Assay Detail
Functional
CHEMBL4339971
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Antagonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of dopamine-induced calcium flux preincubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature and subsequent dopamine addition measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Chemical synthesis, microbial transformation and biological evaluation of tetrahydroprotoberberines as dopamine D1/D2 receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.94 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2314747 | — | — | 1 | 7.40 |
| CHEMBL4438471 | — | — | 1 | 7.12 |
| CHEMBL4582377 | — | — | 1 | 6.72 |
| CHEMBL2314734 | — | — | 1 | 6.38 |
| CHEMBL487182 | TETRAHYDROPALMATINE | 2.0 | 1 | 6.35 |
| CHEMBL4476383 | — | — | 1 | 6.30 |
| CHEMBL4544045 | — | — | 1 | 5.97 |
| CHEMBL4561303 | — | — | 1 | 5.82 |
| CHEMBL62 | SCH-23390 | — | 1 | 5.69 |
| CHEMBL4521450 | — | — | 1 | 5.59 |
| CHEMBL2314745 | — | — | 1 | 5.51 |
| CHEMBL4528264 | — | — | 1 | 5.45 |
| CHEMBL4551037 | — | — | 1 | 5.31 |
| CHEMBL4585730 | — | — | 1 | 5.20 |
| CHEMBL2314740 | — | — | 1 | 5.10 |
| CHEMBL4453330 | — | — | 1 | 5.05 |
| CHEMBL4435291 | — | — | 1 | - |
| CHEMBL2314741 | — | — | 1 | - |
| CHEMBL2314742 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2314747 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4438471 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4582377 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2314734 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL487182 | TETRAHYDROPALMATINE | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4476383 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4544045 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL4561303 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL62 | SCH-23390 | IC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL4521450 | — | IC50 | = | 2590.0 | nM | 5.59 |
| CHEMBL2314745 | — | IC50 | = | 3110.0 | nM | 5.51 |
| CHEMBL4528264 | — | IC50 | = | 3580.0 | nM | 5.45 |
| CHEMBL4551037 | — | IC50 | = | 4940.0 | nM | 5.31 |
| CHEMBL4585730 | — | IC50 | = | 6360.0 | nM | 5.20 |
| CHEMBL2314740 | — | IC50 | = | 7960.0 | nM | 5.10 |
| CHEMBL4453330 | — | IC50 | = | 8810.0 | nM | 5.05 |
| CHEMBL4435291 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2314741 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2314742 | — | IC50 | > | 10000.0 | nM | - |