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Assay Detail

CHEMBL3117736

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

Binding
Displacement of [3H]spiperone from human dopamine D3 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
28
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and characterization of a novel series of agonist compounds as potential radiopharmaceuticals for imaging dopamine D₂/₃ receptors in their high-affinity state.
van Wieringen JP, Shalgunov V, Janssen HM, Fransen PM, Janssen AG, Michel MC, Booij J, Elsinga PH.
J Med Chem (2014) 57 : 391 -410
PubMed 24325578 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 8.02 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2106804 NAXAGOLIDE HYDROCHLORIDE -1.0 2 9.00
CHEMBL3115576 2 8.78
CHEMBL538542 2 8.74
CHEMBL3115575 2 8.54
CHEMBL134807 2 8.50
CHEMBL3115574 2 8.25
CHEMBL3115582 2 8.06
CHEMBL3115579 2 8.04
CHEMBL1557 DOPAMINE HYDROCHLORIDE 4.0 2 7.90
CHEMBL3115585 2 7.72
CHEMBL3115578 2 7.66
CHEMBL3115577 2 7.62
CHEMBL3115580 2 7.49
CHEMBL3115581 2 7.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2106804 NAXAGOLIDE HYDROCHLORIDE Ki = 1.0 nM 9.00
CHEMBL2106804 NAXAGOLIDE HYDROCHLORIDE Ki = 1.08 nM 8.97
CHEMBL3115576 Ki = 1.66 nM 8.78
CHEMBL3115576 Ki = 1.79 nM 8.75
CHEMBL538542 Ki = 1.82 nM 8.74
CHEMBL538542 Ki = 1.91 nM 8.72
CHEMBL3115575 Ki = 2.884 nM 8.54
CHEMBL134807 Ki = 3.162 nM 8.50
CHEMBL134807 Ki = 3.18 nM 8.50
CHEMBL3115574 Ki = 5.623 nM 8.25
CHEMBL3115575 Ki = 7.87 nM 8.10
CHEMBL3115582 Ki = 8.71 nM 8.06
CHEMBL3115579 Ki = 9.12 nM 8.04
CHEMBL3115582 Ki = 10.0 nM 8.00
CHEMBL3115579 Ki = 12.1 nM 7.92
CHEMBL1557 DOPAMINE HYDROCHLORIDE Ki = 12.59 nM 7.90
CHEMBL3115574 Ki = 13.9 nM 7.86
CHEMBL3115585 Ki = 19.05 nM 7.72
CHEMBL3115578 Ki = 21.88 nM 7.66
CHEMBL3115578 Ki = 23.0 nM 7.64
CHEMBL3115577 Ki = 23.99 nM 7.62
CHEMBL3115577 Ki = 24.2 nM 7.62
CHEMBL1557 DOPAMINE HYDROCHLORIDE Ki = 24.8 nM 7.61
CHEMBL3115580 Ki = 32.36 nM 7.49
CHEMBL3115580 Ki = 33.0 nM 7.48
CHEMBL3115581 Ki = 37.15 nM 7.43
CHEMBL3115581 Ki = 39.4 nM 7.41
CHEMBL3115585 Ki = 547.0 nM 6.26