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Assay Detail

CHEMBL805740

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

Functional
Concentration required to inhibit growth of human carcinoma colon (SW620) cell line
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SW-620
Confidence 1 — Organism
Curated By Expert

Target

SW-620 (CHEMBL612262)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2).
Wissner A, Overbeek E, Reich MF, Floyd MB, Johnson BD, Mamuya N, Rosfjord EC, Discafani C, Davis R, Shi X, Rabindran SK, Gruber BC, Ye F, Hallett WA, Nilakantan R, Shen R, Wang YF, Greenberger LM, Tsou HR.
J Med Chem (2003) 46 : 49 -63
PubMed 12502359 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 5.78 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL414631 1 6.64
CHEMBL113900 1 6.60
CHEMBL116853 1 6.52
CHEMBL117326 1 6.50
CHEMBL115440 1 6.47
CHEMBL327023 1 6.46
CHEMBL115187 1 6.40
CHEMBL114392 1 6.31
CHEMBL114593 1 6.28
CHEMBL424252 1 6.18
CHEMBL607707 PELITINIB 2.0 1 6.17
CHEMBL325156 1 6.06
CHEMBL323630 1 6.06
CHEMBL114490 1 6.04
CHEMBL113901 1 5.95
CHEMBL114728 1 5.94
CHEMBL263788 1 5.93
CHEMBL421047 1 5.84
CHEMBL326280 1 5.75
CHEMBL324718 1 5.73
CHEMBL116012 1 5.54
CHEMBL281300 1 5.47
CHEMBL157128 1 5.38
CHEMBL114073 1 5.31
CHEMBL332497 1 5.27
CHEMBL30973 1 5.26
CHEMBL118000 1 5.20
CHEMBL113996 1 5.18
CHEMBL113902 1 5.13
CHEMBL116525 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL414631 IC50 = 230.0 nM 6.64
CHEMBL113900 IC50 = 250.0 nM 6.60
CHEMBL116853 IC50 = 300.0 nM 6.52
CHEMBL117326 IC50 = 320.0 nM 6.50
CHEMBL115440 IC50 = 340.0 nM 6.47
CHEMBL327023 IC50 = 350.0 nM 6.46
CHEMBL115187 IC50 = 400.0 nM 6.40
CHEMBL114392 IC50 = 490.0 nM 6.31
CHEMBL114593 IC50 = 520.0 nM 6.28
CHEMBL424252 IC50 = 660.0 nM 6.18
CHEMBL607707 PELITINIB IC50 = 680.0 nM 6.17
CHEMBL325156 IC50 = 880.0 nM 6.06
CHEMBL323630 IC50 = 880.0 nM 6.06
CHEMBL114490 IC50 = 910.0 nM 6.04
CHEMBL113901 IC50 = 1130.0 nM 5.95
CHEMBL114728 IC50 = 1150.0 nM 5.94
CHEMBL263788 IC50 = 1170.0 nM 5.93
CHEMBL421047 IC50 = 1460.0 nM 5.84
CHEMBL326280 IC50 = 1770.0 nM 5.75
CHEMBL324718 IC50 = 1880.0 nM 5.73
CHEMBL116012 IC50 = 2880.0 nM 5.54
CHEMBL281300 IC50 = 3380.0 nM 5.47
CHEMBL157128 IC50 = 4140.0 nM 5.38
CHEMBL114073 IC50 = 4940.0 nM 5.31
CHEMBL332497 IC50 = 5380.0 nM 5.27
CHEMBL30973 IC50 = 5480.0 nM 5.26
CHEMBL118000 IC50 = 6330.0 nM 5.20
CHEMBL113996 IC50 = 6670.0 nM 5.18
CHEMBL113902 IC50 = 7460.0 nM 5.13
CHEMBL116525 IC50 = 7580.0 nM 5.12
CHEMBL116857 IC50 = 8970.0 nM 5.05
CHEMBL113985 IC50 = 9570.0 nM 5.02
CHEMBL326811 IC50 = 12280.0 nM 4.91
CHEMBL283682 IC50 = 12340.0 nM 4.91