Assay Detail
Binding
CHEMBL5442215
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PDSP Secondary Binding target: DRD2 - 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.
23
Total Activities
23
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 | 23 | 6.52 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2105760 | BREXPIPRAZOLE | 4.0 | 1 | 8.22 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | 4.0 | 1 | 8.20 |
| CHEMBL300555 | SPIROXATRINE | 2.0 | 1 | 8.17 |
| CHEMBL79834 | SPIRAMIDE | 2.0 | 1 | 8.02 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | 4.0 | 1 | 7.21 |
| CHEMBL445102 | — | — | 1 | 7.06 |
| CHEMBL540612 | — | — | 1 | 6.84 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 6.74 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 6.55 |
| CHEMBL1516474 | TEGASEROD MALEATE | 4.0 | 1 | 6.53 |
| CHEMBL1615374 | VILAZODONE HYDROCHLORIDE | 4.0 | 1 | 6.26 |
| CHEMBL567303 | PALOSURAN | 2.0 | 1 | 6.22 |
| CHEMBL2138684 | FROVATRIPTAN SUCCINATE | 4.0 | 1 | 6.16 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | 4.0 | 1 | 6.13 |
| CHEMBL543113 | — | — | 1 | 6.12 |
| CHEMBL24778 | SILODOSIN | 4.0 | 1 | 6.00 |
| CHEMBL1200809 | AZELASTINE HYDROCHLORIDE | 4.0 | 1 | 5.93 |
| CHEMBL589390 | LATREPIRDINE | 3.0 | 1 | 5.81 |
| CHEMBL1633 | KETOTIFEN FUMARATE | 4.0 | 1 | 5.76 |
| CHEMBL5077459 | — | — | 1 | 5.42 |
| CHEMBL1200618 | FEXOFENADINE HYDROCHLORIDE | 4.0 | 1 | 5.05 |
| CHEMBL1334465 | — | — | 1 | 5.01 |
| CHEMBL1256863 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2105760 | BREXPIPRAZOLE | Ki | = | 5.985 | nM | 8.22 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | Ki | = | 6.378 | nM | 8.20 |
| CHEMBL300555 | SPIROXATRINE | Ki | = | 6.711 | nM | 8.17 |
| CHEMBL79834 | SPIRAMIDE | Ki | = | 9.619 | nM | 8.02 |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | Ki | = | 60.92 | nM | 7.21 |
| CHEMBL445102 | — | Ki | = | 87.45 | nM | 7.06 |
| CHEMBL540612 | — | Ki | = | 144.06 | nM | 6.84 |
| CHEMBL267777 | RITANSERIN | Ki | = | 184.04 | nM | 6.74 |
| CHEMBL405355 | NIGULDIPINE | Ki | = | 279.64 | nM | 6.55 |
| CHEMBL1516474 | TEGASEROD MALEATE | Ki | = | 296.96 | nM | 6.53 |
| CHEMBL1615374 | VILAZODONE HYDROCHLORIDE | Ki | = | 552.71 | nM | 6.26 |
| CHEMBL567303 | PALOSURAN | Ki | = | 595.52 | nM | 6.22 |
| CHEMBL2138684 | FROVATRIPTAN SUCCINATE | Ki | = | 694.23 | nM | 6.16 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | Ki | = | 735.53 | nM | 6.13 |
| CHEMBL543113 | — | Ki | = | 767.36 | nM | 6.12 |
| CHEMBL24778 | SILODOSIN | Ki | = | 989.13 | nM | 6.00 |
| CHEMBL1200809 | AZELASTINE HYDROCHLORIDE | Ki | = | 1176.52 | nM | 5.93 |
| CHEMBL589390 | LATREPIRDINE | Ki | = | 1547.75 | nM | 5.81 |
| CHEMBL1633 | KETOTIFEN FUMARATE | Ki | = | 1726.64 | nM | 5.76 |
| CHEMBL5077459 | — | Ki | = | 3845.92 | nM | 5.42 |
| CHEMBL1200618 | FEXOFENADINE HYDROCHLORIDE | Ki | = | 8806.43 | nM | 5.05 |
| CHEMBL1334465 | — | Ki | = | 9765.62 | nM | 5.01 |
| CHEMBL1256863 | — | Ki | > | 10000.0 | nM | - |