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Assay Detail

CHEMBL892800

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

Binding
Displacement of [3H]8-OH-DPAT from serotonin 5HT1A receptor in rat brain hippocampus
16
Total Activities
16
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

Novel class of arylpiperazines containing N-acylated amino acids: their synthesis, 5-HT1A, 5-HT2A receptor affinity, and in vivo pharmacological evaluation.
Zajdel P, Subra G, Bojarski AJ, Duszyńska B, Tatarczyńska E, Nikiforuk A, Chojnacka-Wójcik E, Pawłowski M, Martinez J.
Bioorg Med Chem (2007) 15 : 2907 -2919
PubMed 17321139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.78 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL232246 1 8.52
CHEMBL208905 1 8.40
CHEMBL279841 1 8.19
CHEMBL209007 1 8.05
CHEMBL232449 1 7.89
CHEMBL232036 1 7.84
CHEMBL232035 1 7.72
CHEMBL378298 1 7.72
CHEMBL390037 1 7.68
CHEMBL207493 1 7.64
CHEMBL408589 1 7.58
CHEMBL398209 1 7.55
CHEMBL390659 1 7.51
CHEMBL398181 1 7.50
CHEMBL232247 1 7.43
CHEMBL231825 1 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL232246 Ki = 3.0 nM 8.52
CHEMBL208905 Ki = 4.0 nM 8.40
CHEMBL279841 Ki = 6.4 nM 8.19
CHEMBL209007 Ki = 9.0 nM 8.05
CHEMBL232449 Ki = 13.0 nM 7.89
CHEMBL232036 Ki = 14.5 nM 7.84
CHEMBL232035 Ki = 19.0 nM 7.72
CHEMBL378298 Ki = 19.0 nM 7.72
CHEMBL390037 Ki = 21.0 nM 7.68
CHEMBL207493 Ki = 23.0 nM 7.64
CHEMBL408589 Ki = 26.0 nM 7.58
CHEMBL398209 Ki = 28.0 nM 7.55
CHEMBL390659 Ki = 31.0 nM 7.51
CHEMBL398181 Ki = 32.0 nM 7.50
CHEMBL232247 Ki = 37.0 nM 7.43
CHEMBL231825 Ki = 47.0 nM 7.33