Compound Detail
CHEMBL3219124
AZD-1656 🧪 Phase II
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🧪 Phase II
COC[C@H](C)Oc1cc(Oc2cnc(C(=O)N3CCC3)cn2)cc(C(=O)Nc2cnc(C)cn2)c1
Basic Information
| ChEMBL ID | CHEMBL3219124 |
| Name | AZD-1656 |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | FJEJHJINOKKDCW-INIZCTEOSA-N |
1
Targets
3
Activities
2
Assay Types
7
PK Parameters
10
Publications
3
Known Names
3
Indications
1
Mechanisms
Molecular Properties
478.5
MW (Da)
2.88
ALogP
9
HBA
1
HBD
128.7
PSA (Ų)
0.49
QED
0
Ro5 Violations
9
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Hexokinase type IV activator | ACTIVATOR | Hexokinase-4 | ✓ | ✓ |
Indications
Diabetes Mellitus, Type 2 Severe Acute Respiratory Syndrome Diabetes Mellitus, Type 1
Activity Summary
EC50 2 meas. best 7.55
Kd 1 meas. best 7.97
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Hexokinase-4 CHEMBL3820 | Kd | 7.97 | 7.97 | 10.8 | 1 |
| Hexokinase-4 CHEMBL3820 | EC50 | 7.55 | 7.38 | 28.0 | 2 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 16.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 310.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 8.1 | mL.min-1.kg-1 | Canis lupus familiaris |
| CL | 50.0 | mL.min-1.kg-1 | Canis lupus familiaris |
| F | 100.0 | % | Rattus norvegicus |
| F | 100.0 | % | Canis lupus familiaris |
| T1/2 | 0.03431 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Hexokinase-4 | Kd | = | 10.8 | nM | 7.97 | Binding affinity to biotinylated human recombinant glucokinase expressed in Esch... | - |
| Hexokinase-4 | EC50 | = | 28.0 | nM | 7.55 | Activation of recombinant human glucokinase assessed as formation of glucose-6-p... | - |
| Hexokinase-4 | EC50 | = | 61.0 | nM | 7.21 | Inhibition of recombinant human pancreatic glucokinase by G-6-P dehydrogenase as... | - |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.1039/C2MD20077E | Rattus norvegicus | 5 |
| - | 10.1039/C4MD00027G | Hexokinase-4 | 5 |
| - | 10.1039/C2MD20077E | Canis familiaris | 4 |
| - | 10.1039/C2MD20077E | No relevant target | 2 |
| - | 10.1039/C4MD00027G | Rattus norvegicus | 2 |
| - | 10.1039/C2MD20077E | Hexokinase-4 | 1 |
| - | 10.1039/C2MD20077E | MDCK | 1 |
| - | 10.1039/C2MD20077E | Voltage-gated inwardly rectifying potassium channel KCNH2 | 1 |
| 25815149 | 10.1021/ml5004712 | Mus musculus | 1 |
| - | 10.1039/C4MD00027G | ADMET | 1 |
Data from ChEMBL 36 via Core Engine