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Assay Detail

CHEMBL643608

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

Binding
Displacement of [3H]- ketanserin from porcine Alpha-1 adrenergic receptor
13
Total Activities
13
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

Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.
Bettinetti L, Schlotter K, Hübner H, Gmeiner P.
J Med Chem (2002) 45 : 4594 -4597
PubMed 12361386 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.67 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL124444 1 8.07
CHEMBL141419 1 7.82
CHEMBL424294 1 7.82
CHEMBL344677 1 7.75
CHEMBL336930 1 7.72
CHEMBL25236 BP-897 1 7.60
CHEMBL142020 1 7.58
CHEMBL143352 1 7.55
CHEMBL342060 1 7.50
CHEMBL423735 1 7.32
CHEMBL59725 1 -
CHEMBL139926 1 -
CHEMBL337531 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL124444 Ki = 8.6 nM 8.07
CHEMBL141419 Ki = 15.0 nM 7.82
CHEMBL424294 Ki = 15.0 nM 7.82
CHEMBL344677 Ki = 18.0 nM 7.75
CHEMBL336930 Ki = 19.0 nM 7.72
CHEMBL25236 BP-897 Ki = 25.0 nM 7.60
CHEMBL142020 Ki = 26.0 nM 7.58
CHEMBL143352 Ki = 28.0 nM 7.55
CHEMBL342060 Ki = 32.0 nM 7.50
CHEMBL423735 Ki = 48.0 nM 7.32
CHEMBL59725 Ki > 2000.0 nM -
CHEMBL139926 Ki > 10000.0 nM -
CHEMBL337531 Ki > 1000.0 nM -