Assay Detail
Binding
CHEMBL829049
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | ovary |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 8.71 | 9.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL191962 | N-{4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl}-1-ruthena-1,1'-spirobi[pentacyclo[2.2.0.0^{1,3}.0^{1,5}.0^{2,6}]hexane]-2,2',4,4'-tetraene-6-carboxamide | — | 1 | 9.43 |
| CHEMBL364516 | N-{4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl}-1-ferra-1,1'-spirobi[pentacyclo[2.2.0.0^{1,3}.0^{1,5}.0^{2,6}]hexane]-2,2',4,4'-tetraene-6-carboxamide | — | 1 | 9.28 |
| CHEMBL370297 | Ruthenium complex | — | 1 | 9.22 |
| CHEMBL194555 | Fe complex | — | 1 | 9.20 |
| CHEMBL195083 | N-{4-[4-(3-chloro-2-methoxyphenyl)piperazin-1-yl]butyl}-1-ferra-1,1'-spirobi[pentacyclo[2.2.0.0^{1,3}.0^{1,5}.0^{2,6}]hexane]-2,2',4,4'-tetraene-6-carboxamide | — | 1 | 9.04 |
| CHEMBL425731 | 2-{1-ferra-1,1'-spirobi[pentacyclo[2.2.0.0^{1,3}.0^{1,5}.0^{2,6}]hexane]-2,2',4,4'-tetraen-6-yl}-N-{4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl}acetamide | — | 1 | 8.48 |
| CHEMBL371165 | Fe complex | — | 1 | 7.68 |
| CHEMBL540612 | — | — | 1 | 7.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL191962 | N-{4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl}-1-ruthena-1,1'-spirobi[pentacyclo[2.2.0.0^{1,3}.0^{1,5}.0^{2,6}]hexane]-2,2',4,4'-tetraene-6-carboxamide | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL364516 | N-{4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl}-1-ferra-1,1'-spirobi[pentacyclo[2.2.0.0^{1,3}.0^{1,5}.0^{2,6}]hexane]-2,2',4,4'-tetraene-6-carboxamide | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL370297 | Ruthenium complex | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL194555 | Fe complex | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL195083 | N-{4-[4-(3-chloro-2-methoxyphenyl)piperazin-1-yl]butyl}-1-ferra-1,1'-spirobi[pentacyclo[2.2.0.0^{1,3}.0^{1,5}.0^{2,6}]hexane]-2,2',4,4'-tetraene-6-carboxamide | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL425731 | 2-{1-ferra-1,1'-spirobi[pentacyclo[2.2.0.0^{1,3}.0^{1,5}.0^{2,6}]hexane]-2,2',4,4'-tetraen-6-yl}-N-{4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl}acetamide | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL371165 | Fe complex | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL540612 | — | Ki | = | 44.0 | nM | 7.36 |