Assay Detail
Functional
CHEMBL671493
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Compound was tested for antagonistic activity against D2 receptor from rat striatum, used [3H]raclopride as radioligand
42
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Comparison of 5-HT1A and dopamine D2 pharmacophores. X-ray structures and affinities of conformationally constrained ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 42 | 7.55 | 9.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL25074 | — | — | 1 | 9.33 |
| CHEMBL25013 | — | — | 1 | 9.13 |
| CHEMBL285341 | — | — | 1 | 9.02 |
| CHEMBL531 | PERGOLIDE | 4.0 | 1 | 9.00 |
| CHEMBL11066 | — | — | 1 | 8.70 |
| CHEMBL11363 | — | — | 1 | 8.52 |
| CHEMBL26118 | — | — | 2 | 8.28 |
| CHEMBL26181 | — | — | 1 | 8.27 |
| CHEMBL273412 | — | — | 1 | 7.89 |
| CHEMBL25359 | — | — | 1 | 7.77 |
| CHEMBL24978 | — | — | 1 | 7.73 |
| CHEMBL278751 | — | — | 1 | 7.66 |
| CHEMBL10048 | — | — | 1 | 7.60 |
| CHEMBL280955 | — | — | 1 | 7.60 |
| CHEMBL278285 | — | — | 1 | 7.60 |
| CHEMBL27399 | — | — | 1 | 7.55 |
| CHEMBL10207 | — | — | 2 | 7.48 |
| CHEMBL56519 | — | — | 1 | 7.42 |
| CHEMBL281248 | — | — | 1 | 7.41 |
| CHEMBL10570 | — | — | 1 | 7.38 |
| CHEMBL24050 | — | — | 1 | 7.33 |
| CHEMBL285873 | — | — | 1 | 7.31 |
| CHEMBL10289 | — | — | 2 | 7.27 |
| CHEMBL2051769 | — | — | 1 | 7.20 |
| CHEMBL284585 | — | — | 3 | 7.17 |
| CHEMBL276825 | — | — | 1 | 7.00 |
| CHEMBL27441 | — | — | 1 | 6.75 |
| CHEMBL566133 | — | — | 1 | 6.59 |
| CHEMBL2114337 | — | — | 1 | 6.53 |
| CHEMBL283956 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL25074 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL25013 | — | Ki | = | 0.74 | nM | 9.13 |
| CHEMBL285341 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL531 | PERGOLIDE | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL11066 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL11363 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL26118 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL26181 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL273412 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL25359 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL24978 | — | Ki | = | 18.8 | nM | 7.73 |
| CHEMBL278751 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL278285 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL10048 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL280955 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL27399 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL10207 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL56519 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL281248 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL10570 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL24050 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL285873 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL10289 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL2051769 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL284585 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL276825 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL27441 | — | Ki | = | 179.0 | nM | 6.75 |
| CHEMBL10289 | — | Ki | = | 198.0 | nM | 6.70 |
| CHEMBL566133 | — | Ki | = | 259.0 | nM | 6.59 |
| CHEMBL26118 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL2114337 | — | Ki | = | 296.0 | nM | 6.53 |
| CHEMBL283956 | — | Ki | = | 329.0 | nM | 6.48 |
| CHEMBL2114338 | — | Ki | = | 429.0 | nM | 6.37 |
| CHEMBL278091 | — | Ki | = | 877.0 | nM | 6.06 |
| CHEMBL24129 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL566970 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL284585 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL24110 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL10207 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2051973 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL281614 | — | Ki | > | 630.0 | nM | - |
| CHEMBL284585 | — | Ki | > | 1000.0 | nM | - |