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Assay Detail

CHEMBL860509

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

Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cells
7
Total Activities
6
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 Expert

Target

D(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
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 7.52 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL210567 2 8.27
CHEMBL426863 1 7.75
CHEMBL209876 1 7.48
CHEMBL25236 BP-897 1 7.36
CHEMBL210461 1 6.92
CHEMBL208847 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL210567 Ki = 5.4 nM 8.27
CHEMBL210567 Ki = 9.5 nM 8.02
CHEMBL426863 Ki = 18.0 nM 7.75
CHEMBL209876 Ki = 33.0 nM 7.48
CHEMBL25236 BP-897 Ki = 44.0 nM 7.36
CHEMBL210461 Ki = 120.0 nM 6.92
CHEMBL208847 Ki = 140.0 nM 6.85