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Assay Detail

CHEMBL3773630

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Functional
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay
ChEMBL ↗
88
Total Activities
23
Compounds Tested
2
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 2B (CHEMBL1833) ↗
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 70 6.46 9.00
pEC50 18 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL350221 OXITRIPTAN 3.0 2 9.00
CHEMBL3770689 — — 4 7.60
CHEMBL3770753 — — 4 7.57
CHEMBL3769454 — — 4 7.52
CHEMBL3769543 — — 4 7.51
CHEMBL3770225 — — 4 7.00
CHEMBL3769987 — — 4 6.78
CHEMBL3770963 — — 4 6.68
CHEMBL360328 LORCASERIN 4.0 2 6.48
CHEMBL3769828 — — 4 6.34
CHEMBL3769421 — — 4 6.30
CHEMBL3771152 — — 4 6.15
CHEMBL3769704 — — 4 6.03
CHEMBL3770862 — — 4 6.02
CHEMBL3770174 — — 4 6.00
CHEMBL3769968 — — 4 5.76
CHEMBL3770599 — — 4 5.66
CHEMBL3769499 — — 4 5.48
CHEMBL3770058 — — 4 -
CHEMBL3769633 — — 4 -
CHEMBL3770950 — — 4 -
CHEMBL3770011 — — 4 -
CHEMBL3769581 — — 4 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL350221 OXITRIPTAN EC50 = 1.0 nM 9.00
CHEMBL350221 OXITRIPTAN EC50 = 1.288 nM 8.89
CHEMBL3770689 — EC50 = 25.12 nM 7.60
CHEMBL3770689 — EC50 = 25.0 nM 7.60
CHEMBL3770753 — EC50 = 27.0 nM 7.57
CHEMBL3770753 — EC50 = 27.54 nM 7.56
CHEMBL3769454 — EC50 = 30.0 nM 7.52
CHEMBL3769454 — EC50 = 30.2 nM 7.52
CHEMBL3769543 — EC50 = 31.0 nM 7.51
CHEMBL3769543 — EC50 = 30.9 nM 7.51
CHEMBL3770225 — EC50 = 101.0 nM 7.00
CHEMBL3770225 — EC50 = 102.33 nM 6.99
CHEMBL3769987 — EC50 = 165.0 nM 6.78
CHEMBL3770963 — EC50 = 209.0 nM 6.68
CHEMBL3770963 — EC50 = 208.93 nM 6.68
CHEMBL3770689 — EC50 = 331.13 nM 6.48
CHEMBL3770689 — EC50 = 329.0 nM 6.48
CHEMBL360328 LORCASERIN EC50 = 328.0 nM 6.48
CHEMBL3769987 — EC50 = 354.81 nM 6.45
CHEMBL3769987 — EC50 = 354.0 nM 6.45
CHEMBL3770753 — EC50 = 398.11 nM 6.40
CHEMBL3770753 — EC50 = 400.0 nM 6.40
CHEMBL3769828 — EC50 = 457.09 nM 6.34
CHEMBL3769828 — EC50 = 453.0 nM 6.34
CHEMBL3770963 — EC50 = 457.09 nM 6.34
CHEMBL3769987 — EC50 = 467.74 nM 6.33
CHEMBL3770963 — EC50 = 462.0 nM 6.33
CHEMBL3769421 — EC50 = 506.0 nM 6.30
CHEMBL3769421 — EC50 = 501.19 nM 6.30
CHEMBL360328 LORCASERIN EC50 = 512.86 nM 6.29
CHEMBL3769454 — EC50 = 602.56 nM 6.22
CHEMBL3769454 — EC50 = 605.0 nM 6.22
CHEMBL3771152 — EC50 = 714.0 nM 6.15
CHEMBL3771152 — EC50 = 724.44 nM 6.14
CHEMBL3769704 — EC50 = 933.25 nM 6.03
CHEMBL3769704 — EC50 = 927.0 nM 6.03
CHEMBL3770862 — EC50 = 961.0 nM 6.02
CHEMBL3770862 — EC50 = 954.99 nM 6.02
CHEMBL3770174 — EC50 = 1000.0 nM 6.00
CHEMBL3770174 — EC50 = 1001.0 nM 6.00
CHEMBL3769968 — EC50 = 1737.8 nM 5.76
CHEMBL3769968 — EC50 = 1745.0 nM 5.76
CHEMBL3770174 — EC50 = 1949.84 nM 5.71
CHEMBL3770174 — EC50 = 1957.0 nM 5.71
CHEMBL3770599 — EC50 = 2182.0 nM 5.66
CHEMBL3770599 — EC50 = 2187.76 nM 5.66
CHEMBL3769421 — EC50 = 2521.0 nM 5.60
CHEMBL3769421 — EC50 = 2511.89 nM 5.60
CHEMBL3769499 — EC50 = 3339.0 nM 5.48
CHEMBL3769499 — EC50 = 3311.31 nM 5.48