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Assay Detail

CHEMBL647807

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Functional
Alpha-1 adrenergic receptor agonist activity in rabbit ear artery
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Artery
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-1A adrenergic receptor (CHEMBL229)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Alpha-adrenergic agents. 1. Direct-acting alpha 1 agonists related to methoxamine.
DeMarinis RM, Bryan WM, Shah DH, Hieble JP, Pendleton RG.
J Med Chem (1981) 24 : 1432 -1437
PubMed 6118438 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 5.68 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL30596 1 6.92
CHEMBL286702 1 6.77
CHEMBL33405 1 6.70
CHEMBL285082 1 6.47
CHEMBL524 METHOXAMINE 4.0 1 6.14
CHEMBL284486 1 5.28
CHEMBL287047 1 4.96
CHEMBL286609 1 4.52
CHEMBL286226 1 4.52
CHEMBL284307 1 4.52
CHEMBL284257 1 -
CHEMBL30294 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL30596 EC50 = 120.0 nM 6.92
CHEMBL286702 EC50 = 170.0 nM 6.77
CHEMBL33405 EC50 = 200.0 nM 6.70
CHEMBL285082 EC50 = 340.0 nM 6.47
CHEMBL524 METHOXAMINE EC50 = 720.0 nM 6.14
CHEMBL284486 EC50 = 5300.0 nM 5.28
CHEMBL287047 EC50 = 11000.0 nM 4.96
CHEMBL286609 EC50 = 30000.0 nM 4.52
CHEMBL286226 EC50 = 30000.0 nM 4.52
CHEMBL284307 EC50 = 30000.0 nM 4.52
CHEMBL284257 EC50 > 30000.0 nM -
CHEMBL30294 EC50 > 30000.0 nM -