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Assay Detail

CHEMBL5135840

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Functional
Agonist activity at human 5HT2C receptor stably expressed in Flp-In-T-REx-293 cells assessed as increase in Gq-mediated calcium flux by Fluo-4 direct dye based FLIPR Tetra assay
ChEMBL ↗
198
Total Activities
104
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Flp-In-T-REx-293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of Highly Potent Serotonin 5-HT<sub>2</sub> Receptor Agonists Inspired by Heteroyohimbine Natural Products.
Orr MJ, Cao AB, Wang CT, Gaisin A, Csakai A, Friswold AP, Meltzer HY, McCorvy JD, Scheidt KA.
ACS Med Chem Lett (2022) 13 : 648 -657
PubMed 35450369 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 198 6.83 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5187275 — — 2 9.49
CHEMBL535832 SEROTONIN HYDROCHLORIDE — 2 9.49
CHEMBL5207529 — — 2 9.33
CHEMBL5198213 — — 2 9.10
CHEMBL5204071 — — 2 8.99
CHEMBL5200026 — — 2 8.72
CHEMBL5179588 — — 2 8.37
CHEMBL5178632 — — 2 8.12
CHEMBL5170784 — — 2 8.05
CHEMBL5199923 — — 2 8.00
CHEMBL4790446 — — 2 7.90
CHEMBL5177900 — — 2 7.88
CHEMBL4752798 — — 2 7.82
CHEMBL5194866 — — 2 7.80
CHEMBL5182943 — — 2 7.70
CHEMBL5180401 — — 2 7.69
CHEMBL5180800 — — 2 7.65
CHEMBL4757837 — — 2 7.61
CHEMBL5170614 — — 2 7.53
CHEMBL5170024 — — 2 7.41
CHEMBL5201470 — — 2 7.38
CHEMBL5174331 — — 2 7.36
CHEMBL5201903 — — 2 7.33
CHEMBL5188678 — — 2 7.30
CHEMBL5172342 — — 2 7.21
CHEMBL4749189 — — 2 7.20
CHEMBL5189339 — — 2 7.18
CHEMBL4802359 — — 2 7.16
CHEMBL5194223 — — 2 7.16
CHEMBL5183493 — — 2 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL535832 SEROTONIN HYDROCHLORIDE EC50 = 0.32 nM 9.49
CHEMBL535832 SEROTONIN HYDROCHLORIDE EC50 = 0.3236 nM 9.49
CHEMBL5187275 — EC50 = 0.3236 nM 9.49
CHEMBL5207529 — EC50 = 0.4677 nM 9.33
CHEMBL5207529 — EC50 = 0.5 nM 9.30
CHEMBL5198213 — EC50 = 0.8 nM 9.10
CHEMBL5198213 — EC50 = 0.7943 nM 9.10
CHEMBL5204071 — EC50 = 1.02 nM 8.99
CHEMBL5204071 — EC50 = 1.023 nM 8.99
CHEMBL5200026 — EC50 = 1.9 nM 8.72
CHEMBL5200026 — EC50 = 1.905 nM 8.72
CHEMBL5179588 — EC50 = 4.3 nM 8.37
CHEMBL5179588 — EC50 = 4.365 nM 8.36
CHEMBL5178632 — EC50 = 7.6 nM 8.12
CHEMBL5178632 — EC50 = 7.943 nM 8.10
CHEMBL5170784 — EC50 = 8.9 nM 8.05
CHEMBL5170784 — EC50 = 8.913 nM 8.05
CHEMBL5199923 — EC50 = 10.1 nM 8.00
CHEMBL5199923 — EC50 = 10.0 nM 8.00
CHEMBL4790446 — EC50 = 12.59 nM 7.90
CHEMBL4790446 — EC50 = 12.6 nM 7.90
CHEMBL5177900 — EC50 = 13.2 nM 7.88
CHEMBL5177900 — EC50 = 13.18 nM 7.88
CHEMBL4752798 — EC50 = 15.3 nM 7.82
CHEMBL4752798 — EC50 = 15.49 nM 7.81
CHEMBL5194866 — EC50 = 15.85 nM 7.80
CHEMBL5194866 — EC50 = 15.8 nM 7.80
CHEMBL5182943 — EC50 = 20.0 nM 7.70
CHEMBL5180401 — EC50 = 20.42 nM 7.69
CHEMBL5182943 — EC50 = 20.42 nM 7.69
CHEMBL5180401 — EC50 = 20.4 nM 7.69
CHEMBL5180800 — EC50 = 22.4 nM 7.65
CHEMBL5180800 — EC50 = 22.39 nM 7.65
CHEMBL4757837 — EC50 = 24.55 nM 7.61
CHEMBL4757837 — EC50 = 24.5 nM 7.61
CHEMBL5170614 — EC50 = 29.8 nM 7.53
CHEMBL5170614 — EC50 = 30.2 nM 7.52
CHEMBL5170024 — EC50 = 39.0 nM 7.41
CHEMBL5170024 — EC50 = 38.9 nM 7.41
CHEMBL5201470 — EC50 = 42.0 nM 7.38
CHEMBL5201470 — EC50 = 41.69 nM 7.38
CHEMBL5174331 — EC50 = 44.0 nM 7.36
CHEMBL5174331 — EC50 = 43.65 nM 7.36
CHEMBL5201903 — EC50 = 47.0 nM 7.33
CHEMBL5201903 — EC50 = 46.77 nM 7.33
CHEMBL5188678 — EC50 = 50.1 nM 7.30
CHEMBL5188678 — EC50 = 50.12 nM 7.30
CHEMBL5172342 — EC50 = 61.66 nM 7.21
CHEMBL5172342 — EC50 = 61.0 nM 7.21
CHEMBL4749189 — EC50 = 62.5 nM 7.20