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Assay Detail

CHEMBL2443397

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

Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Tissue Cerebral cortex
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-1 adrenergic receptor (CHEMBL4351)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Click chemistry based synthesis of dopamine D4 selective receptor ligands for the selection of potential PET tracers.
Banerjee A, Maschauer S, Hübner H, Gmeiner P, Prante O.
Bioorg Med Chem Lett (2013) 23 : 6079 -6082
PubMed 24100078 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.52 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2443009 1 6.96
CHEMBL2443006 1 6.92
CHEMBL2443004 1 6.92
CHEMBL2443005 1 6.89
CHEMBL2443008 1 6.68
CHEMBL2443010 1 6.68
CHEMBL2443007 1 6.58
CHEMBL2443002 1 6.31
CHEMBL2443000 1 6.31
CHEMBL2443001 1 5.89
CHEMBL2443003 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2443009 Ki = 110.0 nM 6.96
CHEMBL2443006 Ki = 120.0 nM 6.92
CHEMBL2443004 Ki = 120.0 nM 6.92
CHEMBL2443005 Ki = 130.0 nM 6.89
CHEMBL2443008 Ki = 210.0 nM 6.68
CHEMBL2443010 Ki = 210.0 nM 6.68
CHEMBL2443007 Ki = 260.0 nM 6.58
CHEMBL2443002 Ki = 490.0 nM 6.31
CHEMBL2443000 Ki = 490.0 nM 6.31
CHEMBL2443001 Ki = 1300.0 nM 5.89
CHEMBL2443003 Ki = 2500.0 nM 5.60