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Assay Detail

CHEMBL1768396

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

Binding
Displacement of [3H]spiperone from human dopamine D3 receptor V2.61F mutant expressed in HEK293 cells after 60 mins
9
Total Activities
9
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

Highly potent 5-aminotetrahydropyrazolopyridines: enantioselective dopamine D3 receptor binding, functional selectivity, and analysis of receptor-ligand interactions.
Tschammer N, Elsner J, Goetz A, Ehrlich K, Schuster S, Ruberg M, Kühhorn J, Thompson D, Whistler J, Hübner H, Gmeiner P.
J Med Chem (2011) 54 : 2477 -2491
PubMed 21388142 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.40 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1765633 1 6.77
CHEMBL112065 1 6.75
CHEMBL1765638 1 6.64
CHEMBL1765637 1 6.60
CHEMBL1765635 1 6.48
CHEMBL1196271 1 6.46
CHEMBL193337 1 6.38
CHEMBL1765636 1 6.12
CHEMBL1765634 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1765633 Ki = 170.0 nM 6.77
CHEMBL112065 Ki = 180.0 nM 6.75
CHEMBL1765638 Ki = 230.0 nM 6.64
CHEMBL1765637 Ki = 250.0 nM 6.60
CHEMBL1765635 Ki = 330.0 nM 6.48
CHEMBL1196271 Ki = 350.0 nM 6.46
CHEMBL193337 Ki = 420.0 nM 6.38
CHEMBL1765636 Ki = 760.0 nM 6.12
CHEMBL1765634 Ki = 3700.0 nM 5.43