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Assay Detail

CHEMBL4406547

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

Binding
Displacement of [3H]-7-OH-DPAT from human D3R expressed in HEK293 cell membranes measured after 90 mins in EBSS buffer by topcount assay
2
Total Activities
2
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

Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D3 Dopamine Receptor Agonist.
Moritz AE, Free RB, Weiner WS, Akano EO, Gandhi D, Abramyan A, Keck TM, Ferrer M, Hu X, Southall N, Steiner J, Aubé J, Shi L, Frankowski KJ, Sibley DR.
J Med Chem (2020) 63 : 5526 -5567
PubMed 32342685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.55 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301265 PRAMIPEXOLE 4.0 1 8.96
CHEMBL4476784 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301265 PRAMIPEXOLE Ki = 1.1 nM 8.96
CHEMBL4476784 Ki = 720.0 nM 6.14