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Assay Detail

CHEMBL675848

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

Binding
Relative affinity for dopamine receptor by displacement of [3H]spiroperidol (2.2 nM) from (in vitro) dopamine binding sites in rat caudate nuclei
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Dopamine receptor (CHEMBL2093868)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain.
de Paulis T, Betts CR, Smith HE, Mobley PL, Manier DH, Sulser F.
J Med Chem (1981) 24 : 1021 -1026
PubMed 7288815 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.97 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7617 1 7.41
CHEMBL275696 1 6.47
CHEMBL7430 1 6.17
CHEMBL415300 ISOCLOZAPINE 1 6.12
CHEMBL7821 1 6.09
CHEMBL7828 ISOLOXAPINE 1 5.61
CHEMBL42 CLOZAPINE 4.0 1 5.37
CHEMBL266723 1 4.49
CHEMBL269396 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7617 IC50 = 39.0 nM 7.41
CHEMBL275696 IC50 = 342.0 nM 6.47
CHEMBL7430 IC50 = 678.0 nM 6.17
CHEMBL415300 ISOCLOZAPINE IC50 = 758.0 nM 6.12
CHEMBL7821 IC50 = 808.0 nM 6.09
CHEMBL7828 ISOLOXAPINE IC50 = 2480.0 nM 5.61
CHEMBL42 CLOZAPINE IC50 = 4310.0 nM 5.37
CHEMBL266723 IC50 = 32400.0 nM 4.49
CHEMBL269396 IC50 > 10000.0 nM -