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Assay Detail

CHEMBL857984

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

Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines.
Bromidge SM, Dabbs S, Davies DT, Duckworth DM, Forbes IT, Ham P, Jones GE, King FD, Saunders DV, Starr S, Thewlis KM, Wyman PA, Blaney FE, Naylor CB, Bailey F, Blackburn TP, Holland V, Kennett GA, Riley GJ, Wood MD.
J Med Chem (1998) 41 : 1598 -1612
PubMed 9572885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.71 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41389 1 8.40
CHEMBL289436 1 8.00
CHEMBL276140 1 7.90
CHEMBL41792 1 7.80
CHEMBL297784 1 7.60
CHEMBL44015 1 7.50
CHEMBL297445 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41389 Ki = 3.981 nM 8.40
CHEMBL289436 Ki = 10.0 nM 8.00
CHEMBL276140 Ki = 12.59 nM 7.90
CHEMBL41792 Ki = 15.85 nM 7.80
CHEMBL297784 Ki = 25.12 nM 7.60
CHEMBL44015 Ki = 31.62 nM 7.50
CHEMBL297445 Ki = 158.49 nM 6.80