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Assay Detail

CHEMBL615913

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

Binding
In vitro binding affinity for serotonin 5-hydroxytryptamine 1A receptor fof rat cerebral cortex using [3H]8-OH-DPAT as radioligand
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and pharmacological evaluation of 1-[(1,2-diphenyl-1H-4-imidazolyl)methyl]-4-phenylpiperazines with clozapine-like mixed activities at dopamine D(2), serotonin, and GABA(A) receptors.
Asproni B, Pau A, Bitti M, Melosu M, Cerri R, Dazzi L, Seu E, Maciocco E, Sanna E, Busonero F, Talani G, Pusceddu L, Altomare C, Trapani G, Biggio G.
J Med Chem (2002) 45 : 4655 -4668
PubMed 12361392 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.41 7.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL142147 1 7.29
CHEMBL143744 1 7.25
CHEMBL358316 1 7.13
CHEMBL141824 1 6.78
CHEMBL143372 1 6.77
CHEMBL344796 1 6.71
CHEMBL342119 1 6.69
CHEMBL142825 1 6.65
CHEMBL344084 1 6.59
CHEMBL344202 1 6.57
CHEMBL42 CLOZAPINE 4.0 1 6.57
CHEMBL356993 1 6.48
CHEMBL143218 1 6.28
CHEMBL141077 1 6.09
CHEMBL356116 1 5.95
CHEMBL356068 1 5.72
CHEMBL54 HALOPERIDOL 4.0 1 5.70
CHEMBL142309 1 5.57
CHEMBL341743 1 5.07
CHEMBL344995 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL142147 IC50 = 51.9 nM 7.29
CHEMBL143744 IC50 = 56.9 nM 7.25
CHEMBL358316 IC50 = 73.9 nM 7.13
CHEMBL141824 IC50 = 165.7 nM 6.78
CHEMBL143372 IC50 = 171.2 nM 6.77
CHEMBL344796 IC50 = 197.0 nM 6.71
CHEMBL342119 IC50 = 206.0 nM 6.69
CHEMBL142825 IC50 = 224.0 nM 6.65
CHEMBL344084 IC50 = 255.0 nM 6.59
CHEMBL344202 IC50 = 270.5 nM 6.57
CHEMBL42 CLOZAPINE IC50 = 267.6 nM 6.57
CHEMBL356993 IC50 = 332.0 nM 6.48
CHEMBL143218 IC50 = 525.1 nM 6.28
CHEMBL141077 IC50 = 806.4 nM 6.09
CHEMBL356116 IC50 = 1127.0 nM 5.95
CHEMBL356068 IC50 = 1895.0 nM 5.72
CHEMBL54 HALOPERIDOL IC50 = 1993.0 nM 5.70
CHEMBL142309 IC50 = 2704.0 nM 5.57
CHEMBL341743 IC50 = 8442.0 nM 5.07
CHEMBL344995 IC50 > 10000.0 nM -