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Assay Detail

CHEMBL616061

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

Binding
Binding affinity towards 5-hydroxytryptamine 1A receptor in the rat brain (hippocampus) using [3H]8-OH-DPAT
10
Total Activities
10
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 Expert

Target

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

Publication

8-[4-[2-(1,2,3,4-Tetrahydroisoquinolinyl]butyl-8-azaspiro[4.5]decane-7,9-dione: a new 5-HT1A receptor ligand with the same activity profile as buspirone.
Mokrosz JL, Dereń-Wesołek A, Tatarczyńska E, Duszyńska B, Bojarski AJ, Mokrosz MJ, Chojnacka-Wójcik E.
J Med Chem (1996) 39 : 1125 -1129
PubMed 8676348 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.15 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8618 NAN-190 1 9.22
CHEMBL14161 1 8.30
CHEMBL279841 1 8.19
CHEMBL13647 BMY-7378 1 8.09
CHEMBL49 BUSPIRONE 4.0 1 7.91
CHEMBL273241 1 6.85
CHEMBL14209 1 5.88
CHEMBL14308 1 5.54
CHEMBL14149 1 4.38
CHEMBL14346 1,2,3,4-TETRAHYDROISOQUINOLINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8618 NAN-190 Ki = 0.6 nM 9.22
CHEMBL14161 Ki = 5.0 nM 8.30
CHEMBL279841 Ki = 6.4 nM 8.19
CHEMBL13647 BMY-7378 Ki = 8.2 nM 8.09
CHEMBL49 BUSPIRONE Ki = 12.3 nM 7.91
CHEMBL273241 Ki = 140.0 nM 6.85
CHEMBL14209 Ki = 1330.0 nM 5.88
CHEMBL14308 Ki = 2920.0 nM 5.54
CHEMBL14149 Ki = 41300.0 nM 4.38
CHEMBL14346 1,2,3,4-TETRAHYDROISOQUINOLINE Ki > 50000.0 nM -