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Assay Detail

CHEMBL884530

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

Binding
Inhibition of [3H]ketanserin binding at 5-hydroxytryptamine 2 receptor from rat frontal cortex.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2093870)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives.
Norman MH, Minick DJ, Rigdon GC.
J Med Chem (1996) 39 : 149 -157
PubMed 8568802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 8.13 9.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38409 1 9.16
CHEMBL290953 1 9.11
CHEMBL291070 1 8.77
CHEMBL288450 1 8.77
CHEMBL41536 1 8.74
CHEMBL41636 1 8.66
CHEMBL43069 1 8.49
CHEMBL288930 1 8.40
CHEMBL41626 1 8.29
CHEMBL38747 1 8.27
CHEMBL43410 1 8.26
CHEMBL39226 1 8.22
CHEMBL290937 1 8.12
CHEMBL36423 1 8.01
CHEMBL441430 1 7.89
CHEMBL559330 1 7.75
CHEMBL42 CLOZAPINE 4.0 1 7.55
CHEMBL289275 1 7.52
CHEMBL43513 1 7.37
CHEMBL41309 1 6.92
CHEMBL54 HALOPERIDOL 4.0 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38409 IC50 = 0.69 nM 9.16
CHEMBL290953 IC50 = 0.78 nM 9.11
CHEMBL291070 IC50 = 1.7 nM 8.77
CHEMBL288450 IC50 = 1.7 nM 8.77
CHEMBL41536 IC50 = 1.8 nM 8.74
CHEMBL41636 IC50 = 2.2 nM 8.66
CHEMBL43069 IC50 = 3.2 nM 8.49
CHEMBL288930 IC50 = 4.0 nM 8.40
CHEMBL41626 IC50 = 5.1 nM 8.29
CHEMBL38747 IC50 = 5.4 nM 8.27
CHEMBL43410 IC50 = 5.5 nM 8.26
CHEMBL39226 IC50 = 6.0 nM 8.22
CHEMBL290937 IC50 = 7.6 nM 8.12
CHEMBL36423 IC50 = 9.8 nM 8.01
CHEMBL441430 IC50 = 13.0 nM 7.89
CHEMBL559330 IC50 = 18.0 nM 7.75
CHEMBL42 CLOZAPINE IC50 = 28.0 nM 7.55
CHEMBL289275 IC50 = 30.0 nM 7.52
CHEMBL43513 IC50 = 43.0 nM 7.37
CHEMBL41309 IC50 = 120.0 nM 6.92
CHEMBL54 HALOPERIDOL IC50 = 360.0 nM 6.44