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Assay Detail

CHEMBL934520

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

Binding
Displacement of [3H]spiperone from cloned human dopamine D3 receptor expressed in CHO cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
Prante O, Tietze R, Hocke C, Löber S, Hübner H, Kuwert T, Gmeiner P.
J Med Chem (2008) 51 : 1800 -1810
PubMed 18307287 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 5.69 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL411437 1 6.50
CHEMBL272395 1 6.39
CHEMBL270056 1 6.23
CHEMBL405260 1 6.03
CHEMBL272396 1 6.03
CHEMBL272602 1 5.66
CHEMBL407818 1 5.47
CHEMBL405292 1 5.47
CHEMBL7927 FAUC 113 1 5.35
CHEMBL310843 1 5.28
CHEMBL272873 1 5.06
CHEMBL272853 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL411437 Ki = 320.0 nM 6.50
CHEMBL272395 Ki = 410.0 nM 6.39
CHEMBL270056 Ki = 590.0 nM 6.23
CHEMBL405260 Ki = 940.0 nM 6.03
CHEMBL272396 Ki = 930.0 nM 6.03
CHEMBL272602 Ki = 2200.0 nM 5.66
CHEMBL407818 Ki = 3400.0 nM 5.47
CHEMBL405292 Ki = 3400.0 nM 5.47
CHEMBL7927 FAUC 113 Ki = 4500.0 nM 5.35
CHEMBL310843 Ki = 5300.0 nM 5.28
CHEMBL272873 Ki = 8700.0 nM 5.06
CHEMBL272853 Ki = 15000.0 nM 4.82