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Assay Detail

CHEMBL617853

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Binding
Binding affinity towards 5-HT 2C receptor in rat stomach fundus
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2C (CHEMBL324)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Potent, selective tetrahydro-beta-carboline antagonists of the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus.
Audia JE, Evrard DA, Murdoch GR, Droste JJ, Nissen JS, Schenck KW, Fludzinski P, Lucaites VL, Nelson DL, Cohen ML.
J Med Chem (1996) 39 : 2773 -2780
PubMed 8709108 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.13 9.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL96485 1 9.02
CHEMBL319009 1 8.69
CHEMBL1202891 1 8.68
CHEMBL96480 1 8.51
CHEMBL96782 1 8.11
CHEMBL96559 1 7.92
CHEMBL94644 1 7.73
CHEMBL95121 1 7.61
CHEMBL323330 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL96485 Ki = 0.955 nM 9.02
CHEMBL319009 Ki = 2.042 nM 8.69
CHEMBL1202891 Ki = 2.089 nM 8.68
CHEMBL96480 Ki = 3.09 nM 8.51
CHEMBL96782 Ki = 7.762 nM 8.11
CHEMBL96559 Ki = 12.02 nM 7.92
CHEMBL94644 Ki = 18.62 nM 7.73
CHEMBL95121 Ki = 24.55 nM 7.61
CHEMBL323330 Ki = 125.89 nM 6.90