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Assay Detail

CHEMBL954166

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

Binding
Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
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 18 7.37 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 1 9.82
CHEMBL715 OLANZAPINE 4.0 1 8.40
CHEMBL1112 ARIPIPRAZOLE 4.0 1 8.06
CHEMBL42 CLOZAPINE 4.0 1 8.00
CHEMBL496739 1 7.82
CHEMBL461236 1 7.63
CHEMBL462508 1 7.39
CHEMBL495572 1 7.24
CHEMBL496531 1 7.08
CHEMBL522044 1 6.91
CHEMBL497988 1 6.90
CHEMBL517730 1 6.83
CHEMBL54 HALOPERIDOL 4.0 1 6.79
CHEMBL461023 1 6.79
CHEMBL495573 1 6.70
CHEMBL497574 1 6.52
CHEMBL497573 1 6.41
CHEMBL497604 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 0.15 nM 9.82
CHEMBL715 OLANZAPINE Ki = 4.0 nM 8.40
CHEMBL1112 ARIPIPRAZOLE Ki = 8.7 nM 8.06
CHEMBL42 CLOZAPINE Ki = 10.0 nM 8.00
CHEMBL496739 Ki = 15.3 nM 7.82
CHEMBL461236 Ki = 23.4 nM 7.63
CHEMBL462508 Ki = 41.0 nM 7.39
CHEMBL495572 Ki = 57.0 nM 7.24
CHEMBL496531 Ki = 83.0 nM 7.08
CHEMBL522044 Ki = 122.76 nM 6.91
CHEMBL497988 Ki = 127.0 nM 6.90
CHEMBL517730 Ki = 149.0 nM 6.83
CHEMBL54 HALOPERIDOL Ki = 164.0 nM 6.79
CHEMBL461023 Ki = 164.0 nM 6.79
CHEMBL495573 Ki = 200.0 nM 6.70
CHEMBL497574 Ki = 300.0 nM 6.52
CHEMBL497573 Ki = 389.0 nM 6.41
CHEMBL497604 Ki - -