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Assay Detail

CHEMBL4013756

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Functional
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
ChEMBL ↗
66
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2C (CHEMBL225) ↗
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 66 6.78 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 2 9.77
CHEMBL360328 LORCASERIN 4.0 2 8.68
CHEMBL4091672 — — 2 8.62
CHEMBL4063893 — — 2 8.05
CHEMBL4098721 — — 2 7.89
CHEMBL4082227 — — 2 7.64
CHEMBL4072722 — — 2 7.63
CHEMBL4086286 — — 2 7.55
CHEMBL4083193 — — 2 7.02
CHEMBL4101194 — — 2 6.99
CHEMBL4085380 — — 2 6.92
CHEMBL4103313 — — 2 6.92
CHEMBL4070259 — — 2 6.64
CHEMBL4067525 — — 2 6.64
CHEMBL4064809 — — 2 6.61
CHEMBL4102683 — — 2 6.52
CHEMBL4095562 — — 2 6.51
CHEMBL4090984 — — 2 6.40
CHEMBL4094054 — — 2 6.39
CHEMBL4094164 — — 2 6.36
CHEMBL4101789 — — 2 6.30
CHEMBL4064935 — — 2 6.28
CHEMBL4104218 — — 2 6.28
CHEMBL4091197 — — 2 6.26
CHEMBL4075150 — — 2 6.21
CHEMBL4079976 — — 2 6.17
CHEMBL4073529 — — 2 6.11
CHEMBL4087858 — — 2 6.06
CHEMBL4078425 — — 2 5.92
CHEMBL4073406 — — 2 5.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN EC50 = 0.17 nM 9.77
CHEMBL39 SEROTONIN EC50 = 0.182 nM 9.74
CHEMBL360328 LORCASERIN EC50 = 2.1 nM 8.68
CHEMBL4091672 — EC50 = 2.399 nM 8.62
CHEMBL4091672 — EC50 = 2.4 nM 8.62
CHEMBL360328 LORCASERIN EC50 = 2.63 nM 8.58
CHEMBL4063893 — EC50 = 8.913 nM 8.05
CHEMBL4063893 — EC50 = 9.2 nM 8.04
CHEMBL4098721 — EC50 = 13.0 nM 7.89
CHEMBL4098721 — EC50 = 12.88 nM 7.89
CHEMBL4082227 — EC50 = 23.0 nM 7.64
CHEMBL4082227 — EC50 = 22.91 nM 7.64
CHEMBL4072722 — EC50 = 23.5 nM 7.63
CHEMBL4072722 — EC50 = 23.99 nM 7.62
CHEMBL4086286 — EC50 = 28.18 nM 7.55
CHEMBL4086286 — EC50 = 28.0 nM 7.55
CHEMBL4083193 — EC50 = 95.5 nM 7.02
CHEMBL4083193 — EC50 = 95.0 nM 7.02
CHEMBL4101194 — EC50 = 102.33 nM 6.99
CHEMBL4101194 — EC50 = 103.0 nM 6.99
CHEMBL4103313 — EC50 = 120.23 nM 6.92
CHEMBL4103313 — EC50 = 121.0 nM 6.92
CHEMBL4085380 — EC50 = 120.0 nM 6.92
CHEMBL4085380 — EC50 = 120.23 nM 6.92
CHEMBL4070259 — EC50 = 229.09 nM 6.64
CHEMBL4067525 — EC50 = 231.0 nM 6.64
CHEMBL4067525 — EC50 = 229.09 nM 6.64
CHEMBL4070259 — EC50 = 228.0 nM 6.64
CHEMBL4064809 — EC50 = 245.0 nM 6.61
CHEMBL4064809 — EC50 = 245.47 nM 6.61
CHEMBL4102683 — EC50 = 304.0 nM 6.52
CHEMBL4102683 — EC50 = 302.0 nM 6.52
CHEMBL4095562 — EC50 = 308.0 nM 6.51
CHEMBL4095562 — EC50 = 309.03 nM 6.51
CHEMBL4090984 — EC50 = 399.0 nM 6.40
CHEMBL4094054 — EC50 = 409.0 nM 6.39
CHEMBL4094054 — EC50 = 407.38 nM 6.39
CHEMBL4094164 — EC50 = 436.52 nM 6.36
CHEMBL4094164 — EC50 = 433.0 nM 6.36
CHEMBL4101789 — EC50 = 501.19 nM 6.30
CHEMBL4101789 — EC50 = 502.0 nM 6.30
CHEMBL4104218 — EC50 = 524.81 nM 6.28
CHEMBL4064935 — EC50 = 524.81 nM 6.28
CHEMBL4104218 — EC50 = 529.0 nM 6.28
CHEMBL4064935 — EC50 = 530.0 nM 6.28
CHEMBL4091197 — EC50 = 549.54 nM 6.26
CHEMBL4091197 — EC50 = 556.0 nM 6.25
CHEMBL4075150 — EC50 = 615.0 nM 6.21
CHEMBL4075150 — EC50 = 616.6 nM 6.21
CHEMBL4079976 — EC50 = 670.0 nM 6.17