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Assay Detail

CHEMBL854092

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

Binding
Binding to human 5HT2B receptor expressed in CHO cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
Adams DR, Bentley JM, Benwell KR, Bickerdike MJ, Bodkin CD, Cliffe IA, Dourish CT, George AR, Kennett GA, Knight AR, Malcolm CS, Mansell HL, Misra A, Quirk K, Roffey JR, Vickers SP.
Bioorg Med Chem Lett (2006) 16 : 677 -680
PubMed 16257207 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 7.53 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201930 1 8.96
CHEMBL39 SEROTONIN 3.0 1 8.82
CHEMBL201454 1 8.68
CHEMBL76781 1 8.37
CHEMBL202458 1 7.70
CHEMBL202616 1 7.57
CHEMBL202538 1 7.36
CHEMBL201062 1 7.35
CHEMBL201897 1 7.21
CHEMBL202324 1 7.04
CHEMBL380763 1 7.01
CHEMBL379223 1 6.89
CHEMBL201117 1 6.89
CHEMBL202656 1 6.82
CHEMBL383042 1 6.33
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201930 EC50 = 1.1 nM 8.96
CHEMBL39 SEROTONIN EC50 = 1.5 nM 8.82
CHEMBL201454 EC50 = 2.1 nM 8.68
CHEMBL76781 EC50 = 4.3 nM 8.37
CHEMBL202458 EC50 = 20.0 nM 7.70
CHEMBL202616 EC50 = 27.0 nM 7.57
CHEMBL202538 EC50 = 44.0 nM 7.36
CHEMBL201062 EC50 = 45.0 nM 7.35
CHEMBL201897 EC50 = 62.0 nM 7.21
CHEMBL202324 EC50 = 91.0 nM 7.04
CHEMBL380763 EC50 = 97.0 nM 7.01
CHEMBL379223 EC50 = 128.0 nM 6.89
CHEMBL201117 EC50 = 128.0 nM 6.89
CHEMBL202656 EC50 = 152.0 nM 6.82
CHEMBL383042 EC50 = 462.0 nM 6.33
CHEMBL478 CHLOROPHENYLPIPERAZINE EC50 > 1000.0 nM -