Assay Detail
Binding
CHEMBL675125
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In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | C6 glioma |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
CoMFA-based prediction of agonist affinities at recombinant wild type versus serine to alanine point mutated D2 dopamine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 18 | 6.31 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL157138 | LISURIDE | 3.0 | 1 | 9.52 |
| CHEMBL227213 | — | — | 1 | 8.74 |
| CHEMBL531 | PERGOLIDE | 4.0 | 1 | 8.40 |
| CHEMBL493 | BROMOCRIPTINE | 4.0 | 1 | 8.10 |
| CHEMBL612083 | — | — | 1 | 7.05 |
| CHEMBL225230 | R-N-PROPYLNORAPOMORPHINE | — | 1 | 6.43 |
| CHEMBL53 | APOMORPHINE | 4.0 | 1 | 5.92 |
| CHEMBL104141 | — | — | 1 | 5.89 |
| CHEMBL34095 | — | — | 1 | 5.80 |
| CHEMBL317741 | — | — | 1 | 5.80 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 5.46 |
| CHEMBL1160787 | — | — | 1 | 4.89 |
| CHEMBL25856 | DIHYDREXIDINE | 2.0 | 1 | 4.89 |
| CHEMBL588 | FENOLDOPAM | 4.0 | 1 | 4.89 |
| CHEMBL1160788 | — | — | 1 | 4.77 |
| CHEMBL286080 | SKF-38393 | — | 1 | 4.41 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | - |
| CHEMBL1160785 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL157138 | LISURIDE | Kd | = | 0.3 | nM | 9.52 |
| CHEMBL227213 | — | Kd | = | 1.8 | nM | 8.74 |
| CHEMBL531 | PERGOLIDE | Kd | = | 4.0 | nM | 8.40 |
| CHEMBL493 | BROMOCRIPTINE | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL612083 | — | Kd | = | 90.0 | nM | 7.05 |
| CHEMBL225230 | R-N-PROPYLNORAPOMORPHINE | Kd | = | 370.0 | nM | 6.43 |
| CHEMBL53 | APOMORPHINE | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL104141 | — | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL34095 | — | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL317741 | — | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL240773 | QUINPIROLE | Kd | = | 3500.0 | nM | 5.46 |
| CHEMBL1160787 | — | Kd | = | 13000.0 | nM | 4.89 |
| CHEMBL25856 | DIHYDREXIDINE | Kd | = | 13000.0 | nM | 4.89 |
| CHEMBL588 | FENOLDOPAM | Kd | = | 13000.0 | nM | 4.89 |
| CHEMBL1160788 | — | Kd | = | 17000.0 | nM | 4.77 |
| CHEMBL286080 | SKF-38393 | Kd | = | 39000.0 | nM | 4.41 |
| CHEMBL59 | DOPAMINE | Kd | = | 267000.0 | nM | - |
| CHEMBL1160785 | — | Kd | = | 251000.0 | nM | - |