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Assay Detail

CHEMBL1246630

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

Binding
Displacement [3H]prazosin of human recombinant Alpha-1B adrenergic receptor expressed in CHO cells by rapid filtration technique
15
Total Activities
15
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

1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.
Franchini S, Prandi A, Baraldi A, Sorbi C, Tait A, Buccioni M, Marucci G, Cilia A, Pirona L, Fossa P, Cichero E, Brasili L.
Eur J Med Chem (2010) 45 : 3740 -3751
PubMed 20605276 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.23 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1242352 1 8.17
CHEMBL1242912 1 8.03
CHEMBL1241557 1 8.00
CHEMBL1242633 1 7.74
CHEMBL1242818 1 7.33
CHEMBL1242542 1 7.29
CHEMBL31354 WAY-100,635 1 7.18
CHEMBL1242445 1 7.15
CHEMBL1242632 1 7.14
CHEMBL1242724 1 7.07
CHEMBL1242541 1 6.89
CHEMBL1242819 1 6.88
CHEMBL1242444 1 6.76
CHEMBL1242725 1 6.65
CHEMBL13647 BMY-7378 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1242352 Ki = 6.761 nM 8.17
CHEMBL1242912 Ki = 9.333 nM 8.03
CHEMBL1241557 Ki = 10.0 nM 8.00
CHEMBL1242633 Ki = 18.2 nM 7.74
CHEMBL1242818 Ki = 46.77 nM 7.33
CHEMBL1242542 Ki = 51.29 nM 7.29
CHEMBL31354 WAY-100,635 Ki = 66.07 nM 7.18
CHEMBL1242445 Ki = 70.79 nM 7.15
CHEMBL1242632 Ki = 72.44 nM 7.14
CHEMBL1242724 Ki = 85.11 nM 7.07
CHEMBL1242541 Ki = 128.82 nM 6.89
CHEMBL1242819 Ki = 131.83 nM 6.88
CHEMBL1242444 Ki = 173.78 nM 6.76
CHEMBL1242725 Ki = 223.87 nM 6.65
CHEMBL13647 BMY-7378 Ki = 707.95 nM 6.15