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Assay Detail

CHEMBL860512

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

Binding
Displacement of [3H]prazosin from alpha-1 adrenergic receptor of porcine cortical membrane
7
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL2094251)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Fancy bioisosteres: novel paracyclophane derivatives as super-affinity dopamine D3 receptor antagonists.
Schlotter K, Boeckler F, Hübner H, Gmeiner P.
J Med Chem (2006) 49 : 3628 -3635
PubMed 16759104 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.74 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL210567 2 8.60
CHEMBL25236 BP-897 1 8.30
CHEMBL208847 1 8.08
CHEMBL426863 1 7.35
CHEMBL209876 1 7.10
CHEMBL210461 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL210567 Ki = 2.5 nM 8.60
CHEMBL210567 Ki = 3.9 nM 8.41
CHEMBL25236 BP-897 Ki = 5.0 nM 8.30
CHEMBL208847 Ki = 8.4 nM 8.08
CHEMBL426863 Ki = 45.0 nM 7.35
CHEMBL209876 Ki = 80.0 nM 7.10
CHEMBL210461 Ki = 480.0 nM 6.32