Assay Detail
Binding
CHEMBL1909093
Review assay metadata, readout intent, target linkage, and publication context from the same page.
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 871 | 5.63 | 8.38 |
| Ki | 871 | 5.70 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL723 | CARVEDILOL | 4.0 | 2 | 8.51 |
| CHEMBL117405 | — | — | 2 | 7.44 |
| CHEMBL500 | PINDOLOL | 4.0 | 2 | 7.18 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 2 | 7.00 |
| CHEMBL452861 | LEVOPROPRANOLOL | 2.0 | 2 | 6.91 |
| CHEMBL1201237 | LEVOBUNOLOL | 4.0 | 2 | 6.59 |
| CHEMBL631 | PROPAFENONE | 4.0 | 2 | 6.50 |
| CHEMBL499 | TIMOLOL | 4.0 | 2 | 6.47 |
| CHEMBL357995 | BOPINDOLOL | 2.0 | 2 | 6.46 |
| CHEMBL1403281 | ERGOCRYPTINE | — | 2 | 5.73 |
| CHEMBL305660 | EBASTINE | 4.0 | 2 | 5.72 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | — | 2 | 5.61 |
| CHEMBL1016 | CANDESARTAN | 3.0 | 2 | 5.50 |
| CHEMBL153062 | 4-NONYLPHENOL | — | 2 | 5.50 |
| CHEMBL787 | MONTELUKAST | 4.0 | 2 | 5.50 |
| CHEMBL1262 | OXICONAZOLE | 4.0 | 2 | 5.45 |
| CHEMBL404849 | SULOCTIDIL | 4.0 | 2 | 5.43 |
| CHEMBL91 | MICONAZOLE | 4.0 | 2 | 5.39 |
| CHEMBL954 | ENCLOMIPHENE | 3.0 | 2 | 5.37 |
| CHEMBL808 | ECONAZOLE | 4.0 | 2 | 5.34 |
| CHEMBL104 | CLOTRIMAZOLE | 4.0 | 2 | 5.27 |
| CHEMBL83 | TAMOXIFEN | 4.0 | 2 | 5.24 |
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 2 | 5.22 |
| CHEMBL118 | CELECOXIB | 4.0 | 2 | 4.92 |
| CHEMBL1479 | DANAZOL | 4.0 | 2 | 4.89 |
| CHEMBL7002 | CIGLITAZONE | 2.0 | 2 | 4.87 |
| CHEMBL434063 | — | — | 2 | 4.78 |
| CHEMBL726 | FLUPHENAZINE | 4.0 | 2 | 4.66 |
| CHEMBL584 | NELFINAVIR | 4.0 | 2 | 4.59 |
| CHEMBL633 | AMIODARONE | 4.0 | 2 | 4.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL723 | CARVEDILOL | Ki | = | 3.116 | nM | 8.51 |
| CHEMBL723 | CARVEDILOL | IC50 | = | 4.155 | nM | 8.38 |
| CHEMBL117405 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL117405 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL500 | PINDOLOL | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL500 | PINDOLOL | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL27 | PROPRANOLOL | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL452861 | LEVOPROPRANOLOL | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL27 | PROPRANOLOL | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL452861 | LEVOPROPRANOLOL | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL1201237 | LEVOBUNOLOL | Ki | = | 255.0 | nM | 6.59 |
| CHEMBL631 | PROPAFENONE | Ki | = | 318.0 | nM | 6.50 |
| CHEMBL1201237 | LEVOBUNOLOL | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL499 | TIMOLOL | Ki | = | 339.0 | nM | 6.47 |
| CHEMBL357995 | BOPINDOLOL | Ki | = | 344.0 | nM | 6.46 |
| CHEMBL631 | PROPAFENONE | IC50 | = | 424.0 | nM | 6.37 |
| CHEMBL499 | TIMOLOL | IC50 | = | 452.0 | nM | 6.34 |
| CHEMBL357995 | BOPINDOLOL | IC50 | = | 458.0 | nM | 6.34 |
| CHEMBL1403281 | ERGOCRYPTINE | Ki | = | 1872.0 | nM | 5.73 |
| CHEMBL305660 | EBASTINE | Ki | = | 1909.1 | nM | 5.72 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | Ki | = | 2481.0 | nM | 5.61 |
| CHEMBL1403281 | ERGOCRYPTINE | IC50 | = | 2496.0 | nM | 5.60 |
| CHEMBL305660 | EBASTINE | IC50 | = | 2545.5 | nM | 5.59 |
| CHEMBL153062 | 4-NONYLPHENOL | Ki | = | 3142.0 | nM | 5.50 |
| CHEMBL787 | MONTELUKAST | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL1016 | CANDESARTAN | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | IC50 | = | 3308.0 | nM | 5.48 |
| CHEMBL1262 | OXICONAZOLE | Ki | = | 3558.7 | nM | 5.45 |
| CHEMBL404849 | SULOCTIDIL | Ki | = | 3747.2 | nM | 5.43 |
| CHEMBL91 | MICONAZOLE | Ki | = | 4111.0 | nM | 5.39 |
| CHEMBL153062 | 4-NONYLPHENOL | IC50 | = | 4190.0 | nM | 5.38 |
| CHEMBL787 | MONTELUKAST | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL1016 | CANDESARTAN | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL954 | ENCLOMIPHENE | Ki | = | 4254.0 | nM | 5.37 |
| CHEMBL808 | ECONAZOLE | Ki | = | 4612.0 | nM | 5.34 |
| CHEMBL1262 | OXICONAZOLE | IC50 | = | 4744.9 | nM | 5.32 |
| CHEMBL404849 | SULOCTIDIL | IC50 | = | 4996.3 | nM | 5.30 |
| CHEMBL104 | CLOTRIMAZOLE | Ki | = | 5406.0 | nM | 5.27 |
| CHEMBL91 | MICONAZOLE | IC50 | = | 5482.0 | nM | 5.26 |
| CHEMBL954 | ENCLOMIPHENE | IC50 | = | 5673.0 | nM | 5.25 |
| CHEMBL83 | TAMOXIFEN | Ki | = | 5778.0 | nM | 5.24 |
| CHEMBL296419 | ASTEMIZOLE | Ki | = | 6045.0 | nM | 5.22 |
| CHEMBL808 | ECONAZOLE | IC50 | = | 6150.0 | nM | 5.21 |
| CHEMBL104 | CLOTRIMAZOLE | IC50 | = | 7208.0 | nM | 5.14 |
| CHEMBL83 | TAMOXIFEN | IC50 | = | 7703.0 | nM | 5.11 |
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 8060.0 | nM | 5.09 |
| CHEMBL118 | CELECOXIB | Ki | = | 12093.0 | nM | 4.92 |
| CHEMBL1479 | DANAZOL | Ki | = | 12765.0 | nM | 4.89 |
| CHEMBL7002 | CIGLITAZONE | Ki | = | 13403.0 | nM | 4.87 |
| CHEMBL118 | CELECOXIB | IC50 | = | 16124.0 | nM | 4.79 |