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Assay Detail

CHEMBL818902

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

Binding
Inhibitory activity against avian c-Src tyrosine kinase was determined.
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Aves
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and structure-activity relationships of 7-substituted 3-(2, 6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones as selective inhibitors of pp60(c-src).
Thompson AM, Rewcastle GW, Boushelle SL, Hartl BG, Kraker AJ, Lu GH, Batley BL, Panek RL, Showalter HD, Denny WA.
J Med Chem (2000) 43 : 3134 -3147
PubMed 10956222 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 6.96 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL106772 1 8.10
CHEMBL49120 PD-0166285 1.0 1 8.05
CHEMBL51283 1 8.00
CHEMBL104779 1 8.00
CHEMBL419914 1 7.96
CHEMBL104357 1 7.85
CHEMBL110403 1 7.80
CHEMBL104153 1 7.70
CHEMBL301612 1 7.70
CHEMBL104414 1 7.64
CHEMBL107423 1 7.62
CHEMBL104071 1 7.55
CHEMBL107458 1 7.50
CHEMBL108332 1 7.46
CHEMBL108333 1 7.39
CHEMBL104322 1 7.38
CHEMBL107676 1 7.36
CHEMBL320382 1 7.35
CHEMBL108013 1 7.23
CHEMBL106232 1 7.22
CHEMBL104244 1 7.16
CHEMBL107277 1 7.11
CHEMBL104304 1 6.96
CHEMBL299194 1 6.82
CHEMBL106295 1 6.70
CHEMBL106992 1 6.60
CHEMBL49596 1 6.58
CHEMBL420477 1 6.52
CHEMBL108004 1 6.46
CHEMBL107071 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL106772 IC50 = 8.0 nM 8.10
CHEMBL49120 PD-0166285 IC50 = 9.0 nM 8.05
CHEMBL104779 IC50 = 10.0 nM 8.00
CHEMBL51283 IC50 = 10.0 nM 8.00
CHEMBL419914 IC50 = 11.0 nM 7.96
CHEMBL104357 IC50 = 14.0 nM 7.85
CHEMBL110403 IC50 = 16.0 nM 7.80
CHEMBL104153 IC50 = 20.0 nM 7.70
CHEMBL301612 IC50 = 20.0 nM 7.70
CHEMBL104414 IC50 = 23.0 nM 7.64
CHEMBL107423 IC50 = 24.0 nM 7.62
CHEMBL104071 IC50 = 28.0 nM 7.55
CHEMBL107458 IC50 = 32.0 nM 7.50
CHEMBL108332 IC50 = 35.0 nM 7.46
CHEMBL108333 IC50 = 41.0 nM 7.39
CHEMBL104322 IC50 = 42.0 nM 7.38
CHEMBL107676 IC50 = 44.0 nM 7.36
CHEMBL320382 IC50 = 45.0 nM 7.35
CHEMBL108013 IC50 = 59.0 nM 7.23
CHEMBL106232 IC50 = 60.0 nM 7.22
CHEMBL104244 IC50 = 70.0 nM 7.16
CHEMBL107277 IC50 = 78.0 nM 7.11
CHEMBL104304 IC50 = 110.0 nM 6.96
CHEMBL299194 IC50 = 150.0 nM 6.82
CHEMBL106295 IC50 = 200.0 nM 6.70
CHEMBL106992 IC50 = 250.0 nM 6.60
CHEMBL49596 IC50 = 260.0 nM 6.58
CHEMBL420477 IC50 = 300.0 nM 6.52
CHEMBL108004 IC50 = 350.0 nM 6.46
CHEMBL107071 IC50 = 420.0 nM 6.38
CHEMBL48172 IC50 = 530.0 nM 6.28
CHEMBL106953 IC50 = 540.0 nM 6.27
CHEMBL106839 IC50 = 550.0 nM 6.26
CHEMBL107472 IC50 = 750.0 nM 6.12
CHEMBL323453 IC50 = 790.0 nM 6.10
CHEMBL50470 IC50 = 960.0 nM 6.02
CHEMBL322005 IC50 = 1000.0 nM 6.00
CHEMBL318519 IC50 = 1800.0 nM 5.75
CHEMBL107418 IC50 = 13000.0 nM 4.89
CHEMBL106379 IC50 = 29000.0 nM 4.54
CHEMBL108170 IC50 > 50000.0 nM -
CHEMBL107177 IC50 > 50000.0 nM -
CHEMBL420473 IC50 > 50000.0 nM -
CHEMBL104532 IC50 > 50000.0 nM -
CHEMBL107247 IC50 > 50000.0 nM -
CHEMBL107372 IC50 > 50000.0 nM -
CHEMBL323017 IC50 > 50000.0 nM -