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Assay Detail

CHEMBL928170

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

Binding
Inhibition of cKit
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mast/stem cell growth factor receptor Kit (CHEMBL1936)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors.
Gracias V, Ji Z, Akritopoulou-Zanze I, Abad-Zapatero C, Huth JR, Song D, Hajduk PJ, Johnson EF, Glaser KB, Marcotte PA, Pease L, Soni NB, Stewart KD, Davidsen SK, Michaelides MR, Djuric SW.
Bioorg Med Chem Lett (2008) 18 : 2691 -2695
PubMed 18362070 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.44 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL260092 1 8.22
CHEMBL411903 1 7.96
CHEMBL403706 1 7.92
CHEMBL409872 1 7.75
CHEMBL429516 1 7.66
CHEMBL410731 1 7.55
CHEMBL259013 1 7.46
CHEMBL262607 1 7.43
CHEMBL412102 1 7.30
CHEMBL260848 1 7.04
CHEMBL263374 1 5.52
CHEMBL260093 1 -
CHEMBL409839 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL260092 IC50 = 6.0 nM 8.22
CHEMBL411903 IC50 = 11.0 nM 7.96
CHEMBL403706 IC50 = 12.0 nM 7.92
CHEMBL409872 IC50 = 18.0 nM 7.75
CHEMBL429516 IC50 = 22.0 nM 7.66
CHEMBL410731 IC50 = 28.0 nM 7.55
CHEMBL259013 IC50 = 35.0 nM 7.46
CHEMBL262607 IC50 = 37.0 nM 7.43
CHEMBL412102 IC50 = 50.0 nM 7.30
CHEMBL260848 IC50 = 91.0 nM 7.04
CHEMBL263374 IC50 = 3022.0 nM 5.52
CHEMBL260093 IC50 - -
CHEMBL409839 IC50 > 13000.0 nM -