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Assay Detail

CHEMBL617916

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

Binding
In vitro binding affinity at serotonin 5-hydroxytryptamine 2A receptor in rat cortical membrane
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.
Liégeois JF, Eyrolles L, Ellenbroek BA, Lejeune C, Carato P, Bruhwyler J, Géczy J, Damas J, Delarge J.
J Med Chem (2002) 45 : 5136 -5149
PubMed 12408724 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.43 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 8.17
CHEMBL63576 1 7.46
CHEMBL63329 1 7.43
CHEMBL54 HALOPERIDOL 4.0 1 7.31
CHEMBL148042 1 6.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE Ki = 6.7 nM 8.17
CHEMBL63576 Ki = 35.0 nM 7.46
CHEMBL63329 Ki = 37.0 nM 7.43
CHEMBL54 HALOPERIDOL Ki = 49.0 nM 7.31
CHEMBL148042 Ki = 164.0 nM 6.79