Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5239798

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

Binding
Inhibition of FGFR1 (unknown origin) using TK as substrate incubated for 1 hr in presence of biotin/ATP by HTRF assay
2
Total Activities
2
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

Discovery of 2-Amino-7-sulfonyl-7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidine Derivatives as Potent Reversible FGFR Inhibitors with Gatekeeper Mutation Tolerance: Design, Synthesis, and Biological Evaluation.
Xie W, Yang S, Liang L, Wang M, Zuo W, Lei Y, Zhang Y, Tang W, Lu T, Chen Y, Jiang Y.
J Med Chem (2022) 65 : 16570 -16588
PubMed 36480917 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.04 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3828009 LY-2874455 1.0 1 8.89
CHEMBL5278656 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3828009 LY-2874455 IC50 = 1.3 nM 8.89
CHEMBL5278656 IC50 = 64.3 nM 7.19