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Assay Detail

CHEMBL5335368

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

Binding
Displacement of [3H]N-methylspiperone from human dopamine D2 receptor assessed as inhibition constant
11
Total Activities
11
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(2) dopamine receptor (CHEMBL217)
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 11 6.03 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.02
CHEMBL5425375 1 6.23
CHEMBL5396616 1 6.21
CHEMBL5438487 1 6.09
CHEMBL487387 STEPHOLIDINE 1 6.01
CHEMBL5399568 1 5.84
CHEMBL5410716 1 5.83
CHEMBL5433001 1 5.68
CHEMBL5410387 1 5.57
CHEMBL5399166 1 5.56
CHEMBL5428803 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 9.6 nM 8.02
CHEMBL5425375 Ki = 591.0 nM 6.23
CHEMBL5396616 Ki = 616.0 nM 6.21
CHEMBL5438487 Ki = 811.0 nM 6.09
CHEMBL487387 STEPHOLIDINE Ki = 974.0 nM 6.01
CHEMBL5399568 Ki = 1433.0 nM 5.84
CHEMBL5410716 Ki = 1491.0 nM 5.83
CHEMBL5433001 Ki = 2089.0 nM 5.68
CHEMBL5410387 Ki = 2682.0 nM 5.57
CHEMBL5399166 Ki = 2739.0 nM 5.56
CHEMBL5428803 Ki = 5045.0 nM 5.30