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Assay Detail

CHEMBL642031

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

Binding
In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1d expressed in LTK cell
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1D adrenergic receptor (CHEMBL326)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).
Meyer MD, Altenbach RJ, Basha FZ, Carroll WA, Condon S, Elmore SW, Kerwin JF, Sippy KB, Tietje K, Wendt MD, Hancock AA, Brune ME, Buckner SA, Drizin I.
J Med Chem (2000) 43 : 1586 -1603
PubMed 10780916 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 9.20 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL836 TAMSULOSIN 4.0 1 10.15
CHEMBL295741 1 9.21
CHEMBL611 TERAZOSIN 4.0 1 9.00
CHEMBL290387 1 8.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL836 TAMSULOSIN Ki = 0.07 nM 10.15
CHEMBL295741 Ki = 0.61 nM 9.21
CHEMBL611 TERAZOSIN Ki = 1.01 nM 9.00
CHEMBL290387 Ki = 3.83 nM 8.42