Assay Detail
Binding
CHEMBL615839
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Binding affinity to 5-hydroxytryptamine 1A receptor in rat hippocampus membranes,3H-8-OH-DPAT and buspirone for nonspecific binding (NSB)
22
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Hippocampus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
3-amino-3,4-dihydro-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 2. Synthesis and quantitative structure-activity relationship studies of spiro[pyrrolidine- and piperidine-2,3'(2'H)-benzopyrans]
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.15 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL11592 | — | — | 3 | 9.70 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 8.62 |
| CHEMBL11265 | — | — | 3 | 8.17 |
| CHEMBL422283 | — | — | 1 | 8.05 |
| CHEMBL283606 | — | — | 1 | 7.70 |
| CHEMBL8412 | IPSAPIRONE | 2.0 | 1 | 7.46 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 7.22 |
| CHEMBL334498 | — | — | 1 | 7.20 |
| CHEMBL137486 | — | — | 1 | 7.17 |
| CHEMBL422453 | — | — | 1 | 7.13 |
| CHEMBL133375 | — | — | 1 | 7.00 |
| CHEMBL135952 | — | — | 1 | 6.75 |
| CHEMBL137643 | — | — | 1 | 6.53 |
| CHEMBL137478 | — | — | 1 | 6.38 |
| CHEMBL135490 | — | — | 1 | 5.89 |
| CHEMBL132970 | — | — | 1 | 5.36 |
| CHEMBL137642 | — | — | 1 | 4.85 |
| CHEMBL135335 | — | — | 1 | 4.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL11592 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL11592 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL11592 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL56 | 8-OH-DPAT | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL11265 | — | IC50 | = | 6.72 | nM | 8.17 |
| CHEMBL422283 | — | IC50 | = | 8.81 | nM | 8.05 |
| CHEMBL11265 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL283606 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL8412 | IPSAPIRONE | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL49 | BUSPIRONE | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL334498 | — | IC50 | = | 62.8 | nM | 7.20 |
| CHEMBL137486 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL422453 | — | IC50 | = | 74.6 | nM | 7.13 |
| CHEMBL133375 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL135952 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL137643 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL137478 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL11265 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL135490 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL132970 | — | IC50 | = | 4370.0 | nM | 5.36 |
| CHEMBL137642 | — | IC50 | = | 14200.0 | nM | 4.85 |
| CHEMBL135335 | — | IC50 | = | 81400.0 | nM | 4.09 |