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Assay Detail

CHEMBL4426404

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

Binding
Inhibition of recombinant human FGFR1 using poly (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA
30
Total Activities
30
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 Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors.
Zhao B, Li Y, Xu P, Dai Y, Luo C, Sun Y, Ai J, Geng M, Duan W.
ACS Med Chem Lett (2016) 7 : 629 -634
PubMed 27326339 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 8.38 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4557949 1 9.70
CHEMBL4542061 1 9.70
CHEMBL4447359 1 9.52
CHEMBL4447575 1 9.52
CHEMBL4553127 1 9.52
CHEMBL4469836 1 9.52
CHEMBL4567187 1 9.30
CHEMBL4441872 1 9.22
CHEMBL3348846 FEXAGRATINIB 2.0 1 8.92
CHEMBL4576419 1 8.85
CHEMBL4562845 1 8.48
CHEMBL4559114 1 8.41
CHEMBL4561437 1 8.39
CHEMBL4533292 1 8.21
CHEMBL4467102 1 8.16
CHEMBL4593639 1 8.14
CHEMBL4450368 1 8.11
CHEMBL4445710 1 8.11
CHEMBL4464372 1 8.06
CHEMBL4569919 1 8.06
CHEMBL4574280 1 7.98
CHEMBL4466283 1 7.93
CHEMBL4557543 1 7.85
CHEMBL4571948 1 7.85
CHEMBL4440491 1 7.84
CHEMBL4448605 1 7.78
CHEMBL4535664 1 7.37
CHEMBL4527389 1 7.13
CHEMBL4437058 1 5.43
CHEMBL4580145 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4557949 IC50 = 0.2 nM 9.70
CHEMBL4542061 IC50 = 0.2 nM 9.70
CHEMBL4447359 IC50 = 0.3 nM 9.52
CHEMBL4447575 IC50 = 0.3 nM 9.52
CHEMBL4553127 IC50 = 0.3 nM 9.52
CHEMBL4469836 IC50 = 0.3 nM 9.52
CHEMBL4567187 IC50 = 0.5 nM 9.30
CHEMBL4441872 IC50 = 0.6 nM 9.22
CHEMBL3348846 FEXAGRATINIB IC50 = 1.2 nM 8.92
CHEMBL4576419 IC50 = 1.4 nM 8.85
CHEMBL4562845 IC50 = 3.3 nM 8.48
CHEMBL4559114 IC50 = 3.9 nM 8.41
CHEMBL4561437 IC50 = 4.1 nM 8.39
CHEMBL4533292 IC50 = 6.2 nM 8.21
CHEMBL4467102 IC50 = 6.9 nM 8.16
CHEMBL4593639 IC50 = 7.2 nM 8.14
CHEMBL4450368 IC50 = 7.8 nM 8.11
CHEMBL4445710 IC50 = 7.7 nM 8.11
CHEMBL4464372 IC50 = 8.8 nM 8.06
CHEMBL4569919 IC50 = 8.8 nM 8.06
CHEMBL4574280 IC50 = 10.5 nM 7.98
CHEMBL4466283 IC50 = 11.7 nM 7.93
CHEMBL4557543 IC50 = 14.0 nM 7.85
CHEMBL4571948 IC50 = 14.2 nM 7.85
CHEMBL4440491 IC50 = 14.5 nM 7.84
CHEMBL4448605 IC50 = 16.5 nM 7.78
CHEMBL4535664 IC50 = 42.4 nM 7.37
CHEMBL4527389 IC50 = 74.4 nM 7.13
CHEMBL4437058 IC50 = 3709.0 nM 5.43
CHEMBL4580145 IC50 > 5000.0 nM -