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Assay Detail

CHEMBL4013897

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

Binding
Irreversible inhibition of human FGFR4 preincubated with enzyme followed by peptide substrate addition by caliper capillary electrophoresis method
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fibroblast growth factor receptor 4 (CHEMBL3973)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.
Brameld KA, Owens TD, Verner E, Venetsanakos E, Bradshaw JM, Phan VT, Tam D, Leung K, Shu J, LaStant J, Loughhead DG, Ton T, Karr DE, Gerritsen ME, Goldstein DM, Funk JO.
J Med Chem (2017) 60 : 6516 -6527
PubMed 28665128 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kinact 1 - -
Ki 1 7.14 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4068509 PRN-1371 1.0 2 7.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4068509 PRN-1371 Ki = 73.0 nM 7.14
CHEMBL4068509 PRN-1371 Kinact = 0.00066 /s -