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Assay Detail

CHEMBL616082

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

Binding
Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [125I]trans-8-OH-PIPAT in membrane homogenates of hippocampal tissue of rat brain
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

Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand.
Zhuang ZP, Kung MP, Kung HF.
J Med Chem (1993) 36 : 3161 -3165
PubMed 8230102 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.60 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284716 1 9.52
CHEMBL25554 1 8.57
CHEMBL39 SEROTONIN 3.0 1 8.37
CHEMBL110239 1 8.29
CHEMBL285755 1 7.14
CHEMBL27 PROPRANOLOL 4.0 1 6.95
CHEMBL267930 SPIPERONE 2.0 1 6.22
CHEMBL51 KETANSERIN 3.0 1 5.74
CHEMBL59 DOPAMINE 4.0 1 -
CHEMBL517712 ATROPINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284716 Ki = 0.3 nM 9.52
CHEMBL25554 Ki = 2.68 nM 8.57
CHEMBL39 SEROTONIN Ki = 4.31 nM 8.37
CHEMBL110239 Ki = 5.1 nM 8.29
CHEMBL285755 Ki = 72.7 nM 7.14
CHEMBL27 PROPRANOLOL Ki = 113.0 nM 6.95
CHEMBL267930 SPIPERONE Ki = 602.0 nM 6.22
CHEMBL51 KETANSERIN Ki = 1817.0 nM 5.74
CHEMBL59 DOPAMINE Ki > 10000.0 nM -
CHEMBL517712 ATROPINE Ki > 20000.0 nM -