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Assay Detail

CHEMBL1246631

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

Binding
Displacement [3H]prazosin of human recombinant Alpha-1D 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-1D adrenergic receptor (CHEMBL223)
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 8.27 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1242352 1 9.09
CHEMBL13647 BMY-7378 1 8.89
CHEMBL1241557 1 8.86
CHEMBL1242542 1 8.83
CHEMBL1242633 1 8.60
CHEMBL1242632 1 8.39
CHEMBL31354 WAY-100,635 1 8.34
CHEMBL1242912 1 8.32
CHEMBL1242445 1 8.28
CHEMBL1242819 1 8.07
CHEMBL1242444 1 7.87
CHEMBL1242541 1 7.85
CHEMBL1242725 1 7.79
CHEMBL1242818 1 7.49
CHEMBL1242724 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1242352 Ki = 0.8128 nM 9.09
CHEMBL13647 BMY-7378 Ki = 1.288 nM 8.89
CHEMBL1241557 Ki = 1.38 nM 8.86
CHEMBL1242542 Ki = 1.479 nM 8.83
CHEMBL1242633 Ki = 2.512 nM 8.60
CHEMBL1242632 Ki = 4.074 nM 8.39
CHEMBL31354 WAY-100,635 Ki = 4.571 nM 8.34
CHEMBL1242912 Ki = 4.786 nM 8.32
CHEMBL1242445 Ki = 5.248 nM 8.28
CHEMBL1242819 Ki = 8.511 nM 8.07
CHEMBL1242444 Ki = 13.49 nM 7.87
CHEMBL1242541 Ki = 14.13 nM 7.85
CHEMBL1242725 Ki = 16.22 nM 7.79
CHEMBL1242818 Ki = 32.36 nM 7.49
CHEMBL1242724 Ki = 39.81 nM 7.40