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Assay Detail

CHEMBL893102

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

Binding
Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
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
IC50 18 8.65 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL394325 1 9.96
CHEMBL234464 1 9.55
CHEMBL232995 1 9.54
CHEMBL101008 1 9.52
CHEMBL393077 1 9.51
CHEMBL234682 1 9.42
CHEMBL134519 1 9.34
CHEMBL391196 1 9.15
CHEMBL394508 1 9.07
CHEMBL397321 1 9.06
CHEMBL232594 1 9.00
CHEMBL394664 1 9.00
CHEMBL234837 1 8.80
CHEMBL234683 1 8.59
CHEMBL232996 1 7.85
CHEMBL232997 1 6.98
CHEMBL397166 1 6.04
CHEMBL234671 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL394325 IC50 = 0.11 nM 9.96
CHEMBL234464 IC50 = 0.28 nM 9.55
CHEMBL232995 IC50 = 0.29 nM 9.54
CHEMBL101008 IC50 = 0.3 nM 9.52
CHEMBL393077 IC50 = 0.31 nM 9.51
CHEMBL234682 IC50 = 0.38 nM 9.42
CHEMBL134519 IC50 = 0.46 nM 9.34
CHEMBL391196 IC50 = 0.7 nM 9.15
CHEMBL394508 IC50 = 0.86 nM 9.07
CHEMBL397321 IC50 = 0.88 nM 9.06
CHEMBL232594 IC50 = 1.0 nM 9.00
CHEMBL394664 IC50 = 1.0 nM 9.00
CHEMBL234837 IC50 = 1.6 nM 8.80
CHEMBL234683 IC50 = 2.6 nM 8.59
CHEMBL232996 IC50 = 14.0 nM 7.85
CHEMBL232997 IC50 = 104.0 nM 6.98
CHEMBL397166 IC50 = 910.0 nM 6.04
CHEMBL234671 IC50 = 4700.0 nM 5.33