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Assay Detail

CHEMBL3419957

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

Functional
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2B (CHEMBL1833)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.
Cheng J, Giguère PM, Onajole OK, Lv W, Gaisin A, Gunosewoyo H, Schmerberg CM, Pogorelov VM, Rodriguiz RM, Vistoli G, Wetsel WC, Roth BL, Kozikowski AP.
J Med Chem (2015) 58 : 1992 -2002
PubMed 25633969 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 5.79 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 1 9.04
CHEMBL3416033 1 7.07
CHEMBL3416053 1 6.38
CHEMBL360328 LORCASERIN 4.0 1 6.32
CHEMBL3416055 1 6.20
CHEMBL3416060 1 6.13
CHEMBL3416057 1 6.08
CHEMBL3416039 1 6.00
CHEMBL3416056 1 5.83
CHEMBL3416051 1 5.77
CHEMBL3416061 1 5.70
CHEMBL3416047 1 5.66
CHEMBL3416032 1 5.64
CHEMBL3416040 1 5.52
CHEMBL3416034 1 5.52
CHEMBL3416035 1 5.46
CHEMBL3416046 1 5.37
CHEMBL3416048 1 5.36
CHEMBL3416049 1 5.34
CHEMBL3416054 1 5.34
CHEMBL3416059 1 5.31
CHEMBL3416041 1 5.30
CHEMBL3416042 1 5.28
CHEMBL3416038 1 5.25
CHEMBL3416052 1 5.21
CHEMBL3416058 1 5.21
CHEMBL3416050 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN EC50 = 0.92 nM 9.04
CHEMBL3416033 EC50 = 86.0 nM 7.07
CHEMBL3416053 EC50 = 422.0 nM 6.38
CHEMBL360328 LORCASERIN EC50 = 478.0 nM 6.32
CHEMBL3416055 EC50 = 632.0 nM 6.20
CHEMBL3416060 EC50 = 735.0 nM 6.13
CHEMBL3416057 EC50 = 839.0 nM 6.08
CHEMBL3416039 EC50 = 997.0 nM 6.00
CHEMBL3416056 EC50 = 1485.0 nM 5.83
CHEMBL3416051 EC50 = 1688.0 nM 5.77
CHEMBL3416061 EC50 = 1994.0 nM 5.70
CHEMBL3416047 EC50 = 2211.0 nM 5.66
CHEMBL3416032 EC50 = 2307.0 nM 5.64
CHEMBL3416040 EC50 = 3034.0 nM 5.52
CHEMBL3416034 EC50 = 3004.0 nM 5.52
CHEMBL3416035 EC50 = 3436.0 nM 5.46
CHEMBL3416046 EC50 = 4295.0 nM 5.37
CHEMBL3416048 EC50 = 4411.0 nM 5.36
CHEMBL3416049 EC50 = 4602.0 nM 5.34
CHEMBL3416054 EC50 = 4521.0 nM 5.34
CHEMBL3416059 EC50 = 4911.0 nM 5.31
CHEMBL3416041 EC50 = 5012.0 nM 5.30
CHEMBL3416042 EC50 = 5300.0 nM 5.28
CHEMBL3416038 EC50 = 5660.0 nM 5.25
CHEMBL3416052 EC50 = 6094.0 nM 5.21
CHEMBL3416058 EC50 = 6166.0 nM 5.21
CHEMBL3416050 EC50 = 6877.0 nM 5.16