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Assay Detail

CHEMBL5628119

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Binding
Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant
ChEMBL ↗
16
Total Activities
8
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 relationships of 5-HT<sub>2B</sub> and 5-HT<sub>2C</sub> serotonin receptor antagonists: N<sup>6</sup>, C2 and 5'-Modified (N)-methanocarba-adenosine derivatives.
Tosh DK, Calkins MM, Ivancich MS, Bock HA, Campbell RG, Lewicki SA, Chen E, Gao ZG, McCorvy JD, Jacobson KA.
Eur J Med Chem (2023) 259 : 115691 -115691
PubMed 37562117 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.54 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL331291 — — 2 7.11
CHEMBL4470080 — — 2 6.87
CHEMBL4572905 — — 2 6.87
CHEMBL4436786 — — 2 6.73
CHEMBL4522864 — — 2 6.69
CHEMBL4584140 — — 2 6.22
CHEMBL4554295 — — 2 5.96
CHEMBL4778855 — — 2 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL331291 — Ki = 78.2 nM 7.11
CHEMBL331291 — Ki = 77.62 nM 7.11
CHEMBL4470080 — Ki = 136.0 nM 6.87
CHEMBL4572905 — Ki = 136.0 nM 6.87
CHEMBL4470080 — Ki = 134.9 nM 6.87
CHEMBL4572905 — Ki = 134.9 nM 6.87
CHEMBL4436786 — Ki = 186.0 nM 6.73
CHEMBL4436786 — Ki = 186.21 nM 6.73
CHEMBL4522864 — Ki = 205.0 nM 6.69
CHEMBL4522864 — Ki = 204.17 nM 6.69
CHEMBL4584140 — Ki = 601.0 nM 6.22
CHEMBL4584140 — Ki = 602.56 nM 6.22
CHEMBL4554295 — Ki = 1090.0 nM 5.96
CHEMBL4554295 — Ki = 1096.48 nM 5.96
CHEMBL4778855 — Ki = 1300.0 nM 5.89
CHEMBL4778855 — Ki = 1318.26 nM 5.88