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Assay Detail

CHEMBL827072

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

Binding
Inhibition of 0.4 nM [3H]ketanserin binding to Serotonin 5-HT2A receptor from rat brain cortex
12
Total Activities
12
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 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

New 5-hydroxytryptamine(1A) receptor ligands containing a norbornene nucleus: synthesis and in vitro pharmacological evaluation.
Fiorino F, Perissutti E, Severino B, Santagada V, Cirillo D, Terracciano S, Massarelli P, Bruni G, Collavoli E, Renner C, Caliendo G.
J Med Chem (2005) 48 : 5495 -5503
PubMed 16107148 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 5.80 6.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL192828 1 6.93
CHEMBL189890 1 6.26
CHEMBL191226 1 5.58
CHEMBL362999 1 5.57
CHEMBL365309 1 5.46
CHEMBL193182 1 5.41
CHEMBL364530 1 5.40
CHEMBL191574 1 -
CHEMBL192348 1 -
CHEMBL426813 1 -
CHEMBL191221 1 -
CHEMBL189384 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL192828 Ki = 118.0 nM 6.93
CHEMBL189890 Ki = 547.0 nM 6.26
CHEMBL191226 Ki = 2600.0 nM 5.58
CHEMBL362999 Ki = 2700.0 nM 5.57
CHEMBL365309 Ki = 3510.0 nM 5.46
CHEMBL193182 Ki = 3900.0 nM 5.41
CHEMBL364530 Ki = 4010.0 nM 5.40
CHEMBL191574 Ki > 100000.0 nM -
CHEMBL192348 Ki > 100000.0 nM -
CHEMBL426813 Ki > 100000.0 nM -
CHEMBL191221 Ki > 100000.0 nM -
CHEMBL189384 Ki > 100000.0 nM -