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Assay Detail

CHEMBL3773628

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Functional
Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL ↗
88
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.
Cheng J, Giguere PM, Schmerberg CM, Pogorelov VM, Rodriguiz RM, Huang XP, Zhu H, McCorvy JD, Wetsel WC, Roth BL, Kozikowski AP.
J Med Chem (2016) 59 : 578 -591
PubMed 26704965 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 88 7.42 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL350221 OXITRIPTAN 3.0 2 9.74
CHEMBL3769454 — — 4 9.02
CHEMBL360328 LORCASERIN 4.0 2 8.74
CHEMBL3770753 — — 4 8.50
CHEMBL3770225 — — 4 8.50
CHEMBL3769987 — — 4 8.42
CHEMBL3769828 — — 4 8.14
CHEMBL3770689 — — 4 8.12
CHEMBL3769968 — — 4 8.06
CHEMBL3770963 — — 4 8.02
CHEMBL3769543 — — 4 8.01
CHEMBL3770950 — — 4 7.75
CHEMBL3769421 — — 4 7.62
CHEMBL3770599 — — 4 7.60
CHEMBL3769499 — — 4 7.44
CHEMBL3770174 — — 4 7.38
CHEMBL3770862 — — 4 7.31
CHEMBL3771152 — — 4 7.21
CHEMBL3770058 — — 4 7.15
CHEMBL3769704 — — 4 7.02
CHEMBL3769581 — — 4 6.97
CHEMBL3769633 — — 4 6.94
CHEMBL3770011 — — 4 6.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL350221 OXITRIPTAN EC50 = 0.18 nM 9.74
CHEMBL350221 OXITRIPTAN EC50 = 0.2188 nM 9.66
CHEMBL3769454 — EC50 = 0.95 nM 9.02
CHEMBL3769454 — EC50 = 1.096 nM 8.96
CHEMBL360328 LORCASERIN EC50 = 1.82 nM 8.74
CHEMBL360328 LORCASERIN EC50 = 2.7 nM 8.57
CHEMBL3770225 — EC50 = 3.162 nM 8.50
CHEMBL3770753 — EC50 = 3.162 nM 8.50
CHEMBL3770225 — EC50 = 3.2 nM 8.49
CHEMBL3770753 — EC50 = 3.4 nM 8.47
CHEMBL3769987 — EC50 = 3.802 nM 8.42
CHEMBL3769987 — EC50 = 3.8 nM 8.42
CHEMBL3769828 — EC50 = 7.244 nM 8.14
CHEMBL3769828 — EC50 = 7.3 nM 8.14
CHEMBL3770689 — EC50 = 7.6 nM 8.12
CHEMBL3770689 — EC50 = 7.762 nM 8.11
CHEMBL3769968 — EC50 = 8.7 nM 8.06
CHEMBL3769968 — EC50 = 8.71 nM 8.06
CHEMBL3770963 — EC50 = 9.55 nM 8.02
CHEMBL3770963 — EC50 = 9.5 nM 8.02
CHEMBL3769543 — EC50 = 9.772 nM 8.01
CHEMBL3769543 — EC50 = 9.7 nM 8.01
CHEMBL3769987 — EC50 = 13.0 nM 7.89
CHEMBL3769987 — EC50 = 13.18 nM 7.88
CHEMBL3769543 — EC50 = 13.49 nM 7.87
CHEMBL3769543 — EC50 = 14.0 nM 7.85
CHEMBL3770963 — EC50 = 15.49 nM 7.81
CHEMBL3770963 — EC50 = 16.0 nM 7.80
CHEMBL3770689 — EC50 = 16.0 nM 7.80
CHEMBL3770689 — EC50 = 16.22 nM 7.79
CHEMBL3769454 — EC50 = 16.6 nM 7.78
CHEMBL3770950 — EC50 = 18.0 nM 7.75
CHEMBL3770950 — EC50 = 18.2 nM 7.74
CHEMBL3769454 — EC50 = 21.0 nM 7.68
CHEMBL3769421 — EC50 = 24.0 nM 7.62
CHEMBL3770225 — EC50 = 23.99 nM 7.62
CHEMBL3769421 — EC50 = 23.99 nM 7.62
CHEMBL3770225 — EC50 = 24.0 nM 7.62
CHEMBL3770599 — EC50 = 25.12 nM 7.60
CHEMBL3770599 — EC50 = 25.0 nM 7.60
CHEMBL3770753 — EC50 = 30.0 nM 7.52
CHEMBL3770753 — EC50 = 31.62 nM 7.50
CHEMBL3769499 — EC50 = 36.0 nM 7.44
CHEMBL3769499 — EC50 = 36.31 nM 7.44
CHEMBL3770174 — EC50 = 41.69 nM 7.38
CHEMBL3770174 — EC50 = 42.0 nM 7.38
CHEMBL3770862 — EC50 = 49.0 nM 7.31
CHEMBL3770862 — EC50 = 48.98 nM 7.31
CHEMBL3771152 — EC50 = 61.66 nM 7.21
CHEMBL3771152 — EC50 = 61.0 nM 7.21