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Assay Detail

CHEMBL615917

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

Binding
In vitro binding affinity was measured on serotonergic 5-hydroxytryptamine 1A receptor by displacement of [3H]- tetralin
18
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents.
Norman MH, Rigdon GC, Navas F, Cooper BR.
J Med Chem (1994) 37 : 2552 -2563
PubMed 7914539 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 8.23 10.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL83625 2 10.68
CHEMBL290937 1 9.72
CHEMBL87294 1 9.40
CHEMBL314370 1 9.23
CHEMBL86013 1 9.19
CHEMBL314043 1 8.77
CHEMBL83454 1 8.74
CHEMBL85137 1 8.59
CHEMBL83195 1 8.47
CHEMBL315925 1 8.39
CHEMBL41626 1 8.15
CHEMBL85647 1 8.00
CHEMBL83510 1 7.48
CHEMBL314684 1 6.92
CHEMBL3144650 1 6.46
CHEMBL42 CLOZAPINE 4.0 1 5.70
CHEMBL54 HALOPERIDOL 4.0 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL83625 IC50 = 0.021 nM 10.68
CHEMBL290937 IC50 = 0.19 nM 9.72
CHEMBL87294 IC50 = 0.4 nM 9.40
CHEMBL314370 IC50 = 0.59 nM 9.23
CHEMBL86013 IC50 = 0.64 nM 9.19
CHEMBL83625 IC50 = 0.82 nM 9.09
CHEMBL314043 IC50 = 1.7 nM 8.77
CHEMBL83454 IC50 = 1.8 nM 8.74
CHEMBL85137 IC50 = 2.6 nM 8.59
CHEMBL83195 IC50 = 3.4 nM 8.47
CHEMBL315925 IC50 = 4.1 nM 8.39
CHEMBL41626 IC50 = 7.0 nM 8.15
CHEMBL85647 IC50 = 10.0 nM 8.00
CHEMBL83510 IC50 = 33.0 nM 7.48
CHEMBL314684 IC50 = 120.0 nM 6.92
CHEMBL3144650 IC50 = 350.0 nM 6.46
CHEMBL42 CLOZAPINE IC50 = 2000.0 nM 5.70
CHEMBL54 HALOPERIDOL IC50 = 7000.0 nM 5.16