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Assay Detail

CHEMBL3877885

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

Binding
Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and evaluation of C9 alkoxy analogues of (-)-stepholidine as dopamine receptor ligands.
Madapa S, Gadhiya S, Kurtzman T, Alberts IL, Ramsey S, Reith M, Harding WW.
Eur J Med Chem (2017) 125 : 255 -268
PubMed 27688181 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.44 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL487387 STEPHOLIDINE 1 7.52
CHEMBL3982215 1 7.51
CHEMBL3961827 1 6.97
CHEMBL3975220 1 6.88
CHEMBL3954556 1 6.76
CHEMBL3976659 1 6.71
CHEMBL3966718 1 6.71
CHEMBL3921278 1 6.43
CHEMBL3936976 1 6.35
CHEMBL3945691 1 6.14
CHEMBL3894329 1 5.68
CHEMBL3963862 1 5.50
CHEMBL3945856 1 5.49
CHEMBL3964242 1 5.44
CHEMBL3905947 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL487387 STEPHOLIDINE Ki = 30.0 nM 7.52
CHEMBL3982215 Ki = 31.0 nM 7.51
CHEMBL3961827 Ki = 106.0 nM 6.97
CHEMBL3975220 Ki = 131.0 nM 6.88
CHEMBL3954556 Ki = 175.0 nM 6.76
CHEMBL3976659 Ki = 195.0 nM 6.71
CHEMBL3966718 Ki = 195.0 nM 6.71
CHEMBL3921278 Ki = 373.0 nM 6.43
CHEMBL3936976 Ki = 450.0 nM 6.35
CHEMBL3945691 Ki = 726.0 nM 6.14
CHEMBL3894329 Ki = 2070.0 nM 5.68
CHEMBL3963862 Ki = 3171.0 nM 5.50
CHEMBL3945856 Ki = 3213.0 nM 5.49
CHEMBL3964242 Ki = 3605.0 nM 5.44
CHEMBL3905947 Ki > 10000.0 nM -