Assay Detail
Binding
CHEMBL5442197
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PDSP Secondary Binding target: DRD1 - 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.
17
Total Activities
17
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 | 17 | 6.39 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1489369 | — | — | 1 | 8.54 |
| CHEMBL1256876 | — | — | 1 | 8.03 |
| CHEMBL2105760 | BREXPIPRAZOLE | 4.0 | 1 | 7.43 |
| CHEMBL1633 | KETOTIFEN FUMARATE | 4.0 | 1 | 6.52 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 6.48 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 6.43 |
| CHEMBL281350 | SB-224289 | — | 1 | 6.43 |
| CHEMBL540612 | — | — | 1 | 6.38 |
| CHEMBL1200809 | AZELASTINE HYDROCHLORIDE | 4.0 | 1 | 6.24 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | 4.0 | 1 | 6.15 |
| CHEMBL43383 | — | — | 1 | 6.13 |
| CHEMBL74355 | VOLINANSERIN | 3.0 | 1 | 6.07 |
| CHEMBL445102 | — | — | 1 | 5.97 |
| CHEMBL103769 | — | — | 1 | 5.76 |
| CHEMBL9387 | L-365260 | — | 1 | 5.52 |
| CHEMBL5076314 | — | — | 1 | 5.34 |
| CHEMBL499 | TIMOLOL | 4.0 | 1 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1489369 | — | Ki | = | 2.92 | nM | 8.54 |
| CHEMBL1256876 | — | Ki | = | 9.257 | nM | 8.03 |
| CHEMBL2105760 | BREXPIPRAZOLE | Ki | = | 37.46 | nM | 7.43 |
| CHEMBL1633 | KETOTIFEN FUMARATE | Ki | = | 299.47 | nM | 6.52 |
| CHEMBL267777 | RITANSERIN | Ki | = | 330.14 | nM | 6.48 |
| CHEMBL405355 | NIGULDIPINE | Ki | = | 370.43 | nM | 6.43 |
| CHEMBL281350 | SB-224289 | Ki | = | 369.36 | nM | 6.43 |
| CHEMBL540612 | — | Ki | = | 412.0 | nM | 6.38 |
| CHEMBL1200809 | AZELASTINE HYDROCHLORIDE | Ki | = | 577.17 | nM | 6.24 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | Ki | = | 711.62 | nM | 6.15 |
| CHEMBL43383 | — | Ki | = | 740.29 | nM | 6.13 |
| CHEMBL74355 | VOLINANSERIN | Ki | = | 859.31 | nM | 6.07 |
| CHEMBL445102 | — | Ki | = | 1077.96 | nM | 5.97 |
| CHEMBL103769 | — | Ki | = | 1717.71 | nM | 5.76 |
| CHEMBL9387 | L-365260 | Ki | = | 3019.95 | nM | 5.52 |
| CHEMBL5076314 | — | Ki | = | 4543.6 | nM | 5.34 |
| CHEMBL499 | TIMOLOL | Ki | = | 5280.8 | nM | 5.28 |