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Assay Detail

CHEMBL616574

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Binding
Tested in vitro for receptor binding affinity against 5-hydroxytryptamine 1A receptor using radioligand [3H]8-OH-DPAT
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Structure-activity relationship studies of central nervous system agents. 13. 4-[3-(Benzotriazol-1-yl)propyl]-1-(2-methoxyphenyl)piperazine, a new putative 5-HT1A receptor antagonist, and its analogs.
Mokrosz JL, Paluchowska MH, Chojnacka-Wójcik E, Filip M, Charakchieva-Minol S, Dereń-Wesołek A, Mokrosz MJ.
J Med Chem (1994) 37 : 2754 -2760
PubMed 8064802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.43 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93781 1 8.40
CHEMBL91806 1 7.82
CHEMBL93454 1 7.77
CHEMBL327198 1 7.62
CHEMBL92886 1 7.39
CHEMBL418953 1 7.38
CHEMBL26789 1 7.24
CHEMBL91689 1 6.69
CHEMBL92887 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93781 Ki = 4.0 nM 8.40
CHEMBL91806 Ki = 15.0 nM 7.82
CHEMBL93454 Ki = 17.0 nM 7.77
CHEMBL327198 Ki = 24.0 nM 7.62
CHEMBL92886 Ki = 41.0 nM 7.39
CHEMBL418953 Ki = 42.0 nM 7.38
CHEMBL26789 Ki = 57.0 nM 7.24
CHEMBL91689 Ki = 203.0 nM 6.69
CHEMBL92887 Ki = 249.0 nM 6.60