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Assay Detail

CHEMBL1038855

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

Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
17
Total Activities
16
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(4) dopamine receptor (CHEMBL219)
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 17 6.13 7.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201170 1 7.95
CHEMBL380330 1 7.36
CHEMBL596448 1 5.59
CHEMBL487387 STEPHOLIDINE 1 5.43
CHEMBL593897 1 5.29
CHEMBL594127 1 5.18
CHEMBL593395 1 -
CHEMBL593626 1 -
CHEMBL593394 1 -
CHEMBL595720 1 -
CHEMBL594557 1 -
CHEMBL594789 1 -
CHEMBL596179 1 -
CHEMBL610449 2 -
CHEMBL594798 1 -
CHEMBL594799 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201170 Ki = 11.3 nM 7.95
CHEMBL380330 Ki = 43.4 nM 7.36
CHEMBL596448 Ki = 2565.0 nM 5.59
CHEMBL487387 STEPHOLIDINE Ki = 3748.0 nM 5.43
CHEMBL593897 Ki = 5092.0 nM 5.29
CHEMBL594127 Ki = 6644.0 nM 5.18
CHEMBL593626 Ki > 10000.0 nM -
CHEMBL593394 Ki > 10000.0 nM -
CHEMBL593395 Ki > 10000.0 nM -
CHEMBL594557 Ki > 10000.0 nM -
CHEMBL594789 Ki > 10000.0 nM -
CHEMBL596179 Ki > 10000.0 nM -
CHEMBL610449 Ki > 10000.0 nM -
CHEMBL610449 Ki > 10000.0 nM -
CHEMBL594798 Ki > 10000.0 nM -
CHEMBL594799 Ki > 10000.0 nM -
CHEMBL595720 Ki > 10000.0 nM -