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Assay Detail

CHEMBL882600

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

Binding
Inhibitory concentration against cKit with 4 uM Biotin-Ahx-AEEEYFFLFA-amide for 1 hr at ambient temperature
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.
Dai Y, Guo Y, Frey RR, Ji Z, Curtin ML, Ahmed AA, Albert DH, Arnold L, Arries SS, Barlozzari T, Bauch JL, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Guo J, Li J, Marcotte PA, Marsh KC, Moskey MD, Pease LJ, Stewart KD, Stoll VS, Tapang P, Wishart N, Davidsen SK, Michaelides MR.
J Med Chem (2005) 48 : 6066 -6083
PubMed 16162008 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 7.11 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196363 1 8.22
CHEMBL371329 1 8.05
CHEMBL365784 1 7.82
CHEMBL371206 1 7.72
CHEMBL371889 1 7.72
CHEMBL382517 1 7.66
CHEMBL198297 1 7.58
CHEMBL425749 1 7.57
CHEMBL196747 1 7.57
CHEMBL370545 1 7.55
CHEMBL366241 1 7.55
CHEMBL372174 1 7.54
CHEMBL197592 1 7.50
CHEMBL196499 1 7.48
CHEMBL197353 1 7.43
CHEMBL371510 1 7.42
CHEMBL195828 1 7.37
CHEMBL194236 1 7.32
CHEMBL445394 1 7.30
CHEMBL195955 1 7.30
CHEMBL196615 1 7.27
CHEMBL438797 1 7.17
CHEMBL371225 1 7.09
CHEMBL198267 1 7.08
CHEMBL194321 1 6.96
CHEMBL370325 1 6.85
CHEMBL197635 1 6.80
CHEMBL381034 1 6.76
CHEMBL194366 1 6.75
CHEMBL381207 1 6.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196363 IC50 = 6.0 nM 8.22
CHEMBL371329 IC50 = 9.0 nM 8.05
CHEMBL365784 IC50 = 15.0 nM 7.82
CHEMBL371206 IC50 = 19.0 nM 7.72
CHEMBL371889 IC50 = 19.0 nM 7.72
CHEMBL382517 IC50 = 22.0 nM 7.66
CHEMBL198297 IC50 = 26.0 nM 7.58
CHEMBL425749 IC50 = 27.0 nM 7.57
CHEMBL196747 IC50 = 27.0 nM 7.57
CHEMBL366241 IC50 = 28.0 nM 7.55
CHEMBL370545 IC50 = 28.0 nM 7.55
CHEMBL372174 IC50 = 29.0 nM 7.54
CHEMBL197592 IC50 = 32.0 nM 7.50
CHEMBL196499 IC50 = 33.0 nM 7.48
CHEMBL197353 IC50 = 37.0 nM 7.43
CHEMBL371510 IC50 = 38.0 nM 7.42
CHEMBL195828 IC50 = 43.0 nM 7.37
CHEMBL194236 IC50 = 48.0 nM 7.32
CHEMBL195955 IC50 = 50.0 nM 7.30
CHEMBL445394 IC50 = 50.0 nM 7.30
CHEMBL196615 IC50 = 54.0 nM 7.27
CHEMBL438797 IC50 = 68.0 nM 7.17
CHEMBL371225 IC50 = 82.0 nM 7.09
CHEMBL198267 IC50 = 83.0 nM 7.08
CHEMBL194321 IC50 = 110.0 nM 6.96
CHEMBL370325 IC50 = 140.0 nM 6.85
CHEMBL197635 IC50 = 160.0 nM 6.80
CHEMBL381034 IC50 = 175.0 nM 6.76
CHEMBL194366 IC50 = 180.0 nM 6.75
CHEMBL381207 IC50 = 182.0 nM 6.74
CHEMBL371332 IC50 = 200.0 nM 6.70
CHEMBL198155 IC50 = 360.0 nM 6.44
CHEMBL198601 IC50 = 400.0 nM 6.40
CHEMBL194842 IC50 = 580.0 nM 6.24
CHEMBL372388 IC50 = 800.0 nM 6.10
CHEMBL371379 IC50 = 790.0 nM 6.10
CHEMBL196636 IC50 = 810.0 nM 6.09
CHEMBL382112 IC50 = 930.0 nM 6.03
CHEMBL369908 IC50 = 960.0 nM 6.02