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Assay Detail

CHEMBL4723293

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

Functional
Antiproliferative activity against human HuH7 cells assessed as reduction in cell viability incubated for 3 days by cell proliferation assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Huh-7
Confidence 1 — Organism
Curated By Autocuration

Target

Huh-7 (CHEMBL614039)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
Fairhurst RA,Knoepfel T,Buschmann N,Leblanc C,Mah R,Todorov M,Nimsgern P,Ripoche S,Niklaus M,Warin N,Luu VH,Madoerin M,Wirth J,Graus-Porta D,Weiss A,Kiffe M,Wartmann M,Kinyamu-Akunda J,Sterker D,Stamm C,Adler F,Buhles A,Schadt H,Couttet P,Blank J,Galuba I,Trappe J,Voshol J,Ostermann N,Zou C,Berghausen J,Del Rio Espinola A,Jahnke W,Furet P
J Med Chem (2020) 63 : 12542 -12573
PubMed 32930584 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 6.87 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3973674 1 7.92
CHEMBL4796410 1 7.68
CHEMBL3968334 1 7.60
CHEMBL4284069 1 7.58
CHEMBL4742811 1 7.57
CHEMBL3983290 1 7.39
CHEMBL4745780 1 7.33
CHEMBL3951479 1 7.28
CHEMBL3912070 1 7.28
CHEMBL3946444 1 7.17
CHEMBL3972276 1 7.14
CHEMBL1852688 INFIGRATINIB 4.0 1 7.10
CHEMBL4784921 1 7.05
CHEMBL3904499 1 6.97
CHEMBL4294665 1 6.87
CHEMBL4759211 1 6.85
CHEMBL4784243 1 6.75
CHEMBL4756889 1 6.75
CHEMBL4764394 1 6.75
CHEMBL3950552 1 6.71
CHEMBL4279514 1 6.62
CHEMBL3916036 1 6.59
CHEMBL3904341 1 6.47
CHEMBL3966721 1 6.41
CHEMBL4106685 1 6.33
CHEMBL4758832 1 6.22
CHEMBL3925900 1 6.18
CHEMBL3920470 1 5.96
CHEMBL3964830 1 5.79
CHEMBL4776082 1 5.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3973674 IC50 = 12.0 nM 7.92
CHEMBL4796410 IC50 = 21.0 nM 7.68
CHEMBL3968334 IC50 = 25.0 nM 7.60
CHEMBL4284069 IC50 = 26.0 nM 7.58
CHEMBL4742811 IC50 = 27.0 nM 7.57
CHEMBL3983290 IC50 = 41.0 nM 7.39
CHEMBL4745780 IC50 = 47.0 nM 7.33
CHEMBL3951479 IC50 = 52.0 nM 7.28
CHEMBL3912070 IC50 = 53.0 nM 7.28
CHEMBL3946444 IC50 = 68.0 nM 7.17
CHEMBL3972276 IC50 = 72.0 nM 7.14
CHEMBL1852688 INFIGRATINIB IC50 = 80.0 nM 7.10
CHEMBL4784921 IC50 = 89.0 nM 7.05
CHEMBL3904499 IC50 = 106.0 nM 6.97
CHEMBL4294665 IC50 = 135.0 nM 6.87
CHEMBL4759211 IC50 = 141.0 nM 6.85
CHEMBL4784243 IC50 = 178.0 nM 6.75
CHEMBL4756889 IC50 = 178.0 nM 6.75
CHEMBL4764394 IC50 = 178.0 nM 6.75
CHEMBL3950552 IC50 = 193.0 nM 6.71
CHEMBL4279514 IC50 = 237.0 nM 6.62
CHEMBL3916036 IC50 = 255.0 nM 6.59
CHEMBL3904341 IC50 = 340.0 nM 6.47
CHEMBL3966721 IC50 = 387.0 nM 6.41
CHEMBL4106685 IC50 = 463.0 nM 6.33
CHEMBL4758832 IC50 = 604.0 nM 6.22
CHEMBL3925900 IC50 = 656.0 nM 6.18
CHEMBL3920470 IC50 = 1092.0 nM 5.96
CHEMBL3964830 IC50 = 1635.0 nM 5.79
CHEMBL4776082 IC50 = 2056.0 nM 5.69
CHEMBL4750281 IC50 > 3000.0 nM -
CHEMBL4277111 IC50 > 3000.0 nM -
CHEMBL3969343 IC50 > 3000.0 nM -
CHEMBL3929437 IC50 > 3000.0 nM -
CHEMBL3908044 IC50 > 3000.0 nM -
CHEMBL3954670 IC50 > 3000.0 nM -
CHEMBL3911617 IC50 > 3000.0 nM -
CHEMBL4279848 IC50 > 3000.0 nM -
CHEMBL4287768 IC50 > 3000.0 nM -
CHEMBL3971213 IC50 > 3000.0 nM -
CHEMBL3977760 IC50 > 3000.0 nM -