Compound Detail
CHEMBL3329435
PF-05212377 🧪 Phase II
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🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL3329435 |
| Name | PF-05212377 |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | MAYQIFVKVAUMPD-UHFFFAOYSA-N |
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
4
Known Names
1
Indications
1
Mechanisms
Molecular Properties
356.4
MW (Da)
1.99
ALogP
6
HBA
1
HBD
67.2
PSA (Ų)
0.78
QED
0
Ro5 Violations
3
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Serotonin 6 (5-HT6) receptor antagonist | ANTAGONIST | 5-hydroxytryptamine receptor 6 | ✓ | ✓ |
Indications
Alzheimer Disease
Activity Summary
Ki 3 meas. best 9.3
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | Ki | 9.3 | 9.2867 | 0.5 | 3 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 6 | Ki | = | 0.5 | nM | 9.3 | Binding affinity to 5HT6R (unknown origin) | 33439019 |
| 5-hydroxytryptamine receptor 6 | Ki | = | 0.53 | nM | 9.28 | Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells | 24850589 |
| 5-hydroxytryptamine receptor 6 | Ki | = | 0.53 | nM | 9.28 | Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constant | 34311086 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 24850589 | 10.1021/jm5003952 | 5-hydroxytryptamine receptor 6 | 1 |
| 33439019 | 10.1021/acs.jmedchem.0c02009 | 5-hydroxytryptamine receptor 6 | 1 |
| 34311086 | 10.1016/j.bmcl.2021.128275 | 5-hydroxytryptamine receptor 6 | 1 |
Data from ChEMBL 36 via Core Engine