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Assay Detail

CHEMBL617254

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

Binding
Binding affinity at human cloned 5-hydroxytryptamine 2A receptor.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of a novel series of selective 5-HT7 receptor antagonists.
Forbes IT, Cooper DG, Dodds EK, Douglas SE, Gribble AD, Ife RJ, Lightfoot AP, Meeson M, Campbell LP, Coleman T, Riley GJ, Thomas DR.
Bioorg Med Chem Lett (2003) 13 : 1055 -1058
PubMed 12643910 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.21 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267062 1 8.77
CHEMBL9951 1 8.16
CHEMBL9616 1 7.77
CHEMBL9952 1 7.71
CHEMBL275451 1 7.50
CHEMBL9446 1 7.37
CHEMBL9347 1 7.31
CHEMBL9770 1 7.26
CHEMBL429202 1 7.13
CHEMBL275343 1 7.11
CHEMBL9564 1 6.81
CHEMBL9250 1 6.73
CHEMBL275258 1 6.65
CHEMBL275475 1 6.57
CHEMBL273921 1 6.52
CHEMBL273821 1 6.01
CHEMBL273872 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267062 Ki = 1.698 nM 8.77
CHEMBL9951 Ki = 6.918 nM 8.16
CHEMBL9616 Ki = 16.98 nM 7.77
CHEMBL9952 Ki = 19.5 nM 7.71
CHEMBL275451 Ki = 31.62 nM 7.50
CHEMBL9446 Ki = 42.66 nM 7.37
CHEMBL9347 Ki = 48.98 nM 7.31
CHEMBL9770 Ki = 54.95 nM 7.26
CHEMBL429202 Ki = 74.13 nM 7.13
CHEMBL275343 Ki = 77.62 nM 7.11
CHEMBL9564 Ki = 154.88 nM 6.81
CHEMBL9250 Ki = 186.21 nM 6.73
CHEMBL275258 Ki = 223.87 nM 6.65
CHEMBL275475 Ki = 269.15 nM 6.57
CHEMBL273921 Ki = 302.0 nM 6.52
CHEMBL273821 Ki = 977.24 nM 6.01
CHEMBL273872 Ki < 1584.89 nM -