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Assay Detail

CHEMBL4714289

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

ADMET
Displacement of [3H]-LSB from recombinant human 5HT2BR transfected in human HEK293 cells incubated for 45 mins by radioligand binding assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines as potent and selective agonists of the 5-HT receptor.
Schrader TO,Zhu X,Kasem M,Ren A,Liu C,Wu C,Dang H,Le M,Gatlin J,Chase K,Frazer J,Whelan KT,Grottick AJ,Hutton C,Barden J,Chen C,Ortiz A,Feichtinger K,Semple G
Bioorg Med Chem Lett (2021) 38 : 127872 -127872
PubMed 33636307 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.25 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4765074 1 8.00
CHEMBL4776557 1 7.90
CHEMBL4213379 1 7.60
CHEMBL4777852 1 7.50
CHEMBL4213447 1 7.40
CHEMBL4757718 1 7.00
CHEMBL4785566 1 6.90
CHEMBL4218374 1 6.90
CHEMBL4206126 1 6.70
CHEMBL4778570 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4765074 Ki = 10.0 nM 8.00
CHEMBL4776557 Ki = 12.59 nM 7.90
CHEMBL4213379 Ki = 25.12 nM 7.60
CHEMBL4777852 Ki = 31.62 nM 7.50
CHEMBL4213447 Ki = 39.81 nM 7.40
CHEMBL4757718 Ki = 100.0 nM 7.00
CHEMBL4785566 Ki = 125.89 nM 6.90
CHEMBL4218374 Ki = 125.89 nM 6.90
CHEMBL4206126 Ki = 199.53 nM 6.70
CHEMBL4778570 Ki = 251.19 nM 6.60