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Assay Detail

CHEMBL4670126

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Binding
Antagonist activity at 5HT2B receptor (unknown origin) by radioligand binding assay
10
Total Activities
10
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

Structure activity relationship exploration of 5-hydroxy-2-(3-phenylpropyl)chromones as a unique 5-HT receptor antagonist scaffold.
Kim M,Truss M,Pagare PP,Essandoh MA,Zhang Y,Williams DA
Bioorg Med Chem Lett (2020) 30 : 127511 -127511
PubMed 32853682 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 5.90 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4796102 1 7.10
CHEMBL4780527 1 6.00
CHEMBL4795598 1 6.00
CHEMBL4755344 1 5.90
CHEMBL4741776 1 5.80
CHEMBL4763861 1 5.70
CHEMBL4790230 1 5.70
CHEMBL4783824 1 5.60
CHEMBL4743625 1 5.60
CHEMBL4746138 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4796102 Ki = 79.43 nM 7.10
CHEMBL4780527 Ki = 1000.0 nM 6.00
CHEMBL4795598 Ki = 1000.0 nM 6.00
CHEMBL4755344 Ki = 1258.93 nM 5.90
CHEMBL4741776 Ki = 1584.89 nM 5.80
CHEMBL4763861 Ki = 1995.26 nM 5.70
CHEMBL4790230 Ki = 1995.26 nM 5.70
CHEMBL4783824 Ki = 2511.89 nM 5.60
CHEMBL4743625 Ki = 2511.89 nM 5.60
CHEMBL4746138 Ki = 2511.89 nM 5.60