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Assay Detail

CHEMBL647819

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

Functional
Alpha-1 adrenergic receptor activation causing vasoconstriction in the isolated rabbit ear artery
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Artery
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

alpha-Adrenergic agents. 2. Synthesis and alpha 1-agonist activity of 2-aminotetralins.
DeMarinis RM, Shah DH, Hall RF, Hieble JP, Pendleton RG.
J Med Chem (1982) 25 : 136 -141
PubMed 6120238 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 6.69 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL280395 1 7.92
CHEMBL30722 1 7.85
CHEMBL283415 1 7.68
CHEMBL30319 1 7.58
CHEMBL30378 1 7.19
CHEMBL30650 1 7.19
CHEMBL31006 1 7.09
CHEMBL31160 1 7.09
CHEMBL21961 1 7.07
CHEMBL30596 1 6.92
CHEMBL283678 1 6.85
CHEMBL1437 NOREPINEPHRINE 4.0 1 6.82
CHEMBL283502 1 6.64
CHEMBL30569 1 6.16
CHEMBL524 METHOXAMINE 4.0 1 6.14
CHEMBL30771 1 5.96
CHEMBL26688 1 5.77
CHEMBL30560 1 5.66
CHEMBL286968 1 5.28
CHEMBL31620 1 5.00
CHEMBL31098 1 -
CHEMBL30294 1 -
CHEMBL31179 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL280395 EC50 = 12.0 nM 7.92
CHEMBL30722 EC50 = 14.0 nM 7.85
CHEMBL283415 EC50 = 21.0 nM 7.68
CHEMBL30319 EC50 = 26.0 nM 7.58
CHEMBL30378 EC50 = 64.0 nM 7.19
CHEMBL30650 EC50 = 64.0 nM 7.19
CHEMBL31006 EC50 = 81.0 nM 7.09
CHEMBL31160 EC50 = 81.0 nM 7.09
CHEMBL21961 EC50 = 86.0 nM 7.07
CHEMBL30596 EC50 = 120.0 nM 6.92
CHEMBL283678 EC50 = 140.0 nM 6.85
CHEMBL1437 NOREPINEPHRINE EC50 = 150.0 nM 6.82
CHEMBL283502 EC50 = 230.0 nM 6.64
CHEMBL30569 EC50 = 700.0 nM 6.16
CHEMBL524 METHOXAMINE EC50 = 720.0 nM 6.14
CHEMBL30771 EC50 = 1100.0 nM 5.96
CHEMBL26688 EC50 = 1700.0 nM 5.77
CHEMBL30560 EC50 = 2200.0 nM 5.66
CHEMBL286968 EC50 = 5300.0 nM 5.28
CHEMBL31620 EC50 = 10000.0 nM 5.00
CHEMBL31098 EC50 > 10000.0 nM -
CHEMBL30294 EC50 > 30000.0 nM -
CHEMBL31179 EC50 > 10000.0 nM -