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Assay Detail

CHEMBL1764817

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Binding
Inhibition FGFR1
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series.
Barlaam B, Ducray R, Lambert-van der Brempt C, Plé P, Bardelle C, Brooks N, Coleman T, Cross D, Kettle JG, Read J.
Bioorg Med Chem Lett (2011) 21 : 2207 -2211
PubMed 21441027 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.30 7.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1762531 1 7.25
CHEMBL1762524 1 6.95
CHEMBL1762535 1 6.85
CHEMBL1762525 1 6.74
CHEMBL1762521 1 6.50
CHEMBL1762527 1 6.46
CHEMBL1762529 1 6.35
CHEMBL1762523 1 6.30
CHEMBL1762522 1 6.18
CHEMBL1762549 1 6.14
CHEMBL1762528 1 6.13
CHEMBL1762534 1 6.00
CHEMBL1762533 1 5.86
CHEMBL1762532 1 5.81
CHEMBL1762526 1 5.80
CHEMBL1762530 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1762531 IC50 = 56.0 nM 7.25
CHEMBL1762524 IC50 = 112.0 nM 6.95
CHEMBL1762535 IC50 = 140.0 nM 6.85
CHEMBL1762525 IC50 = 183.0 nM 6.74
CHEMBL1762521 IC50 = 313.0 nM 6.50
CHEMBL1762527 IC50 = 350.0 nM 6.46
CHEMBL1762529 IC50 = 447.0 nM 6.35
CHEMBL1762523 IC50 = 501.0 nM 6.30
CHEMBL1762522 IC50 = 662.0 nM 6.18
CHEMBL1762549 IC50 = 720.0 nM 6.14
CHEMBL1762528 IC50 = 738.0 nM 6.13
CHEMBL1762534 IC50 = 998.0 nM 6.00
CHEMBL1762533 IC50 = 1380.0 nM 5.86
CHEMBL1762532 IC50 = 1550.0 nM 5.81
CHEMBL1762526 IC50 = 1580.0 nM 5.80
CHEMBL1762530 IC50 = 3340.0 nM 5.48