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Assay Detail

CHEMBL676879

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

Binding
Inhibition of mouse fibroblast growth factor receptor tyrosine kinase (FGFr)
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Expert

Target

Fibroblast growth factor receptor (CHEMBL2111391)
Type PROTEIN FAMILY
Organism Mus musculus

Publication

Synthesis and tyrosine kinase inhibitory activity of a series of 2-amino-8H-pyrido[2,3-d]pyrimidines: identification of potent, selective platelet-derived growth factor receptor tyrosine kinase inhibitors.
Boschelli DH, Wu Z, Klutchko SR, Showalter HD, Hamby JM, Lu GH, Major TC, Dahring TK, Batley B, Panek RL, Keiser J, Hartl BG, Kraker AJ, Klohs WD, Roberts BJ, Patmore S, Elliott WL, Steinkampf R, Bradford LA, Hallak H, Doherty AM.
J Med Chem (1998) 41 : 4365 -4377
PubMed 9784112 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.03 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112914 1 7.52
CHEMBL49120 PD-0166285 1.0 1 7.37
CHEMBL136106 1 7.06
CHEMBL136244 1 6.46
CHEMBL136280 1 6.43
CHEMBL337157 1 6.30
CHEMBL136775 1 6.29
CHEMBL139249 1 6.27
CHEMBL138319 1 6.24
CHEMBL336093 1 6.14
CHEMBL140242 1 6.06
CHEMBL134851 1 5.96
CHEMBL49596 1 5.89
CHEMBL341579 1 5.85
CHEMBL434448 1 5.82
CHEMBL138994 1 5.77
CHEMBL136457 1 5.77
CHEMBL136332 1 5.54
CHEMBL139040 1 5.50
CHEMBL136688 1 5.33
CHEMBL137611 1 5.30
CHEMBL136874 1 5.10
CHEMBL136724 1 4.65
CHEMBL343705 1 -
CHEMBL139633 1 -
CHEMBL421928 1 -
CHEMBL337100 1 -
CHEMBL342475 1 -
CHEMBL137388 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112914 IC50 = 30.0 nM 7.52
CHEMBL49120 PD-0166285 IC50 = 43.0 nM 7.37
CHEMBL136106 IC50 = 88.0 nM 7.06
CHEMBL136244 IC50 = 350.0 nM 6.46
CHEMBL136280 IC50 = 370.0 nM 6.43
CHEMBL337157 IC50 = 500.0 nM 6.30
CHEMBL136775 IC50 = 510.0 nM 6.29
CHEMBL139249 IC50 = 540.0 nM 6.27
CHEMBL138319 IC50 = 580.0 nM 6.24
CHEMBL336093 IC50 = 720.0 nM 6.14
CHEMBL140242 IC50 = 880.0 nM 6.06
CHEMBL134851 IC50 = 1100.0 nM 5.96
CHEMBL49596 IC50 = 1300.0 nM 5.89
CHEMBL341579 IC50 = 1400.0 nM 5.85
CHEMBL434448 IC50 = 1500.0 nM 5.82
CHEMBL138994 IC50 = 1700.0 nM 5.77
CHEMBL136457 IC50 = 1700.0 nM 5.77
CHEMBL136332 IC50 = 2900.0 nM 5.54
CHEMBL139040 IC50 = 3200.0 nM 5.50
CHEMBL136688 IC50 = 4700.0 nM 5.33
CHEMBL137611 IC50 = 5000.0 nM 5.30
CHEMBL136874 IC50 = 7900.0 nM 5.10
CHEMBL136724 IC50 = 22600.0 nM 4.65
CHEMBL343705 IC50 > 50000.0 nM -
CHEMBL139633 IC50 > 50000.0 nM -
CHEMBL421928 IC50 > 50000.0 nM -
CHEMBL337100 IC50 > 50000.0 nM -
CHEMBL342475 IC50 > 50000.0 nM -
CHEMBL137388 IC50 > 50000.0 nM -