Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4681089

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

Functional
Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL ↗
88
Total Activities
44
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Flp-In-293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design and Discovery of Functionally Selective Serotonin 2C (5-HT) Receptor Agonists.
Cheng J,McCorvy JD,Giguere PM,Zhu H,Kenakin T,Roth BL,Kozikowski AP
J Med Chem (2016) 59 : 9866 -9880
PubMed 27726356 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 86 7.65 9.78
pEC50 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 2 9.78
CHEMBL4779260 — — 2 9.23
CHEMBL4751981 — — 2 8.80
CHEMBL4756903 — — 2 8.59
CHEMBL360328 LORCASERIN 4.0 2 8.58
CHEMBL4748110 — — 2 8.57
CHEMBL4790652 — — 2 8.57
CHEMBL4790992 — — 2 8.28
CHEMBL4759181 — — 2 8.21
CHEMBL4739937 — — 2 8.18
CHEMBL4761526 — — 2 8.05
CHEMBL4759878 — — 2 8.04
CHEMBL4782824 — — 2 8.00
CHEMBL4743977 — — 2 7.96
CHEMBL4761064 — — 2 7.96
CHEMBL4757214 — — 2 7.92
CHEMBL4740346 — — 2 7.84
CHEMBL4777303 — — 2 7.72
CHEMBL4752412 — — 2 7.70
CHEMBL4786831 — — 2 7.68
CHEMBL4781163 — — 2 7.65
CHEMBL4753812 — — 2 7.60
CHEMBL4800666 — — 2 7.59
CHEMBL4758641 — — 2 7.58
CHEMBL4762225 — — 2 7.50
CHEMBL4789310 — — 2 7.39
CHEMBL4762474 — — 2 7.25
CHEMBL4752976 — — 2 7.14
CHEMBL4752611 — — 2 7.09
CHEMBL4796472 — — 2 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN EC50 = 0.166 nM 9.78
CHEMBL39 SEROTONIN EC50 = 0.17 nM 9.77
CHEMBL4779260 — EC50 = 0.59 nM 9.23
CHEMBL4779260 — EC50 = 0.6026 nM 9.22
CHEMBL4751981 — EC50 = 1.6 nM 8.80
CHEMBL4751981 — EC50 = 1.622 nM 8.79
CHEMBL4756903 — EC50 = 2.6 nM 8.59
CHEMBL4756903 — EC50 = 2.57 nM 8.59
CHEMBL360328 LORCASERIN EC50 = 2.64 nM 8.58
CHEMBL360328 LORCASERIN EC50 = 2.63 nM 8.58
CHEMBL4790652 — EC50 = 2.692 nM 8.57
CHEMBL4790652 — EC50 = 2.7 nM 8.57
CHEMBL4748110 — EC50 = 2.7 nM 8.57
CHEMBL4748110 — EC50 = 2.692 nM 8.57
CHEMBL4790992 — EC50 = 5.3 nM 8.28
CHEMBL4790992 — EC50 = 5.37 nM 8.27
CHEMBL4759181 — EC50 = 6.166 nM 8.21
CHEMBL4759181 — EC50 = 6.2 nM 8.21
CHEMBL4739937 — EC50 = 6.6 nM 8.18
CHEMBL4739937 — EC50 = 6.761 nM 8.17
CHEMBL4761526 — EC50 = 8.913 nM 8.05
CHEMBL4761526 — EC50 = 8.9 nM 8.05
CHEMBL4759878 — EC50 = 9.2 nM 8.04
CHEMBL4759878 — EC50 = 9.333 nM 8.03
CHEMBL4782824 — EC50 = 10.0 nM 8.00
CHEMBL4782824 — EC50 = 10.23 nM 7.99
CHEMBL4743977 — EC50 = 11.0 nM 7.96
CHEMBL4743977 — EC50 = 10.96 nM 7.96
CHEMBL4761064 — EC50 = 11.0 nM 7.96
CHEMBL4761064 — EC50 = 10.96 nM 7.96
CHEMBL4757214 — EC50 = 12.0 nM 7.92
CHEMBL4757214 — EC50 = 12.3 nM 7.91
CHEMBL4740346 — EC50 = 14.45 nM 7.84
CHEMBL4740346 — EC50 = 15.0 nM 7.82
CHEMBL4777303 — EC50 = 19.0 nM 7.72
CHEMBL4777303 — EC50 = 19.5 nM 7.71
CHEMBL4752412 — EC50 = 20.0 nM 7.70
CHEMBL4752412 — EC50 = 20.42 nM 7.69
CHEMBL4786831 — EC50 = 21.0 nM 7.68
CHEMBL4786831 — EC50 = 21.38 nM 7.67
CHEMBL4781163 — EC50 = 22.39 nM 7.65
CHEMBL4781163 — EC50 = 23.0 nM 7.64
CHEMBL4753812 — EC50 = 25.12 nM 7.60
CHEMBL4753812 — EC50 = 25.0 nM 7.60
CHEMBL4800666 — EC50 = 25.7 nM 7.59
CHEMBL4758641 — EC50 = 26.3 nM 7.58
CHEMBL4758641 — EC50 = 26.0 nM 7.58
CHEMBL4800666 — EC50 = 26.0 nM 7.58
CHEMBL4762225 — EC50 = 31.62 nM 7.50
CHEMBL4762225 — EC50 = 33.0 nM 7.48