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Assay Detail

CHEMBL875910

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Binding
Binding affinity for 5-HT 2A in rat stomach fundus
11
Total Activities
11
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 2A (CHEMBL322)
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 11 7.81 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL96485 1 8.57
CHEMBL319009 1 8.53
CHEMBL1202891 1 8.45
CHEMBL96480 1 8.33
CHEMBL96782 1 8.06
CHEMBL94644 1 7.78
CHEMBL95121 1 7.71
CHEMBL96559 1 7.65
CHEMBL323330 1 7.18
CHEMBL15245 YOHIMBINE 3.0 1 5.79
CHEMBL85194 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL96485 Ki = 2.692 nM 8.57
CHEMBL319009 Ki = 2.951 nM 8.53
CHEMBL1202891 Ki = 3.548 nM 8.45
CHEMBL96480 Ki = 4.677 nM 8.33
CHEMBL96782 Ki = 8.71 nM 8.06
CHEMBL94644 Ki = 16.6 nM 7.78
CHEMBL95121 Ki = 19.5 nM 7.71
CHEMBL96559 Ki = 22.39 nM 7.65
CHEMBL323330 Ki = 66.07 nM 7.18
CHEMBL15245 YOHIMBINE Ki = 1621.81 nM 5.79
CHEMBL85194 Ki > 6309.57 nM -