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Assay Detail

CHEMBL4723345

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Functional
Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability by cell proliferation assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Hep 3B2
Confidence 1 — Organism
Curated By Autocuration

Target

Hep 3B2 (CHEMBL4296437)
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 11 7.05 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4284069 1 8.17
CHEMBL3973674 1 8.05
CHEMBL4742811 1 7.36
CHEMBL3972276 1 7.14
CHEMBL1852688 INFIGRATINIB 4.0 1 7.07
CHEMBL4279514 1 6.58
CHEMBL3966721 1 6.58
CHEMBL3916036 1 6.32
CHEMBL3929437 1 6.14
CHEMBL3904499 1 -
CHEMBL3983290 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4284069 IC50 = 6.8 nM 8.17
CHEMBL3973674 IC50 = 9.0 nM 8.05
CHEMBL4742811 IC50 = 44.0 nM 7.36
CHEMBL3972276 IC50 = 73.0 nM 7.14
CHEMBL1852688 INFIGRATINIB IC50 = 85.0 nM 7.07
CHEMBL4279514 IC50 = 261.0 nM 6.58
CHEMBL3966721 IC50 = 265.0 nM 6.58
CHEMBL3916036 IC50 = 483.0 nM 6.32
CHEMBL3929437 IC50 = 719.0 nM 6.14
CHEMBL3904499 IC50 > 3000.0 nM -
CHEMBL3983290 IC50 > 3000.0 nM -