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Assay Detail

CHEMBL5509697

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Functional
Agonist activity at human 5-HT2AR expressed in HEK293 cells incubated upto 90 sec by Fluo-4 AM dye based Ca2+ imaging assay
40
Total Activities
24
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 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Structure-Activity Relationships of 2,5-Dimethoxyphenylpiperidines as Selective Serotonin 5-HT<sub>2A</sub> Receptor Agonists.
M Ro Rsted E, Jensen AA, Smits G, Frydenvang K, Kristensen JL.
J Med Chem (2024) 67 : 7224 -7244
PubMed 38648420 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 40 6.98 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL292821 1 8.80
CHEMBL5527952 1 8.80
CHEMBL5531940 2 8.49
CHEMBL5532283 2 8.28
CHEMBL39 SEROTONIN 3.0 1 8.14
CHEMBL5532020 2 8.00
CHEMBL5555278 2 7.58
CHEMBL5558376 2 7.43
CHEMBL5517964 2 7.42
CHEMBL5557170 2 7.42
CHEMBL5558409 2 7.39
CHEMBL5557122 2 7.18
CHEMBL5560448 1 7.16
CHEMBL5517765 2 7.16
CHEMBL5555473 2 7.00
CHEMBL5556954 2 7.00
CHEMBL5565114 1 6.82
CHEMBL5517969 2 6.80
CHEMBL5537031 2 6.57
CHEMBL5556242 2 6.57
CHEMBL5537074 1 6.41
CHEMBL5523588 1 5.96
CHEMBL5542989 1 5.82
CHEMBL5556762 2 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL292821 EC50 = 1.6 nM 8.80
CHEMBL5527952 EC50 = 1.6 nM 8.80
CHEMBL5531940 EC50 = 3.2 nM 8.49
CHEMBL5531940 EC50 = 3.236 nM 8.49
CHEMBL5532283 EC50 = 5.3 nM 8.28
CHEMBL39 SEROTONIN EC50 = 7.3 nM 8.14
CHEMBL5532283 EC50 = 7.7 nM 8.11
CHEMBL5532020 EC50 = 10.0 nM 8.00
CHEMBL5555278 EC50 = 26.0 nM 7.58
CHEMBL5558376 EC50 = 37.0 nM 7.43
CHEMBL5557170 EC50 = 38.0 nM 7.42
CHEMBL5517964 EC50 = 38.0 nM 7.42
CHEMBL5558409 EC50 = 41.0 nM 7.39
CHEMBL5557122 EC50 = 66.0 nM 7.18
CHEMBL5517765 EC50 = 69.0 nM 7.16
CHEMBL5560448 EC50 = 69.0 nM 7.16
CHEMBL5555473 EC50 = 100.0 nM 7.00
CHEMBL5556954 EC50 = 100.0 nM 7.00
CHEMBL5558409 EC50 = 110.0 nM 6.96
CHEMBL5565114 EC50 = 150.0 nM 6.82
CHEMBL5517969 EC50 = 160.0 nM 6.80
CHEMBL5555278 EC50 = 180.0 nM 6.75
CHEMBL5517964 EC50 = 190.0 nM 6.72
CHEMBL5558376 EC50 = 260.0 nM 6.58
CHEMBL5555473 EC50 = 260.0 nM 6.58
CHEMBL5537031 EC50 = 270.0 nM 6.57
CHEMBL5556242 EC50 = 270.0 nM 6.57
CHEMBL5517969 EC50 = 290.0 nM 6.54
CHEMBL5532020 EC50 = 320.0 nM 6.50
CHEMBL5537031 EC50 = 340.0 nM 6.47
CHEMBL5537074 EC50 = 390.0 nM 6.41
CHEMBL5557170 EC50 = 410.0 nM 6.39
CHEMBL5517765 EC50 = 660.0 nM 6.18
CHEMBL5557122 EC50 = 690.0 nM 6.16
CHEMBL5523588 EC50 = 1100.0 nM 5.96
CHEMBL5542989 EC50 = 1500.0 nM 5.82
CHEMBL5556762 EC50 = 1800.0 nM 5.75
CHEMBL5556242 EC50 = 2200.0 nM 5.66
CHEMBL5556762 EC50 = 2500.0 nM 5.60
CHEMBL5556954 EC50 = 3000.0 nM 5.52