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Assay Detail

CHEMBL617107

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

Binding
Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type NIH3T3
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Enantiospecific synthesis and pharmacological evaluation of a series of super-potent, conformationally restricted 5-HT(2A/2C) receptor agonists.
Chambers JJ, Kurrasch-Orbaugh DM, Parker MA, Nichols DE.
J Med Chem (2001) 44 : 1003 -1010
PubMed 11300881 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 7.20 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6706 1 8.57
CHEMBL7132 1 8.42
CHEMBL6710 1 8.08
CHEMBL6907 1 7.92
CHEMBL263083 1 7.72
CHEMBL6452 1 7.55
CHEMBL268542 1 7.52
CHEMBL263078 1 7.46
CHEMBL6620 1 7.17
CHEMBL6607 BROLAMFETAMINE 2.0 1 7.14
CHEMBL6871 1 6.23
CHEMBL6838 1 6.19
CHEMBL268587 1 5.63
CHEMBL268072 1 5.25
CHEMBL6737 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6706 EC50 = 2.7 nM 8.57
CHEMBL7132 EC50 = 3.8 nM 8.42
CHEMBL6710 EC50 = 8.38 nM 8.08
CHEMBL6907 EC50 = 12.0 nM 7.92
CHEMBL263083 EC50 = 19.0 nM 7.72
CHEMBL6452 EC50 = 28.0 nM 7.55
CHEMBL268542 EC50 = 30.0 nM 7.52
CHEMBL263078 EC50 = 35.0 nM 7.46
CHEMBL6620 EC50 = 68.4 nM 7.17
CHEMBL6607 BROLAMFETAMINE EC50 = 72.0 nM 7.14
CHEMBL6871 EC50 = 590.0 nM 6.23
CHEMBL6838 EC50 = 650.0 nM 6.19
CHEMBL268587 EC50 = 2360.0 nM 5.63
CHEMBL268072 EC50 = 5650.0 nM 5.25
CHEMBL6737 EC50 > 10000.0 nM -