7
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Voltage-gated N-type calcium channel alpha-1B subunit blocker | BLOCKER | Voltage-dependent N-type calcium channel subunit alpha-1B | ✓ | ✓ |
Indications
Neuralgia, Postherpetic Radiculopathy
Activity Summary
IC50 6 meas. best 6.96
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Voltage-dependent L-type calcium channel subunit beta-1/alpha-1B/alpha-2/delta-1 CHEMBL3885653 | IC50 | 6.96 | 6.96 | 110.0 | 1 |
| N-type calcium channel alpha-1b/alpha2delta-1/beta-1b CHEMBL4106160 | IC50 | 6.96 | 6.96 | 110.0 | 1 |
| Voltage-dependent L-type calcium channel alpha1C/alpha2delta/beta1b CHEMBL3988638 | IC50 | 4.91 | 4.91 | 12200.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 4.91 | 4.91 | 12200.0 | 1 |
| Voltage-dependent N-type calcium channel subunit alpha-1B CHEMBL4478 | IC50 | 4.41 | 4.41 | 39000.0 | 1 |
| Voltage-dependent T-type calcium channel subunit alpha-1H CHEMBL1859 | IC50 | 4.35 | 4.35 | 45000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 715.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 761.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 999.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 1136.0 | ng.hr.mL-1 | Rattus norvegicus |
| CL | 45.5 | mL.min-1.kg-1 | Rattus norvegicus |
| Cmax | 1673.83 | nM | Rattus norvegicus |
| Cmax | 510.18 | nM | Rattus norvegicus |
| F | 30.0 | % | Rattus norvegicus |
| T1/2 | 3.3 | hr | Rattus norvegicus |
| T1/2 | 2.1 | hr | Rattus norvegicus |
| Tmax | 2.3 | ng.hr/ml | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 19815411 | 10.1016/j.bmcl.2009.09.008 | Rattus norvegicus | 14 |
| 19815411 | 10.1016/j.bmcl.2009.09.008 | Unchecked | 4 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| 19815411 | 10.1016/j.bmcl.2009.09.008 | Voltage-gated inwardly rectifying potassium channel KCNH2 | 2 |
| 20117000 | 10.1016/j.bmcl.2010.01.008 | Rattus norvegicus | 2 |
| - | 10.6019/CHEMBL3301361 | ADMET | 2 |
| 19815411 | 10.1016/j.bmcl.2009.09.008 | Mu-type opioid receptor | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| 29622412 | 10.1016/j.bmc.2018.03.031 | Voltage-dependent T-type calcium channel subunit alpha-1H | 1 |
| 29622412 | 10.1016/j.bmc.2018.03.031 | Voltage-dependent N-type calcium channel subunit alpha-1B | 1 |
| 19815411 | 10.1016/j.bmcl.2009.09.008 | Cannabinoid receptor 1 | 1 |
| 19815411 | 10.1016/j.bmcl.2009.09.008 | Voltage-dependent L-type calcium channel subunit beta-1/alpha-1B/alpha-2/delta-1 | 1 |
| 20117000 | 10.1016/j.bmcl.2010.01.008 | N-type calcium channel alpha-1b/alpha2delta-1/beta-1b | 1 |
| 20117000 | 10.1016/j.bmcl.2010.01.008 | Voltage-dependent L-type calcium channel alpha1C/alpha2delta/beta1b | 1 |
| 20117000 | 10.1016/j.bmcl.2010.01.008 | No relevant target | 1 |
Data from ChEMBL 36 via Core Engine