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Assay Detail

CHEMBL617081

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

Binding
Binding affinity towards human 5-hydroxytryptamine 2A receptor by the displacement of [3H]ketanserin radioligand from the cloned receptor expressed in CHO cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thiazoles and thiopyridines: novel series of high affinity h5HT(7) ligands.
Thomson CG, Beer MS, Curtis NR, Diggle HJ, Handford E, Kulagowski JJ.
Bioorg Med Chem Lett (2004) 14 : 677 -680
PubMed 14741267 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.39 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL158973 1 7.00
CHEMBL158402 1 6.64
CHEMBL158285 1 6.57
CHEMBL161765 1 6.50
CHEMBL159143 1 6.32
CHEMBL345803 1 6.19
CHEMBL161846 1 6.00
CHEMBL161203 1 5.92
CHEMBL350166 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL158973 Ki = 100.0 nM 7.00
CHEMBL158402 Ki = 230.0 nM 6.64
CHEMBL158285 Ki = 270.0 nM 6.57
CHEMBL161765 Ki = 320.0 nM 6.50
CHEMBL159143 Ki = 480.0 nM 6.32
CHEMBL345803 Ki = 640.0 nM 6.19
CHEMBL161846 Ki = 1000.0 nM 6.00
CHEMBL161203 Ki = 1200.0 nM 5.92
CHEMBL350166 Ki > 200.0 nM -