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Assay Detail

CHEMBL617472

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 in NIH3T3 cell line membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type NIH3T3
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 7 8.12 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL539057 1 8.52
CHEMBL90882 1 8.52
CHEMBL89970 1 8.40
CHEMBL556969 1 8.22
CHEMBL163863 1 8.22
CHEMBL544418 1 7.66
CHEMBL432762 1 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL539057 Ki = 3.0 nM 8.52
CHEMBL90882 Ki = 3.0 nM 8.52
CHEMBL89970 Ki = 4.0 nM 8.40
CHEMBL556969 Ki = 6.0 nM 8.22
CHEMBL163863 Ki = 6.0 nM 8.22
CHEMBL544418 Ki = 22.0 nM 7.66
CHEMBL432762 Ki = 47.0 nM 7.33