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Assay Detail

CHEMBL936729

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

Binding
Displacement of [3H]5-HT from human 5HT2C receptor expressed in CHO cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
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 a series of benzazepine derivatives as 5-HT2C receptor agonists.
Shimada I, Maeno K, Kondoh Y, Kaku H, Sugasawa K, Kimura Y, Hatanaka K, Naitou Y, Wanibuchi F, Sakamoto S, Tsukamoto S.
Bioorg Med Chem (2008) 16 : 3309 -3320
PubMed 18083579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.89 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL407909 1 9.05
CHEMBL259480 1 8.62
CHEMBL406585 1 8.29
CHEMBL262862 1 8.06
CHEMBL405829 1 7.85
CHEMBL261489 1 7.70
CHEMBL406957 1 7.70
CHEMBL261490 1 7.64
CHEMBL429689 1 7.37
CHEMBL405717 1 7.34
CHEMBL407636 1 7.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL407909 Ki = 0.89 nM 9.05
CHEMBL259480 Ki = 2.4 nM 8.62
CHEMBL406585 Ki = 5.1 nM 8.29
CHEMBL262862 Ki = 8.8 nM 8.06
CHEMBL405829 Ki = 14.0 nM 7.85
CHEMBL261489 Ki = 20.0 nM 7.70
CHEMBL406957 Ki = 20.0 nM 7.70
CHEMBL261490 Ki = 23.0 nM 7.64
CHEMBL429689 Ki = 43.0 nM 7.37
CHEMBL405717 Ki = 46.0 nM 7.34
CHEMBL407636 Ki = 66.0 nM 7.18