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Assay Detail

CHEMBL1176239

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

Binding
Displacement of [3H]8OH-DPAT from 5HT1A receptor in rat CRL:CD(SD)BR-COBS hippocampus by scintillation spectrometry
17
Total Activities
17
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 bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors.
Butini S, Campiani G, Franceschini S, Trotta F, Kumar V, Guarino E, Borrelli G, Fiorini I, Novellino E, Fattorusso C, Persico M, Orteca N, Sandager-Nielsen K, Jacobsen TA, Madsen K, Scheel-Kruger J, Gemma S.
J Med Chem (2010) 53 : 4803 -4807
PubMed 20481570 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.81 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1173143 1 9.00
CHEMBL1173018 1 8.70
CHEMBL1172205 1 8.52
CHEMBL1112 ARIPIPRAZOLE 4.0 1 8.25
CHEMBL1172206 1 8.10
CHEMBL1171824 1 8.10
CHEMBL1173077 1 7.96
CHEMBL496739 1 7.92
CHEMBL1171823 1 7.80
CHEMBL1171644 1 7.80
CHEMBL1172734 1 7.72
CHEMBL1171646 1 7.52
CHEMBL1172204 1 7.32
CHEMBL1173017 1 7.31
CHEMBL42 CLOZAPINE 4.0 1 6.80
CHEMBL715 OLANZAPINE 4.0 1 6.21
CHEMBL1173142 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1173143 Ki = 1.0 nM 9.00
CHEMBL1173018 Ki = 2.0 nM 8.70
CHEMBL1172205 Ki = 3.0 nM 8.52
CHEMBL1112 ARIPIPRAZOLE Ki = 5.6 nM 8.25
CHEMBL1172206 Ki = 8.0 nM 8.10
CHEMBL1171824 Ki = 8.0 nM 8.10
CHEMBL1173077 Ki = 11.0 nM 7.96
CHEMBL496739 Ki = 11.9 nM 7.92
CHEMBL1171823 Ki = 16.0 nM 7.80
CHEMBL1171644 Ki = 16.0 nM 7.80
CHEMBL1172734 Ki = 19.0 nM 7.72
CHEMBL1171646 Ki = 30.0 nM 7.52
CHEMBL1172204 Ki = 48.0 nM 7.32
CHEMBL1173017 Ki = 49.0 nM 7.31
CHEMBL42 CLOZAPINE Ki = 160.0 nM 6.80
CHEMBL715 OLANZAPINE Ki = 610.0 nM 6.21
CHEMBL1173142 Ki - -