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Assay Detail

CHEMBL676506

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

Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.
Liégeois JF, Eyrolles L, Ellenbroek BA, Lejeune C, Carato P, Bruhwyler J, Géczy J, Damas J, Delarge J.
J Med Chem (2002) 45 : 5136 -5149
PubMed 12408724 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 7.11 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.66
CHEMBL42 CLOZAPINE 4.0 1 7.75
CHEMBL63576 1 7.62
CHEMBL63329 1 7.44
CHEMBL422310 1 7.43
CHEMBL436274 1 7.40
CHEMBL358657 1 7.34
CHEMBL148559 1 7.32
CHEMBL148752 1 7.08
CHEMBL342536 1 7.05
CHEMBL146856 1 6.96
CHEMBL148353 1 6.94
CHEMBL148694 1 6.88
CHEMBL148042 1 6.79
CHEMBL148965 1 6.74
CHEMBL146410 1 6.47
CHEMBL356171 1 6.45
CHEMBL356149 1 6.41
CHEMBL347959 1 6.29
CHEMBL424314 1 -
CHEMBL148952 1 -
CHEMBL345964 1 -
CHEMBL357743 1 -
CHEMBL357391 1 -
CHEMBL148836 1 -
CHEMBL147473 1 -
CHEMBL149987 1 -
CHEMBL347292 1 -
CHEMBL357320 1 -
CHEMBL357325 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 2.2 nM 8.66
CHEMBL42 CLOZAPINE Ki = 18.0 nM 7.75
CHEMBL63576 Ki = 24.0 nM 7.62
CHEMBL63329 Ki = 36.0 nM 7.44
CHEMBL422310 Ki = 37.0 nM 7.43
CHEMBL436274 Ki = 40.0 nM 7.40
CHEMBL358657 Ki = 46.0 nM 7.34
CHEMBL148559 Ki = 48.0 nM 7.32
CHEMBL148752 Ki = 84.0 nM 7.08
CHEMBL342536 Ki = 89.0 nM 7.05
CHEMBL146856 Ki = 109.0 nM 6.96
CHEMBL148353 Ki = 115.0 nM 6.94
CHEMBL148694 Ki = 131.0 nM 6.88
CHEMBL148042 Ki = 163.0 nM 6.79
CHEMBL148965 Ki = 183.0 nM 6.74
CHEMBL146410 Ki = 341.0 nM 6.47
CHEMBL356171 Ki = 356.0 nM 6.45
CHEMBL356149 Ki = 393.0 nM 6.41
CHEMBL347959 Ki = 510.0 nM 6.29
CHEMBL424314 Ki > 1000.0 nM -
CHEMBL148952 Ki > 1000.0 nM -
CHEMBL345964 Ki > 1000.0 nM -
CHEMBL357743 Ki > 1000.0 nM -
CHEMBL357391 Ki > 1000.0 nM -
CHEMBL148836 Ki > 1000.0 nM -
CHEMBL147473 Ki > 1000.0 nM -
CHEMBL149987 Ki > 1000.0 nM -
CHEMBL347292 Ki > 1000.0 nM -
CHEMBL357320 Ki > 1000.0 nM -
CHEMBL357325 Ki > 1000.0 nM -
CHEMBL355907 Ki > 1000.0 nM -
CHEMBL423760 Ki > 1000.0 nM -
CHEMBL149493 Ki > 1000.0 nM -