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Assay Detail

CHEMBL617774

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

Binding
Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2B (CHEMBL1833)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole.
May JA, Chen HH, Rusinko A, Lynch VM, Sharif NA, McLaughlin MA.
J Med Chem (2003) 46 : 4188 -4195
PubMed 12954071 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.89 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL133455 1 8.28
CHEMBL31115 1 8.11
CHEMBL131736 1 7.96
CHEMBL133868 1 7.89
CHEMBL39 SEROTONIN 3.0 1 7.89
CHEMBL275854 1 7.89
CHEMBL27173 1 7.85
CHEMBL134519 1 7.75
CHEMBL135076 1 7.72
CHEMBL412876 1 7.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL133455 Ki = 5.3 nM 8.28
CHEMBL31115 Ki = 7.8 nM 8.11
CHEMBL131736 Ki = 11.0 nM 7.96
CHEMBL133868 Ki = 13.0 nM 7.89
CHEMBL39 SEROTONIN Ki = 13.0 nM 7.89
CHEMBL275854 Ki = 13.0 nM 7.89
CHEMBL27173 Ki = 14.0 nM 7.85
CHEMBL134519 Ki = 18.0 nM 7.75
CHEMBL135076 Ki = 19.0 nM 7.72
CHEMBL412876 Ki = 26.0 nM 7.58