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Assay Detail

CHEMBL4013760

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ADMET
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL ↗
64
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2A (CHEMBL224) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications.
Zhang G, Cheng J, McCorvy JD, Lorello PJ, Caldarone BJ, Roth BL, Kozikowski AP.
J Med Chem (2017) 60 : 6273 -6288
PubMed 28657744 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 64 6.34 8.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 2 8.63
CHEMBL4091672 — — 2 7.62
CHEMBL4063893 — — 2 7.56
CHEMBL4101194 — — 2 7.15
CHEMBL4102683 — — 2 7.11
CHEMBL4072722 — — 2 6.86
CHEMBL4070259 — — 2 6.84
CHEMBL4103313 — — 2 6.83
CHEMBL4066538 — — 2 6.62
CHEMBL360328 LORCASERIN 4.0 2 6.61
CHEMBL4082227 — — 2 6.57
CHEMBL4098721 — — 2 6.55
CHEMBL4075150 — — 2 6.51
CHEMBL4086286 — — 2 6.40
CHEMBL4085380 — — 2 6.36
CHEMBL4064935 — — 2 6.34
CHEMBL4091197 — — 2 6.33
CHEMBL4087858 — — 2 6.18
CHEMBL4095562 — — 2 6.17
CHEMBL4064809 — — 2 6.14
CHEMBL4090984 — — 2 5.96
CHEMBL4094164 — — 2 5.89
CHEMBL4094054 — — 2 5.88
CHEMBL4101789 — — 2 5.73
CHEMBL4073406 — — 2 5.73
CHEMBL4073529 — — 2 5.65
CHEMBL4079976 — — 2 5.60
CHEMBL4083787 — — 2 5.53
CHEMBL4104218 — — 2 5.45
CHEMBL4067525 — — 2 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN EC50 = 2.344 nM 8.63
CHEMBL39 SEROTONIN EC50 = 2.35 nM 8.63
CHEMBL4091672 — EC50 = 23.99 nM 7.62
CHEMBL4091672 — EC50 = 24.0 nM 7.62
CHEMBL4063893 — EC50 = 27.54 nM 7.56
CHEMBL4063893 — EC50 = 28.0 nM 7.55
CHEMBL4101194 — EC50 = 70.79 nM 7.15
CHEMBL4101194 — EC50 = 72.0 nM 7.14
CHEMBL4102683 — EC50 = 77.0 nM 7.11
CHEMBL4102683 — EC50 = 77.62 nM 7.11
CHEMBL4072722 — EC50 = 139.0 nM 6.86
CHEMBL4072722 — EC50 = 138.04 nM 6.86
CHEMBL4070259 — EC50 = 144.54 nM 6.84
CHEMBL4070259 — EC50 = 145.0 nM 6.84
CHEMBL4103313 — EC50 = 147.91 nM 6.83
CHEMBL4103313 — EC50 = 148.0 nM 6.83
CHEMBL4066538 — EC50 = 239.88 nM 6.62
CHEMBL4066538 — EC50 = 238.0 nM 6.62
CHEMBL360328 LORCASERIN EC50 = 245.47 nM 6.61
CHEMBL360328 LORCASERIN EC50 = 248.0 nM 6.61
CHEMBL4082227 — EC50 = 269.15 nM 6.57
CHEMBL4082227 — EC50 = 271.0 nM 6.57
CHEMBL4098721 — EC50 = 284.0 nM 6.55
CHEMBL4098721 — EC50 = 281.84 nM 6.55
CHEMBL4075150 — EC50 = 307.0 nM 6.51
CHEMBL4075150 — EC50 = 309.03 nM 6.51
CHEMBL4086286 — EC50 = 398.0 nM 6.40
CHEMBL4086286 — EC50 = 398.11 nM 6.40
CHEMBL4085380 — EC50 = 436.52 nM 6.36
CHEMBL4085380 — EC50 = 438.0 nM 6.36
CHEMBL4064935 — EC50 = 457.09 nM 6.34
CHEMBL4064935 — EC50 = 460.0 nM 6.34
CHEMBL4091197 — EC50 = 467.74 nM 6.33
CHEMBL4091197 — EC50 = 463.0 nM 6.33
CHEMBL4087858 — EC50 = 655.0 nM 6.18
CHEMBL4087858 — EC50 = 660.69 nM 6.18
CHEMBL4095562 — EC50 = 674.0 nM 6.17
CHEMBL4095562 — EC50 = 676.08 nM 6.17
CHEMBL4064809 — EC50 = 724.44 nM 6.14
CHEMBL4064809 — EC50 = 721.0 nM 6.14
CHEMBL4090984 — EC50 = 1096.48 nM 5.96
CHEMBL4090984 — EC50 = 1090.0 nM 5.96
CHEMBL4094164 — EC50 = 1288.25 nM 5.89
CHEMBL4094164 — EC50 = 1290.0 nM 5.89
CHEMBL4094054 — EC50 = 1310.0 nM 5.88
CHEMBL4094054 — EC50 = 1318.26 nM 5.88
CHEMBL4073406 — EC50 = 1880.0 nM 5.73
CHEMBL4101789 — EC50 = 1880.0 nM 5.73
CHEMBL4101789 — EC50 = 1862.09 nM 5.73
CHEMBL4073406 — EC50 = 1862.09 nM 5.73