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Assay Detail

CHEMBL908982

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

Binding
Inhibition of human recombinant Src kinase
45
Total Activities
45
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

Proto-oncogene tyrosine-protein kinase Src (CHEMBL267)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.
Noronha G, Barrett K, Cao J, Dneprovskaia E, Fine R, Gong X, Gritzen C, Hood J, Kang X, Klebansky B, Li G, Liao W, Lohse D, Mak CC, McPherson A, Palanki MS, Pathak VP, Renick J, Soll R, Splittgerber U, Wrasidlo W, Zeng B, Zhao N, Zhou Y.
Bioorg Med Chem Lett (2006) 16 : 5546 -5550
PubMed 16931012 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 6.72 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL218549 1 8.22
CHEMBL436137 1 8.15
CHEMBL221742 1 8.05
CHEMBL218656 1 8.00
CHEMBL218102 1 8.00
CHEMBL221236 1 7.68
CHEMBL220931 1 7.58
CHEMBL434578 1 7.50
CHEMBL220929 1 7.44
CHEMBL375433 1 7.40
CHEMBL221582 1 7.40
CHEMBL218386 1 7.39
CHEMBL221431 1 6.96
CHEMBL217961 1 6.89
CHEMBL221975 1 6.89
CHEMBL218281 1 6.89
CHEMBL446951 1 6.86
CHEMBL218597 1 6.85
CHEMBL220798 1 6.85
CHEMBL218742 1 6.75
CHEMBL220912 1 6.62
CHEMBL436516 1 6.50
CHEMBL374248 1 6.39
CHEMBL218049 1 6.32
CHEMBL220480 1 6.02
CHEMBL218317 1 5.82
CHEMBL218042 1 5.82
CHEMBL218598 1 5.75
CHEMBL374002 1 5.66
CHEMBL218072 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL218549 IC50 = 6.0 nM 8.22
CHEMBL436137 IC50 = 7.0 nM 8.15
CHEMBL221742 IC50 = 9.0 nM 8.05
CHEMBL218656 IC50 = 10.0 nM 8.00
CHEMBL218102 IC50 = 10.0 nM 8.00
CHEMBL221236 IC50 = 21.0 nM 7.68
CHEMBL220931 IC50 = 26.0 nM 7.58
CHEMBL434578 IC50 = 32.0 nM 7.50
CHEMBL220929 IC50 = 36.0 nM 7.44
CHEMBL375433 IC50 = 40.0 nM 7.40
CHEMBL221582 IC50 = 40.0 nM 7.40
CHEMBL218386 IC50 = 41.0 nM 7.39
CHEMBL221431 IC50 = 110.0 nM 6.96
CHEMBL218281 IC50 = 128.0 nM 6.89
CHEMBL221975 IC50 = 130.0 nM 6.89
CHEMBL217961 IC50 = 130.0 nM 6.89
CHEMBL446951 IC50 = 137.0 nM 6.86
CHEMBL218597 IC50 = 140.0 nM 6.85
CHEMBL220798 IC50 = 140.0 nM 6.85
CHEMBL218742 IC50 = 180.0 nM 6.75
CHEMBL220912 IC50 = 240.0 nM 6.62
CHEMBL436516 IC50 = 320.0 nM 6.50
CHEMBL374248 IC50 = 410.0 nM 6.39
CHEMBL218049 IC50 = 480.0 nM 6.32
CHEMBL220480 IC50 = 960.0 nM 6.02
CHEMBL218317 IC50 = 1500.0 nM 5.82
CHEMBL218042 IC50 = 1500.0 nM 5.82
CHEMBL218598 IC50 = 1800.0 nM 5.75
CHEMBL374002 IC50 = 2200.0 nM 5.66
CHEMBL218072 IC50 = 3600.0 nM 5.44
CHEMBL385112 IC50 = 5200.0 nM 5.28
CHEMBL218177 IC50 = 7400.0 nM 5.13
CHEMBL218003 IC50 = 12000.0 nM 4.92
CHEMBL384877 IC50 = 12000.0 nM 4.92
CHEMBL218842 IC50 > 50000.0 nM -
CHEMBL218551 IC50 > 50000.0 nM -
CHEMBL441545 IC50 > 50000.0 nM -
CHEMBL374868 IC50 > 50000.0 nM -
CHEMBL218738 IC50 > 50000.0 nM -
CHEMBL221739 IC50 > 50000.0 nM -
CHEMBL218411 IC50 > 50000.0 nM -
CHEMBL376052 IC50 > 50000.0 nM -
CHEMBL218160 IC50 > 50000.0 nM -
CHEMBL376860 IC50 > 50000.0 nM -
CHEMBL218109 IC50 > 50000.0 nM -