Assay Detail
Binding
CHEMBL3706100
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
81
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Heteroaromatic compounds and their use as dopamine D1 ligands
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 81 | 7.27 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3697581 | — | — | 1 | 9.24 |
| CHEMBL3697613 | — | — | 2 | 8.51 |
| CHEMBL3697564 | — | — | 1 | 8.44 |
| CHEMBL3697596 | — | — | 1 | 8.38 |
| CHEMBL3697574 | — | — | 1 | 8.27 |
| CHEMBL3697578 | RAZPIPADON | 2.0 | 2 | 8.16 |
| CHEMBL3697579 | — | — | 1 | 8.12 |
| CHEMBL3697570 | — | — | 1 | 8.07 |
| CHEMBL3697617 | TAVAPADON | 3.0 | 2 | 8.07 |
| CHEMBL3697587 | — | — | 2 | 8.03 |
| CHEMBL3697576 | — | — | 1 | 8.02 |
| CHEMBL3697583 | — | — | 1 | 8.00 |
| CHEMBL3697619 | — | — | 1 | 7.96 |
| CHEMBL3697594 | — | — | 1 | 7.92 |
| CHEMBL3697624 | — | — | 1 | 7.89 |
| CHEMBL3697595 | — | — | 1 | 7.87 |
| CHEMBL3697572 | — | — | 1 | 7.82 |
| CHEMBL3697599 | — | — | 1 | 7.77 |
| CHEMBL3697621 | — | — | 2 | 7.76 |
| CHEMBL3697593 | — | — | 1 | 7.62 |
| CHEMBL3697597 | — | — | 2 | 7.57 |
| CHEMBL3697589 | — | — | 1 | 7.52 |
| CHEMBL3697571 | — | — | 1 | 7.51 |
| CHEMBL3697609 | — | — | 1 | 7.49 |
| CHEMBL3697616 | — | — | 1 | 7.48 |
| CHEMBL3697623 | — | — | 1 | 7.45 |
| CHEMBL3697560 | — | — | 1 | 7.44 |
| CHEMBL3697558 | — | — | 1 | 7.42 |
| CHEMBL3697600 | — | — | 1 | 7.42 |
| CHEMBL3697614 | — | — | 2 | 7.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3697581 | — | Ki | = | 0.571 | nM | 9.24 |
| CHEMBL3697613 | — | Ki | = | 3.11 | nM | 8.51 |
| CHEMBL3697564 | — | Ki | = | 3.61 | nM | 8.44 |
| CHEMBL3697596 | — | Ki | = | 4.17 | nM | 8.38 |
| CHEMBL3697574 | — | Ki | = | 5.41 | nM | 8.27 |
| CHEMBL3697578 | RAZPIPADON | Ki | = | 6.91 | nM | 8.16 |
| CHEMBL3697579 | — | Ki | = | 7.66 | nM | 8.12 |
| CHEMBL3697617 | TAVAPADON | Ki | = | 8.54 | nM | 8.07 |
| CHEMBL3697570 | — | Ki | = | 8.42 | nM | 8.07 |
| CHEMBL3697587 | — | Ki | = | 9.33 | nM | 8.03 |
| CHEMBL3697576 | — | Ki | = | 9.65 | nM | 8.02 |
| CHEMBL3697583 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL3697619 | — | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL3697594 | — | Ki | = | 12.1 | nM | 7.92 |
| CHEMBL3697624 | — | Ki | = | 12.9 | nM | 7.89 |
| CHEMBL3697595 | — | Ki | = | 13.4 | nM | 7.87 |
| CHEMBL3697613 | — | Ki | = | 15.3 | nM | 7.82 |
| CHEMBL3697572 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3697599 | — | Ki | = | 16.9 | nM | 7.77 |
| CHEMBL3697621 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL3697578 | RAZPIPADON | Ki | = | 18.6 | nM | 7.73 |
| CHEMBL3697617 | TAVAPADON | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL3697587 | — | Ki | = | 24.2 | nM | 7.62 |
| CHEMBL3697593 | — | Ki | = | 23.8 | nM | 7.62 |
| CHEMBL3697597 | — | Ki | = | 26.9 | nM | 7.57 |
| CHEMBL3697589 | — | Ki | = | 30.5 | nM | 7.52 |
| CHEMBL3697571 | — | Ki | = | 31.1 | nM | 7.51 |
| CHEMBL3697609 | — | Ki | = | 32.3 | nM | 7.49 |
| CHEMBL3697616 | — | Ki | = | 33.1 | nM | 7.48 |
| CHEMBL3697597 | — | Ki | = | 34.4 | nM | 7.46 |
| CHEMBL3697623 | — | Ki | = | 35.7 | nM | 7.45 |
| CHEMBL3697560 | — | Ki | = | 36.2 | nM | 7.44 |
| CHEMBL3697558 | — | Ki | = | 38.5 | nM | 7.42 |
| CHEMBL3697600 | — | Ki | = | 38.3 | nM | 7.42 |
| CHEMBL3697614 | — | Ki | = | 40.6 | nM | 7.39 |
| CHEMBL3697604 | — | Ki | = | 43.4 | nM | 7.36 |
| CHEMBL3697622 | — | Ki | = | 44.3 | nM | 7.35 |
| CHEMBL3697556 | — | Ki | = | 45.9 | nM | 7.34 |
| CHEMBL3697553 | — | Ki | = | 52.7 | nM | 7.28 |
| CHEMBL3697620 | — | Ki | = | 55.1 | nM | 7.26 |
| CHEMBL3697621 | — | Ki | = | 54.7 | nM | 7.26 |
| CHEMBL3697612 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL3697615 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL3697622 | — | Ki | = | 59.1 | nM | 7.23 |
| CHEMBL3697585 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL3697580 | — | Ki | = | 82.3 | nM | 7.08 |
| CHEMBL3697618 | — | Ki | = | 82.3 | nM | 7.08 |
| CHEMBL3697573 | — | Ki | = | 82.7 | nM | 7.08 |
| CHEMBL3697555 | — | Ki | = | 82.7 | nM | 7.08 |
| CHEMBL3697606 | — | Ki | = | 87.0 | nM | 7.06 |