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Assay Detail

CHEMBL617259

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

Binding
Binding affinity was evaluated in vitro by displacement of [3H]ketanserin from 5-hydroxytryptamine 2A receptor on rat cortical membrane
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation.
Orjales A, Mosquera R, Labeaga L, Rodes R.
J Med Chem (1997) 40 : 586 -593
PubMed 9046349 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 9.20 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267777 RITANSERIN 2.0 1 9.20
CHEMBL64489 1 -
CHEMBL60102 1 -
CHEMBL63025 1 -
CHEMBL294083 1 -
CHEMBL62778 1 -
CHEMBL59689 1 -
CHEMBL64782 1 -
CHEMBL294522 1 -
CHEMBL64801 1 -
CHEMBL56900 LERISETRON 3.0 1 -
CHEMBL62692 1 -
CHEMBL64060 1 -
CHEMBL294109 1 -
CHEMBL60103 1 -
CHEMBL64880 1 -
CHEMBL62270 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267777 RITANSERIN Ki = 0.631 nM 9.20
CHEMBL64489 Ki < 1000.0 nM -
CHEMBL60102 Ki < 1000.0 nM -
CHEMBL63025 Ki < 1000.0 nM -
CHEMBL294083 Ki < 1000.0 nM -
CHEMBL62778 Ki < 1000.0 nM -
CHEMBL59689 Ki < 1000.0 nM -
CHEMBL64782 Ki < 1000.0 nM -
CHEMBL294522 Ki < 1000.0 nM -
CHEMBL64801 Ki < 1000.0 nM -
CHEMBL56900 LERISETRON Ki < 1000.0 nM -
CHEMBL62692 Ki < 1000.0 nM -
CHEMBL64060 Ki < 1000.0 nM -
CHEMBL294109 Ki < 1000.0 nM -
CHEMBL60103 Ki < 1000.0 nM -
CHEMBL64880 Ki < 1000.0 nM -
CHEMBL62270 Ki < 1000.0 nM -