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Assay Detail

CHEMBL931956

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Binding
Binding affinity to human dopamine D4.4 receptor
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

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 10 8.12 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL270406 1 8.89
CHEMBL270408 1 8.80
CHEMBL256637 1 8.77
CHEMBL256492 1 8.74
CHEMBL310843 1 8.66
CHEMBL271513 1 8.43
CHEMBL404888 1 7.92
CHEMBL272073 1 7.30
CHEMBL255163 1 7.09
CHEMBL404570 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL270406 Ki = 1.3 nM 8.89
CHEMBL270408 Ki = 1.6 nM 8.80
CHEMBL256637 Ki = 1.7 nM 8.77
CHEMBL256492 Ki = 1.8 nM 8.74
CHEMBL310843 Ki = 2.2 nM 8.66
CHEMBL271513 Ki = 3.7 nM 8.43
CHEMBL404888 Ki = 12.0 nM 7.92
CHEMBL272073 Ki = 50.0 nM 7.30
CHEMBL255163 Ki = 82.0 nM 7.09
CHEMBL404570 Ki = 250.0 nM 6.60