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Assay Detail

CHEMBL617033

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

Binding
Tested in vitro for receptor binding affinity against 5-hydroxytryptamine 2 receptor using radioligand [3H]ketanserin
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2093870)
Type PROTEIN FAMILY
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 5.94 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93454 1 6.80
CHEMBL93781 1 6.67
CHEMBL91806 1 5.98
CHEMBL327198 1 5.80
CHEMBL418953 1 5.79
CHEMBL92886 1 5.75
CHEMBL26789 1 5.64
CHEMBL91689 1 5.51
CHEMBL92887 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93454 Ki = 160.0 nM 6.80
CHEMBL93781 Ki = 214.0 nM 6.67
CHEMBL91806 Ki = 1040.0 nM 5.98
CHEMBL327198 Ki = 1580.0 nM 5.80
CHEMBL418953 Ki = 1620.0 nM 5.79
CHEMBL92886 Ki = 1760.0 nM 5.75
CHEMBL26789 Ki = 2280.0 nM 5.64
CHEMBL91689 Ki = 3120.0 nM 5.51
CHEMBL92887 Ki = 3290.0 nM 5.48