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Assay Detail

CHEMBL615976

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

Binding
In vitro binding affinity for 5-hydroxytryptamine 1A receptor in rat hippocampal membranes by [125I]-labeled agonist displacement.
17
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Hippocampus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Isoindol-1-one analogues of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridyl)-p-iodobenzamido]ethyl]pipera zine (p-MPPI) as 5-HT1A receptor ligands.
Zhuang ZP, Kung MP, Mu M, Kung HF.
J Med Chem (1998) 41 : 157 -166
PubMed 9457239 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.93 10.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL43327 1 10.35
CHEMBL43099 2 10.16
CHEMBL29027 1 9.70
CHEMBL439740 1 9.47
CHEMBL296081 1 9.30
CHEMBL8618 NAN-190 1 9.22
CHEMBL295130 1 9.19
CHEMBL296036 1 8.96
CHEMBL296675 1 8.73
CHEMBL42993 2 8.60
CHEMBL295245 1 8.19
CHEMBL42711 1 8.05
CHEMBL290430 1 8.03
CHEMBL42780 1 7.83
CHEMBL43209 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL43327 Ki = 0.045 nM 10.35
CHEMBL43099 Ki = 0.069 nM 10.16
CHEMBL43099 Ki = 0.069 nM 10.16
CHEMBL29027 Ki = 0.2 nM 9.70
CHEMBL439740 Ki = 0.34 nM 9.47
CHEMBL296081 Ki = 0.5 nM 9.30
CHEMBL8618 NAN-190 Ki = 0.6 nM 9.22
CHEMBL295130 Ki = 0.65 nM 9.19
CHEMBL296036 Ki = 1.09 nM 8.96
CHEMBL296675 Ki = 1.85 nM 8.73
CHEMBL42993 Ki = 2.54 nM 8.60
CHEMBL42993 Ki = 2.54 nM 8.60
CHEMBL295245 Ki = 6.5 nM 8.19
CHEMBL42711 Ki = 8.9 nM 8.05
CHEMBL290430 Ki = 9.3 nM 8.03
CHEMBL42780 Ki = 14.9 nM 7.83
CHEMBL43209 Ki = 51.7 nM 7.29