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Assay Detail

CHEMBL861745

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

Binding
Displacement of [3H]spiroperidol from cloned human dopamine receptor D3 expressed in CHO cells
26
Total Activities
26
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 Expert

Target

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

Publication

Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands for visualization of brain dopamine D3 receptors.
Leopoldo M, Lacivita E, De Giorgio P, Colabufo NA, Niso M, Berardi F, Perrone R.
J Med Chem (2006) 49 : 358 -365
PubMed 16392820 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 7.14 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196476 1 9.89
CHEMBL201270 1 8.32
CHEMBL201551 1 7.83
CHEMBL199859 1 7.71
CHEMBL199836 1 7.67
CHEMBL199329 1 7.65
CHEMBL203302 1 7.62
CHEMBL201698 1 7.59
CHEMBL197660 1 7.42
CHEMBL424667 1 7.23
CHEMBL126780 1 7.22
CHEMBL199498 1 7.11
CHEMBL372308 1 7.07
CHEMBL198404 1 7.01
CHEMBL201027 1 6.99
CHEMBL200024 1 6.93
CHEMBL202713 1 6.90
CHEMBL199746 1 6.66
CHEMBL201326 1 6.58
CHEMBL197762 1 5.94
CHEMBL426834 1 5.89
CHEMBL199480 1 5.84
CHEMBL435939 1 5.26
CHEMBL202762 1 -
CHEMBL200243 1 -
CHEMBL201275 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196476 Ki = 0.13 nM 9.89
CHEMBL201270 Ki = 4.79 nM 8.32
CHEMBL201551 Ki = 14.7 nM 7.83
CHEMBL199859 Ki = 19.3 nM 7.71
CHEMBL199836 Ki = 21.4 nM 7.67
CHEMBL199329 Ki = 22.6 nM 7.65
CHEMBL203302 Ki = 23.9 nM 7.62
CHEMBL201698 Ki = 25.5 nM 7.59
CHEMBL197660 Ki = 38.0 nM 7.42
CHEMBL424667 Ki = 58.5 nM 7.23
CHEMBL126780 Ki = 60.1 nM 7.22
CHEMBL199498 Ki = 77.9 nM 7.11
CHEMBL372308 Ki = 85.0 nM 7.07
CHEMBL198404 Ki = 98.0 nM 7.01
CHEMBL201027 Ki = 102.0 nM 6.99
CHEMBL200024 Ki = 118.0 nM 6.93
CHEMBL202713 Ki = 127.0 nM 6.90
CHEMBL199746 Ki = 220.0 nM 6.66
CHEMBL201326 Ki = 262.0 nM 6.58
CHEMBL197762 Ki = 1140.0 nM 5.94
CHEMBL426834 Ki = 1285.0 nM 5.89
CHEMBL199480 Ki = 1440.0 nM 5.84
CHEMBL435939 Ki = 5539.0 nM 5.26
CHEMBL202762 Ki > 8500.0 nM -
CHEMBL200243 Ki > 8500.0 nM -
CHEMBL201275 Ki > 2700.0 nM -