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Assay Detail

CHEMBL673252

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

Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors.
Phillips ST, de Paulis T, Baron BM, Siegel BW, Seeman P, Van Tol HH, Guan HC, Smith HE.
J Med Chem (1994) 37 : 2686 -2696
PubMed 8064797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.57 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL90882 1 9.27
CHEMBL88464 1 9.05
CHEMBL7617 1 9.00
CHEMBL89970 1 8.70
CHEMBL831 LOXAPINE 4.0 1 8.31
CHEMBL432762 1 7.92
CHEMBL7828 ISOLOXAPINE 1 7.64
CHEMBL91310 1 7.33
CHEMBL90977 1 6.52
CHEMBL328246 1 6.03
CHEMBL88870 1 5.57
CHEMBL275696 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL90882 Ki = 0.54 nM 9.27
CHEMBL88464 Ki = 0.9 nM 9.05
CHEMBL7617 Ki = 1.0 nM 9.00
CHEMBL89970 Ki = 2.0 nM 8.70
CHEMBL831 LOXAPINE Ki = 4.9 nM 8.31
CHEMBL432762 Ki = 12.0 nM 7.92
CHEMBL7828 ISOLOXAPINE Ki = 23.0 nM 7.64
CHEMBL91310 Ki = 47.0 nM 7.33
CHEMBL90977 Ki = 300.0 nM 6.52
CHEMBL328246 Ki = 930.0 nM 6.03
CHEMBL88870 Ki = 2700.0 nM 5.57
CHEMBL275696 Ki = 2900.0 nM 5.54