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Assay Detail

CHEMBL5547423

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]LSD from human 5-HT2C receptor expressed in HEK293 cell membrane incubated for 90 mins by microbeta liquid scintillation counting method
28
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and Structure-Activity Relationships of 2,5-Dimethoxy-4-Substituted Phenethylamines and the Discovery of CYB210010: A Potent, Orally Bioavailable and Long-Acting Serotonin 5-HT<sub>2</sub> Receptor Agonist.
Varty GB, Canal CE, Mueller TA, Hartsel JA, Tyagi R, Avery K, Morgan ME, Reichelt AC, Pathare P, Stang E, Palfreyman MG, Nivorozhkin A.
J Med Chem (2024) 67 : 6144 -6188
PubMed 38593423 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 7.63 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5589604 2 8.16
CHEMBL5563542 2 8.05
CHEMBL5569144 2 7.97
CHEMBL5573972 2 7.96
CHEMBL5574455 2 7.89
CHEMBL5565116 2 7.80
CHEMBL5572387 2 7.68
CHEMBL5594012 2 7.59
CHEMBL5584114 2 7.59
CHEMBL5566251 2 7.18
CHEMBL5573377 2 7.09
CHEMBL5572320 2 7.08
CHEMBL5566821 1 7.02
CHEMBL5570285 1 -
CHEMBL5570258 1 -
CHEMBL5570359 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5589604 Ki = 6.9 nM 8.16
CHEMBL5589604 Ki = 6.918 nM 8.16
CHEMBL5563542 Ki = 8.913 nM 8.05
CHEMBL5563542 Ki = 8.9 nM 8.05
CHEMBL5569144 Ki = 10.72 nM 7.97
CHEMBL5573972 Ki = 11.0 nM 7.96
CHEMBL5569144 Ki = 11.0 nM 7.96
CHEMBL5574455 Ki = 13.0 nM 7.89
CHEMBL5574455 Ki = 13.49 nM 7.87
CHEMBL5565116 Ki = 16.0 nM 7.80
CHEMBL5565116 Ki = 16.6 nM 7.78
CHEMBL5572387 Ki = 21.0 nM 7.68
CHEMBL5572387 Ki = 20.89 nM 7.68
CHEMBL5573972 Ki = 21.38 nM 7.67
CHEMBL5594012 Ki = 25.7 nM 7.59
CHEMBL5584114 Ki = 25.7 nM 7.59
CHEMBL5584114 Ki = 26.0 nM 7.58
CHEMBL5594012 Ki = 26.0 nM 7.58
CHEMBL5566251 Ki = 66.07 nM 7.18
CHEMBL5566251 Ki = 67.0 nM 7.17
CHEMBL5573377 Ki = 82.0 nM 7.09
CHEMBL5573377 Ki = 83.18 nM 7.08
CHEMBL5572320 Ki = 83.18 nM 7.08
CHEMBL5572320 Ki = 83.0 nM 7.08
CHEMBL5566821 Ki = 95.0 nM 7.02
CHEMBL5570285 Ki - -
CHEMBL5570359 Ki - -
CHEMBL5570258 Ki - -