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Assay Detail

CHEMBL3706134

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

Binding
ADP-Glo Kinase Assay: In this assay, the inhibitory activity of a test substance against the tyrosine kinase activity of FGFR3 protein is measured.To each well of a flat bottom 96 well white plate (Sumitomo Bakelite Co., Ltd., MS-8496W), 10 ul of FGFR3 protein (Cama Biosciences, Inc., 08-135) solution diluted to 1 ug/mL with an assay buffer (20 mM HEPES NaOH, 0.01% Triton X-100, 2 mM DTT, and 5 mM MgCl2), 10 uL of an assay buffer solution containing CSK-tide substrate (Ana Spec Inc., 63843) in a final concentration 011000 nM and ATP (Promega Corporation, V9102) in a final concentration of 16.7 uM, and 5 ul of a test substance diluted with the assay buffer were added, and the reaction was performed at room temperature for 2 hours (kinase reaction). For measuring kinase activity, ADP-Glo Kinase Assay (Promega Corporation, V9102) was used. After the reaction, 25 pt of ADP-Glo reagent was added to each well of the plate, and the reaction was performed at room temperature for 40 minutes.
3
Total Activities
3
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

Monocyclic pyridine derivative
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.20 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3686884 E-7090 2.0 1 8.27
CHEMBL3686883 1 8.22
CHEMBL3686864 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3686884 E-7090 IC50 = 5.4 nM 8.27
CHEMBL3686883 IC50 = 6.0 nM 8.22
CHEMBL3686864 IC50 = 7.9 nM 8.10