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Assay Detail

CHEMBL2343279

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

Binding
Displacement of [3H]spiperone from dopamine D2 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
34
Total Activities
34
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(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile.
Sun H, Zhu L, Yang H, Qian W, Guo L, Zhou S, Gao B, Li Z, Zhou Y, Jiang H, Chen K, Zhen X, Liu H.
Bioorg Med Chem (2013) 21 : 856 -868
PubMed 23332346 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 7.11 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267930 SPIPERONE 2.0 1 8.92
CHEMBL487387 STEPHOLIDINE 1 7.96
CHEMBL2334893 1 7.50
CHEMBL2334891 1 7.04
CHEMBL2334892 1 6.98
CHEMBL320397 1 6.95
CHEMBL490533 CANADINE 1 6.92
CHEMBL1457510 1 6.84
CHEMBL2057456 1 6.83
CHEMBL2057457 1 6.79
CHEMBL1235966 SCOULERINE 1 6.67
CHEMBL448891 1 6.52
CHEMBL2057453 1 6.46
CHEMBL2334888 1 -
CHEMBL2334886 1 -
CHEMBL2334885 1 -
CHEMBL2314733 1 -
CHEMBL2334884 1 -
CHEMBL522746 TETRAHYDROPALMATRUBINE 1 -
CHEMBL2334889 1 -
CHEMBL476501 1 -
CHEMBL2334890 1 -
CHEMBL1395394 1 -
CHEMBL2057455 1 -
CHEMBL13668 1 -
CHEMBL2334882 1 -
CHEMBL2334881 1 -
CHEMBL2334880 1 -
CHEMBL2334883 1 -
CHEMBL2334894 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267930 SPIPERONE Ki = 1.2 nM 8.92
CHEMBL487387 STEPHOLIDINE Ki = 11.0 nM 7.96
CHEMBL2334893 Ki = 32.0 nM 7.50
CHEMBL2334891 Ki = 91.0 nM 7.04
CHEMBL2334892 Ki = 105.0 nM 6.98
CHEMBL320397 Ki = 113.0 nM 6.95
CHEMBL490533 CANADINE Ki = 119.0 nM 6.92
CHEMBL1457510 Ki = 145.0 nM 6.84
CHEMBL2057456 Ki = 147.0 nM 6.83
CHEMBL2057457 Ki = 161.0 nM 6.79
CHEMBL1235966 SCOULERINE Ki = 214.0 nM 6.67
CHEMBL448891 Ki = 305.0 nM 6.52
CHEMBL2057453 Ki = 347.0 nM 6.46
CHEMBL2314732 Ki > 5000.0 nM -
CHEMBL487182 TETRAHYDROPALMATINE Ki > 5000.0 nM -
CHEMBL39 SEROTONIN Ki - -
CHEMBL2334887 Ki > 5000.0 nM -
CHEMBL2334888 Ki - -
CHEMBL2334886 Ki - -
CHEMBL2334885 Ki - -
CHEMBL2314733 Ki - -
CHEMBL2334884 Ki - -
CHEMBL522746 TETRAHYDROPALMATRUBINE Ki - -
CHEMBL2334889 Ki - -
CHEMBL476501 Ki - -
CHEMBL2334890 Ki - -
CHEMBL1395394 Ki - -
CHEMBL2057455 Ki - -
CHEMBL13668 Ki - -
CHEMBL2334882 Ki - -
CHEMBL2334881 Ki - -
CHEMBL2334880 Ki - -
CHEMBL2334883 Ki - -
CHEMBL2334894 Ki - -