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Assay Detail

CHEMBL1909092

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL ↗
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Beta-2 adrenergic receptor (CHEMBL210) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

DrugMatrix in vitro pharmacology data
Scott S. Auerbach, DrugMatrix¨ and ToxFX¨ Coordinator National Toxicology Program

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 871 7.07 9.62
Ki 871 7.23 9.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL723 CARVEDILOL 4.0 2 9.78
CHEMBL499 TIMOLOL 4.0 2 9.70
CHEMBL452861 LEVOPROPRANOLOL 2.0 2 9.61
CHEMBL500 PINDOLOL 4.0 2 9.42
CHEMBL1201237 LEVOBUNOLOL 4.0 2 9.26
CHEMBL27 PROPRANOLOL 4.0 2 9.12
CHEMBL117405 — — 2 8.97
CHEMBL429 LABETALOL 4.0 2 7.96
CHEMBL357995 BOPINDOLOL 2.0 2 7.85
CHEMBL49080 CLENBUTEROL 2.0 2 7.55
CHEMBL157138 LISURIDE 3.0 2 7.54
CHEMBL631 PROPAFENONE 4.0 2 7.44
CHEMBL275742 DEXPROPRANOLOL 2.0 2 7.28
CHEMBL434 ISOPROTERENOL 4.0 2 6.77
CHEMBL679 EPINEPHRINE 4.0 2 6.71
CHEMBL471 SOTALOL 4.0 2 6.53
CHEMBL714 ALBUTEROL 4.0 2 6.25
CHEMBL926 DOBUTAMINE 4.0 2 5.98
CHEMBL1902627 CLORPRENALINE 2.0 2 5.86
CHEMBL13 METOPROLOL 4.0 2 5.75
CHEMBL442 ERGOTAMINE 4.0 2 5.72
CHEMBL707 DOXAZOSIN 4.0 2 5.72
CHEMBL841 LOPERAMIDE 4.0 2 5.68
CHEMBL787 MONTELUKAST 4.0 2 5.62
CHEMBL24 ATENOLOL 4.0 2 5.00
CHEMBL1630578 TIRILAZAD 3.0 2 4.81
CHEMBL12089 BERBERINE CHLORIDE 1.0 2 -
CHEMBL1231530 BETAMIPRON 2.0 2 -
CHEMBL844 BRIMONIDINE 4.0 2 -
CHEMBL3084803 ASTROMICIN 2.0 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL723 CARVEDILOL Ki = 0.166 nM 9.78
CHEMBL499 TIMOLOL Ki = 0.201 nM 9.70
CHEMBL723 CARVEDILOL IC50 = 0.241 nM 9.62
CHEMBL452861 LEVOPROPRANOLOL Ki = 0.244 nM 9.61
CHEMBL499 TIMOLOL IC50 = 0.292 nM 9.54
CHEMBL452861 LEVOPROPRANOLOL IC50 = 0.355 nM 9.45
CHEMBL500 PINDOLOL Ki = 0.377 nM 9.42
CHEMBL1201237 LEVOBUNOLOL Ki = 0.546 nM 9.26
CHEMBL500 PINDOLOL IC50 = 0.549 nM 9.26
CHEMBL27 PROPRANOLOL Ki = 0.767 nM 9.12
CHEMBL1201237 LEVOBUNOLOL IC50 = 0.793 nM 9.10
CHEMBL117405 — Ki = 1.08 nM 8.97
CHEMBL27 PROPRANOLOL IC50 = 1.116 nM 8.95
CHEMBL117405 — IC50 = 1.571 nM 8.80
CHEMBL429 LABETALOL Ki = 11.0 nM 7.96
CHEMBL357995 BOPINDOLOL Ki = 14.0 nM 7.85
CHEMBL429 LABETALOL IC50 = 16.0 nM 7.80
CHEMBL357995 BOPINDOLOL IC50 = 20.0 nM 7.70
CHEMBL49080 CLENBUTEROL Ki = 28.0 nM 7.55
CHEMBL157138 LISURIDE Ki = 29.0 nM 7.54
CHEMBL631 PROPAFENONE Ki = 36.0 nM 7.44
CHEMBL157138 LISURIDE IC50 = 41.0 nM 7.39
CHEMBL49080 CLENBUTEROL IC50 = 41.0 nM 7.39
CHEMBL275742 DEXPROPRANOLOL Ki = 52.0 nM 7.28
CHEMBL631 PROPAFENONE IC50 = 52.0 nM 7.28
CHEMBL275742 DEXPROPRANOLOL IC50 = 76.0 nM 7.12
CHEMBL434 ISOPROTERENOL Ki = 169.0 nM 6.77
CHEMBL679 EPINEPHRINE Ki = 196.0 nM 6.71
CHEMBL434 ISOPROTERENOL IC50 = 246.0 nM 6.61
CHEMBL679 EPINEPHRINE IC50 = 284.0 nM 6.55
CHEMBL471 SOTALOL Ki = 298.3 nM 6.53
CHEMBL471 SOTALOL IC50 = 433.9 nM 6.36
CHEMBL714 ALBUTEROL Ki = 557.0 nM 6.25
CHEMBL714 ALBUTEROL IC50 = 810.2 nM 6.09
CHEMBL926 DOBUTAMINE Ki = 1043.0 nM 5.98
CHEMBL1902627 CLORPRENALINE Ki = 1370.0 nM 5.86
CHEMBL926 DOBUTAMINE IC50 = 1517.0 nM 5.82
CHEMBL13 METOPROLOL Ki = 1769.0 nM 5.75
CHEMBL707 DOXAZOSIN Ki = 1889.0 nM 5.72
CHEMBL442 ERGOTAMINE Ki = 1898.0 nM 5.72
CHEMBL1902627 CLORPRENALINE IC50 = 1993.0 nM 5.70
CHEMBL841 LOPERAMIDE Ki = 2066.0 nM 5.68
CHEMBL787 MONTELUKAST Ki = 2398.0 nM 5.62
CHEMBL13 METOPROLOL IC50 = 2573.0 nM 5.59
CHEMBL707 DOXAZOSIN IC50 = 2748.0 nM 5.56
CHEMBL442 ERGOTAMINE IC50 = 2761.0 nM 5.56
CHEMBL841 LOPERAMIDE IC50 = 3005.0 nM 5.52
CHEMBL787 MONTELUKAST IC50 = 3488.0 nM 5.46
CHEMBL24 ATENOLOL Ki = 10061.0 nM 5.00
CHEMBL24 ATENOLOL IC50 = 14634.0 nM 4.83