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Assay Detail

CHEMBL4810137

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

Binding
Inhibition of human FGFR1 using biotinylated-EQEDEPEGDYFEWLE peptide as substrate incubated for 1 hr in presence of ATP by FRET assay
17
Total Activities
17
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 Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.
Wu L, Zhang C, He C, Qian D, Lu L, Sun Y, Xu M, Zhuo J, Liu PCC, Klabe R, Wynn R, Covington M, Gallagher K, Leffet L, Bowman K, Diamond S, Koblish H, Zhang Y, Soloviev M, Hollis G, Burn TC, Scherle P, Yeleswaram S, Huber R, Yao W.
J Med Chem (2021) 64 : 10666 -10679
PubMed 34269576 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 8.36 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4870179 1 9.92
CHEMBL4862823 1 9.77
CHEMBL4846809 1 9.10
CHEMBL4863146 1 8.96
CHEMBL4863224 1 8.96
CHEMBL4851637 1 8.82
CHEMBL4847441 1 8.72
CHEMBL4874869 1 8.36
CHEMBL4862283 1 8.22
CHEMBL4856613 1 8.12
CHEMBL4871046 1 8.04
CHEMBL4858423 1 8.01
CHEMBL4848530 1 7.70
CHEMBL4873003 1 7.68
CHEMBL4866178 1 7.57
CHEMBL4868291 1 7.09
CHEMBL4861534 1 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4870179 IC50 = 0.12 nM 9.92
CHEMBL4862823 IC50 = 0.17 nM 9.77
CHEMBL4846809 IC50 = 0.79 nM 9.10
CHEMBL4863146 IC50 = 1.1 nM 8.96
CHEMBL4863224 IC50 = 1.1 nM 8.96
CHEMBL4851637 IC50 = 1.5 nM 8.82
CHEMBL4847441 IC50 = 1.9 nM 8.72
CHEMBL4874869 IC50 = 4.4 nM 8.36
CHEMBL4862283 IC50 = 6.0 nM 8.22
CHEMBL4856613 IC50 = 7.5 nM 8.12
CHEMBL4871046 IC50 = 9.2 nM 8.04
CHEMBL4858423 IC50 = 9.8 nM 8.01
CHEMBL4848530 IC50 = 20.0 nM 7.70
CHEMBL4873003 IC50 = 21.0 nM 7.68
CHEMBL4866178 IC50 = 27.0 nM 7.57
CHEMBL4868291 IC50 = 82.0 nM 7.09
CHEMBL4861534 IC50 = 83.0 nM 7.08