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Assay Detail

CHEMBL832302

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

Binding
Inhibition of glutamate/tyrosine (4:1) copolymer phosphorylation by mouse platelet-derived growth factor receptor-beta
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Platelet-derived growth factor receptor beta (CHEMBL2749)
Type SINGLE PROTEIN
Organism Mus musculus

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 47 5.16 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190162 1 6.80
CHEMBL189542 1 6.35
CHEMBL365377 1 6.32
CHEMBL190188 1 6.27
CHEMBL191389 1 6.21
CHEMBL425552 1 5.92
CHEMBL191023 1 5.58
CHEMBL190161 1 5.44
CHEMBL188648 1 5.40
CHEMBL191189 1 5.33
CHEMBL192856 1 5.30
CHEMBL190389 1 5.19
CHEMBL190132 1 5.06
CHEMBL365727 1 4.96
CHEMBL190351 1 4.92
CHEMBL189584 PD-173074 1 4.85
CHEMBL187396 1 4.82
CHEMBL189995 1 4.80
CHEMBL363551 1 4.75
CHEMBL425363 1 4.64
CHEMBL190783 1 4.57
CHEMBL189691 1 4.57
CHEMBL188087 1 4.52
CHEMBL189059 1 4.51
CHEMBL278472 1 4.50
CHEMBL189851 1 4.35
CHEMBL339856 1 4.35
CHEMBL191265 1 4.30
CHEMBL189325 1 -
CHEMBL189628 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190162 IC50 = 160.0 nM 6.80
CHEMBL189542 IC50 = 450.0 nM 6.35
CHEMBL365377 IC50 = 480.0 nM 6.32
CHEMBL190188 IC50 = 540.0 nM 6.27
CHEMBL191389 IC50 = 620.0 nM 6.21
CHEMBL425552 IC50 = 1200.0 nM 5.92
CHEMBL191023 IC50 = 2600.0 nM 5.58
CHEMBL190161 IC50 = 3600.0 nM 5.44
CHEMBL188648 IC50 = 4000.0 nM 5.40
CHEMBL191189 IC50 = 4700.0 nM 5.33
CHEMBL192856 IC50 = 5000.0 nM 5.30
CHEMBL190389 IC50 = 6500.0 nM 5.19
CHEMBL190132 IC50 = 8800.0 nM 5.06
CHEMBL365727 IC50 = 11000.0 nM 4.96
CHEMBL190351 IC50 = 12000.0 nM 4.92
CHEMBL189584 PD-173074 IC50 = 14000.0 nM 4.85
CHEMBL187396 IC50 = 15000.0 nM 4.82
CHEMBL189995 IC50 = 16000.0 nM 4.80
CHEMBL363551 IC50 = 18000.0 nM 4.75
CHEMBL425363 IC50 = 23000.0 nM 4.64
CHEMBL190783 IC50 = 27000.0 nM 4.57
CHEMBL189691 IC50 = 27000.0 nM 4.57
CHEMBL188087 IC50 = 30000.0 nM 4.52
CHEMBL189059 IC50 = 31000.0 nM 4.51
CHEMBL278472 IC50 = 32000.0 nM 4.50
CHEMBL189851 IC50 = 45000.0 nM 4.35
CHEMBL339856 IC50 = 45000.0 nM 4.35
CHEMBL191265 IC50 = 50000.0 nM 4.30
CHEMBL188431 IC50 > 50000.0 nM -
CHEMBL190210 IC50 > 50000.0 nM -
CHEMBL190443 IC50 > 50000.0 nM -
CHEMBL363304 IC50 > 50000.0 nM -
CHEMBL191372 IC50 > 50000.0 nM -
CHEMBL192668 IC50 > 50000.0 nM -
CHEMBL365140 IC50 > 50000.0 nM -
CHEMBL188978 IC50 > 50000.0 nM -
CHEMBL191070 IC50 > 50000.0 nM -
CHEMBL361886 IC50 > 50000.0 nM -
CHEMBL370328 IC50 > 50000.0 nM -
CHEMBL190405 IC50 > 50000.0 nM -
CHEMBL189322 IC50 > 50000.0 nM -
CHEMBL190991 IC50 > 50000.0 nM -
CHEMBL365133 IC50 > 50000.0 nM -
CHEMBL190866 IC50 > 50000.0 nM -
CHEMBL362502 IC50 > 50000.0 nM -
CHEMBL189628 IC50 > 50000.0 nM -
CHEMBL189325 IC50 > 50000.0 nM -