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Assay Detail

CHEMBL653377

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

Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Cardiac atrium
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Beta-1 adrenergic receptor (CHEMBL5471)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis and beta-adrenergic antagonism of 2-(aryloxy)-1-(2-piperidyl)ethanols.
Mauleón D, Pujol MD, Rosell G.
J Med Chem (1988) 31 : 2122 -2126
PubMed 2903245 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 24 7.58 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL304344 1 9.82
CHEMBL7154 1 8.77
CHEMBL69635 1 8.75
CHEMBL67096 TOLIPROLOL 2.0 1 8.75
CHEMBL27 PROPRANOLOL 4.0 1 8.60
CHEMBL67151 1 8.40
CHEMBL302339 1 8.06
CHEMBL68419 1 7.71
CHEMBL66384 1 7.39
CHEMBL302935 1 7.31
CHEMBL63582 1 7.25
CHEMBL67631 1 7.24
CHEMBL66702 1 7.09
CHEMBL419994 1 7.02
CHEMBL66662 1 7.00
CHEMBL66724 1 6.80
CHEMBL66449 1 6.60
CHEMBL66324 1 6.56
CHEMBL302605 1 6.42
CHEMBL66331 1 5.98
CHEMBL68996 1 -
CHEMBL68945 1 -
CHEMBL67331 1 -
CHEMBL304725 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL304344 Kd = 0.1514 nM 9.82
CHEMBL7154 Kd = 1.698 nM 8.77
CHEMBL69635 Kd = 1.778 nM 8.75
CHEMBL67096 TOLIPROLOL Kd = 1.778 nM 8.75
CHEMBL27 PROPRANOLOL Kd = 2.512 nM 8.60
CHEMBL67151 Kd = 3.981 nM 8.40
CHEMBL302339 Kd = 8.71 nM 8.06
CHEMBL68419 Kd = 19.5 nM 7.71
CHEMBL66384 Kd = 40.74 nM 7.39
CHEMBL302935 Kd = 48.98 nM 7.31
CHEMBL63582 Kd = 56.23 nM 7.25
CHEMBL67631 Kd = 57.54 nM 7.24
CHEMBL66702 Kd = 81.28 nM 7.09
CHEMBL419994 Kd = 95.5 nM 7.02
CHEMBL66662 Kd = 100.0 nM 7.00
CHEMBL66724 Kd = 158.49 nM 6.80
CHEMBL66449 Kd = 251.19 nM 6.60
CHEMBL66324 Kd = 275.42 nM 6.56
CHEMBL302605 Kd = 380.19 nM 6.42
CHEMBL66331 Kd = 1047.13 nM 5.98
CHEMBL68996 Kd > 257.04 nM -
CHEMBL68945 Kd > 7.943 nM -
CHEMBL67331 Kd > 102.33 nM -
CHEMBL304725 Kd > 70.79 nM -