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Assay Detail

CHEMBL617459

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

Binding
Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor from rat brain
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
Liao Y, DeBoer P, Meier E, Wikström H.
J Med Chem (1997) 40 : 4146 -4153
PubMed 9406603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.37 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 8.11
CHEMBL72292 1 8.10
CHEMBL415300 ISOCLOZAPINE 1 7.92
CHEMBL72794 1 7.92
CHEMBL308090 1 7.46
CHEMBL54 HALOPERIDOL 4.0 1 7.26
CHEMBL73074 1 6.80
CHEMBL70377 1 6.51
CHEMBL310712 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE IC50 = 7.8 nM 8.11
CHEMBL72292 IC50 = 8.0 nM 8.10
CHEMBL415300 ISOCLOZAPINE IC50 = 12.0 nM 7.92
CHEMBL72794 IC50 = 12.0 nM 7.92
CHEMBL308090 IC50 = 35.0 nM 7.46
CHEMBL54 HALOPERIDOL IC50 = 55.0 nM 7.26
CHEMBL73074 IC50 = 160.0 nM 6.80
CHEMBL70377 IC50 = 310.0 nM 6.51
CHEMBL310712 IC50 = 550.0 nM 6.26