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Assay Detail

CHEMBL653458

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

Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Beta-2 adrenergic receptor (CHEMBL3373)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Quantitative evaluation of the beta 2-adrenoceptor affinity of phenoxypropanolamines and phenylethanolamines.
IJzerman AP, Aué GH, Bultsma T, Linschoten MR, Timmerman H.
J Med Chem (1985) 28 : 1328 -1334
PubMed 2993621 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 34 6.56 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1159892 PROCINOLOL 2.0 1 9.41
CHEMBL1159723 1 9.20
CHEMBL1671 PROPRANOLOL HYDROCHLORIDE 4.0 1 9.05
CHEMBL6920 1 7.99
CHEMBL1159714 1 7.99
CHEMBL1159889 1 7.75
CHEMBL1159888 1 7.66
CHEMBL49080 CLENBUTEROL 2.0 1 7.44
CHEMBL67096 TOLIPROLOL 2.0 1 7.36
CHEMBL1159891 1 7.30
CHEMBL1159713 1 7.24
CHEMBL1159717 TULOBUTEROL 2.0 1 6.89
CHEMBL16476 PRONETALOL 4.0 1 6.80
CHEMBL434 ISOPROTERENOL 4.0 1 6.48
CHEMBL349845 1 6.33
CHEMBL1159712 1 6.28
CHEMBL714 ALBUTEROL 4.0 1 6.28
CHEMBL471 SOTALOL 4.0 1 6.24
CHEMBL1159715 COLTEROL 2.0 1 6.22
CHEMBL327122 METATEROL 2.0 1 6.04
CHEMBL1160714 PRENALTEROL 2.0 1 5.97
CHEMBL1159887 1 5.90
CHEMBL127349 NIFENALOL 2.0 1 5.88
CHEMBL1159711 1 5.71
CHEMBL1159710 1 5.69
CHEMBL1159890 1 5.67
CHEMBL321468 1 5.50
CHEMBL1760 TERBUTALINE 4.0 1 5.40
CHEMBL109378 DETERENOL 2.0 1 5.37
CHEMBL1159719 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1159892 PROCINOLOL Kd = 0.39 nM 9.41
CHEMBL1159723 Kd = 0.63 nM 9.20
CHEMBL1671 PROPRANOLOL HYDROCHLORIDE Kd = 0.89 nM 9.05
CHEMBL6920 Kd = 10.23 nM 7.99
CHEMBL1159714 Kd = 10.23 nM 7.99
CHEMBL1159889 Kd = 17.78 nM 7.75
CHEMBL1159888 Kd = 21.88 nM 7.66
CHEMBL49080 CLENBUTEROL Kd = 36.0 nM 7.44
CHEMBL67096 TOLIPROLOL Kd = 43.65 nM 7.36
CHEMBL1159891 Kd = 50.12 nM 7.30
CHEMBL1159713 Kd = 58.0 nM 7.24
CHEMBL1159717 TULOBUTEROL Kd = 130.0 nM 6.89
CHEMBL16476 PRONETALOL Kd = 160.0 nM 6.80
CHEMBL434 ISOPROTERENOL Kd = 330.0 nM 6.48
CHEMBL349845 Kd = 470.0 nM 6.33
CHEMBL1159712 Kd = 520.0 nM 6.28
CHEMBL714 ALBUTEROL Kd = 520.0 nM 6.28
CHEMBL471 SOTALOL Kd = 580.0 nM 6.24
CHEMBL1159715 COLTEROL Kd = 600.0 nM 6.22
CHEMBL327122 METATEROL Kd = 910.0 nM 6.04
CHEMBL1160714 PRENALTEROL Kd = 1072.0 nM 5.97
CHEMBL1159887 Kd = 1260.0 nM 5.90
CHEMBL127349 NIFENALOL Kd = 1320.0 nM 5.88
CHEMBL1159711 Kd = 1950.0 nM 5.71
CHEMBL1159710 Kd = 2040.0 nM 5.69
CHEMBL1159890 Kd = 2140.0 nM 5.67
CHEMBL321468 Kd = 3160.0 nM 5.50
CHEMBL1760 TERBUTALINE Kd = 3980.0 nM 5.40
CHEMBL109378 DETERENOL Kd = 4270.0 nM 5.37
CHEMBL1159719 Kd = 5130.0 nM 5.29
CHEMBL776 METAPROTERENOL Kd = 9120.0 nM 5.04
CHEMBL6995 PRACTOLOL Kd = 20417.0 nM 4.69
CHEMBL7154 Kd = 53700.0 nM 4.27
CHEMBL423 BETAXOLOL Kd = 186210.0 nM -