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Assay Detail

CHEMBL693874

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

Functional
Inhibitory activity against HT-29 human colon adenocarcinoma cells was determined.
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HT-29
Confidence 1 — Organism
Curated By Expert

Target

HT-29 (CHEMBL384)
Type CELL-LINE
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 13 5.95 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL104779 1 6.85
CHEMBL106772 1 6.70
CHEMBL51283 1 6.62
CHEMBL49120 PD-0166285 1.0 1 6.55
CHEMBL107277 1 6.12
CHEMBL104414 1 6.08
CHEMBL108333 1 5.80
CHEMBL108004 1 5.72
CHEMBL108013 1 5.66
CHEMBL107071 1 5.55
CHEMBL106839 1 5.43
CHEMBL107472 1 5.39
CHEMBL299194 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL104779 IC50 = 140.0 nM 6.85
CHEMBL106772 IC50 = 200.0 nM 6.70
CHEMBL51283 IC50 = 240.0 nM 6.62
CHEMBL49120 PD-0166285 IC50 = 280.0 nM 6.55
CHEMBL107277 IC50 = 750.0 nM 6.12
CHEMBL104414 IC50 = 830.0 nM 6.08
CHEMBL108333 IC50 = 1600.0 nM 5.80
CHEMBL108004 IC50 = 1900.0 nM 5.72
CHEMBL108013 IC50 = 2200.0 nM 5.66
CHEMBL107071 IC50 = 2800.0 nM 5.55
CHEMBL106839 IC50 = 3700.0 nM 5.43
CHEMBL107472 IC50 = 4100.0 nM 5.39
CHEMBL299194 IC50 = 15000.0 nM 4.82