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Assay Detail

CHEMBL826373

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

Functional
Inhibition of FGF-dependent human umbilical vein endothelial cell proliferation
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Endothelial cell
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Fibroblast growth factor receptor (CHEMBL2095217)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of soluble 7-substituted 3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-amines and related ureas as dual inhibitors of the fibroblast growth factor receptor-1 and vascular endothelial growth factor receptor-2 tyrosine kinases.
Thompson AM, Delaney AM, Hamby JM, Schroeder MC, Spoon TA, Crean SM, Showalter HD, Denny WA.
J Med Chem (2005) 48 : 4628 -4653
PubMed 16000000 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.92 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190161 1 9.40
CHEMBL191070 1 9.30
CHEMBL189995 1 8.72
CHEMBL192856 1 8.70
CHEMBL191023 1 8.57
CHEMBL365727 1 8.40
CHEMBL187396 1 8.36
CHEMBL425363 1 8.22
CHEMBL278472 1 8.22
CHEMBL363551 1 7.92
CHEMBL190389 1 7.85
CHEMBL188087 1 7.82
CHEMBL189584 PD-173074 1 7.82
CHEMBL189059 1 7.55
CHEMBL365140 1 7.43
CHEMBL339856 1 7.07
CHEMBL189851 1 7.06
CHEMBL188978 1 6.89
CHEMBL191265 1 6.82
CHEMBL190783 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190161 IC50 = 0.4 nM 9.40
CHEMBL191070 IC50 = 0.5 nM 9.30
CHEMBL189995 IC50 = 1.9 nM 8.72
CHEMBL192856 IC50 = 2.0 nM 8.70
CHEMBL191023 IC50 = 2.7 nM 8.57
CHEMBL365727 IC50 = 4.0 nM 8.40
CHEMBL187396 IC50 = 4.4 nM 8.36
CHEMBL425363 IC50 = 6.0 nM 8.22
CHEMBL278472 IC50 = 6.0 nM 8.22
CHEMBL363551 IC50 = 12.0 nM 7.92
CHEMBL190389 IC50 = 14.0 nM 7.85
CHEMBL188087 IC50 = 15.0 nM 7.82
CHEMBL189584 PD-173074 IC50 = 15.0 nM 7.82
CHEMBL189059 IC50 = 28.0 nM 7.55
CHEMBL365140 IC50 = 37.0 nM 7.43
CHEMBL339856 IC50 = 85.0 nM 7.07
CHEMBL189851 IC50 = 88.0 nM 7.06
CHEMBL188978 IC50 = 130.0 nM 6.89
CHEMBL191265 IC50 = 150.0 nM 6.82
CHEMBL190783 IC50 = 430.0 nM 6.37