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Assay Detail

CHEMBL5540232

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Functional
Antiproliferative activity against human 92-1 cells incubated for 72 hrs by microplate reader analysis
21
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type 92-1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 18 6.68 7.96
IC50 3 6.29 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3982497 1 7.96
CHEMBL3966643 1 7.85
CHEMBL3966595 1 7.66
CHEMBL5573642 1 7.44
CHEMBL3957149 1 7.22
CHEMBL3943147 1 7.18
CHEMBL5592487 1 6.85
CHEMBL3890986 1 6.85
CHEMBL3946659 1 6.82
CHEMBL3982723 DAROVASERTIB 2.0 1 6.77
CHEMBL3915489 1 6.75
CHEMBL5566264 1 6.64
CHEMBL565612 SOTRASTAURIN 2.0 1 6.60
CHEMBL3924825 1 6.21
CHEMBL3957715 1 6.16
CHEMBL3950697 1 6.11
CHEMBL5564760 1 5.86
CHEMBL5565713 1 5.76
CHEMBL3965722 1 5.55
CHEMBL5571382 1 5.44
CHEMBL5591535 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3982497 EC50 = 11.0 nM 7.96
CHEMBL3966643 EC50 = 14.0 nM 7.85
CHEMBL3966595 EC50 = 22.0 nM 7.66
CHEMBL5573642 EC50 = 36.0 nM 7.44
CHEMBL3957149 EC50 = 60.0 nM 7.22
CHEMBL3943147 EC50 = 66.0 nM 7.18
CHEMBL5592487 IC50 = 140.0 nM 6.85
CHEMBL3890986 EC50 = 140.0 nM 6.85
CHEMBL3946659 EC50 = 153.0 nM 6.82
CHEMBL3982723 DAROVASERTIB EC50 = 170.0 nM 6.77
CHEMBL3915489 EC50 = 180.0 nM 6.75
CHEMBL5566264 EC50 = 230.0 nM 6.64
CHEMBL565612 SOTRASTAURIN IC50 = 250.0 nM 6.60
CHEMBL3924825 EC50 = 620.0 nM 6.21
CHEMBL3957715 EC50 = 700.0 nM 6.16
CHEMBL3950697 EC50 = 780.0 nM 6.11
CHEMBL5564760 EC50 = 1390.0 nM 5.86
CHEMBL5565713 EC50 = 1740.0 nM 5.76
CHEMBL3965722 EC50 = 2800.0 nM 5.55
CHEMBL5571382 EC50 = 3660.0 nM 5.44
CHEMBL5591535 IC50 = 3700.0 nM 5.43