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Assay Detail

CHEMBL954165

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

Binding
Displacement of [3H]8OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus by scintillation spectrometry
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Hippocampus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.
Butini S, Gemma S, Campiani G, Franceschini S, Trotta F, Borriello M, Ceres N, Ros S, Coccone SS, Bernetti M, De Angelis M, Brindisi M, Nacci V, Fiorini I, Novellino E, Cagnotto A, Mennini T, Sandager-Nielsen K, Andreasen JT, Scheel-Kruger J, Mikkelsen JD, Fattorusso C.
J Med Chem (2009) 52 : 151 -169
PubMed 19072656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.35 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL497988 1 8.40
CHEMBL462508 1 8.30
CHEMBL1112 ARIPIPRAZOLE 4.0 1 8.25
CHEMBL496531 1 8.03
CHEMBL496739 1 7.92
CHEMBL461236 1 7.83
CHEMBL495572 1 7.75
CHEMBL522044 1 7.62
CHEMBL461023 1 7.55
CHEMBL495573 1 7.48
CHEMBL517730 1 6.93
CHEMBL42 CLOZAPINE 4.0 1 6.80
CHEMBL85 RISPERIDONE 4.0 1 6.72
CHEMBL715 OLANZAPINE 4.0 1 6.21
CHEMBL497604 1 6.06
CHEMBL54 HALOPERIDOL 4.0 1 5.75
CHEMBL497574 1 -
CHEMBL497573 1 -
CHEMBL126889 1 -
CHEMBL339960 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL497988 Ki = 4.0 nM 8.40
CHEMBL462508 Ki = 5.0 nM 8.30
CHEMBL1112 ARIPIPRAZOLE Ki = 5.6 nM 8.25
CHEMBL496531 Ki = 9.3 nM 8.03
CHEMBL496739 Ki = 11.9 nM 7.92
CHEMBL461236 Ki = 14.7 nM 7.83
CHEMBL495572 Ki = 18.0 nM 7.75
CHEMBL522044 Ki = 24.2 nM 7.62
CHEMBL461023 Ki = 28.0 nM 7.55
CHEMBL495573 Ki = 33.0 nM 7.48
CHEMBL517730 Ki = 118.0 nM 6.93
CHEMBL42 CLOZAPINE Ki = 160.0 nM 6.80
CHEMBL85 RISPERIDONE Ki = 190.0 nM 6.72
CHEMBL715 OLANZAPINE Ki = 610.0 nM 6.21
CHEMBL497604 Ki = 876.0 nM 6.06
CHEMBL54 HALOPERIDOL Ki = 1800.0 nM 5.75
CHEMBL497574 Ki - -
CHEMBL497573 Ki - -
CHEMBL126889 Ki > 10000.0 nM -
CHEMBL339960 Ki > 10000.0 nM -