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Assay Detail

CHEMBL617214

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

Binding
Binding affinity for porcine 5-hydroxytryptamine 2 receptor using [3H]- ketanserin with 10 uM prazosin
9
Total Activities
9
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

Serotonin 2 (5-HT2) receptor (CHEMBL2095200)
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 9 6.03 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL424294 1 6.46
CHEMBL141419 1 6.30
CHEMBL342060 1 6.13
CHEMBL25236 BP-897 1 6.08
CHEMBL336930 1 6.02
CHEMBL142020 1 5.92
CHEMBL423735 1 5.89
CHEMBL143352 1 5.80
CHEMBL344677 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL424294 Ki = 350.0 nM 6.46
CHEMBL141419 Ki = 500.0 nM 6.30
CHEMBL342060 Ki = 740.0 nM 6.13
CHEMBL25236 BP-897 Ki = 840.0 nM 6.08
CHEMBL336930 Ki = 950.0 nM 6.02
CHEMBL142020 Ki = 1200.0 nM 5.92
CHEMBL423735 Ki = 1300.0 nM 5.89
CHEMBL143352 Ki = 1600.0 nM 5.80
CHEMBL344677 Ki = 2000.0 nM 5.70