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Assay Detail

CHEMBL5540235

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

Toxicity
Agonist activity at 5HT2B (unknown origin)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Toxicity
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

Discovery of Darovasertib (NVP-LXS196), a Pan-PKC Inhibitor for the Treatment of Metastatic Uveal Melanoma.
Visser M, Papillon JPN, Luzzio M, LaMarche MJ, Fan J, Michael W, Wang D, Zhang A, Straub C, Mathieu S, Kato M, Palermo M, Chen C, Ramsey T, Joud C, Barrett R, Vattay A, Guo R, Bric A, Chung F, Liang G, Romanowski MJ, Lam J, Thohan S, Atassi F, Wylie A, Cooke VG.
J Med Chem (2024) 67 : 1447 -1459
PubMed 38198520 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 6.71 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3950697 1 7.39
CHEMBL3946659 1 7.37
CHEMBL3966643 1 6.82
CHEMBL3890986 1 6.80
CHEMBL3966595 1 6.80
CHEMBL3915489 1 6.70
CHEMBL3982497 1 6.11
CHEMBL5565713 1 5.70
CHEMBL3965722 1 -
CHEMBL5564760 1 -
CHEMBL3982723 DAROVASERTIB 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3950697 EC50 = 41.0 nM 7.39
CHEMBL3946659 EC50 = 43.0 nM 7.37
CHEMBL3966643 EC50 = 150.0 nM 6.82
CHEMBL3890986 EC50 = 160.0 nM 6.80
CHEMBL3966595 EC50 = 160.0 nM 6.80
CHEMBL3915489 EC50 = 200.0 nM 6.70
CHEMBL3982497 EC50 = 780.0 nM 6.11
CHEMBL5565713 EC50 = 2000.0 nM 5.70
CHEMBL3965722 EC50 > 30000.0 nM -
CHEMBL5564760 EC50 > 30000.0 nM -
CHEMBL3982723 DAROVASERTIB EC50 > 30000.0 nM -