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Assay Detail

CHEMBL768493

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

Binding
Inhibition of the phosphorylation of a random glutamate-tyrosine (4:1) copolymer by isolated mouse Platelet-derived growth factor protein.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Platelet-derived growth factor receptor beta (CHEMBL2749)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and related 2-urea derivatives are potent and selective inhibitors of the FGF receptor-1 tyrosine kinase.
Thompson AM, Connolly CJ, Hamby JM, Boushelle S, Hartl BG, Amar AM, Kraker AJ, Driscoll DL, Steinkampf RW, Patmore SJ, Vincent PW, Roberts BJ, Elliott WL, Klohs W, Leopold WR, Showalter HD, Denny WA.
J Med Chem (2000) 43 : 4200 -4211
PubMed 11063616 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.12 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL57366 1 5.96
CHEMBL432738 1 5.89
CHEMBL132358 1 5.75
CHEMBL133436 1 5.58
CHEMBL135889 1 5.33
CHEMBL76599 1 5.33
CHEMBL135267 1 5.11
CHEMBL422797 1 4.96
CHEMBL135061 1 4.77
CHEMBL58627 1 4.68
CHEMBL132089 1 4.46
CHEMBL134354 1 4.42
CHEMBL339856 1 4.35
CHEMBL135074 1 -
CHEMBL299763 1 -
CHEMBL422625 1 -
CHEMBL133604 1 -
CHEMBL134801 1 -
CHEMBL134066 1 -
CHEMBL56942 1 -
CHEMBL134334 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL57366 IC50 = 1100.0 nM 5.96
CHEMBL432738 IC50 = 1300.0 nM 5.89
CHEMBL132358 IC50 = 1800.0 nM 5.75
CHEMBL133436 IC50 = 2600.0 nM 5.58
CHEMBL135889 IC50 = 4700.0 nM 5.33
CHEMBL76599 IC50 = 4700.0 nM 5.33
CHEMBL135267 IC50 = 7700.0 nM 5.11
CHEMBL422797 IC50 = 11000.0 nM 4.96
CHEMBL135061 IC50 = 17000.0 nM 4.77
CHEMBL58627 IC50 = 21000.0 nM 4.68
CHEMBL132089 IC50 = 35000.0 nM 4.46
CHEMBL134354 IC50 = 38000.0 nM 4.42
CHEMBL339856 IC50 = 45000.0 nM 4.35
CHEMBL135074 IC50 > 50000.0 nM -
CHEMBL299763 IC50 > 50000.0 nM -
CHEMBL422625 IC50 > 50000.0 nM -
CHEMBL133604 IC50 > 50000.0 nM -
CHEMBL134801 IC50 > 50000.0 nM -
CHEMBL134066 IC50 > 50000.0 nM -
CHEMBL56942 IC50 > 50000.0 nM -
CHEMBL134334 IC50 > 50000.0 nM -