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Assay Detail

CHEMBL3773632

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Functional
Agonist activity at recombinant human 5HT2A 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 2A (CHEMBL224) ↗
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 72 6.65 8.87
pEC50 16 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL350221 OXITRIPTAN 3.0 2 8.87
CHEMBL3769454 — — 4 7.75
CHEMBL3769543 — — 4 7.68
CHEMBL3769987 — — 4 7.17
CHEMBL3770753 — — 4 7.09
CHEMBL3770689 — — 4 7.09
CHEMBL3770950 — — 4 7.04
CHEMBL3770225 — — 4 6.92
CHEMBL360328 LORCASERIN 4.0 2 6.78
CHEMBL3771152 — — 4 6.78
CHEMBL3769828 — — 4 6.44
CHEMBL3769581 — — 4 6.37
CHEMBL3770963 — — 4 6.36
CHEMBL3769968 — — 4 6.31
CHEMBL3769421 — — 4 6.19
CHEMBL3770862 — — 4 6.10
CHEMBL3770058 — — 4 6.03
CHEMBL3770011 — — 4 6.02
CHEMBL3769633 — — 4 5.97
CHEMBL3770599 — — 4 5.63
CHEMBL3770174 — — 4 -
CHEMBL3769704 — — 4 -
CHEMBL3769499 — — 4 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL350221 OXITRIPTAN EC50 = 1.349 nM 8.87
CHEMBL350221 OXITRIPTAN EC50 = 1.9 nM 8.72
CHEMBL3769454 — EC50 = 17.78 nM 7.75
CHEMBL3769543 — EC50 = 21.0 nM 7.68
CHEMBL3769543 — EC50 = 20.89 nM 7.68
CHEMBL3769454 — EC50 = 38.0 nM 7.42
CHEMBL3769987 — EC50 = 68.0 nM 7.17
CHEMBL3769987 — EC50 = 67.61 nM 7.17
CHEMBL3770753 — EC50 = 81.0 nM 7.09
CHEMBL3770689 — EC50 = 81.28 nM 7.09
CHEMBL3770753 — EC50 = 81.28 nM 7.09
CHEMBL3770689 — EC50 = 81.0 nM 7.09
CHEMBL3769543 — EC50 = 84.0 nM 7.08
CHEMBL3769543 — EC50 = 85.11 nM 7.07
CHEMBL3770950 — EC50 = 92.0 nM 7.04
CHEMBL3770950 — EC50 = 93.33 nM 7.03
CHEMBL3770225 — EC50 = 119.0 nM 6.92
CHEMBL3770225 — EC50 = 120.23 nM 6.92
CHEMBL3769454 — EC50 = 151.36 nM 6.82
CHEMBL3771152 — EC50 = 165.96 nM 6.78
CHEMBL3771152 — EC50 = 167.0 nM 6.78
CHEMBL360328 LORCASERIN EC50 = 165.96 nM 6.78
CHEMBL3769454 — EC50 = 203.0 nM 6.69
CHEMBL3769987 — EC50 = 212.0 nM 6.67
CHEMBL3769987 — EC50 = 213.8 nM 6.67
CHEMBL3770689 — EC50 = 234.42 nM 6.63
CHEMBL3770689 — EC50 = 235.0 nM 6.63
CHEMBL360328 LORCASERIN EC50 = 258.0 nM 6.59
CHEMBL3769828 — EC50 = 363.08 nM 6.44
CHEMBL3769828 — EC50 = 361.0 nM 6.44
CHEMBL3769581 — EC50 = 426.0 nM 6.37
CHEMBL3769581 — EC50 = 426.58 nM 6.37
CHEMBL3770963 — EC50 = 436.52 nM 6.36
CHEMBL3770963 — EC50 = 437.0 nM 6.36
CHEMBL3770963 — EC50 = 457.09 nM 6.34
CHEMBL3770963 — EC50 = 461.0 nM 6.34
CHEMBL3769968 — EC50 = 489.78 nM 6.31
CHEMBL3769968 — EC50 = 491.0 nM 6.31
CHEMBL3770753 — EC50 = 511.0 nM 6.29
CHEMBL3770753 — EC50 = 512.86 nM 6.29
CHEMBL3769421 — EC50 = 645.65 nM 6.19
CHEMBL3769421 — EC50 = 654.0 nM 6.18
CHEMBL3770225 — EC50 = 769.0 nM 6.11
CHEMBL3770225 — EC50 = 776.25 nM 6.11
CHEMBL3770862 — EC50 = 794.33 nM 6.10
CHEMBL3770862 — EC50 = 798.0 nM 6.10
CHEMBL3769968 — EC50 = 831.76 nM 6.08
CHEMBL3769968 — EC50 = 831.0 nM 6.08
CHEMBL3770058 — EC50 = 933.25 nM 6.03
CHEMBL3770058 — EC50 = 934.0 nM 6.03