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Assay Detail

CHEMBL1049083

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

Binding
Displacement of [3H]5-HT from human cloned 5HT2C receptor expressed in CHO cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
Bernotas RC, Lenicek S, Antane S, Cole DC, Harrison BL, Robichaud AJ, Zhang GM, Smith D, Platt B, Lin Q, Li P, Coupet J, Rosenzweig-Lipson S, Beyer CE, Schechter LE.
Bioorg Med Chem (2009) 17 : 5153 -5163
PubMed 19523834 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.46 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL565745 1 7.36
CHEMBL584046 1 6.32
CHEMBL571858 1 6.19
CHEMBL565552 1 5.95
CHEMBL576315 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL565745 IC50 = 44.0 nM 7.36
CHEMBL584046 IC50 = 477.0 nM 6.32
CHEMBL571858 IC50 = 644.0 nM 6.19
CHEMBL565552 IC50 = 1135.0 nM 5.95
CHEMBL576315 IC50 > 5000.0 nM -