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Assay Detail

CHEMBL893103

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Functional
Agonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HT
30
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type A7R5
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
EC50 18 7.20 8.44
Emax 12 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL394325 2 8.44
CHEMBL232995 1 8.21
CHEMBL234464 1 7.92
CHEMBL101008 2 7.89
CHEMBL234682 1 7.77
CHEMBL134519 2 7.75
CHEMBL394508 2 7.58
CHEMBL391196 1 7.49
CHEMBL393077 2 7.48
CHEMBL234837 1 7.31
CHEMBL397321 1 7.15
CHEMBL234683 2 7.06
CHEMBL394664 2 6.76
CHEMBL232996 2 6.06
CHEMBL232997 2 5.30
CHEMBL397166 2 5.09
CHEMBL234671 2 -
CHEMBL232594 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL394325 EC50 = 3.6 nM 8.44
CHEMBL232995 EC50 = 6.2 nM 8.21
CHEMBL234464 EC50 = 12.0 nM 7.92
CHEMBL101008 EC50 = 13.0 nM 7.89
CHEMBL234682 EC50 = 16.9 nM 7.77
CHEMBL134519 EC50 = 17.8 nM 7.75
CHEMBL394508 EC50 = 26.0 nM 7.58
CHEMBL391196 EC50 = 32.7 nM 7.49
CHEMBL393077 EC50 = 33.0 nM 7.48
CHEMBL234837 EC50 = 49.2 nM 7.31
CHEMBL397321 EC50 = 71.0 nM 7.15
CHEMBL234683 EC50 = 87.8 nM 7.06
CHEMBL394664 EC50 = 175.0 nM 6.76
CHEMBL232996 EC50 = 880.0 nM 6.06
CHEMBL232997 EC50 = 4970.0 nM 5.30
CHEMBL397166 EC50 = 8192.0 nM 5.09
CHEMBL394664 Emax = 43.0 % -
CHEMBL101008 Emax = 47.0 % -
CHEMBL232996 Emax = 48.0 % -
CHEMBL234671 EC50 > 1000.0 nM -
CHEMBL394508 Emax = 40.0 % -
CHEMBL232997 Emax = 45.0 % -
CHEMBL234671 Emax = 15.0 % -
CHEMBL397166 Emax = 27.0 % -
CHEMBL232594 Emax = 7.0 % -
CHEMBL232594 EC50 > 10000.0 nM -
CHEMBL393077 Emax = 38.0 % -
CHEMBL394325 Emax = 72.0 % -
CHEMBL234683 Emax = 56.0 % -
CHEMBL134519 Emax = 33.0 % -