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Assay Detail

CHEMBL617619

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

Binding
Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Stomach
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2B (CHEMBL323)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis, biological activity, and molecular modeling of selective 5-HT(2C/2B) receptor antagonists.
Forbes IT, Dabbs S, Duckworth DM, Ham P, Jones GE, King FD, Saunders DV, Blaney FE, Naylor CB, Baxter GS, Blackburn TP, Kennett GA, Wood MD.
J Med Chem (1996) 39 : 4966 -4977
PubMed 8960557 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 12 7.96 8.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL148346 1 8.90
CHEMBL297784 1 8.50
CHEMBL148347 1 8.20
CHEMBL147820 1 8.20
CHEMBL2112859 1 8.10
CHEMBL148385 1 8.00
CHEMBL343666 1 8.00
CHEMBL144567 1 7.90
CHEMBL315223 1 7.80
CHEMBL343455 1 7.70
CHEMBL357870 1 7.50
CHEMBL356146 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL148346 Kd = 1.259 nM 8.90
CHEMBL297784 Kd = 3.162 nM 8.50
CHEMBL148347 Kd = 6.31 nM 8.20
CHEMBL147820 Kd = 6.31 nM 8.20
CHEMBL2112859 Kd = 7.943 nM 8.10
CHEMBL148385 Kd = 10.0 nM 8.00
CHEMBL343666 Kd = 10.0 nM 8.00
CHEMBL144567 Kd = 12.59 nM 7.90
CHEMBL315223 Kd = 15.85 nM 7.80
CHEMBL343455 Kd = 19.95 nM 7.70
CHEMBL357870 Kd = 31.62 nM 7.50
CHEMBL356146 Kd = 199.53 nM 6.70