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Assay Detail

CHEMBL642904

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

Binding
In vitro blocking activity against alpha adrenergic receptor, isolated from rabbit aortic strip
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL2094251)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Salicylamide derivatives related to medroxalol with alpha- and beta-adrenergic antagonist and antihypertension activity.
Grisar JM, Claxton GP, Bare TM, Dage RC, Cheng HC, Woodward JK.
J Med Chem (1981) 24 : 327 -336
PubMed 6115059 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 40 6.43 7.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1203119 1 7.95
CHEMBL1204146 PHENTOLAMINE HYDROCHLORIDE -1.0 1 7.78
CHEMBL1203110 1 7.57
CHEMBL323702 1 7.56
CHEMBL1203123 1 7.45
CHEMBL1203140 1 7.42
CHEMBL1203124 1 7.21
CHEMBL1203139 1 7.04
CHEMBL1203108 1 7.00
CHEMBL1203117 1 6.94
CHEMBL326283 1 6.87
CHEMBL1203148 1 6.80
CHEMBL1203116 1 6.70
CHEMBL1203118 1 6.63
CHEMBL1203106 1 6.54
CHEMBL1203115 1 6.33
CHEMBL1203126 1 6.27
CHEMBL1204337 NYLIDRIN HYDROCHLORIDE -1.0 1 6.21
CHEMBL1203102 1 6.21
CHEMBL114349 1 6.20
CHEMBL1203138 1 6.13
CHEMBL1203112 1 6.08
CHEMBL1203100 1 6.05
CHEMBL112157 1 6.04
CHEMBL1203109 1 5.90
CHEMBL1203120 1 5.86
CHEMBL1203113 1 5.85
CHEMBL1203122 1 5.73
CHEMBL1203099 1 5.56
CHEMBL1203111 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1203119 Kd = 11.22 nM 7.95
CHEMBL1204146 PHENTOLAMINE HYDROCHLORIDE Kd = 16.6 nM 7.78
CHEMBL1203110 Kd = 26.92 nM 7.57
CHEMBL323702 Kd = 27.54 nM 7.56
CHEMBL1203123 Kd = 35.48 nM 7.45
CHEMBL1203140 Kd = 38.02 nM 7.42
CHEMBL1203124 Kd = 61.66 nM 7.21
CHEMBL1203139 Kd = 91.2 nM 7.04
CHEMBL1203108 Kd = 100.0 nM 7.00
CHEMBL1203117 Kd = 114.82 nM 6.94
CHEMBL326283 Kd = 134.9 nM 6.87
CHEMBL1203148 Kd = 158.49 nM 6.80
CHEMBL1203116 Kd = 199.53 nM 6.70
CHEMBL1203118 Kd = 234.42 nM 6.63
CHEMBL1203106 Kd = 288.4 nM 6.54
CHEMBL1203115 Kd = 467.74 nM 6.33
CHEMBL1203126 Kd = 537.03 nM 6.27
CHEMBL1204337 NYLIDRIN HYDROCHLORIDE Kd = 616.6 nM 6.21
CHEMBL1203102 Kd = 616.6 nM 6.21
CHEMBL114349 Kd = 630.96 nM 6.20
CHEMBL1203138 Kd = 741.31 nM 6.13
CHEMBL1203112 Kd = 831.76 nM 6.08
CHEMBL1203100 Kd = 891.25 nM 6.05
CHEMBL112157 Kd = 912.01 nM 6.04
CHEMBL1203109 Kd = 1258.93 nM 5.90
CHEMBL1203120 Kd = 1380.38 nM 5.86
CHEMBL1203113 Kd = 1412.54 nM 5.85
CHEMBL1203122 Kd = 1862.09 nM 5.73
CHEMBL1203099 Kd = 2754.23 nM 5.56
CHEMBL1203111 Kd = 3388.44 nM 5.47
CHEMBL1203101 Kd = 3467.37 nM 5.46
CHEMBL1203097 Kd = 4897.79 nM 5.31
CHEMBL1203107 Kd = 6309.57 nM 5.20
CHEMBL1203114 Kd = 7413.1 nM 5.13
CHEMBL1671 PROPRANOLOL HYDROCHLORIDE Kd > 10000.0 nM -
CHEMBL116504 Kd > 10000.0 nM -
CHEMBL1203098 Kd > 10000.0 nM -
CHEMBL1203105 Kd > 7244.36 nM -
CHEMBL1203103 Kd > 10000.0 nM -
CHEMBL1203125 Kd > 10000.0 nM -