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Assay Detail

CHEMBL616274

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

Binding
In vitro inhibitory concentration required against [3H]8-OH-DPAT binding to cloned human 5-hydroxytryptamine 1A receptor
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 1A (CHEMBL214)
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
IC50 10 6.33 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 1 8.92
CHEMBL275854 1 7.71
CHEMBL31115 1 7.06
CHEMBL27173 1 6.54
CHEMBL412876 1 6.25
CHEMBL134519 1 5.42
CHEMBL25800 1 5.08
CHEMBL135076 1 5.06
CHEMBL131736 1 4.91
CHEMBL133455 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN IC50 = 1.2 nM 8.92
CHEMBL275854 IC50 = 19.6 nM 7.71
CHEMBL31115 IC50 = 86.4 nM 7.06
CHEMBL27173 IC50 = 287.0 nM 6.54
CHEMBL412876 IC50 = 562.0 nM 6.25
CHEMBL134519 IC50 = 3843.0 nM 5.42
CHEMBL25800 IC50 = 8410.0 nM 5.08
CHEMBL135076 IC50 = 8650.0 nM 5.06
CHEMBL131736 IC50 = 12200.0 nM 4.91
CHEMBL133455 IC50 > 10000.0 nM -