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Assay Detail

CHEMBL672657

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

Binding
Binding affinity for Dopamine receptor D2 using [3H]spiperone in rat brain
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.
Davis DA, de Paulis T, Janowsky A, Smith HE.
J Med Chem (1990) 33 : 809 -814
PubMed 1967652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.21 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL72162 1 7.57
CHEMBL415300 ISOCLOZAPINE 1 6.66
CHEMBL355107 1 6.52
CHEMBL91310 1 6.52
CHEMBL42 CLOZAPINE 4.0 1 5.56
CHEMBL88870 1 5.32
CHEMBL328246 1 5.30
CHEMBL73082 1 -
CHEMBL73538 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL72162 IC50 = 27.0 nM 7.57
CHEMBL415300 ISOCLOZAPINE IC50 = 218.0 nM 6.66
CHEMBL355107 IC50 = 300.0 nM 6.52
CHEMBL91310 IC50 = 305.0 nM 6.52
CHEMBL42 CLOZAPINE IC50 = 2770.0 nM 5.56
CHEMBL88870 IC50 = 4750.0 nM 5.32
CHEMBL328246 IC50 = 5000.0 nM 5.30
CHEMBL73082 IC50 > 10000.0 nM -
CHEMBL73538 IC50 > 10000.0 nM -