Assay Detail
Binding
CHEMBL4406065
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-Mesulergine from recombinant human 5HT2C receptor expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 51 | 6.69 | 7.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4522558 | — | — | 1 | 7.35 |
| CHEMBL4541924 | — | — | 1 | 7.31 |
| CHEMBL4561808 | — | — | 1 | 7.31 |
| CHEMBL4593394 | — | — | 1 | 7.30 |
| CHEMBL4442408 | — | — | 1 | 7.28 |
| CHEMBL4452683 | — | — | 1 | 7.24 |
| CHEMBL4586582 | — | — | 1 | 7.21 |
| CHEMBL4454872 | — | — | 1 | 7.20 |
| CHEMBL4531363 | — | — | 1 | 7.17 |
| CHEMBL4456964 | — | — | 1 | 7.07 |
| CHEMBL4577162 | — | — | 1 | 7.07 |
| CHEMBL4527244 | — | — | 1 | 7.01 |
| CHEMBL4456007 | — | — | 1 | 6.98 |
| CHEMBL4590839 | — | — | 1 | 6.97 |
| CHEMBL4590211 | — | — | 1 | 6.91 |
| CHEMBL4440698 | — | — | 1 | 6.90 |
| CHEMBL4453478 | — | — | 1 | 6.88 |
| CHEMBL4455719 | — | — | 1 | 6.87 |
| CHEMBL4525624 | — | — | 1 | 6.87 |
| CHEMBL4580817 | — | — | 1 | 6.86 |
| CHEMBL4472900 | — | — | 1 | 6.86 |
| CHEMBL4439535 | — | — | 1 | 6.78 |
| CHEMBL4469584 | — | — | 1 | 6.75 |
| CHEMBL4578364 | — | — | 1 | 6.69 |
| CHEMBL540612 | — | — | 1 | 6.66 |
| CHEMBL4569006 | — | — | 1 | 6.66 |
| CHEMBL4550187 | — | — | 1 | 6.62 |
| CHEMBL4475699 | — | — | 1 | 6.56 |
| CHEMBL4543870 | — | — | 1 | 6.55 |
| CHEMBL4442936 | — | — | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4522558 | — | Ki | = | 44.7 | nM | 7.35 |
| CHEMBL4541924 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL4561808 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL4593394 | — | Ki | = | 50.1 | nM | 7.30 |
| CHEMBL4442408 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL4452683 | — | Ki | = | 57.5 | nM | 7.24 |
| CHEMBL4586582 | — | Ki | = | 61.7 | nM | 7.21 |
| CHEMBL4454872 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL4531363 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL4456964 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL4577162 | — | Ki | = | 85.1 | nM | 7.07 |
| CHEMBL4527244 | — | Ki | = | 97.7 | nM | 7.01 |
| CHEMBL4456007 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL4590839 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL4590211 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL4440698 | — | Ki | = | 125.9 | nM | 6.90 |
| CHEMBL4453478 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL4455719 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL4525624 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL4580817 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL4472900 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL4439535 | — | Ki | = | 165.0 | nM | 6.78 |
| CHEMBL4469584 | — | Ki | = | 179.0 | nM | 6.75 |
| CHEMBL4578364 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL4569006 | — | Ki | = | 219.0 | nM | 6.66 |
| CHEMBL540612 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL4550187 | — | Ki | = | 238.0 | nM | 6.62 |
| CHEMBL4475699 | — | Ki | = | 274.0 | nM | 6.56 |
| CHEMBL4543870 | — | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL4442936 | — | Ki | = | 412.1 | nM | 6.38 |
| CHEMBL4443039 | — | Ki | = | 417.0 | nM | 6.38 |
| CHEMBL4454380 | — | Ki | = | 427.0 | nM | 6.37 |
| CHEMBL4453405 | — | Ki | = | 495.4 | nM | 6.30 |
| CHEMBL4439544 | — | Ki | = | 513.0 | nM | 6.29 |
| CHEMBL4584372 | — | Ki | = | 535.0 | nM | 6.27 |
| CHEMBL4568916 | — | Ki | = | 898.0 | nM | 6.05 |
| CHEMBL4475406 | — | Ki | = | 1122.0 | nM | 5.95 |
| CHEMBL4444691 | — | Ki | = | 1259.0 | nM | 5.90 |
| CHEMBL4584481 | — | Ki | = | 1308.0 | nM | 5.88 |
| CHEMBL4452329 | — | Ki | = | 1339.0 | nM | 5.87 |
| CHEMBL4467486 | — | Ki | = | 2171.0 | nM | 5.66 |
| CHEMBL4470439 | — | Ki | = | 2362.0 | nM | 5.63 |
| CHEMBL4585289 | — | Ki | - | — | - | |
| CHEMBL4448853 | — | Ki | - | — | - | |
| CHEMBL4590356 | — | Ki | - | — | - | |
| CHEMBL4467528 | — | Ki | - | — | - | |
| CHEMBL4450429 | — | Ki | - | — | - | |
| CHEMBL4514586 | — | Ki | - | — | - | |
| CHEMBL4514800 | — | Ki | - | — | - | |
| CHEMBL4590966 | — | Ki | - | — | - |