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Assay Detail

CHEMBL670885

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

Binding
In vitro affinity at human cloned Dopamine receptor D2A by [3H]-raclopride displacement.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

10-substituted 11-oxygenated (R)-aporphines: synthesis, pharmacology, and modeling of 5-HT1A receptor interactions.
Hedberg MH, Jansen JM, Nordvall G, Hjorth S, Unelius L, Johansson AM.
J Med Chem (1996) 39 : 3491 -3502
PubMed 8784447 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.40 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53 APOMORPHINE 4.0 1 7.38
CHEMBL119455 1 7.23
CHEMBL118771 1 6.62
CHEMBL332178 1 6.61
CHEMBL119593 1 6.60
CHEMBL119900 1 6.39
CHEMBL331005 1 6.39
CHEMBL334116 1 5.98
CHEMBL53510 1 5.97
CHEMBL115524 1 5.69
CHEMBL326159 1 5.56
CHEMBL116367 1 -
CHEMBL119577 1 -
CHEMBL332490 1 -
CHEMBL332771 1 -
CHEMBL435779 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53 APOMORPHINE Ki = 41.9 nM 7.38
CHEMBL119455 Ki = 58.5 nM 7.23
CHEMBL118771 Ki = 238.0 nM 6.62
CHEMBL332178 Ki = 248.0 nM 6.61
CHEMBL119593 Ki = 249.0 nM 6.60
CHEMBL119900 Ki = 403.0 nM 6.39
CHEMBL331005 Ki = 411.0 nM 6.39
CHEMBL334116 Ki = 1040.0 nM 5.98
CHEMBL53510 Ki = 1070.0 nM 5.97
CHEMBL115524 Ki = 2050.0 nM 5.69
CHEMBL326159 Ki = 2760.0 nM 5.56
CHEMBL116367 Ki > 10000.0 nM -
CHEMBL119577 Ki > 1000.0 nM -
CHEMBL332490 Ki > 1000.0 nM -
CHEMBL332771 Ki > 1000.0 nM -
CHEMBL435779 Ki > 1000.0 nM -