Assay Detail
Binding
CHEMBL5442177
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Category | PDSP assay |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
EUbOPEN Chemogenomics Library - PDSP Secondary Binding
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.27 | 8.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1489369 | — | — | 1 | 8.71 |
| CHEMBL1256876 | — | — | 1 | 8.52 |
| CHEMBL3039520 | LASMIDITAN | 4.0 | 1 | 6.60 |
| CHEMBL2105760 | BREXPIPRAZOLE | 4.0 | 1 | 6.46 |
| CHEMBL543113 | — | — | 1 | 6.41 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 6.31 |
| CHEMBL259656 | — | — | 1 | 6.15 |
| CHEMBL1766103 | — | — | 1 | 6.00 |
| CHEMBL4743495 | — | — | 1 | 5.98 |
| CHEMBL281350 | SB-224289 | — | 1 | 5.97 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 5.91 |
| CHEMBL43383 | — | — | 1 | 5.73 |
| CHEMBL103769 | — | — | 1 | 5.70 |
| CHEMBL540612 | — | — | 1 | 5.68 |
| CHEMBL1633 | KETOTIFEN FUMARATE | 4.0 | 1 | 5.58 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | 4.0 | 1 | 5.53 |
| CHEMBL1516474 | TEGASEROD MALEATE | 4.0 | 1 | 5.38 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | - |
| CHEMBL1256844 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1489369 | — | Ki | = | 1.95 | nM | 8.71 |
| CHEMBL1256876 | — | Ki | = | 3.02 | nM | 8.52 |
| CHEMBL3039520 | LASMIDITAN | Ki | = | 252.67 | nM | 6.60 |
| CHEMBL2105760 | BREXPIPRAZOLE | Ki | = | 344.47 | nM | 6.46 |
| CHEMBL543113 | — | Ki | = | 392.92 | nM | 6.41 |
| CHEMBL267777 | RITANSERIN | Ki | = | 493.01 | nM | 6.31 |
| CHEMBL259656 | — | Ki | = | 708.43 | nM | 6.15 |
| CHEMBL1766103 | — | Ki | = | 992.66 | nM | 6.00 |
| CHEMBL4743495 | — | Ki | = | 1048.94 | nM | 5.98 |
| CHEMBL281350 | SB-224289 | Ki | = | 1077.83 | nM | 5.97 |
| CHEMBL405355 | NIGULDIPINE | Ki | = | 1242.51 | nM | 5.91 |
| CHEMBL43383 | — | Ki | = | 1845.44 | nM | 5.73 |
| CHEMBL103769 | — | Ki | = | 1976.06 | nM | 5.70 |
| CHEMBL540612 | — | Ki | = | 2087.61 | nM | 5.68 |
| CHEMBL1633 | KETOTIFEN FUMARATE | Ki | = | 2660.11 | nM | 5.58 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | Ki | = | 2948.83 | nM | 5.53 |
| CHEMBL1516474 | TEGASEROD MALEATE | Ki | = | 4124.77 | nM | 5.38 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | > | 10000.0 | nM | - |
| CHEMBL1256844 | — | Ki | > | 10000.0 | nM | - |