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Assay Detail

CHEMBL672007

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

Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

D(1A) dopamine receptor (CHEMBL265)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 8 7.39 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL91310 1 8.33
CHEMBL415300 ISOCLOZAPINE 1 7.85
CHEMBL432762 1 7.80
CHEMBL42 CLOZAPINE 4.0 1 7.37
CHEMBL90977 1 7.17
CHEMBL328246 1 7.01
CHEMBL88870 1 6.92
CHEMBL73538 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL91310 Ki = 4.7 nM 8.33
CHEMBL415300 ISOCLOZAPINE Ki = 14.0 nM 7.85
CHEMBL432762 Ki = 16.0 nM 7.80
CHEMBL42 CLOZAPINE Ki = 43.0 nM 7.37
CHEMBL90977 Ki = 68.0 nM 7.17
CHEMBL328246 Ki = 98.0 nM 7.01
CHEMBL88870 Ki = 120.0 nM 6.92
CHEMBL73538 Ki = 200.0 nM 6.70