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Assay Detail

CHEMBL616680

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

Binding
Ability to bind to central serotonin 5-hydroxytryptamine 1A receptor in vitro in hippocampus of the rat brain using [3H]8-OH-DPAT radioligand
16
Total Activities
16
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

New arylpiperazine 5-HT(1A) receptor ligands containing the pyrimido[2,1-f]purine fragment: synthesis, in vitro, and in vivo pharmacological evaluation.
Jurczyk S, Kołaczkowski M, Maryniak E, Zajdel P, Pawłowski M, Tatarczyńska E, Kłodzińska A, Chojnacka-Wójcik E, Bojarski AJ, Charakchieva-Minol S, Duszyńska B, Nowak G, Maciag D.
J Med Chem (2004) 47 : 2659 -2666
PubMed 15115407 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.70 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112360 1 8.96
CHEMBL86719 1 8.68
CHEMBL91588 1 7.98
CHEMBL195047 1 7.96
CHEMBL2112363 1 7.94
CHEMBL328292 1 7.76
CHEMBL193595 1 7.72
CHEMBL2112351 1 7.64
CHEMBL91021 1 7.60
CHEMBL425567 1 7.47
CHEMBL193867 1 7.44
CHEMBL191907 1 7.34
CHEMBL195849 1 7.31
CHEMBL2112361 1 7.21
CHEMBL2112359 1 7.17
CHEMBL2112362 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112360 Ki = 1.1 nM 8.96
CHEMBL86719 Ki = 2.1 nM 8.68
CHEMBL91588 Ki = 10.4 nM 7.98
CHEMBL195047 Ki = 11.0 nM 7.96
CHEMBL2112363 Ki = 11.5 nM 7.94
CHEMBL328292 Ki = 17.2 nM 7.76
CHEMBL193595 Ki = 19.0 nM 7.72
CHEMBL2112351 Ki = 23.0 nM 7.64
CHEMBL91021 Ki = 25.0 nM 7.60
CHEMBL425567 Ki = 34.0 nM 7.47
CHEMBL193867 Ki = 36.0 nM 7.44
CHEMBL191907 Ki = 46.0 nM 7.34
CHEMBL195849 Ki = 49.0 nM 7.31
CHEMBL2112361 Ki = 62.0 nM 7.21
CHEMBL2112359 Ki = 68.0 nM 7.17
CHEMBL2112362 Ki = 87.0 nM 7.06