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Assay Detail

CHEMBL2422547

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

Binding
Displacement of [3H]prazosin from human alpha-1B adrenoreceptor expressed in CHO cells after 30 mins
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

6-methoxy-7-benzofuranoxy and 6-methoxy-7-indolyloxy analogues of 2-[2-(2,6-Dimethoxyphenoxy)ethyl]aminomethyl-1,4-benzodioxane (WB4101):1 discovery of a potent and selective α1D-adrenoceptor antagonist.
Fumagalli L, Pallavicini M, Budriesi R, Bolchi C, Canovi M, Chiarini A, Chiodini G, Gobbi M, Laurino P, Micucci M, Straniero V, Valoti E.
J Med Chem (2013) 56 : 6402 -6412
PubMed 23902232 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.08 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL215421 1 8.24
CHEMBL217469 1 7.80
CHEMBL2419771 1 7.66
CHEMBL2419769 1 7.54
CHEMBL3216590 1 7.45
CHEMBL2419770 1 6.90
CHEMBL2419772 1 6.79
CHEMBL3217244 1 6.43
CHEMBL2419765 1 6.31
CHEMBL2419766 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL215421 Ki = 5.754 nM 8.24
CHEMBL217469 Ki = 15.85 nM 7.80
CHEMBL2419771 Ki = 21.88 nM 7.66
CHEMBL2419769 Ki = 28.84 nM 7.54
CHEMBL3216590 Ki = 35.48 nM 7.45
CHEMBL2419770 Ki = 125.89 nM 6.90
CHEMBL2419772 Ki = 162.18 nM 6.79
CHEMBL3217244 Ki = 371.54 nM 6.43
CHEMBL2419765 Ki = 489.78 nM 6.31
CHEMBL2419766 Ki = 1905.46 nM 5.72