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Assay Detail

CHEMBL672525

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

Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D2L in COS7 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type COS-7
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors.
Phillips ST, de Paulis T, Neergaard JR, Baron BM, Siegel BW, Seeman P, Van Tol HH, Guan HC, Smith HE.
J Med Chem (1995) 38 : 708 -714
PubMed 7861418 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.18 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 1 8.85
CHEMBL90882 1 8.60
CHEMBL89970 1 7.68
CHEMBL831 LOXAPINE 4.0 1 7.68
CHEMBL542029 1 7.36
CHEMBL556969 1 7.21
CHEMBL539057 1 7.09
CHEMBL555362 1 7.08
CHEMBL554670 1 7.05
CHEMBL544418 1 6.96
CHEMBL42 CLOZAPINE 4.0 1 6.66
CHEMBL163863 1 6.64
CHEMBL163239 1 6.36
CHEMBL94067 1 6.24
CHEMBL544184 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 1.4 nM 8.85
CHEMBL90882 Ki = 2.5 nM 8.60
CHEMBL89970 Ki = 21.0 nM 7.68
CHEMBL831 LOXAPINE Ki = 21.0 nM 7.68
CHEMBL542029 Ki = 44.0 nM 7.36
CHEMBL556969 Ki = 61.0 nM 7.21
CHEMBL539057 Ki = 82.0 nM 7.09
CHEMBL555362 Ki = 83.0 nM 7.08
CHEMBL554670 Ki = 89.0 nM 7.05
CHEMBL544418 Ki = 110.0 nM 6.96
CHEMBL42 CLOZAPINE Ki = 220.0 nM 6.66
CHEMBL163863 Ki = 230.0 nM 6.64
CHEMBL163239 Ki = 440.0 nM 6.36
CHEMBL94067 Ki = 570.0 nM 6.24
CHEMBL544184 Ki = 680.0 nM 6.17