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Assay Detail

CHEMBL678320

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

Binding
FGFR-1 (FTK) inhibitory activity at 2 uM of ATP in vitro.
33
Total Activities
33
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

Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors.
Hennequin LF, Thomas AP, Johnstone C, Stokes ES, Plé PA, Lohmann JJ, Ogilvie DJ, Dukes M, Wedge SR, Curwen JO, Kendrew J, Lambert-van der Brempt C.
J Med Chem (1999) 42 : 5369 -5389
PubMed 10639280 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 5.06 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL433936 1 5.85
CHEMBL434311 1 5.82
CHEMBL25579 1 5.80
CHEMBL357815 1 5.75
CHEMBL440727 1 5.60
CHEMBL147192 1 5.58
CHEMBL150187 1 5.21
CHEMBL24137 1 5.17
CHEMBL150315 1 5.16
CHEMBL421961 1 5.16
CHEMBL347086 1 5.13
CHEMBL150817 1 5.03
CHEMBL147180 1 5.03
CHEMBL127907 1 4.96
CHEMBL150825 1 4.85
CHEMBL150657 1 4.80
CHEMBL25610 1 4.72
CHEMBL356658 1 4.70
CHEMBL150606 1 4.60
CHEMBL286160 1 4.57
CHEMBL26050 1 4.40
CHEMBL358672 1 4.35
CHEMBL346200 1 4.24
CHEMBL151948 1 -
CHEMBL147138 1 -
CHEMBL150826 1 -
CHEMBL151015 1 -
CHEMBL301018 1 -
CHEMBL281872 ZD-4190 FREE BASE 1.0 1 -
CHEMBL150581 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL433936 IC50 = 1400.0 nM 5.85
CHEMBL434311 IC50 = 1500.0 nM 5.82
CHEMBL25579 IC50 = 1600.0 nM 5.80
CHEMBL357815 IC50 = 1800.0 nM 5.75
CHEMBL440727 IC50 = 2500.0 nM 5.60
CHEMBL147192 IC50 = 2600.0 nM 5.58
CHEMBL150187 IC50 = 6100.0 nM 5.21
CHEMBL24137 IC50 = 6700.0 nM 5.17
CHEMBL150315 IC50 = 7000.0 nM 5.16
CHEMBL421961 IC50 = 7000.0 nM 5.16
CHEMBL347086 IC50 = 7400.0 nM 5.13
CHEMBL150817 IC50 = 9300.0 nM 5.03
CHEMBL147180 IC50 = 9400.0 nM 5.03
CHEMBL127907 IC50 = 11000.0 nM 4.96
CHEMBL150825 IC50 = 14000.0 nM 4.85
CHEMBL150657 IC50 = 16000.0 nM 4.80
CHEMBL25610 IC50 = 19000.0 nM 4.72
CHEMBL356658 IC50 = 20000.0 nM 4.70
CHEMBL150606 IC50 = 25000.0 nM 4.60
CHEMBL286160 IC50 = 27000.0 nM 4.57
CHEMBL26050 IC50 = 40000.0 nM 4.40
CHEMBL358672 IC50 = 45000.0 nM 4.35
CHEMBL346200 IC50 = 58000.0 nM 4.24
CHEMBL151948 IC50 > 50000.0 nM -
CHEMBL147138 IC50 > 100000.0 nM -
CHEMBL150826 IC50 > 33000.0 nM -
CHEMBL151015 IC50 > 100000.0 nM -
CHEMBL301018 IC50 > 100000.0 nM -
CHEMBL281872 ZD-4190 FREE BASE IC50 > 100000.0 nM -
CHEMBL150581 IC50 > 100000.0 nM -
CHEMBL148869 IC50 > 100000.0 nM -
CHEMBL151067 IC50 > 50000.0 nM -
CHEMBL345943 IC50 > 33000.0 nM -