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Assay Detail

CHEMBL673251

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Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptor
13
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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 13 6.57 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415300 ISOCLOZAPINE 1 7.80
CHEMBL42 CLOZAPINE 4.0 1 7.68
CHEMBL266723 1 6.92
CHEMBL94067 3 6.82
CHEMBL90654 1 6.72
CHEMBL91350 1 6.50
CHEMBL327713 1 6.48
CHEMBL89719 1 6.40
CHEMBL73538 1 6.38
CHEMBL269396 1 6.00
CHEMBL7430 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415300 ISOCLOZAPINE Ki = 16.0 nM 7.80
CHEMBL42 CLOZAPINE Ki = 21.0 nM 7.68
CHEMBL266723 Ki = 120.0 nM 6.92
CHEMBL94067 Ki = 150.0 nM 6.82
CHEMBL90654 Ki = 190.0 nM 6.72
CHEMBL94067 Ki = 270.0 nM 6.57
CHEMBL91350 Ki = 320.0 nM 6.50
CHEMBL327713 Ki = 330.0 nM 6.48
CHEMBL89719 Ki = 400.0 nM 6.40
CHEMBL73538 Ki = 420.0 nM 6.38
CHEMBL269396 Ki = 1000.0 nM 6.00
CHEMBL94067 Ki = 2500.0 nM 5.60
CHEMBL7430 Ki = 2700.0 nM 5.57