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Assay Detail

CHEMBL617473

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

Binding
Ability to inhibit the binding of iodine-125-labelled lysergic acid diethylamide([125I]-LSD) to the S-2A serotonin receptor.
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 Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 8 7.67 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 1 9.80
CHEMBL542029 1 8.35
CHEMBL554670 1 8.22
CHEMBL42 CLOZAPINE 4.0 1 8.10
CHEMBL555362 1 7.70
CHEMBL544184 1 7.14
CHEMBL163239 1 6.12
CHEMBL94067 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 0.16 nM 9.80
CHEMBL542029 Ki = 4.5 nM 8.35
CHEMBL554670 Ki = 6.0 nM 8.22
CHEMBL42 CLOZAPINE Ki = 8.0 nM 8.10
CHEMBL555362 Ki = 20.0 nM 7.70
CHEMBL544184 Ki = 72.0 nM 7.14
CHEMBL163239 Ki = 760.0 nM 6.12
CHEMBL94067 Ki = 1200.0 nM 5.92