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Assay Detail

CHEMBL961037

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

Binding
Inhibition of human cloned 5HT2B receptor by competitive binding experiment
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2B (CHEMBL1833)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.
Herth MM, Kramer V, Piel M, Palner M, Riss PJ, Knudsen GM, Rösch F.
Bioorg Med Chem (2009) 17 : 2989 -3002
PubMed 19329329 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.07 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL402143 1 6.52
CHEMBL515472 1 6.50
CHEMBL476839 1 6.33
CHEMBL490632 1 6.25
CHEMBL516088 1 6.02
CHEMBL490634 1 5.98
CHEMBL476838 1 5.73
CHEMBL489408 1 5.71
CHEMBL490633 1 5.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL402143 Ki = 299.0 nM 6.52
CHEMBL515472 Ki = 320.0 nM 6.50
CHEMBL476839 Ki = 466.0 nM 6.33
CHEMBL490632 Ki = 559.0 nM 6.25
CHEMBL516088 Ki = 960.0 nM 6.02
CHEMBL490634 Ki = 1052.0 nM 5.98
CHEMBL476838 Ki = 1844.0 nM 5.73
CHEMBL489408 Ki = 1972.0 nM 5.71
CHEMBL490633 Ki = 2751.0 nM 5.56