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Assay Detail

CHEMBL647281

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

Binding
Binding affinity towards Alpha-1B adrenergic receptor in rat liver using [3H]prazosin as radioligand
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1B adrenergic receptor (CHEMBL315)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis, absolute configuration, and biological profile of the enantiomers of trans-[2-(2,6-dimethoxyphenoxy)ethyl] [(3-p-tolyl-2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amine (mephendioxan), a potent competitive alpha 1A-adrenoreceptor antagonist.
Quaglia W, Pigini M, Tayebati SK, Piergentili A, Giannella M, Leonardi A, Taddei C, Melchiorre C.
J Med Chem (1996) 39 : 2253 -2258
PubMed 8667368 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.68 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL72657 1 7.20
CHEMBL42539 1 6.99
CHEMBL76168 1 6.66
CHEMBL405355 NIGULDIPINE 2.0 1 6.42
CHEMBL286565 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL72657 Ki = 62.61 nM 7.20
CHEMBL42539 Ki = 102.9 nM 6.99
CHEMBL76168 Ki = 220.2 nM 6.66
CHEMBL405355 NIGULDIPINE Ki = 379.9 nM 6.42
CHEMBL286565 Ki = 774.3 nM 6.11