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Assay Detail

CHEMBL676971

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

Binding
Inhibition fibroblast growth factor receptor TK kinase activity at a concentration of 2 uM
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Fibroblast growth factor receptor 1 (CHEMBL3650)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors.
Hennequin LF, Stokes ES, Thomas AP, Johnstone C, Plé PA, Ogilvie DJ, Dukes M, Wedge SR, Kendrew J, Curwen JO.
J Med Chem (2002) 45 : 1300 -1312
PubMed 11881999 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 5.40 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2448066 1 6.05
CHEMBL1202473 1 5.82
CHEMBL416191 1 5.82
CHEMBL25579 1 5.80
CHEMBL422758 1 5.77
CHEMBL1907764 1 5.75
CHEMBL1907763 1 5.75
CHEMBL279459 1 5.72
CHEMBL1744349 1 5.72
CHEMBL1202477 1 5.70
CHEMBL1202478 1 5.68
CHEMBL1744347 1 5.68
CHEMBL24979 1 5.68
CHEMBL25450 1 5.60
CHEMBL26641 1 5.57
CHEMBL533849 1 5.44
CHEMBL25425 1 5.39
CHEMBL2448067 1 5.38
CHEMBL2448065 1 5.37
CHEMBL2448064 1 5.30
CHEMBL1907944 1 5.30
CHEMBL24828 VANDETANIB 4.0 1 5.22
CHEMBL24137 1 5.17
CHEMBL283088 1 5.10
CHEMBL428534 1 4.91
CHEMBL281990 1 4.87
CHEMBL25610 1 4.72
CHEMBL24026 1 4.72
CHEMBL286160 1 4.57
CHEMBL26050 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2448066 IC50 = 900.0 nM 6.05
CHEMBL1202473 IC50 = 1500.0 nM 5.82
CHEMBL416191 IC50 = 1500.0 nM 5.82
CHEMBL25579 IC50 = 1600.0 nM 5.80
CHEMBL422758 IC50 = 1700.0 nM 5.77
CHEMBL1907764 IC50 = 1800.0 nM 5.75
CHEMBL1907763 IC50 = 1800.0 nM 5.75
CHEMBL279459 IC50 = 1900.0 nM 5.72
CHEMBL1744349 IC50 = 1900.0 nM 5.72
CHEMBL1202477 IC50 = 2000.0 nM 5.70
CHEMBL1202478 IC50 = 2100.0 nM 5.68
CHEMBL1744347 IC50 = 2100.0 nM 5.68
CHEMBL24979 IC50 = 2100.0 nM 5.68
CHEMBL25450 IC50 = 2500.0 nM 5.60
CHEMBL26641 IC50 = 2700.0 nM 5.57
CHEMBL533849 IC50 = 3600.0 nM 5.44
CHEMBL25425 IC50 = 4100.0 nM 5.39
CHEMBL2448067 IC50 = 4200.0 nM 5.38
CHEMBL2448065 IC50 = 4300.0 nM 5.37
CHEMBL2448064 IC50 = 5000.0 nM 5.30
CHEMBL1907944 IC50 = 5000.0 nM 5.30
CHEMBL24828 VANDETANIB IC50 = 6000.0 nM 5.22
CHEMBL24137 IC50 = 6700.0 nM 5.17
CHEMBL283088 IC50 = 8000.0 nM 5.10
CHEMBL428534 IC50 = 12300.0 nM 4.91
CHEMBL281990 IC50 = 13500.0 nM 4.87
CHEMBL25610 IC50 = 19000.0 nM 4.72
CHEMBL24026 IC50 = 19000.0 nM 4.72
CHEMBL286160 IC50 = 27000.0 nM 4.57
CHEMBL26050 IC50 = 50000.0 nM 4.30
CHEMBL281872 ZD-4190 FREE BASE IC50 > 100000.0 nM -