Assay Detail
Functional
CHEMBL961820
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Antagonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
N-(4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl)heterobiarylcarboxamides with functionalized linking chains as high affinity and enantioselective D3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.94 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL424294 | — | — | 1 | 9.66 |
| CHEMBL1627304 | — | — | 1 | 8.96 |
| CHEMBL1627314 | — | — | 1 | 8.82 |
| CHEMBL1627315 | — | — | 1 | 8.80 |
| CHEMBL1627311 | — | — | 1 | 8.75 |
| CHEMBL124444 | — | — | 1 | 8.62 |
| CHEMBL59725 | — | — | 1 | 8.31 |
| CHEMBL1627309 | — | — | 1 | 8.19 |
| CHEMBL1627307 | — | — | 1 | 8.18 |
| CHEMBL1627323 | — | — | 1 | 8.15 |
| CHEMBL139926 | — | — | 1 | 8.04 |
| CHEMBL175734 | — | — | 1 | 8.02 |
| CHEMBL1627317 | — | — | 1 | 7.95 |
| CHEMBL1627308 | — | — | 1 | 7.92 |
| CHEMBL1627316 | — | — | 1 | 7.86 |
| CHEMBL1627319 | — | — | 1 | 7.84 |
| CHEMBL1627324 | — | — | 1 | 7.83 |
| CHEMBL1627306 | — | — | 1 | 7.74 |
| CHEMBL366904 | — | — | 1 | 7.73 |
| CHEMBL182379 | — | — | 1 | 7.64 |
| CHEMBL1627310 | — | — | 1 | 7.62 |
| CHEMBL1627321 | — | — | 1 | 7.59 |
| CHEMBL1627305 | — | — | 1 | 7.52 |
| CHEMBL1627312 | — | — | 1 | 7.42 |
| CHEMBL1627320 | — | — | 1 | 7.41 |
| CHEMBL1627313 | — | — | 1 | 6.76 |
| CHEMBL1627318 | — | — | 1 | 6.66 |
| CHEMBL184383 | — | — | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL424294 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL1627304 | — | IC50 | = | 1.09 | nM | 8.96 |
| CHEMBL1627314 | — | IC50 | = | 1.51 | nM | 8.82 |
| CHEMBL1627315 | — | IC50 | = | 1.58 | nM | 8.80 |
| CHEMBL1627311 | — | IC50 | = | 1.76 | nM | 8.75 |
| CHEMBL124444 | — | IC50 | = | 2.39 | nM | 8.62 |
| CHEMBL59725 | — | IC50 | = | 4.94 | nM | 8.31 |
| CHEMBL1627309 | — | IC50 | = | 6.51 | nM | 8.19 |
| CHEMBL1627307 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL1627323 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL139926 | — | IC50 | = | 9.01 | nM | 8.04 |
| CHEMBL175734 | — | IC50 | = | 9.62 | nM | 8.02 |
| CHEMBL1627317 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL1627308 | — | IC50 | = | 12.1 | nM | 7.92 |
| CHEMBL1627316 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL1627319 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL1627324 | — | IC50 | = | 14.9 | nM | 7.83 |
| CHEMBL1627306 | — | IC50 | = | 18.2 | nM | 7.74 |
| CHEMBL366904 | — | IC50 | = | 18.7 | nM | 7.73 |
| CHEMBL182379 | — | IC50 | = | 22.9 | nM | 7.64 |
| CHEMBL1627310 | — | IC50 | = | 23.9 | nM | 7.62 |
| CHEMBL1627321 | — | IC50 | = | 25.7 | nM | 7.59 |
| CHEMBL1627305 | — | IC50 | = | 29.9 | nM | 7.52 |
| CHEMBL1627312 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL1627320 | — | IC50 | = | 39.1 | nM | 7.41 |
| CHEMBL1627313 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL1627318 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL184383 | — | IC50 | = | 520.0 | nM | 6.28 |