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Assay Detail

CHEMBL992750

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

Binding
Binding affinity to human cloned 5HT2A receptor
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
Ablordeppey SY, Altundas R, Bricker B, Zhu XY, Kumar EV, Jackson T, Khan A, Roth BL.
Bioorg Med Chem (2008) 16 : 7291 -7301
PubMed 18595716 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.61 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 1 9.54
CHEMBL708 ZIPRASIDONE 4.0 1 9.41
CHEMBL715 OLANZAPINE 4.0 1 8.48
CHEMBL42 CLOZAPINE 4.0 1 8.05
CHEMBL478617 1 7.91
CHEMBL140872 1 7.66
CHEMBL476108 1 7.63
CHEMBL210578 1 7.51
CHEMBL150161 2 7.12
CHEMBL340816 1 6.97
CHEMBL476935 1 6.96
CHEMBL54 HALOPERIDOL 4.0 1 6.92
CHEMBL476109 1 6.71
CHEMBL716 QUETIAPINE 4.0 1 6.66
CHEMBL476934 1 -
CHEMBL476933 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 0.29 nM 9.54
CHEMBL708 ZIPRASIDONE Ki = 0.39 nM 9.41
CHEMBL715 OLANZAPINE Ki = 3.3 nM 8.48
CHEMBL42 CLOZAPINE Ki = 8.9 nM 8.05
CHEMBL478617 Ki = 12.3 nM 7.91
CHEMBL140872 Ki = 22.0 nM 7.66
CHEMBL476108 Ki = 23.6 nM 7.63
CHEMBL210578 Ki = 30.9 nM 7.51
CHEMBL150161 Ki = 75.8 nM 7.12
CHEMBL340816 Ki = 106.0 nM 6.97
CHEMBL476935 Ki = 109.6 nM 6.96
CHEMBL54 HALOPERIDOL Ki = 120.0 nM 6.92
CHEMBL476109 Ki = 194.8 nM 6.71
CHEMBL716 QUETIAPINE Ki = 220.0 nM 6.66
CHEMBL150161 Ki = 241.5 nM 6.62
CHEMBL476933 Ki - -
CHEMBL476934 Ki - -