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Assay Detail

CHEMBL770466

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

Binding
Inhibitory activity against platelet-derived growth factor receptor tyrosine kinase in Swiss 3T3 cells
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type NIH3T3
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Platelet-derived growth factor receptor (CHEMBL2096980)
Type PROTEIN COMPLEX
Organism Mus musculus

Publication

Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: structure-activity relationships in quinoxalines, quinolines, and indole tyrphostins.
Gazit A, App H, McMahon G, Chen J, Levitzki A, Bohmer FD.
J Med Chem (1996) 39 : 2170 -2177
PubMed 8667360 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 5.08 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7724 AG1295 1 6.40
CHEMBL420364 1 6.22
CHEMBL71191 1 6.10
CHEMBL69644 1 6.05
CHEMBL441987 1 6.00
CHEMBL68902 1 5.22
CHEMBL69695 1 5.00
CHEMBL69737 1 5.00
CHEMBL69438 1 4.60
CHEMBL309129 1 4.46
CHEMBL69272 1 4.05
CHEMBL67748 1 4.00
CHEMBL264381 1 4.00
CHEMBL69151 1 4.00
CHEMBL305978 1 -
CHEMBL70241 1 -
CHEMBL68613 1 -
CHEMBL71691 1 -
CHEMBL71268 1 -
CHEMBL67865 1 -
CHEMBL69931 1 -
CHEMBL66444 1 -
CHEMBL65927 1 -
CHEMBL71623 1 -
CHEMBL65968 1 -
CHEMBL68500 ALLOXAZINE 1 -
CHEMBL69328 1 -
CHEMBL70063 1 -
CHEMBL68612 1 -
CHEMBL302245 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7724 AG1295 IC50 = 400.0 nM 6.40
CHEMBL420364 IC50 = 600.0 nM 6.22
CHEMBL71191 IC50 = 800.0 nM 6.10
CHEMBL69644 IC50 = 900.0 nM 6.05
CHEMBL441987 IC50 = 1000.0 nM 6.00
CHEMBL68902 IC50 = 6000.0 nM 5.22
CHEMBL69695 IC50 = 10000.0 nM 5.00
CHEMBL69737 IC50 = 10000.0 nM 5.00
CHEMBL69438 IC50 = 25000.0 nM 4.60
CHEMBL309129 IC50 = 35000.0 nM 4.46
CHEMBL69272 IC50 = 90000.0 nM 4.05
CHEMBL67748 IC50 = 100000.0 nM 4.00
CHEMBL264381 IC50 = 100000.0 nM 4.00
CHEMBL69151 IC50 = 100000.0 nM 4.00
CHEMBL302548 IC50 > 100000.0 nM -
CHEMBL67261 IC50 > 50000.0 nM -
CHEMBL67260 IC50 > 50000.0 nM -
CHEMBL69930 IC50 > 100000.0 nM -
CHEMBL71884 IC50 > 50000.0 nM -
CHEMBL71181 IC50 > 50000.0 nM -
CHEMBL68783 IC50 > 50000.0 nM -
CHEMBL66073 IC50 > 50000.0 nM -
CHEMBL305450 IC50 > 50000.0 nM -
CHEMBL69156 IC50 > 50000.0 nM -
CHEMBL66174 IC50 > 50000.0 nM -
CHEMBL307118 IC50 > 50000.0 nM -
CHEMBL69087 IC50 > 50000.0 nM -
CHEMBL69662 IC50 > 100000.0 nM -
CHEMBL65998 IC50 > 100000.0 nM -
CHEMBL305451 IC50 > 100000.0 nM -
CHEMBL305978 IC50 > 100000.0 nM -
CHEMBL70241 IC50 > 50000.0 nM -
CHEMBL68613 IC50 > 100000.0 nM -
CHEMBL71691 IC50 > 50000.0 nM -
CHEMBL71268 IC50 > 50000.0 nM -
CHEMBL67865 IC50 > 100000.0 nM -
CHEMBL69931 IC50 > 50000.0 nM -
CHEMBL66444 IC50 > 50000.0 nM -
CHEMBL65927 IC50 > 100000.0 nM -
CHEMBL71623 IC50 > 50000.0 nM -
CHEMBL65968 IC50 > 50000.0 nM -
CHEMBL68500 ALLOXAZINE IC50 > 50000.0 nM -
CHEMBL69328 IC50 > 100000.0 nM -
CHEMBL70063 IC50 > 100000.0 nM -
CHEMBL68612 IC50 > 50000.0 nM -
CHEMBL302245 IC50 > 50000.0 nM -