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Assay Detail

CHEMBL617085

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

Binding
Binding affinity for human 5-hydroxytryptamine 2A receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Current and novel approaches to the drug treatment of schizophrenia.
Rowley M, Bristow LJ, Hutson PH.
J Med Chem (2001) 44 : 477 -501
PubMed 11170639 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 8.57 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL83894 FANANSERIN 2.0 1 10.40
CHEMBL708 ZIPRASIDONE 4.0 1 9.60
CHEMBL85 RISPERIDONE 4.0 1 9.41
CHEMBL74355 VOLINANSERIN 3.0 1 8.82
CHEMBL715 OLANZAPINE 4.0 1 8.72
CHEMBL18972 GLEMANSERIN 2.0 1 8.60
CHEMBL285802 ZOTEPINE 2.0 1 8.57
CHEMBL42 CLOZAPINE 4.0 1 8.40
CHEMBL19259 1 8.28
CHEMBL19589 1 8.02
CHEMBL716 QUETIAPINE 4.0 1 7.09
CHEMBL18904 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL83894 FANANSERIN Ki = 0.04 nM 10.40
CHEMBL708 ZIPRASIDONE Ki = 0.25 nM 9.60
CHEMBL85 RISPERIDONE Ki = 0.39 nM 9.41
CHEMBL74355 VOLINANSERIN Ki = 1.5 nM 8.82
CHEMBL715 OLANZAPINE Ki = 1.9 nM 8.72
CHEMBL18972 GLEMANSERIN Ki = 2.5 nM 8.60
CHEMBL285802 ZOTEPINE Ki = 2.7 nM 8.57
CHEMBL42 CLOZAPINE Ki = 4.0 nM 8.40
CHEMBL19259 Ki = 5.3 nM 8.28
CHEMBL19589 Ki = 9.6 nM 8.02
CHEMBL716 QUETIAPINE Ki = 82.0 nM 7.09
CHEMBL18904 Ki = 126.0 nM 6.90