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Assay Detail

CHEMBL1038853

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

Binding
Displacement of [3H]spiperone from human dopamine D2L receptor expressed in CHO cells by scintillation counting
18
Total Activities
17
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 Autocuration

Target

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

Publication

Dibenzazecine scaffold rebuilding--is the flexibility always essential for high dopamine receptor affinities?
Schulze M, Müller FK, Mason JM, Görls H, Lehmann J, Enzensperger C.
Bioorg Med Chem (2009) 17 : 6898 -6907
PubMed 19744859 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.34 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL380330 1 7.89
CHEMBL201170 1 7.76
CHEMBL596448 1 6.50
CHEMBL593897 1 6.31
CHEMBL487387 STEPHOLIDINE 1 6.01
CHEMBL25856 DIHYDREXIDINE 2.0 1 5.58
CHEMBL594798 1 5.57
CHEMBL594127 1 5.13
CHEMBL593626 1 -
CHEMBL593394 1 -
CHEMBL593395 1 -
CHEMBL594557 1 -
CHEMBL594789 1 -
CHEMBL596179 1 -
CHEMBL610449 2 -
CHEMBL594799 1 -
CHEMBL595720 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL380330 Ki = 13.0 nM 7.89
CHEMBL201170 Ki = 17.5 nM 7.76
CHEMBL596448 Ki = 320.0 nM 6.50
CHEMBL593897 Ki = 486.0 nM 6.31
CHEMBL487387 STEPHOLIDINE Ki = 974.0 nM 6.01
CHEMBL25856 DIHYDREXIDINE Ki = 2607.0 nM 5.58
CHEMBL594798 Ki = 2724.0 nM 5.57
CHEMBL594127 Ki = 7371.0 nM 5.13
CHEMBL593395 Ki > 10000.0 nM -
CHEMBL594799 Ki > 10000.0 nM -
CHEMBL593626 Ki > 10000.0 nM -
CHEMBL610449 Ki > 10000.0 nM -
CHEMBL610449 Ki > 10000.0 nM -
CHEMBL596179 Ki > 10000.0 nM -
CHEMBL594789 Ki > 10000.0 nM -
CHEMBL594557 Ki > 10000.0 nM -
CHEMBL593394 Ki > 10000.0 nM -
CHEMBL595720 Ki > 10000.0 nM -