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Assay Detail

CHEMBL676884

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

Binding
Inhibition of the fibroblast growth factor receptor (FGFR1)
28
Total Activities
28
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

Discovery and structure-activity studies of a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors
Connolly CJ, Hamby JM, Schroeder MC, Barvian M, Lu GH, Panek RL, Amar A, Shen C, Kraker AJ, Fry DW, Klohs WD, Doherty AM
Bioorg Med Chem Lett (1997) 7 : 2415 -2420
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.02 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL299763 1 7.22
CHEMBL77781 1 6.96
CHEMBL312048 1 6.96
CHEMBL57366 1 6.85
CHEMBL79274 1 6.80
CHEMBL312454 1 6.75
CHEMBL81615 1 6.57
CHEMBL300171 1 6.54
CHEMBL82431 1 6.47
CHEMBL81146 1 6.44
CHEMBL57323 1 6.40
CHEMBL78485 1 6.17
CHEMBL56236 1 6.15
CHEMBL312148 1 6.05
CHEMBL81975 1 5.96
CHEMBL81474 1 5.95
CHEMBL78393 1 5.85
CHEMBL78555 1 5.79
CHEMBL309470 1 5.78
CHEMBL48809 1 5.78
CHEMBL312055 1 5.40
CHEMBL445893 1 5.11
CHEMBL76599 1 5.10
CHEMBL421145 1 4.95
CHEMBL79241 1 4.95
CHEMBL50371 1 4.80
CHEMBL78802 1 4.69
CHEMBL49658 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL299763 IC50 = 60.0 nM 7.22
CHEMBL77781 IC50 = 110.0 nM 6.96
CHEMBL312048 IC50 = 110.0 nM 6.96
CHEMBL57366 IC50 = 140.0 nM 6.85
CHEMBL79274 IC50 = 160.0 nM 6.80
CHEMBL312454 IC50 = 180.0 nM 6.75
CHEMBL81615 IC50 = 270.0 nM 6.57
CHEMBL300171 IC50 = 290.0 nM 6.54
CHEMBL82431 IC50 = 340.0 nM 6.47
CHEMBL81146 IC50 = 360.0 nM 6.44
CHEMBL57323 IC50 = 400.0 nM 6.40
CHEMBL78485 IC50 = 670.0 nM 6.17
CHEMBL56236 IC50 = 710.0 nM 6.15
CHEMBL312148 IC50 = 890.0 nM 6.05
CHEMBL81975 IC50 = 1100.0 nM 5.96
CHEMBL81474 IC50 = 1130.0 nM 5.95
CHEMBL78393 IC50 = 1400.0 nM 5.85
CHEMBL78555 IC50 = 1620.0 nM 5.79
CHEMBL309470 IC50 = 1670.0 nM 5.78
CHEMBL48809 IC50 = 1650.0 nM 5.78
CHEMBL312055 IC50 = 3970.0 nM 5.40
CHEMBL445893 IC50 = 7760.0 nM 5.11
CHEMBL76599 IC50 = 8000.0 nM 5.10
CHEMBL421145 IC50 = 11220.0 nM 4.95
CHEMBL79241 IC50 = 11220.0 nM 4.95
CHEMBL50371 IC50 = 16000.0 nM 4.80
CHEMBL78802 IC50 = 20250.0 nM 4.69
CHEMBL49658 IC50 > 50000.0 nM -