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Assay Detail

CHEMBL4018627

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

Binding
Inhibition of recombinant human FGFR3 using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA
35
Total Activities
35
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 3 (CHEMBL2742)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer.
Zhu W, Chen H, Wang Y, Wang J, Peng X, Chen X, Gao Y, Li C, He Y, Ai J, Geng M, Zheng M, Liu H.
J Med Chem (2017) 60 : 6018 -6035
PubMed 28714692 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 6.95 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3348846 FEXAGRATINIB 2.0 1 8.26
CHEMBL4073545 1 8.10
CHEMBL4075917 1 7.80
CHEMBL4084388 1 7.64
CHEMBL4067871 1 7.64
CHEMBL4074407 1 7.56
CHEMBL4062877 1 7.56
CHEMBL4076118 1 7.45
CHEMBL4077448 1 7.23
CHEMBL4105329 1 7.14
CHEMBL4082721 1 7.03
CHEMBL4084547 1 6.60
CHEMBL4086068 1 6.55
CHEMBL4094883 1 6.41
CHEMBL4095830 1 6.40
CHEMBL4071491 1 6.37
CHEMBL4100031 1 6.36
CHEMBL4060706 1 6.25
CHEMBL4077119 1 6.23
CHEMBL4078176 1 6.01
CHEMBL4062871 1 5.44
CHEMBL4075768 1 -
CHEMBL4092280 1 -
CHEMBL4082577 1 -
CHEMBL4102355 1 -
CHEMBL4064545 1 -
CHEMBL4068491 1 -
CHEMBL4100109 1 -
CHEMBL4101681 1 -
CHEMBL4091460 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3348846 FEXAGRATINIB IC50 = 5.5 nM 8.26
CHEMBL4073545 IC50 = 8.0 nM 8.10
CHEMBL4075917 IC50 = 15.9 nM 7.80
CHEMBL4084388 IC50 = 22.8 nM 7.64
CHEMBL4067871 IC50 = 23.0 nM 7.64
CHEMBL4074407 IC50 = 27.6 nM 7.56
CHEMBL4062877 IC50 = 27.5 nM 7.56
CHEMBL4076118 IC50 = 35.3 nM 7.45
CHEMBL4077448 IC50 = 58.4 nM 7.23
CHEMBL4105329 IC50 = 73.1 nM 7.14
CHEMBL4082721 IC50 = 93.9 nM 7.03
CHEMBL4084547 IC50 = 250.5 nM 6.60
CHEMBL4086068 IC50 = 279.9 nM 6.55
CHEMBL4094883 IC50 = 388.0 nM 6.41
CHEMBL4095830 IC50 = 401.5 nM 6.40
CHEMBL4071491 IC50 = 430.5 nM 6.37
CHEMBL4100031 IC50 = 433.8 nM 6.36
CHEMBL4060706 IC50 = 560.7 nM 6.25
CHEMBL4077119 IC50 = 591.5 nM 6.23
CHEMBL4078176 IC50 = 969.7 nM 6.01
CHEMBL4062871 IC50 = 3653.5 nM 5.44
CHEMBL4101542 IC50 > 1000.0 nM -
CHEMBL4082023 IC50 > 1000.0 nM -
CHEMBL4102447 IC50 > 1000.0 nM -
CHEMBL4063010 IC50 > 1000.0 nM -
CHEMBL4083543 IC50 > 1000.0 nM -
CHEMBL4091460 IC50 > 1000.0 nM -
CHEMBL4101681 IC50 > 1000.0 nM -
CHEMBL4100109 IC50 > 1000.0 nM -
CHEMBL4068491 IC50 > 1000.0 nM -
CHEMBL4064545 IC50 > 1000.0 nM -
CHEMBL4102355 IC50 > 1000.0 nM -
CHEMBL4082577 IC50 > 1000.0 nM -
CHEMBL4092280 IC50 > 1000.0 nM -
CHEMBL4075768 IC50 > 1000.0 nM -