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Assay Detail

CHEMBL674942

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

Binding
Inhibition of [125 I]iodosulpiride binding to human Dopamine receptor D2 expressed in CHO cell membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Tetracyclic analogues of [+]-S 14297: Synthesis and determination of affinity and selectivity at cloned human dopamine D3 vs D2 receptors
Peglion J, Vian J, Goument B, Despaux N, Audinot V, Millan MJ
Bioorg Med Chem Lett (1997) 7 : 881 -886
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 5.94 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL140184 1 6.60
CHEMBL169323 1 6.40
CHEMBL171826 1 6.40
CHEMBL170976 1 6.30
CHEMBL171825 1 6.00
CHEMBL171672 1 5.60
CHEMBL169322 1 5.30
CHEMBL170923 1 4.90
CHEMBL354845 1 -
CHEMBL435272 1 -
CHEMBL173803 1 -
CHEMBL355065 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL140184 Ki = 251.19 nM 6.60
CHEMBL169323 Ki = 398.11 nM 6.40
CHEMBL171826 Ki = 398.11 nM 6.40
CHEMBL170976 Ki = 501.19 nM 6.30
CHEMBL171825 Ki = 1000.0 nM 6.00
CHEMBL171672 Ki = 2511.89 nM 5.60
CHEMBL169322 Ki = 5011.87 nM 5.30
CHEMBL170923 Ki = 12589.25 nM 4.90
CHEMBL354845 Ki < 100000.0 nM -
CHEMBL435272 Ki < 10000.0 nM -
CHEMBL173803 Ki < 10000.0 nM -
CHEMBL355065 Ki < 10000.0 nM -