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Assay Detail

CHEMBL868697

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

Binding
Displacement of [3H]prazosin from cloned human ADRA1B expressed in CHO cells
16
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Alpha-1B adrenergic receptor (CHEMBL232)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships in 1,4-benzodioxan-related compounds. 8.(1) {2-[2-(4-chlorobenzyloxy)phenoxy]ethyl}-[2-(2,6-dimethoxyphenoxy)ethyl]amine (clopenphendioxan) as a tool to highlight the involvement of alpha1D- and alpha1B-adrenoreceptor subtypes in the regulation of human PC-3 prostate cancer cell apoptosis and proliferation.
Quaglia W, Santoni G, Pigini M, Piergentili A, Gentili F, Buccioni M, Mosca M, Lucciarini R, Amantini C, Nabissi MI, Ballarini P, Poggesi E, Leonardi A, Giannella M.
J Med Chem (2005) 48 : 7750 -7763
PubMed 16302814 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 9.15 9.80
Log Ki 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL198860 1 9.80
CHEMBL200366 1 9.60
CHEMBL199080 1 9.60
CHEMBL200580 1 9.40
CHEMBL196817 1 9.40
CHEMBL43116 1 9.27
CHEMBL200839 1 9.25
CHEMBL197442 1 9.10
CHEMBL382972 1 9.10
CHEMBL707 DOXAZOSIN 4.0 1 9.09
CHEMBL200446 CLOPENPHENDIOXAN 1 9.00
CHEMBL427552 1 8.70
CHEMBL200136 1 8.60
CHEMBL198431 1 8.20
CHEMBL199077 1 -
CHEMBL200777 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL198860 Ki = 0.1585 nM 9.80
CHEMBL200366 Ki = 0.2512 nM 9.60
CHEMBL199080 Ki = 0.2512 nM 9.60
CHEMBL200580 Ki = 0.3981 nM 9.40
CHEMBL196817 Ki = 0.3981 nM 9.40
CHEMBL43116 Ki = 0.537 nM 9.27
CHEMBL200839 Ki = 0.5623 nM 9.25
CHEMBL197442 Ki = 0.7943 nM 9.10
CHEMBL382972 Ki = 0.7943 nM 9.10
CHEMBL707 DOXAZOSIN Ki = 0.8128 nM 9.09
CHEMBL200446 CLOPENPHENDIOXAN Ki = 1.0 nM 9.00
CHEMBL427552 Ki = 1.995 nM 8.70
CHEMBL200136 Ki = 2.512 nM 8.60
CHEMBL198431 Ki = 6.31 nM 8.20
CHEMBL199077 Log Ki - -
CHEMBL200777 Log Ki - -