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Assay Detail

CHEMBL3299342

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

Binding
Inhibition of PDGFRbeta in human SH-SY5Y cells by phosphotyrosine ELISA assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SH-SY5Y
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Platelet-derived growth factor receptor beta (CHEMBL1913)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
Zhang X, Raghavan S, Ihnat M, Thorpe JE, Disch BC, Bastian A, Bailey-Downs LC, Dybdal-Hargreaves NF, Rohena CC, Hamel E, Mooberry SL, Gangjee A.
Bioorg Med Chem (2014) 22 : 3753 -3772
PubMed 24890652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.50 7.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3297892 1 7.79
CHEMBL3298000 1 7.66
CHEMBL3297898 1 7.64
CHEMBL3297999 1 7.64
CHEMBL3297899 1 7.57
CHEMBL3297896 1 7.55
CHEMBL3297900 1 7.52
CHEMBL3297998 1 7.25
CHEMBL3297897 1 7.20
CHEMBL3297893 1 7.18
CHEMBL553 ERLOTINIB 4.0 1 -
CHEMBL53463 DOXORUBICIN 4.0 1 -
CHEMBL276711 SEMAXANIB 3.0 1 -
CHEMBL3297895 1 -
CHEMBL3297894 1 -
CHEMBL3297891 1 -
CHEMBL535 SUNITINIB 4.0 1 -
CHEMBL3297816 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3297892 IC50 = 16.2 nM 7.79
CHEMBL3298000 IC50 = 21.9 nM 7.66
CHEMBL3297898 IC50 = 22.8 nM 7.64
CHEMBL3297999 IC50 = 23.1 nM 7.64
CHEMBL3297899 IC50 = 27.1 nM 7.57
CHEMBL3297896 IC50 = 28.3 nM 7.55
CHEMBL3297900 IC50 = 29.9 nM 7.52
CHEMBL3297998 IC50 = 56.5 nM 7.25
CHEMBL3297897 IC50 = 63.5 nM 7.20
CHEMBL3297893 IC50 = 66.1 nM 7.18
CHEMBL553 ERLOTINIB IC50 - -
CHEMBL53463 DOXORUBICIN IC50 - -
CHEMBL276711 SEMAXANIB IC50 - -
CHEMBL3297895 IC50 - -
CHEMBL3297894 IC50 - -
CHEMBL3297891 IC50 - -
CHEMBL535 SUNITINIB IC50 = 83.1 nM -
CHEMBL3297816 IC50 - -