Assay Detail
Binding
CHEMBL4709841
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Displacement of [3H](+)8-OH-DPAT from rat cerebral cortex 5HT1A receptor measured after 30 mins by liquid scintillation counting method
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Isoquinolinone derivatives as potent CNS multi-receptor D/5-HT/5-HT/5-HT/5-HT agents: Synthesis and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 6.97 | 8.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4764679 | — | — | 1 | 8.04 |
| CHEMBL4756417 | — | — | 1 | 7.99 |
| CHEMBL4743324 | — | — | 1 | 7.92 |
| CHEMBL4741087 | — | — | 1 | 7.91 |
| CHEMBL4795287 | — | — | 1 | 7.74 |
| CHEMBL4749019 | — | — | 1 | 7.70 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 7.70 |
| CHEMBL4783375 | — | — | 1 | 7.51 |
| CHEMBL4761213 | — | — | 1 | 7.23 |
| CHEMBL3965773 | — | — | 1 | 7.19 |
| CHEMBL4790565 | — | — | 1 | 7.17 |
| CHEMBL4753384 | — | — | 1 | 7.05 |
| CHEMBL4759887 | — | — | 1 | 6.92 |
| CHEMBL4778204 | — | — | 1 | 6.80 |
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 6.74 |
| CHEMBL4797306 | — | — | 1 | 6.73 |
| CHEMBL4746373 | — | — | 1 | 6.70 |
| CHEMBL4777373 | — | — | 1 | 6.58 |
| CHEMBL4749033 | — | — | 1 | 6.45 |
| CHEMBL3911283 | — | — | 1 | 6.37 |
| CHEMBL4795213 | — | — | 1 | 6.07 |
| CHEMBL4779075 | — | — | 1 | 5.98 |
| CHEMBL4781390 | — | — | 1 | 5.98 |
| CHEMBL4788000 | — | — | 1 | 5.96 |
| CHEMBL4751120 | — | — | 1 | 5.89 |
| CHEMBL4758213 | — | — | 1 | - |
| CHEMBL4742251 | — | — | 1 | - |
| CHEMBL4761618 | — | — | 1 | - |
| CHEMBL4800484 | — | — | 1 | - |
| CHEMBL4798115 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4764679 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL4756417 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL4743324 | — | Ki | = | 12.1 | nM | 7.92 |
| CHEMBL4741087 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL4795287 | — | Ki | = | 18.3 | nM | 7.74 |
| CHEMBL4749019 | — | Ki | = | 20.1 | nM | 7.70 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 19.8 | nM | 7.70 |
| CHEMBL4783375 | — | Ki | = | 30.6 | nM | 7.51 |
| CHEMBL4761213 | — | Ki | = | 59.3 | nM | 7.23 |
| CHEMBL3965773 | — | Ki | = | 65.2 | nM | 7.19 |
| CHEMBL4790565 | — | Ki | = | 68.2 | nM | 7.17 |
| CHEMBL4753384 | — | Ki | = | 89.2 | nM | 7.05 |
| CHEMBL4759887 | — | Ki | = | 119.2 | nM | 6.92 |
| CHEMBL4778204 | — | Ki | = | 158.2 | nM | 6.80 |
| CHEMBL85 | RISPERIDONE | Ki | = | 182.0 | nM | 6.74 |
| CHEMBL4797306 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL4746373 | — | Ki | = | 198.3 | nM | 6.70 |
| CHEMBL4777373 | — | Ki | = | 262.2 | nM | 6.58 |
| CHEMBL4749033 | — | Ki | = | 356.2 | nM | 6.45 |
| CHEMBL3911283 | — | Ki | = | 431.0 | nM | 6.37 |
| CHEMBL4795213 | — | Ki | = | 856.0 | nM | 6.07 |
| CHEMBL4779075 | — | Ki | = | 1039.0 | nM | 5.98 |
| CHEMBL4781390 | — | Ki | = | 1039.0 | nM | 5.98 |
| CHEMBL4788000 | — | Ki | = | 1109.0 | nM | 5.96 |
| CHEMBL4751120 | — | Ki | = | 1295.5 | nM | 5.89 |
| CHEMBL4758213 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4742251 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4761618 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4800484 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4798115 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4754923 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4743127 | — | Ki | > | 10000.0 | nM | - |