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Assay Detail

CHEMBL4838111

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

Binding
Inhibition of FGFR1 (unknown origin)
4
Total Activities
4
Compounds Tested
1
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 1 (CHEMBL3650)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors.
Ran K, Zeng J, Wan G, He X, Feng Z, Xiang W, Wei W, Hu X, Wang N, Liu Z, Yu L.
Eur J Med Chem (2021) 220 : 113499 -113499
PubMed 33940465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.98 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297522 PEMIGATINIB 4.0 1 9.40
CHEMBL1852688 INFIGRATINIB 4.0 1 9.05
CHEMBL3545376 ERDAFITINIB 4.0 1 8.92
CHEMBL3828009 LY-2874455 1.0 1 8.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297522 PEMIGATINIB IC50 = 0.4 nM 9.40
CHEMBL1852688 INFIGRATINIB IC50 = 0.9 nM 9.05
CHEMBL3545376 ERDAFITINIB IC50 = 1.2 nM 8.92
CHEMBL3828009 LY-2874455 IC50 = 2.8 nM 8.55