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Assay Detail

CHEMBL893105

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Functional
Agonist activity at 5HT2C receptor expressed in rat SR3T3 cells assessed as intracellular calcium mobilization relative to 5HT
8
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type SR3T3
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity.
Feng Z, Mohapatra S, Klimko PG, Hellberg MR, May JA, Kelly C, Williams G, McLaughlin MA, Sharif NA.
Bioorg Med Chem Lett (2007) 17 : 2998 -3002
PubMed 17419053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.50 8.35
Emax 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL232995 1 8.35
CHEMBL397321 1 8.07
CHEMBL234464 1 7.90
CHEMBL134519 2 7.52
CHEMBL391196 1 7.41
CHEMBL234682 1 7.09
CHEMBL234837 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL232995 EC50 = 4.5 nM 8.35
CHEMBL397321 EC50 = 8.6 nM 8.07
CHEMBL234464 EC50 = 12.6 nM 7.90
CHEMBL134519 EC50 = 30.2 nM 7.52
CHEMBL391196 EC50 = 39.0 nM 7.41
CHEMBL234682 EC50 = 82.0 nM 7.09
CHEMBL234837 EC50 = 689.0 nM 6.16
CHEMBL134519 Emax = 84.0 % -