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Assay Detail

CHEMBL1107672

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

Binding
Displacement of [125I]7OH-PIPAT from dopamine D2 receptor from rat brain homogenate
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1,2,4-Triazolyl azabicyclo[3.1.0]hexanes: a new series of potent and selective dopamine D(3) receptor antagonists.
Micheli F, Arista L, Bonanomi G, Blaney FE, Braggio S, Capelli AM, Checchia A, Damiani F, Di-Fabio R, Fontana S, Gentile G, Griffante C, Hamprecht D, Marchioro C, Mugnaini M, Piner J, Ratti E, Tedesco G, Tarsi L, Terreni S, Worby A, Ashby CR, Heidbreder C.
J Med Chem (2010) 53 : 374 -391
PubMed 19891474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.87 9.19
pKi 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1081746 1 9.19
CHEMBL1081409 1 9.05
CHEMBL1081687 1 9.01
CHEMBL1081867 1 8.70
CHEMBL1081023 1 8.38
CHEMBL1080490 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1081746 Ki = 0.6457 nM 9.19
CHEMBL1081409 Ki = 0.8913 nM 9.05
CHEMBL1081687 Ki = 0.9772 nM 9.01
CHEMBL1081867 Ki = 1.995 nM 8.70
CHEMBL1081023 Ki = 4.169 nM 8.38
CHEMBL1080490 pKi - -