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Assay Detail

CHEMBL931952

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

Binding
Displacement of [3H]prazosin from pig cortical membrane adrenergic alpha-1 receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker.
Tietze R, Löber S, Hübner H, Gmeiner P, Kuwert T, Prante O.
Bioorg Med Chem Lett (2008) 18 : 983 -988
PubMed 18164618 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.39 8.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL256637 1 8.36
CHEMBL270406 1 7.89
CHEMBL404888 1 7.75
CHEMBL256492 1 7.68
CHEMBL270408 1 7.44
CHEMBL271513 1 7.33
CHEMBL272073 1 6.80
CHEMBL255163 1 6.72
CHEMBL310843 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL256637 Ki = 4.4 nM 8.36
CHEMBL270406 Ki = 13.0 nM 7.89
CHEMBL404888 Ki = 18.0 nM 7.75
CHEMBL256492 Ki = 21.0 nM 7.68
CHEMBL270408 Ki = 36.0 nM 7.44
CHEMBL271513 Ki = 47.0 nM 7.33
CHEMBL272073 Ki = 160.0 nM 6.80
CHEMBL255163 Ki = 190.0 nM 6.72
CHEMBL310843 Ki = 270.0 nM 6.57