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Assay Detail

CHEMBL957592

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

Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
72
Total Activities
72
Compounds Tested
2
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

Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action.
Cho SJ, Jensen NH, Kurome T, Kadari S, Manzano ML, Malberg JE, Caldarone B, Roth BL, Kozikowski AP.
J Med Chem (2009) 52 : 1885 -1902
PubMed 19284718 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 50 7.12 9.30
Activity 22 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 1 9.30
CHEMBL492926 1 8.44
CHEMBL492916 1 8.32
CHEMBL474633 1 8.31
CHEMBL510383 1 8.26
CHEMBL474634 1 8.15
CHEMBL475642 1 8.08
CHEMBL475643 1 7.92
CHEMBL467736 1 7.89
CHEMBL464475 1 7.85
CHEMBL493130 1 7.68
CHEMBL451232 1 7.66
CHEMBL492306 1 7.55
CHEMBL443128 1 7.50
CHEMBL452719 1 7.43
CHEMBL471202 1 7.43
CHEMBL450599 1 7.28
CHEMBL493128 1 7.23
CHEMBL445747 1 7.19
CHEMBL510308 1 7.16
CHEMBL493129 1 7.12
CHEMBL490064 1 7.11
CHEMBL452458 1 7.08
CHEMBL500093 1 7.07
CHEMBL475641 1 6.94
CHEMBL508680 1 6.94
CHEMBL506727 1 6.85
CHEMBL450178 1 6.73
CHEMBL451368 1 6.70
CHEMBL474230 1 6.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN EC50 = 0.5 nM 9.30
CHEMBL492926 EC50 = 3.6 nM 8.44
CHEMBL492916 EC50 = 4.8 nM 8.32
CHEMBL474633 EC50 = 4.9 nM 8.31
CHEMBL510383 EC50 = 5.5 nM 8.26
CHEMBL474634 EC50 = 7.0 nM 8.15
CHEMBL475642 EC50 = 8.4 nM 8.08
CHEMBL475643 EC50 = 12.0 nM 7.92
CHEMBL467736 EC50 = 13.0 nM 7.89
CHEMBL464475 EC50 = 14.0 nM 7.85
CHEMBL493130 EC50 = 21.0 nM 7.68
CHEMBL451232 EC50 = 22.0 nM 7.66
CHEMBL492306 EC50 = 28.0 nM 7.55
CHEMBL443128 EC50 = 32.0 nM 7.50
CHEMBL471202 EC50 = 37.0 nM 7.43
CHEMBL452719 EC50 = 37.0 nM 7.43
CHEMBL450599 EC50 = 53.0 nM 7.28
CHEMBL493128 EC50 = 59.0 nM 7.23
CHEMBL445747 EC50 = 65.0 nM 7.19
CHEMBL510308 EC50 = 69.0 nM 7.16
CHEMBL493129 EC50 = 75.0 nM 7.12
CHEMBL490064 EC50 = 77.0 nM 7.11
CHEMBL452458 EC50 = 83.0 nM 7.08
CHEMBL500093 EC50 = 85.0 nM 7.07
CHEMBL508680 EC50 = 116.0 nM 6.94
CHEMBL475641 EC50 = 116.0 nM 6.94
CHEMBL506727 EC50 = 141.0 nM 6.85
CHEMBL450178 EC50 = 185.0 nM 6.73
CHEMBL451368 EC50 = 199.0 nM 6.70
CHEMBL474230 EC50 = 204.0 nM 6.69
CHEMBL360328 LORCASERIN EC50 = 219.0 nM 6.66
CHEMBL509418 EC50 = 224.0 nM 6.65
CHEMBL492917 EC50 = 350.0 nM 6.46
CHEMBL492305 EC50 = 366.0 nM 6.44
CHEMBL469729 EC50 = 404.0 nM 6.39
CHEMBL471802 EC50 = 415.0 nM 6.38
CHEMBL501526 EC50 = 459.0 nM 6.34
CHEMBL501117 EC50 = 492.0 nM 6.31
CHEMBL474885 EC50 = 510.0 nM 6.29
CHEMBL472678 EC50 = 1739.0 nM 5.76
CHEMBL501854 EC50 = 2737.0 nM 5.56
CHEMBL449134 EC50 = 3092.0 nM 5.51
CHEMBL498863 EC50 = 3342.0 nM 5.48
CHEMBL474950 Activity - -
CHEMBL492698 Activity - -
CHEMBL474232 Activity - -
CHEMBL474231 Activity - -
CHEMBL474229 Activity - -
CHEMBL469808 Activity - -
CHEMBL475383 Activity - -