Assay Detail
Binding
CHEMBL5442198
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PDSP Secondary Binding target: DRD3 - 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.
56
Total Activities
56
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 | 56 | 6.38 | 9.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | 4.0 | 1 | 9.01 |
| CHEMBL540612 | — | — | 1 | 8.65 |
| CHEMBL300555 | SPIROXATRINE | 2.0 | 1 | 8.11 |
| CHEMBL2105760 | BREXPIPRAZOLE | 4.0 | 1 | 7.98 |
| CHEMBL79834 | SPIRAMIDE | 2.0 | 1 | 7.49 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | 4.0 | 1 | 7.47 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 7.45 |
| CHEMBL24778 | SILODOSIN | 4.0 | 1 | 7.14 |
| CHEMBL543113 | — | — | 1 | 6.94 |
| CHEMBL1615374 | VILAZODONE HYDROCHLORIDE | 4.0 | 1 | 6.88 |
| CHEMBL445102 | — | — | 1 | 6.69 |
| CHEMBL2440454 | — | — | 1 | 6.57 |
| CHEMBL4743049 | — | — | 1 | 6.55 |
| CHEMBL542139 | — | — | 1 | 6.50 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | 4.0 | 1 | 6.42 |
| CHEMBL1200776 | CINACALCET HYDROCHLORIDE | 4.0 | 1 | 6.41 |
| CHEMBL1766103 | — | — | 1 | 6.38 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 6.37 |
| CHEMBL1516474 | TEGASEROD MALEATE | 4.0 | 1 | 6.37 |
| CHEMBL5087452 | — | — | 1 | 6.35 |
| CHEMBL589390 | LATREPIRDINE | 3.0 | 1 | 6.34 |
| CHEMBL2048820 | — | — | 1 | 6.32 |
| CHEMBL1836317 | — | — | 1 | 6.30 |
| CHEMBL1256876 | — | — | 1 | 6.26 |
| CHEMBL1256844 | — | — | 1 | 6.25 |
| CHEMBL180465 | — | — | 1 | 6.25 |
| CHEMBL218071 | — | — | 1 | 6.24 |
| CHEMBL256470 | — | — | 1 | 6.24 |
| CHEMBL3919973 | — | — | 1 | 6.23 |
| CHEMBL1200809 | AZELASTINE HYDROCHLORIDE | 4.0 | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | Ki | = | 0.9749 | nM | 9.01 |
| CHEMBL540612 | — | Ki | = | 2.213 | nM | 8.65 |
| CHEMBL300555 | SPIROXATRINE | Ki | = | 7.739 | nM | 8.11 |
| CHEMBL2105760 | BREXPIPRAZOLE | Ki | = | 10.42 | nM | 7.98 |
| CHEMBL79834 | SPIRAMIDE | Ki | = | 32.76 | nM | 7.49 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | Ki | = | 33.96 | nM | 7.47 |
| CHEMBL267777 | RITANSERIN | Ki | = | 35.54 | nM | 7.45 |
| CHEMBL24778 | SILODOSIN | Ki | = | 71.55 | nM | 7.14 |
| CHEMBL543113 | — | Ki | = | 115.8 | nM | 6.94 |
| CHEMBL1615374 | VILAZODONE HYDROCHLORIDE | Ki | = | 133.28 | nM | 6.88 |
| CHEMBL445102 | — | Ki | = | 205.04 | nM | 6.69 |
| CHEMBL2440454 | — | Ki | = | 269.85 | nM | 6.57 |
| CHEMBL4743049 | — | Ki | = | 284.08 | nM | 6.55 |
| CHEMBL542139 | — | Ki | = | 314.59 | nM | 6.50 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | Ki | = | 380.19 | nM | 6.42 |
| CHEMBL1200776 | CINACALCET HYDROCHLORIDE | Ki | = | 390.88 | nM | 6.41 |
| CHEMBL1766103 | — | Ki | = | 415.96 | nM | 6.38 |
| CHEMBL405355 | NIGULDIPINE | Ki | = | 424.72 | nM | 6.37 |
| CHEMBL1516474 | TEGASEROD MALEATE | Ki | = | 426.48 | nM | 6.37 |
| CHEMBL5087452 | — | Ki | = | 445.35 | nM | 6.35 |
| CHEMBL589390 | LATREPIRDINE | Ki | = | 461.42 | nM | 6.34 |
| CHEMBL2048820 | — | Ki | = | 480.01 | nM | 6.32 |
| CHEMBL1836317 | — | Ki | = | 498.26 | nM | 6.30 |
| CHEMBL1256876 | — | Ki | = | 545.01 | nM | 6.26 |
| CHEMBL180465 | — | Ki | = | 558.6 | nM | 6.25 |
| CHEMBL1256844 | — | Ki | = | 568.2 | nM | 6.25 |
| CHEMBL218071 | — | Ki | = | 582.44 | nM | 6.24 |
| CHEMBL256470 | — | Ki | = | 580.7 | nM | 6.24 |
| CHEMBL3919973 | — | Ki | = | 590.54 | nM | 6.23 |
| CHEMBL1200809 | AZELASTINE HYDROCHLORIDE | Ki | = | 636.36 | nM | 6.20 |
| CHEMBL103769 | — | Ki | = | 641.14 | nM | 6.19 |
| CHEMBL1256998 | — | Ki | = | 668.88 | nM | 6.17 |
| CHEMBL1633 | KETOTIFEN FUMARATE | Ki | = | 717.13 | nM | 6.14 |
| CHEMBL214957 | — | Ki | = | 767.89 | nM | 6.12 |
| CHEMBL2107572 | TECALCET HYDROCHLORIDE | Ki | = | 874.58 | nM | 6.06 |
| CHEMBL360648 | — | Ki | = | 912.36 | nM | 6.04 |
| CHEMBL2103873 | MACITENTAN | Ki | = | 1004.5 | nM | 6.00 |
| CHEMBL500 | PINDOLOL | Ki | = | 994.49 | nM | 6.00 |
| CHEMBL3342358 | — | Ki | = | 1018.95 | nM | 5.99 |
| CHEMBL83894 | FANANSERIN | Ki | = | 1022.94 | nM | 5.99 |
| CHEMBL2386353 | — | Ki | = | 1097.11 | nM | 5.96 |
| CHEMBL426559 | LAROPIPRANT | Ki | = | 1122.15 | nM | 5.95 |
| CHEMBL3086703 | — | Ki | = | 1111.61 | nM | 5.95 |
| CHEMBL273083 | — | Ki | = | 1189.78 | nM | 5.92 |
| CHEMBL1263 | SALMETEROL | Ki | = | 1260.37 | nM | 5.90 |
| CHEMBL1095777 | INDACATEROL | Ki | = | 1339.37 | nM | 5.87 |
| CHEMBL1672558 | — | Ki | = | 1417.53 | nM | 5.85 |
| CHEMBL21283 | — | Ki | = | 1612.13 | nM | 5.79 |
| CHEMBL1235246 | — | Ki | = | 1763.87 | nM | 5.75 |
| CHEMBL49302 | — | Ki | = | 1958.39 | nM | 5.71 |