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Assay Detail

CHEMBL4714284

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

ADMET
Agonist activity at 5-HT2BR (unknown origin) transfected in human HEK293 cells by IP3 accumulation assay
17
Total Activities
17
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
EC50 17 6.65 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4778104 1 7.80
CHEMBL4747291 1 7.40
CHEMBL4750216 1 7.30
CHEMBL4209572 1 7.20
CHEMBL4776557 1 7.00
CHEMBL4213447 1 6.80
CHEMBL4765074 1 6.70
CHEMBL4777852 1 6.50
CHEMBL4213379 1 6.10
CHEMBL4217846 1 6.10
CHEMBL4785566 1 6.10
CHEMBL4206126 1 5.90
CHEMBL4757718 1 5.50
CHEMBL4218374 1 -
CHEMBL4778570 1 -
CHEMBL4791279 1 -
CHEMBL4750329 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4778104 EC50 = 15.85 nM 7.80
CHEMBL4747291 EC50 = 39.81 nM 7.40
CHEMBL4750216 EC50 = 50.12 nM 7.30
CHEMBL4209572 EC50 = 63.1 nM 7.20
CHEMBL4776557 EC50 = 100.0 nM 7.00
CHEMBL4213447 EC50 = 158.49 nM 6.80
CHEMBL4765074 EC50 = 199.53 nM 6.70
CHEMBL4777852 EC50 = 316.23 nM 6.50
CHEMBL4213379 EC50 = 794.33 nM 6.10
CHEMBL4217846 EC50 = 794.33 nM 6.10
CHEMBL4785566 EC50 = 794.33 nM 6.10
CHEMBL4206126 EC50 = 1258.93 nM 5.90
CHEMBL4757718 EC50 = 3162.28 nM 5.50
CHEMBL4218374 EC50 > 1000.0 nM -
CHEMBL4778570 EC50 > 10000.0 nM -
CHEMBL4791279 EC50 > 10000.0 nM -
CHEMBL4750329 EC50 > 10000.0 nM -