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Assay Detail

CHEMBL673081

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

Binding
In vitro binding affinity at human cloned Dopamine receptor D2L expressed in Sf9 cell membranes
15
Total Activities
15
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(2) dopamine receptor (CHEMBL217)
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 15 6.15 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.07
CHEMBL148353 1 6.87
CHEMBL148694 1 6.83
CHEMBL358657 1 6.74
CHEMBL342536 1 6.74
CHEMBL42 CLOZAPINE 4.0 1 6.43
CHEMBL148559 1 6.24
CHEMBL422310 1 6.20
CHEMBL436274 1 6.05
CHEMBL356149 1 5.96
CHEMBL63576 1 5.65
CHEMBL347959 1 5.59
CHEMBL63329 1 5.23
CHEMBL146856 1 5.00
CHEMBL148042 1 4.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 8.5 nM 8.07
CHEMBL148353 Ki = 136.0 nM 6.87
CHEMBL148694 Ki = 149.0 nM 6.83
CHEMBL358657 Ki = 183.0 nM 6.74
CHEMBL342536 Ki = 183.0 nM 6.74
CHEMBL42 CLOZAPINE Ki = 372.0 nM 6.43
CHEMBL148559 Ki = 571.0 nM 6.24
CHEMBL422310 Ki = 635.0 nM 6.20
CHEMBL436274 Ki = 892.0 nM 6.05
CHEMBL356149 Ki = 1099.0 nM 5.96
CHEMBL63576 Ki = 2235.0 nM 5.65
CHEMBL347959 Ki = 2596.0 nM 5.59
CHEMBL63329 Ki = 5940.0 nM 5.23
CHEMBL146856 Ki = 9943.0 nM 5.00
CHEMBL148042 Ki = 19117.0 nM 4.72