Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL921963

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

Binding
Displacement of [3H]5-HT from human 5HT2A receptor expressed in CHO cells
20
Total Activities
20
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 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
Shimada I, Maeno K, Kazuta K, Kubota H, Kimizuka T, Kimura Y, Hatanaka K, Naitou Y, Wanibuchi F, Sakamoto S, Tsukamoto S.
Bioorg Med Chem (2008) 16 : 1966 -1982
PubMed 18035544 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.63 9.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261476 1 9.11
CHEMBL408579 1 9.11
CHEMBL406851 1 8.17
CHEMBL262092 1 8.06
CHEMBL264172 1 8.04
CHEMBL256420 1 7.96
CHEMBL261045 1 7.96
CHEMBL407909 1 7.89
CHEMBL404969 1 7.77
CHEMBL199775 1 7.43
CHEMBL273163 1 7.42
CHEMBL76781 1 7.41
CHEMBL403926 1 7.34
CHEMBL261046 1 7.33
CHEMBL403927 1 7.29
CHEMBL404970 1 7.19
CHEMBL256623 1 7.09
CHEMBL272755 1 7.06
CHEMBL257503 1 7.05
CHEMBL404065 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261476 Ki = 0.78 nM 9.11
CHEMBL408579 Ki = 0.78 nM 9.11
CHEMBL406851 Ki = 6.7 nM 8.17
CHEMBL262092 Ki = 8.7 nM 8.06
CHEMBL264172 Ki = 9.1 nM 8.04
CHEMBL256420 Ki = 11.0 nM 7.96
CHEMBL261045 Ki = 11.0 nM 7.96
CHEMBL407909 Ki = 13.0 nM 7.89
CHEMBL404969 Ki = 17.0 nM 7.77
CHEMBL199775 Ki = 37.0 nM 7.43
CHEMBL273163 Ki = 38.0 nM 7.42
CHEMBL76781 Ki = 39.0 nM 7.41
CHEMBL403926 Ki = 46.0 nM 7.34
CHEMBL261046 Ki = 47.0 nM 7.33
CHEMBL403927 Ki = 51.0 nM 7.29
CHEMBL404970 Ki = 64.0 nM 7.19
CHEMBL256623 Ki = 82.0 nM 7.09
CHEMBL272755 Ki = 87.0 nM 7.06
CHEMBL257503 Ki = 89.0 nM 7.05
CHEMBL404065 Ki = 1200.0 nM 5.92