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Assay Detail

CHEMBL1959283

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

Binding
Inhibition of PDGFBB-induced PDGFRbeta autophosphorylation in human SF539 cells incubated for 60 mins prior to PDGFBB-induction measured after 10 mins by phosphotyrosine ELISA
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SF-539
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

N⁴-(3-Bromophenyl)-7-(substituted benzyl) pyrrolo[2,3-d]pyrimidines as potent multiple receptor tyrosine kinase inhibitors: design, synthesis, and in vivo evaluation.
Gangjee A, Zaware N, Raghavan S, Yang J, Thorpe JE, Ihnat MA.
Bioorg Med Chem (2012) 20 : 2444 -2454
PubMed 22370340 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.31 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1956890 1 5.82
CHEMBL1956898 1 5.75
CHEMBL7724 AG1295 1 5.21
CHEMBL1956893 1 4.47
CHEMBL1956891 1 -
CHEMBL1956888 1 -
CHEMBL1956894 1 -
CHEMBL1956896 1 -
CHEMBL1956889 1 -
CHEMBL1956895 1 -
CHEMBL1956897 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1956890 IC50 = 1500.0 nM 5.82
CHEMBL1956898 IC50 = 1800.0 nM 5.75
CHEMBL7724 AG1295 IC50 = 6200.0 nM 5.21
CHEMBL1956893 IC50 = 34200.0 nM 4.47
CHEMBL1956891 IC50 > 500000.0 nM -
CHEMBL1956888 IC50 > 500000.0 nM -
CHEMBL1956894 IC50 = 229600.0 nM -
CHEMBL1956896 IC50 = 212400.0 nM -
CHEMBL1956889 IC50 = 159600.0 nM -
CHEMBL1956895 IC50 = 129300.0 nM -
CHEMBL1956897 IC50 = 129100.0 nM -