Assay Detail
ADMET
CHEMBL4397357
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]IABN from recombinant human D2 long receptor stably expressed in HEK293 cell membranes measured after 60 mins by scintillation counting analysis
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D<sub>3</sub> Receptor (D<sub>3</sub>R) Ligand Promiscuity across Highly Conserved Aminergic G-Protein-Coupled Receptors (GPCRs).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 44 | 5.21 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | 2.0 | 1 | 10.22 |
| CHEMBL26789 | — | — | 1 | 7.69 |
| CHEMBL4438361 | — | — | 1 | 7.65 |
| CHEMBL4525842 | — | — | 1 | 6.71 |
| CHEMBL4083252 | — | — | 1 | 6.58 |
| CHEMBL4438524 | — | — | 1 | 5.93 |
| CHEMBL4549664 | — | — | 1 | 5.80 |
| CHEMBL4590969 | — | — | 1 | 5.67 |
| CHEMBL4558652 | — | — | 1 | 5.58 |
| CHEMBL4516504 | — | — | 1 | 5.56 |
| CHEMBL4541692 | — | — | 1 | 5.49 |
| CHEMBL4528652 | — | — | 1 | 5.42 |
| CHEMBL4475482 | — | — | 1 | 5.29 |
| CHEMBL4554630 | — | — | 1 | 5.25 |
| CHEMBL4461920 | — | — | 1 | 5.23 |
| CHEMBL4062553 | — | — | 1 | 5.21 |
| CHEMBL4471201 | — | — | 1 | 5.20 |
| CHEMBL4514100 | — | — | 1 | 5.05 |
| CHEMBL4466055 | — | — | 1 | 5.03 |
| CHEMBL4073927 | — | — | 1 | 5.01 |
| CHEMBL4084262 | — | — | 1 | 4.96 |
| CHEMBL4541869 | — | — | 1 | 4.92 |
| CHEMBL4451865 | — | — | 1 | 4.90 |
| CHEMBL4552459 | — | — | 1 | 4.86 |
| CHEMBL4535104 | — | — | 1 | 4.80 |
| CHEMBL4591835 | — | — | 1 | 4.75 |
| CHEMBL4459784 | — | — | 1 | 4.71 |
| CHEMBL4534961 | — | — | 1 | 4.71 |
| CHEMBL4476163 | — | — | 1 | 4.68 |
| CHEMBL4435765 | — | — | 1 | 4.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL26789 | — | Ki | = | 20.6 | nM | 7.69 |
| CHEMBL4438361 | — | Ki | = | 22.3 | nM | 7.65 |
| CHEMBL4525842 | — | Ki | = | 197.0 | nM | 6.71 |
| CHEMBL4083252 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL4438524 | — | Ki | = | 1162.0 | nM | 5.93 |
| CHEMBL4549664 | — | Ki | = | 1574.0 | nM | 5.80 |
| CHEMBL4590969 | — | Ki | = | 2112.0 | nM | 5.67 |
| CHEMBL4558652 | — | Ki | = | 2630.0 | nM | 5.58 |
| CHEMBL4516504 | — | Ki | = | 2766.0 | nM | 5.56 |
| CHEMBL4541692 | — | Ki | = | 3250.0 | nM | 5.49 |
| CHEMBL4528652 | — | Ki | = | 3762.0 | nM | 5.42 |
| CHEMBL4475482 | — | Ki | = | 5165.0 | nM | 5.29 |
| CHEMBL4554630 | — | Ki | = | 5650.0 | nM | 5.25 |
| CHEMBL4461920 | — | Ki | = | 5891.0 | nM | 5.23 |
| CHEMBL4062553 | — | Ki | = | 6168.0 | nM | 5.21 |
| CHEMBL4471201 | — | Ki | = | 6379.0 | nM | 5.20 |
| CHEMBL4514100 | — | Ki | = | 9004.0 | nM | 5.05 |
| CHEMBL4466055 | — | Ki | = | 9248.0 | nM | 5.03 |
| CHEMBL4073927 | — | Ki | = | 9792.0 | nM | 5.01 |
| CHEMBL4084262 | — | Ki | = | 10895.0 | nM | 4.96 |
| CHEMBL4541869 | — | Ki | = | 12137.0 | nM | 4.92 |
| CHEMBL4451865 | — | Ki | = | 12584.0 | nM | 4.90 |
| CHEMBL4552459 | — | Ki | = | 13904.0 | nM | 4.86 |
| CHEMBL4535104 | — | Ki | = | 15768.0 | nM | 4.80 |
| CHEMBL4591835 | — | Ki | = | 17595.0 | nM | 4.75 |
| CHEMBL4459784 | — | Ki | = | 19634.0 | nM | 4.71 |
| CHEMBL4534961 | — | Ki | = | 19655.0 | nM | 4.71 |
| CHEMBL4476163 | — | Ki | = | 21098.0 | nM | 4.68 |
| CHEMBL4435765 | — | Ki | = | 21172.0 | nM | 4.67 |
| CHEMBL4453955 | — | Ki | = | 25823.0 | nM | 4.59 |
| CHEMBL4483472 | — | Ki | = | 26050.0 | nM | 4.58 |
| CHEMBL4555876 | — | Ki | = | 26253.0 | nM | 4.58 |
| CHEMBL4435834 | — | Ki | = | 26739.0 | nM | 4.57 |
| CHEMBL4515093 | — | Ki | = | 35720.0 | nM | 4.45 |
| CHEMBL4516927 | — | Ki | = | 48584.0 | nM | 4.31 |
| CHEMBL4555952 | — | Ki | = | 59994.0 | nM | 4.22 |
| CHEMBL4483044 | — | Ki | = | 65229.0 | nM | 4.19 |
| CHEMBL4591203 | — | Ki | = | 74272.0 | nM | 4.13 |
| CHEMBL4473583 | — | Ki | = | 98462.0 | nM | 4.01 |
| CHEMBL4470847 | — | Ki | = | 99379.0 | nM | 4.00 |
| CHEMBL4588709 | — | Ki | = | 180375.0 | nM | 3.74 |
| CHEMBL4100699 | — | Ki | = | 104847.0 | nM | - |
| CHEMBL4472434 | — | Ki | > | 225748.0 | nM | - |