Assay Detail
Binding
CHEMBL1776019
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in HeLa cells
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of PF-00217830: aryl piperazine napthyridinones as D2 partial agonists for schizophrenia and bipolar disorder.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 8.38 | 9.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1774078 | — | — | 1 | 9.11 |
| CHEMBL1774087 | — | — | 1 | 9.11 |
| CHEMBL1774081 | — | — | 1 | 9.08 |
| CHEMBL1774074 | — | — | 1 | 9.02 |
| CHEMBL1774086 | — | — | 1 | 8.96 |
| CHEMBL1774079 | — | — | 1 | 8.96 |
| CHEMBL1774073 | — | — | 1 | 8.92 |
| CHEMBL1774085 | — | — | 1 | 8.92 |
| CHEMBL1774068 | — | — | 1 | 8.77 |
| CHEMBL1774083 | — | — | 1 | 8.70 |
| CHEMBL1774084 | — | — | 1 | 8.52 |
| CHEMBL1774082 | — | — | 1 | 8.48 |
| CHEMBL1774075 | — | — | 1 | 8.46 |
| CHEMBL1774080 | PF-00217830 | 2.0 | 1 | 8.43 |
| CHEMBL1774070 | — | — | 1 | 8.41 |
| CHEMBL1774067 | — | — | 1 | 8.34 |
| CHEMBL1774076 | — | — | 1 | 8.20 |
| CHEMBL1774072 | — | — | 1 | 8.08 |
| CHEMBL1774071 | — | — | 1 | 8.07 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 7.99 |
| CHEMBL1774062 | — | — | 1 | 7.94 |
| CHEMBL1774069 | — | — | 1 | 7.86 |
| CHEMBL1774064 | — | — | 1 | 7.85 |
| CHEMBL1774063 | — | — | 1 | 7.75 |
| CHEMBL1774077 | — | — | 1 | 7.55 |
| CHEMBL1774065 | — | — | 1 | 7.39 |
| CHEMBL1774066 | — | — | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1774078 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL1774087 | — | Ki | = | 0.77 | nM | 9.11 |
| CHEMBL1774081 | — | Ki | = | 0.84 | nM | 9.08 |
| CHEMBL1774074 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL1774086 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1774079 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1774073 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL1774085 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL1774068 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL1774083 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1774084 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL1774082 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL1774075 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL1774080 | PF-00217830 | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL1774070 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL1774067 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL1774076 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL1774072 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL1774071 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL1774062 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL1774069 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL1774064 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1774063 | — | Ki | = | 17.7 | nM | 7.75 |
| CHEMBL1774077 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL1774065 | — | Ki | = | 40.7 | nM | 7.39 |
| CHEMBL1774066 | — | Ki | = | 52.7 | nM | 7.28 |