Assay Detail
Binding
CHEMBL669082
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity for dopamine receptor D2 binding sites by its ability to displace [3H]spiperone from rat striatum.
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 6.85 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14380 | — | — | 1 | 8.07 |
| CHEMBL14322 | — | — | 1 | 7.80 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.75 |
| CHEMBL274039 | — | — | 1 | 7.64 |
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 7.43 |
| CHEMBL14538 | — | — | 1 | 7.40 |
| CHEMBL14395 | — | — | 1 | 7.35 |
| CHEMBL14727 | — | — | 1 | 7.24 |
| CHEMBL273307 | — | — | 1 | 7.23 |
| CHEMBL274223 | — | — | 1 | 7.18 |
| CHEMBL14556 | — | — | 1 | 7.18 |
| CHEMBL14539 | — | — | 1 | 7.18 |
| CHEMBL276799 | — | — | 1 | 7.05 |
| CHEMBL440768 | — | — | 1 | 7.01 |
| CHEMBL275016 | — | — | 1 | 6.97 |
| CHEMBL14393 | — | — | 1 | 6.97 |
| CHEMBL14509 | — | — | 1 | 6.96 |
| CHEMBL14376 | ILOPERIDONE | 4.0 | 1 | 6.96 |
| CHEMBL14206 | — | — | 1 | 6.96 |
| CHEMBL273907 | — | — | 1 | 6.96 |
| CHEMBL14610 | — | — | 1 | 6.95 |
| CHEMBL14077 | — | — | 1 | 6.94 |
| CHEMBL14148 | — | — | 1 | 6.93 |
| CHEMBL436141 | — | — | 1 | 6.90 |
| CHEMBL14415 | — | — | 1 | 6.90 |
| CHEMBL14163 | — | — | 1 | 6.87 |
| CHEMBL14470 | — | — | 1 | 6.83 |
| CHEMBL279996 | — | — | 1 | 6.78 |
| CHEMBL14389 | — | — | 1 | 6.77 |
| CHEMBL417620 | — | — | 1 | 6.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14380 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL14322 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL274039 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL85 | RISPERIDONE | IC50 | = | 37.5 | nM | 7.43 |
| CHEMBL14538 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL14395 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL14727 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL273307 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL274223 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL14556 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL14539 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL276799 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL440768 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL14393 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL275016 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL14509 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL14376 | ILOPERIDONE | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL14206 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL273907 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL14610 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL14077 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL14148 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL436141 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL14415 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL14163 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL14470 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL279996 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL14389 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL417620 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL14510 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL14681 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL14365 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL14348 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL14100 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL14306 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL14246 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL275064 | — | IC50 | = | 295.0 | nM | 6.53 |
| CHEMBL14494 | — | IC50 | = | 336.0 | nM | 6.47 |
| CHEMBL427822 | — | IC50 | = | 364.0 | nM | 6.44 |
| CHEMBL276750 | — | IC50 | = | 427.0 | nM | 6.37 |
| CHEMBL14522 | — | IC50 | = | 455.0 | nM | 6.34 |
| CHEMBL14158 | — | IC50 | = | 454.0 | nM | 6.34 |
| CHEMBL14218 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL273633 | — | IC50 | = | 571.0 | nM | 6.24 |
| CHEMBL14394 | — | IC50 | = | 727.0 | nM | 6.14 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL14361 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL274462 | — | IC50 | = | 969.0 | nM | 6.01 |
| CHEMBL14219 | — | IC50 | > | 1000.0 | nM | - |