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Assay Detail

CHEMBL5335369

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

Binding
Displacement of [3H]N-methylspiperone from human dopamine D3 receptor assessed as inhibition constant
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of Selective Dopamine Receptor Ligands Derived from (-)-Stepholidine via C-3 Alkoxylation and C-3/C-9 Dialkoxylation.
Namballa HK, Dorogan M, Gudipally AR, Okafor S, Gadhiya S, Harding WW.
J Med Chem (2023) 66 : 10060 -10079
PubMed 37421373 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 6.66 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71 CHLORPROMAZINE 4.0 1 7.96
CHEMBL5410716 1 7.58
CHEMBL487387 STEPHOLIDINE 1 7.52
CHEMBL5399568 1 7.48
CHEMBL5433001 1 7.40
CHEMBL5410387 1 7.34
CHEMBL5399166 1 7.29
CHEMBL5429932 1 7.18
CHEMBL5428803 1 7.07
CHEMBL5439212 1 7.05
CHEMBL5396616 1 6.58
CHEMBL5399422 1 6.57
CHEMBL5437148 1 6.56
CHEMBL5420387 1 6.38
CHEMBL5414499 1 6.28
CHEMBL5399933 1 6.26
CHEMBL5435602 1 6.24
CHEMBL5394838 1 6.12
CHEMBL5402269 1 6.05
CHEMBL5409939 1 6.03
CHEMBL5425375 1 5.98
CHEMBL5395272 1 5.73
CHEMBL5420515 1 5.67
CHEMBL5438487 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71 CHLORPROMAZINE Ki = 11.0 nM 7.96
CHEMBL5410716 Ki = 26.0 nM 7.58
CHEMBL487387 STEPHOLIDINE Ki = 30.0 nM 7.52
CHEMBL5399568 Ki = 33.0 nM 7.48
CHEMBL5433001 Ki = 40.0 nM 7.40
CHEMBL5410387 Ki = 46.0 nM 7.34
CHEMBL5399166 Ki = 51.0 nM 7.29
CHEMBL5429932 Ki = 66.0 nM 7.18
CHEMBL5428803 Ki = 86.0 nM 7.07
CHEMBL5439212 Ki = 90.0 nM 7.05
CHEMBL5396616 Ki = 262.0 nM 6.58
CHEMBL5399422 Ki = 268.0 nM 6.57
CHEMBL5437148 Ki = 275.0 nM 6.56
CHEMBL5420387 Ki = 415.0 nM 6.38
CHEMBL5414499 Ki = 524.0 nM 6.28
CHEMBL5399933 Ki = 551.0 nM 6.26
CHEMBL5435602 Ki = 576.0 nM 6.24
CHEMBL5394838 Ki = 753.0 nM 6.12
CHEMBL5402269 Ki = 898.0 nM 6.05
CHEMBL5409939 Ki = 929.0 nM 6.03
CHEMBL5425375 Ki = 1045.0 nM 5.98
CHEMBL5395272 Ki = 1852.0 nM 5.73
CHEMBL5420515 Ki = 2131.0 nM 5.67
CHEMBL5438487 Ki = 2618.0 nM 5.58