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Assay Detail

CHEMBL617461

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

Binding
Binding affinity for 5-hydroxytryptamine 2A receptor, activity is expressed as IC50 values.
33
Total Activities
22
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 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity.
Bøgesø KP, Arnt J, Frederiksen K, Hansen HO, Hyttel J, Pedersen H.
J Med Chem (1995) 38 : 4380 -4392
PubMed 7473566 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 7.97 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL343282 3 9.00
CHEMBL136630 2 8.96
CHEMBL140032 1 8.82
CHEMBL136226 1 8.77
CHEMBL136235 3 8.72
CHEMBL136722 3 8.54
CHEMBL136776 1 8.52
CHEMBL136683 3 8.49
CHEMBL137960 3 8.49
CHEMBL140189 1 8.47
CHEMBL343078 1 8.35
CHEMBL136648 1 8.12
CHEMBL42 CLOZAPINE 4.0 1 8.11
CHEMBL136891 1 8.03
CHEMBL137536 1 8.01
CHEMBL136190 1 7.85
CHEMBL136468 1 7.68
CHEMBL344680 1 7.68
CHEMBL136873 1 7.58
CHEMBL138964 1 7.54
CHEMBL136334 1 7.51
CHEMBL139258 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL343282 IC50 = 1.0 nM 9.00
CHEMBL136630 IC50 = 1.1 nM 8.96
CHEMBL140032 IC50 = 1.5 nM 8.82
CHEMBL136226 IC50 = 1.7 nM 8.77
CHEMBL136235 IC50 = 1.9 nM 8.72
CHEMBL343282 IC50 = 1.9 nM 8.72
CHEMBL136630 IC50 = 2.1 nM 8.68
CHEMBL136722 IC50 = 2.9 nM 8.54
CHEMBL136776 IC50 = 3.0 nM 8.52
CHEMBL137960 IC50 = 3.2 nM 8.49
CHEMBL136683 IC50 = 3.2 nM 8.49
CHEMBL140189 IC50 = 3.4 nM 8.47
CHEMBL136235 IC50 = 3.6 nM 8.44
CHEMBL136683 IC50 = 3.7 nM 8.43
CHEMBL137960 IC50 = 4.4 nM 8.36
CHEMBL343078 IC50 = 4.5 nM 8.35
CHEMBL136722 IC50 = 5.1 nM 8.29
CHEMBL136648 IC50 = 7.5 nM 8.12
CHEMBL42 CLOZAPINE IC50 = 7.8 nM 8.11
CHEMBL136891 IC50 = 9.3 nM 8.03
CHEMBL137536 IC50 = 9.8 nM 8.01
CHEMBL136190 IC50 = 14.0 nM 7.85
CHEMBL136468 IC50 = 21.0 nM 7.68
CHEMBL344680 IC50 = 21.0 nM 7.68
CHEMBL136873 IC50 = 26.0 nM 7.58
CHEMBL138964 IC50 = 29.0 nM 7.54
CHEMBL136334 IC50 = 31.0 nM 7.51
CHEMBL139258 IC50 = 32.0 nM 7.50
CHEMBL137960 IC50 = 68.0 nM 7.17
CHEMBL136235 IC50 = 360.0 nM 6.44
CHEMBL136722 IC50 = 650.0 nM 6.19
CHEMBL343282 IC50 = 1100.0 nM 5.96
CHEMBL136683 IC50 = 3600.0 nM 5.44