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Assay Detail

CHEMBL704660

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Functional
In vitro inhibitory activity against EGF-stimulated proliferation of KB2 cells in culture
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KB 3-1
Confidence 1 — Organism
Curated By Expert

Target

KB 3-1 (CHEMBL614590)
Type CELL-LINE
Organism Homo sapiens

Publication

Studies leading to the identification of ZD1839 (IRESSA): an orally active, selective epidermal growth factor receptor tyrosine kinase inhibitor targeted to the treatment of cancer.
Barker AJ, Gibson KH, Grundy W, Godfrey AA, Barlow JJ, Healy MP, Woodburn JR, Ashton SE, Curry BJ, Scarlett L, Henthorn L, Richards L.
Bioorg Med Chem Lett (2001) 11 : 1911 -1914
PubMed 11459659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.67 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56802 1 7.30
CHEMBL939 GEFITINIB 4.0 1 7.10
CHEMBL301018 1 7.10
CHEMBL300791 1 7.05
CHEMBL291514 1 6.92
CHEMBL57759 1 6.92
CHEMBL299672 1 6.92
CHEMBL1788321 1 6.89
CHEMBL56936 1 6.82
CHEMBL57990 1 6.82
CHEMBL1744086 1 6.80
CHEMBL55425 1 6.80
CHEMBL55424 1 6.80
CHEMBL294395 1 6.77
CHEMBL56912 1 6.75
CHEMBL56142 1 6.72
CHEMBL56266 1 6.66
CHEMBL55794 1 6.66
CHEMBL293064 1 6.51
CHEMBL57892 1 6.50
CHEMBL293090 1 6.46
CHEMBL14699 1 6.42
CHEMBL60826 1 6.42
CHEMBL56502 1 6.41
CHEMBL56505 1 6.34
CHEMBL294034 1 6.19
CHEMBL57758 1 6.14
CHEMBL299893 1 6.07
CHEMBL56027 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56802 IC50 = 50.0 nM 7.30
CHEMBL939 GEFITINIB IC50 = 80.0 nM 7.10
CHEMBL301018 IC50 = 80.0 nM 7.10
CHEMBL300791 IC50 = 90.0 nM 7.05
CHEMBL291514 IC50 = 120.0 nM 6.92
CHEMBL57759 IC50 = 120.0 nM 6.92
CHEMBL299672 IC50 = 120.0 nM 6.92
CHEMBL1788321 IC50 = 130.0 nM 6.89
CHEMBL56936 IC50 = 150.0 nM 6.82
CHEMBL57990 IC50 = 150.0 nM 6.82
CHEMBL1744086 IC50 = 160.0 nM 6.80
CHEMBL55425 IC50 = 160.0 nM 6.80
CHEMBL55424 IC50 = 160.0 nM 6.80
CHEMBL294395 IC50 = 170.0 nM 6.77
CHEMBL56912 IC50 = 180.0 nM 6.75
CHEMBL56142 IC50 = 190.0 nM 6.72
CHEMBL56266 IC50 = 220.0 nM 6.66
CHEMBL55794 IC50 = 220.0 nM 6.66
CHEMBL293064 IC50 = 310.0 nM 6.51
CHEMBL57892 IC50 = 320.0 nM 6.50
CHEMBL293090 IC50 = 350.0 nM 6.46
CHEMBL14699 IC50 = 380.0 nM 6.42
CHEMBL60826 IC50 = 380.0 nM 6.42
CHEMBL56502 IC50 = 390.0 nM 6.41
CHEMBL56505 IC50 = 460.0 nM 6.34
CHEMBL294034 IC50 = 640.0 nM 6.19
CHEMBL57758 IC50 = 730.0 nM 6.14
CHEMBL299893 IC50 = 850.0 nM 6.07
CHEMBL56027 IC50 = 910.0 nM 6.04